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Academic literature on the topic 'Novel Potent Enzyme Inhibitors'

Author: Grafiati

Published: 3 June 2025

Last updated: 22 June 2025

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Journal articles on the topic "Novel Potent Enzyme Inhibitors"

1

Yamali, Cem, Halise Inci Gul, Tahir Cakir, Yeliz Demir, and Ilhami Gulcin. "Aminoalkylated Phenolic Chalcones: Investigation of Biological Effects on Acetylcholinesterase and Carbonic Anhydrase I and II as Potential Lead Enzyme Inhibitors." Letters in Drug Design & Discovery 17, no. 10 (2020): 1283–92. http://dx.doi.org/10.2174/1570180817999200520123510.

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Background: Phenolic Mannich bases have been reported as acetylcholinesterase (AChE) inhibitors for the medication of Alzheimer's disease. Carbonic Anhydrases (CAs) are molecular targets for anticonvulsant, diuretic and antiglaucoma drugs in the clinic. Phenolic compounds have also been mentioned as CA inhibitors. The importance of Mannich bases in drug design inspired our research group to design novel phenolic Mannic bases as potent enzyme inhibitors. Objective: In this study, novel Mannich bases, 1-(3,5-bis-aminomethyl-4-hydroxyphenyl)-3-(4- substitutedphenyl)-2-propen-1-ones (1-9), were designed to discover new and potent AChE inhibitors for the treatment of Alzheimer's disease and also to report their carbonic anhydrase inhibitory potency against the most studied hCA I and hCA II isoenzymes with the hope to find out promising enzyme inhibitors. Methods: Mannich bases were synthesized by the Mannich reaction. The structures of the compounds were elucidated by 1H NMR, 13C NMR, and HRMS. Enzyme inhibitory potency of the compounds was evaluated spectrophotometrically towards AChE, hCA I and hCA II enzymes. Results and Discussion: The compounds showed inhibition potency in nanomolar concentrations against AChE with Ki values ranging from 20.44±3.17 nM to 43.25±6.28 nM. They also showed CAs inhibition potency with Ki values in the range of 11.76±1.29-31.09±2.7 nM (hCA I) and 6.08 ± 1.18-23.12±4.26 nM (hCA II). Compounds 1 (hCA I), 5 (hCA II), and 4 (AChE) showed significant inhibitory potency against the enzymes targeted. Conclusion: Enzyme assays showed that Mannich derivatives might be considered as lead enzyme inhibitors to design more selective and potent compounds targeting enzyme-based diseases.

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Pilkington, Leung, and Barker. "Development of Novel, Potent Phosphatidyl–Choline-Specific Phospholipase C Inhibitors." Proceedings 22, no. 1 (2019): 67. http://dx.doi.org/10.3390/proceedings2019022067.

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The phosphatidyl–choline-specific phospholipase C (PC-PLC) enzyme has been shown to be an important enzyme involved in various cell-signaling processes. Furthermore, PC-PLC has been shown to be upregulated in various cancer cell lines, thereby presenting itself as a potential anti-cancer therapeutic target. Current PC-PLC inhibitors, including the literature standard inhibitor D609 possess characteristics making them unsuitable for clinical use. We have discovered a new class of potent PC-PLC inhibitors with much improved activity and drug-like properties than D609. The synthesis and SAR study of this class of active compounds is presented.

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Jeng, Arco Y., Paul Mulder, Aij-Lie Kwan, and Bruno Battistini. "Nonpeptidic endothelin-converting enzyme inhibitors and their potential therapeutic applications." Canadian Journal of Physiology and Pharmacology 80, no. 5 (2002): 440–49. http://dx.doi.org/10.1139/y02-025.

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Endothelins (ETs) are potent vasoconstrictors, promitogens, and inflammatory mediators. They have been implicated in the pathogenesis of various cardiovascular, renal, pulmonary, and central nervous system diseases. Since the final step of the biosynthesis of ETs is catalyzed by a family of endothelin-converting enzymes (ECEs), inhibitors of these enzymes may represent novel therapeutic agents. Currently, seven isoforms of these metalloproteases have been identified; they all share a significant amino acid sequence identity with neutral endopeptidase 24.11 (NEP), another metalloprotease. Therefore, it is not surprising that the majority of ECE inhibitors also possess potent NEP inhibitory activity. To date, three classes of ECE inhibitors have been synthesized: dual ECE/NEP inhibitors, triple ECE/NEP/ACE inhibitors, and selective ECE inhibitors. Potential clinical applications of these compounds in hypertension, chronic heart failure, restenosis, renal failure, and cerebral vasospasm deduced from studies with relevant animal models are reviewed.Key words: endothelin-converting enzyme, ECE, inhibitors, phosphoramidon, CGS 26303, CGS 35066, FR 901533, SCH 54470, metalloprotease.

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Hassan, Sidra, Pervaiz Ali Channar, Fayaz Ali Larik, et al. "Synthesis of novel ( E )-1-(2-(2-(4(dimethylamino) benzylidene) hydrazinyl)-4-methylthiazol-5-yl)ethanone derivatives as ecto-5′-nucleotidase inhibitors." Royal Society Open Science 5, no. 9 (2018): 180837. http://dx.doi.org/10.1098/rsos.180837.

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Ecto-5′-nucleotidase (e5′NT), a membrane-bound enzyme and an essential member of ecto-nucleotidases which regulates extracellular purinergic signalling. Their upregulation results in various disease conditions, for example, inflammation, hypoxia and cancer. Therefore, efforts have been made to synthesize potent and selective inhibitors of e5′NT. Here we have synthesized, characterized and evaluated six thiazole derivatives (3a–3f) as potent e5′NT inhibitors. Among all derivatives, the compound ( E )-1-(4-methyl-2-(2-(pyridin-3-ylmethylene)hydrazinyl) thiazol-5-yl)ethanone (3a) exhibited maximum inhibition towards both human and rat enzymes. However, their potency against h -e5′NT was 24-fold higher than r -e5′NT. Only two compounds exhibited inhibitory behaviour towards r -e5′NT. The molecular structures of these derivatives were confirmed with the help of solid-state characterization through NMR ( 1 H and 13 C), FTIR and elemental analysis. Additionally, molecular docking was also implemented to explain putative bonding interaction between the active site of an enzyme and potent inhibitors.

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Wang, Q. May, Robert B. Johnson, Louis N. Jungheim, Jeffrey D. Cohen, and Elcira C. Villarreal. "Dual Inhibition of Human Rhinovirus 2A and 3C Proteases by Homophthalimides." Antimicrobial Agents and Chemotherapy 42, no. 4 (1998): 916–20. http://dx.doi.org/10.1128/aac.42.4.916.

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ABSTRACT The 2A and 3C proteases encoded by human rhinoviruses (HRVs) are attractive targets for antiviral drug development due to their important roles in viral replication. Homophthalimides were originally identified as inhibitors of rhinovirus 3C protease through our screening effort. Previous studies have indicated that the antiviral activity of certain homophthalimides exceeded their in vitro inhibitory activity against the viral 3C protease, suggesting that an additional mechanism might be involved. Reported here is the identification of homophthalimides as potent inhibitors for another rhinovirus protease, designated 2A. Several homophthalimides exhibit time-dependent inhibition of the 2A protease in the low-micromolar range, and enzyme-inhibitor complexes were identified by mass spectrometry. Compound LY343814, one of the most potent inhibitors against HRV14 2A protease, had an antiviral 50% inhibitory concentration of 4.2 μM in the cell-based assay. Our data reveal that homophthalimides are not only 3C but also 2A protease inhibitors in vitro, implying that the antiviral activity associated with these compounds might result from inactivation of both 2A and 3C proteases in vivo. Since the processing of the viral polyprotein is hierarchical, dual inhibition of the two enzymes may result in cooperative inhibition of viral replication. On the basis of the current understanding of their enzyme inhibitory mechanism, homophthalimides, as a group of novel nonpeptidic antirhinovirus agents, merit further structure-action relationship studies.

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Buryska, Tomas, Lukas Daniel, Antonin Kunka, Jan Brezovsky, Jiri Damborsky, and Zbynek Prokop. "Discovery of Novel Haloalkane Dehalogenase Inhibitors." Applied and Environmental Microbiology 82, no. 6 (2016): 1958–65. http://dx.doi.org/10.1128/aem.03916-15.

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ABSTRACTHaloalkane dehalogenases (HLDs) have recently been discovered in a number of bacteria, including symbionts and pathogens of both plants and humans. However, the biological roles of HLDs in these organisms are unclear. The development of efficient HLD inhibitors serving as molecular probes to explore their function would represent an important step toward a better understanding of these interesting enzymes. Here we report the identification of inhibitors for this enzyme family using two different approaches. The first builds on the structures of the enzymes' known substrates and led to the discovery of less potent nonspecific HLD inhibitors. The second approach involved the virtual screening of 150,000 potential inhibitors against the crystal structure of an HLD from the human pathogenMycobacterium tuberculosisH37Rv. The best inhibitor exhibited high specificity for the target structure, with an inhibition constant of 3 μM and a molecular architecture that clearly differs from those of all known HLD substrates. The new inhibitors will be used to study the natural functions of HLDs in bacteria, to probe their mechanisms, and to achieve their stabilization.

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Hurst, Douglas R., Martin A. Schwartz, Yonghao Jin, et al. "Inhibition of enzyme activity of and cell-mediated substrate cleavage by membrane type 1 matrix metalloproteinase by newly developed mercaptosulphide inhibitors." Biochemical Journal 392, no. 3 (2005): 527–36. http://dx.doi.org/10.1042/bj20050545.

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MT1-MMP (membrane type 1 matrix metalloproteinase, or MMP-14) is a key enzyme in molecular carcinogenesis, tumour-cell growth, invasion and angiogenesis. Novel and potent MMP inhibitors with a mercaptosulphide zinc-binding functionality have been designed and synthesized, and tested against human MT1-MMP and other MMPs. Binding to the MT1-MMP active site was verified by the competitive-inhibition mechanism and stereochemical requirements. MT1-MMP preferred deep P1′ substituents, such as homophenylalanine instead of phenylalanine. Novel inhibitors with a non-prime phthalimido substituent had Ki values in the low-nanomolar range; the most potent of these inhibitors was tested and found to be stable against air-oxidation in calf serum for at least 2 days. To illustrate the molecular interactions of the inhibitor–enzyme complex, theoretical docking of the inhibitors into the active site of MT1-MMP and molecular minimization of the complex were performed. In addition to maintaining the substrate-specificity pocket (S1′ site) van der Waals interactions, the P1′ position side chain may be critical for the peptide-backbone hydrogen-bonding network. To test the inhibition of cell-mediated substrate cleavage, two human cancer-cell culture models were used. Two of the most potent inhibitors tested reached the target enzyme and effectively inhibited activation of proMMP-2 by endogenous MT1-MMP produced by HT1080 human fibrosarcoma cells, and blocked fibronectin degradation by prostate cancer LNCaP cells stably transfected with MT1-MMP. These results provide a model for mercaptosulphide inhibitor binding to MT1-MMP that may aid in the design of more potent and selective inhibitors for MT1-MMP.

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Ma, Ling, Jiajia Wen, Biao Dong, et al. "Design and Evaluation of Novel HIV-1 Protease Inhibitors Containing Phenols or Polyphenols as P2 Ligands with High Activity against DRV-Resistant HIV-1 Variants." International Journal of Molecular Sciences 23, no. 22 (2022): 14178. http://dx.doi.org/10.3390/ijms232214178.

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With the increasing prevalence of drug-resistant variants, novel potent HIV-1 protease inhibitors with broad-spectrum antiviral activity against multidrug-resistant causative viruses are urgently needed. Herein, we designed and synthesized a new series of HIV-1 protease inhibitors with phenols or polyphenols as the P2 ligands and a variety of sulfonamide analogs as the P2′ ligands. A number of these new inhibitors showed superb enzymatic inhibitory activity and antiviral activity. In particular, inhibitors 15d and 15f exhibited potent enzymatic inhibitory activity in the low picomolar range, and the latter showed excellent activity against the Darunavir-resistant HIV-1 variant. Furthermore, the molecular modeling studies provided insight into the ligand-binding site interactions between inhibitors and the enzyme cavity, and they sparked inspiration for the further optimization of potent inhibitors.

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Khunluck, Tueanjai, Veerapol Kukongviriyapan, Laddawan Senggunprai, Wutthipong Duangarsong, and Auemduan Prawan. "The Inhibition Kinetics and Potential Anti-Migration Activity of NQO1 Inhibitory Coumarins on Cholangiocarcinoma Cells." Integrative Cancer Therapies 18 (December 25, 2018): 153473541882044. http://dx.doi.org/10.1177/1534735418820444.

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Altered expression of a cytosolic flavoenzyme NAD(P)H:quinone oxidoreductase-1 (NQO1) has been seen in many human tumors. Its remarkable overexpression in cholangiocarcinoma (CCA; an aggressive malignancy of the biliary duct system) was associated with poor prognosis and short survival of the patients. Inhibition of NQO1 has been proposed as a potential strategy to improve the efficacy of anticancer drugs in various cancers including CCA. This study investigated novel NQO1 inhibitors and verified the mechanisms of their enzyme inhibition. Among the different chemical classes of natural NQO1 inhibitors are coumarins, flavonoids, and triterpenoids. Coumarins are a group of particularly potent NQO1 inhibitors. The mechanisms and kinetics of enzyme inhibition of coumarin, aesculetin, umbelliferone, and scopoletin using the cell lysates as a source of NQO1 enzyme best fit with an uncompetitive inhibition model. Among the NOQ1 inhibitors tested in KKU-100 CCA cells, scopoletin and umbelliferone had the strongest inhibitory effect on this enzyme, while aesculetin and coumarin barely affected intracellular NQO1. All coumarins were further tested for cytotoxicity and anti-migration activity. At modest cytotoxic doses, scopoletin and umbelliferone greatly inhibited the migration of KKU-100 cells, whereas coumarin and aesculetin barely reduced cell migration. The anti-migration effect of scopoletin was associated with decreased ratio of matrix metalloproteinase 9/tissue inhibitors of metalloproteinases 1 ( MMP9/ TIMP1) mRNA. These findings suggest that natural compounds with potent inhibitory effect on intracellular NQO1 have useful anti-migration effects on CCA cells. In order to prove that the potent NQO1 inhibitor, scopoletin, is clinically useful in the enhancement of CCA treatment, additional in vivo studies to elucidate the mechanism of these effects are needed.

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Chu, Ming-Jie, Wei Wang, Zi-Li Ren, et al. "Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents." Molecules 24, no. 7 (2019): 1311. http://dx.doi.org/10.3390/molecules24071311.

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To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized and their biological activities were evaluated as potential topoisomerase II inhibitors. Compound 4d exhibited the most potent antibacterial activity with Minimum inhibitory concentration (MIC) alues of 4 µg/mL, 2 µg/mL, 4 µg/mL, and 0.5 µg/mL against Staphylococcus aureus, Listeria monocytogenes, Escherichia coli, and Salmonella gallinarum, respectively. The in vivo enzyme inhibition assay 4d displayed the most potent topoisomerase II (IC50 = 13.5 µg/mL) and topoisomerase IV (IC50 = 24.2 µg/mL) inhibitory activity. Molecular docking was performed to position compound 4d into the topoisomerase II active site to determine the probable binding conformation. In summary, compound 4d may serve as potential topoisomerase II inhibitor.

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Dissertations / Theses on the topic "Novel Potent Enzyme Inhibitors"

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Varley, Denise Joyce. "Novel inhibitors of glutamine synthase." Thesis, University of Oxford, 1990. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.308650.

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Olomola, Temitope Oloruntoba. "Synthesis and evaluation of novel HIV-1 enzyme inhibitors." Thesis, Rhodes University, 2011. http://hdl.handle.net/10962/d1005034.

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This study has involved the design, synthesis and evaluation of novel HIV-1 enzyme inhibitors accessed by synthetic elaboration of Baylis-Hillman adducts. Several series of complex coumarin-AZT and cinnamate ester-AZT conjugates have been prepared, in high yields, by exploiting the click reaction between appropriate Baylis-Hillman derived precursors and azidothymidine (AZT), all of which have been fully characterised using spectroscopic techniques. These conjugates, designed as potential dual-action HIV-1 inhibitors, were tested against the appropriate HIV-1 enzymes, i.e. HIV-1 reverse transcriptase and protease or HIV-1 reverse transcriptase and integrase. A number of the ligands have exhibited % inhibition levels and IC50 values comparable to drugs in clinical use, permitting their identification as lead compounds for the development of novel dual-action inhibitors. In silico docking of selected ligands into the active sites of the respective enzymes has provided useful insight into binding conformations and potential hydrogen-bonding interactions with active-site amino acid residues. A series of furocoumarin carboxamide derivatives have been synthesised in four steps starting from resorcinol and these compounds have also been tested for HIV-1 integrase inhibition activity. The structures of unexpected products isolated from Aza-Baylis-Hillman reactions of N-tosylaldimines have been elucidated by spectroscopic analysis, and confirmed by single crystal X-ray analysis. A mechanism for what appears to be an unprecedented transformation has been proposed. Microwave-assisted SeO₂ oxidation of Baylis-Hillman-derived 3-methylcoumarins has provided convenient and efficient access to coumarin-3-carbaldehydes, and a pilot study has revealed the potential of these coumarin-3-carbaldehydes as scaffolds for the construction of tricyclic compounds. The HCl-catalysed reaction of tert-butyl acrylate derived Baylis-Hillman adducts has been shown to afford 3-(chloromethyl)coumarins and α-(chloromethyl)cinnamic acids, the Zstereochemistry of the latter being established by X-ray crystallography. ¹H NMR-based experimental kinetic and DFT-level theoretical studies have been undertaken to establish the reaction sequence and other mechanistic details. Base-catalysed cyclisation on the other hand, has been shown to afford 2H-chromene rather than coumarin derivatives.

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Capicciotti, Chantelle. "The Rational Design of Potent Ice Recrystallization Inhibitors for Use as Novel Cryoprotectants." Thèse, Université d'Ottawa / University of Ottawa, 2014. http://hdl.handle.net/10393/30634.

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The development of effective methods to cryopreserve precious cell types has had tremendous impact on regenerative and transfusion medicine. Hematopoietic stem cell (HSC) transplants from cryopreserved umbilical cord blood (UCB) have been used for regenerative medicine therapies to treat conditions including hematological cancers and immodeficiencies. Red blood cell (RBC) cryopreservation in blood banks extends RBC storage time from 42 days (for hypothermic storage) to 10 years and can overcome shortages in blood supplies from the high demand of RBC transfusions. Currently, the most commonly utilized cryoprotectants are 10% dimethyl sulfoxide (DMSO) for UCB and 40% glycerol for RBCs. DMSO is significantly toxic both to cells and patients upon its infusion. Glycerol must be removed to <1% post-thaw using complicated, time consuming and expensive deglycerolization procedures prior to transfusion to prevent intravascular hemolysis. Thus, there is an urgent need for improvements in cryopreservation processes to reduce/eliminate the use of DMSO and glycerol. Ice recrystallization during cryopreservation is a significant contributor to cellular injury and reduced cell viability. Compounds capable of inhibiting this process are thus highly desirable as novel cryoprotectants to mitigate this damage. The first compounds discovered that were ice recrystallization inhibitors were the biological antifreezes (BAs), consisting of antifreeze proteins and glycoproteins (AFPs and AFGPs). As such, BAs have been explored as potential cryoprotectants, however this has been met with limited success. The thermal hysteresis (TH)activity and ice binding capabilities associated with these compounds can facilitate cellular damage, especially at the temperatures associated with cryopreservation. Consequently, compounds that possess “custom-tailored” antifreeze activity, meaning they exhibit the potent ice recrystallization inhibition (IRI) activity without the ability to bind to ice or exhibit TH activity,are highly desirable for potential use in cryopreservation. This thesis focuses on the rational design of potent ice recrystallization inhibitors and on elucidating important key structural motifs that are essential for potent IRI activity. While particular emphasis in on the development of small molecule IRIs, exploration into structural features that influence the IRI of natural and synthetic BAs and BA analogues is also described as these are some of the most potent inhibitors known to date. Furthermore, this thesis also investigates the use of small molecule IRIs for the cryopreservation of various different cell types to ascertain their potential as novel cryoprotectants to improve upon current cryopreservation protocols, in particular those used for the long-term storage of blood and blood products. Through structure-function studies the influence of (glyco)peptide length, glycosylation and solution structure for the IRI activity of synthetic AFGPs and their analogues is described. This thesis also explores the relationship between IRI, TH and cryopreservation ability of natural AFGPs, AFPs and mutants of AFPs. While these results further demonstrated that BAs are ineffective as cryoprotectants, it revealed the potential influence of ice crystal shape and growth progression on cell survival during cryopreservation. One of the most significant results of this thesis is the discovery of alkyl- and phenolicglycosides as the first small molecule ice recrystallization inhibitors. Prior to this discovery, all reported small molecules exhibited only a weak to moderate ability to inhibit ice recrystallization. To understand how these novel small molecules inhibit this process, structure-function studies were conducted on highly IRI active molecules. These results indicated that key structural features, including the configuration of carbons bearing hydroxyl groups and the configuration of the anomeric center bearing the aglycone, are crucial for potent activity. Furthermore, studies on the phenolic-glycosides determined that the presence of specific substituents and their position on the aryl ring could result in potent activity. Moreover, these studies underscored the sensitivity of IRI activity to structural modifications as simply altering a single atom or functional group on this substituent could be detrimental for activity. Finally, various IRI active small molecules were explored for their cryopreservation potential with different cell types including a human liver cell line (HepG2), HSCs obtained from human UCB, and RBCs obtained from human peripheral blood. A number of phenolic-glycosides were found to be effective cryo-additives for RBC freezing with significantly reduced glycerol concentrations (less than 15%). This is highly significant as it could drastically decrease the deglycerolization processing times that are required when RBCs are cryopreserved with 40% glycerol. Furthermore, it demonstrates the potential for IRI active small molecules as novel cryoprotectants that can improve upon current cryopreservation protocols that are limited in terms of the commonly used cryoprotectants, DMSO and glycerol.

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Ekici, Ozlem Dogan. "Design, synthesis, and evaluation of novel irreversible inhibitors for caspases." Diss., Georgia Institute of Technology, 2003. http://hdl.handle.net/1853/5333.

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Takeuchi, Toshihiko Gray Harry B. Goddard William A. Meade Thomas J. "The electronic structure of distorted porphyins and cobalt schiff base derivatives as novel enzyme inhibitors." Diss., Pasadena, Calif. : California Institute of Technology, 1996. http://resolver.caltech.edu/CaltechTHESIS:11052009-085123252.

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Thesis (Ph. D.)--California Institute of Technology, 1996. UM #9617425.<br>Advisor names found in the Acknowledgments pages of the thesis. Title from home page. Viewed 01/19/2010. Includes bibliographical references.

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Wiencek, Patrick. "Secondary Functions And Novel Inhibitors Of Aminoacyl-Trna Synthetases." ScholarWorks @ UVM, 2018. https://scholarworks.uvm.edu/graddis/941.

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The aminoacyl-tRNA synthetases are a family of enzymes involved in the process of translation, more specifically, ligating amino acids to their cognate tRNA molecules. Recent evidence suggests that aminoacyl-tRNA synthetases are capable of aminoacylating proteins, some of which are involved in the autophagy pathway. Here, we test the conditions under which E. coli and human threonyl-tRNA synthetases, as well as hisidyl-tRNA synthetase aminoacylate themselves. These reactions are ATP dependent, stimulated by Mg2+, and are inhibited by increasing cognate tRNA concentrations. These data represent the foundation for future aminoacylation experiments, specifically delving into the relationship between the autophagy pathway and the aminoacylation of proteins. Additionally, we provide evidence of the inhibitory abilities of the compound EHTS-0 on both E. coli and human threonyl-tRNA synthetases. Further, we also show that an EHTS-0 analog, EHTS-1, also significantly inhibits E. coli threonyl-tRNA synthetase but not the human enzyme. These data could be useful in determining the potential for EHTS-0 and EHTS-1 as possibly anti-angiogenic drugs.

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Boulton, Sallyanne. "Biological effects of novel poly (adenosine diphosphate ribose) polymerase inhibitors." Thesis, University of Newcastle Upon Tyne, 1995. http://hdl.handle.net/10443/1004.

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Poly(ADP-ribose) polymerase (PADPRP) is a nuclear enzyme with a well documented role in DNA repair. Inhibitors of PADPRP, (e.g. 3' substituted benzamides) potentiate the cytotoxicity of a wide range of antitumour drugs. The results presented in this thesis represent, to the best of my knowledge, the first comprehensive and quantitative assessment of the ability of a range of P ADPRP inhibitors to modulate the cellular responses to damaging agents. Two novel PADPRP inhibitors, 8-hydroxy-2-methyl quinazolin-4(3H)-one (NU1025) and 3,4 dihydro-5-methoxyisoquinolin-1-(2H)-one (PD 128763) were compared with two "classical" PADPRP inhibitors, 3-aminobenzamide (3AB) and benzamide (BZ). The relative potencies for 3AB, BZ, NU1025 and PD 128763 as PADPRP inhibitors in vitro were 1.0, ~1.0, ~43 and ~53 respectively. All compounds potentiated the growth inhibition and cytotoxicity of the monofunctional alkylating agent temozolomide (TM) in L1210 cells. For example, 10/-lM NUI025 and PD 128763 gave dose enhancement factors (DEF) of ~2 at 100/0 survival, whereas ImM 3AB and 0.5mM BZ where required to give similar DEF values. Cellular NADl- levels were depleted up to 50% by 1-2mM TM and this depletion was completely prevented by coincubation with 50-100µM PD 128763 and 1-3mM 3AB. TM induced DNA single strand break levels were increased in a concentration dependent manner by the P ADPRP inhibitors. Overall, the relative potencies for ability of the compounds to potentiate TM induced growth inhibition, cytotoxicity and DNA single strand breaks showed good correlation with those determined in an in vitro inhibition study, with both NU1025 and PD 128763 exhibiting ~60 fold increased inhibitory activity as compared to 3AB. The PADPRP inhibitors per se did not effect the growth or survival of the L 121 0 cells, nor increase DNA strand breakage. NAD+ is the substrate for PADPRP. A L1210 cell line made resistant to tiazofurin (TZ) utilising a step wise selection protocol was shown to be deficient in nicotinamide mononucleotide adenyl transferase (NMNAT) , the final enzyme required for NAD+ biosynthesis. The consequences of a reduced NMNAT activity (<3% of the parental line ) and an ~40% reduction in intracellular NAD+ levels were determined. The resistant cells showed an ~3 fold increased sensitivity to TM as compared to the parental cells. Upon coincubation with increasing concentrations of NU1025 in the presence of a fixed concentration of TM, growth inhibition was potentiated ~70 fold in the resistant cells but only ~10 fold in the parental cell line, demonstrating the reduced level of competition between NAD+ and NUI025 for PADPRP. However, DNA single strand breaks were increased in the resistant compared to the parental cell line only when NU1025 was coincubated with TM. In contrast, in the presence of the PADPRP inhibitors alone, equivalent growth inhibitory effects were observed in each of the cell lines, suggesting inhibition of PADPRP was not the cytotoxic effector. The ~40% NAD+ depletion observed could therefore suggest, that NAD+ levels in the resistant cells were reduced to, or near to the KmNAD+ for PADPRP.

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PRENCIPE, Filippo. "Synthesis and biological evaluation in vitro and in vivo of novel potent anticancer agents affecting tubulin polymerization." Doctoral thesis, Università degli studi di Ferrara, 2017. http://hdl.handle.net/11392/2487939.

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L’attività di ricerca svolta durante i tre anni di dottorato ha avuto come obiettivo la progettazione, la sintesi e l’ottimizzazione di nuovi potenziali agenti antitumorali dotati di attività antiproliferativa e antivascolare che hanno come target biologico i microtubuli, strutture dinamiche cellulari generate dalla polimerizzazione di eterodimeri di α,β tubulina. Il sistema di microtubuli è essenziale per la divisione cellulare, essendo coinvolto nella formazione del fuso mitotico, ed è importante per diversi processi cellulari quali la regolazione della motilità, segnalazione cellulare, secrezione e trasporto intracellulare. Tra le molecole di derivazione naturale, il cis-stilbene Combretastatina A-4 (CA-4), legando la tubulina a livello del sito di legame della colchicina, ne inibisce la polimerizzazione mostrando una potente attività antiproliferativa contro diverse linee cellulari tumorali. L’attività di ricerca relativa al primo anno di dottorato ha riguardato la sintesi di una nuova serie di composti a struttura 1-(3',4',5' trimetossibenzoil)-3-arilamino-5-amino-1,2,4-triazolica per i quali si è andati a valutare l’attività antiproliferativa in vitro, l’interazione con la tubulina e gli effetti prodotti sul ciclo cellulare. Per il derivato più attivo della serie, 1-(3,4,5-trimetossibenzoil)-3-(p-toluidino)-5-ammino-1,2,4-triazolo 3c è stata valutata l’attività antitumorale in vivo. I migliori risultati in termini di inibizione della proliferazione di linnee cellulari tumorali sono stati ottenuti con i derivati p-Me, m,p-diMe and p-Et fenil 3c, 3e e 3f, rispettivamente, i quali sono risultati essere equipotenti rispetto al composto di riferimento Combretastatina A-4 (CA-4). Proseguendo nel nostro lavoro di ricerca, nel corso del secondo anno di dottorato, una nuova serie di composti caratterizzati dalla presenza di un gruppo 2-metossi/etossicarbonile sono stati valutati per l’attività antiproliferativa su linee cellulari tumorali e per i composti più attivi della serie si è andati a valutare l’inibizione della polimerizzazione della tubulina, gli effetti sul ciclo cellulare e l’attività antitumorale in vivo. I migliori risultati in termini di attività antiproliferativa si sono ottenuti introducendo il sostituente metossilico in posizione C-6. Il composto più attivo della serie è risultato essere il derivato 2-metossicarbonil-3-(3’,4’,5’-trimetossianilino)-6-metossi-benzo[b]furano 3g, il quale ha prodotto una inibizione della proliferazione di linee cellulari tumorali a concentrazioni nanomolari (IC50’s, 0.3-27 nM), lega la tubulina a livello del sito di legame della colchicina, induce l’apoptosi e ha mostrato, sia in vitro che in vivo, una potente attività antivascolare su cellule endoteliali vascolari. Infine durante il terzo anno di dottorato è stata messa a punto la sintesi di una nuova serie di inibitori della polimerizzazione della tubulina a struttura 1- (3’,4’,5- trimetossiifenil) -2-aril-1H-imidazolica e progettati come cis-analoghi della combretastatina A-4, con l’obiettivo di valutare l’effetto sull’attività biologica prodotto dall’introduzione di diversi gruppi sostituenti a livello dell’anello fenilico in posizione C-2 dell’eterociclo imidazolico. L’introduzione di un atomo di cloro e di un gruppo etossilico nelle posizioni meta- e para-, rispettivamente, ha prodotto il composto più attivo della serie 1-(3’,4’ ,5’ -trimetossifenil)-2-(3’-Cl, 4’-OEt fenil)-1H-imidazolo 4o, con un valori di IC50 di 0.4-3.8 nM su un pannello di sette linee cellulari tumorali. Esperimenti condotti su un modello di topo singenico hanno dimostrato una potente attività antitumorale del composto 4o, il quale ha prodotto una significativa riduzione della massa tumorale a dosi trenta volte più basse rispetto a quelle richieste per la CA-4P usato come composto di riferimento.<br>During these three years of PhD our research work has been focused on the design, synthesis and optimization of novel potential anticancer agents with antivascular and antiproliferative activities which target microtubules, dynamic tubular proteins that are assembled from α tubulin/β tubulin (αβ-tubulin) heterodimers. The microtubule system is essential in a variety of fundamental cellular processes, including mitosis, formation and maintenance of cell shape, regulation of motility, cell signaling, secretion and intracellular transport. Among natural occurring compounds, Combretastatin A-4 (CA-4), a cis-stilbene isolated from the bark of the South African bush willow tree Combretum caffrum , is one of the most potent inhibitors of colchicine binding presently known. CA-4 has been shown to possess a powerful cytotoxic activity against a panel of tumor cell line, including multi-drug resistant cells. During the first year of PhD, a new class of compounds that incorporated the structural motif of the 1-(3’,4’,5’-trimethoxtbenzoyl)-3-arylamino-5-amino-1,2,4-triazole molecular skeleton was synthesized and evaluated for their in vitro antiproliferative activity, interactions with tubulin and cell cycle effects. The most active agent,( 1-(3,4,5-trimethoxybenzoyl)-3-(p-toluyl)-5-ammino-1,2,4-triazole, 3c), was evaluated for antitumor activity in vivo. The best results for inhibition of cancer cell growth were obtained with the p-Me, m,p-diMe and p-Et phenyl derivatives 3c, 3e and 3f, respectively, and, overall, these compounds were more or less as active as CA-4. Their vascular disrupting activity was evaluated in HUVEC cells, with compound 3c showing activity comparable with that of CA-4. Compound 3c almost eliminated the growth of syngeneic hepatocellular carcinoma in Balb/c mice, suggesting that 3c could be a new antimitotic agent with clinical potential. During the second year a new series of compounds characterized by the presence of a 2-methoxy/ethoxycarbonyl group were evaluated for antiproliferative activity against cancer cells in culture, and, for selected, highly active compounds, inhibition of tubulin polymerization, cell cycle effects and in vivo potency. The greatest antiproliferative activity occurred with a methoxy group introduced at the C-6 position, the least with this substituent at C-4. Thus far, the most promising compound in this series was 2-methoxycarbonyl-3-(3’,4’,5’-trimethoxyanilino)-6-methoxybenzo[b]furan (3g), which inhibited cancer cell growth at nanomolar concentrations (IC50’s, 0.3-27 nM), induced apoptosis and showed, both in vitro and in vivo, potent vascular disrupting properties derived from the effect of this compound on vascular endothelial cells. Compound 3g had in vivo antitumor activity in a murine model comparable to the activity obtained with combretastatin A-4 phosphate. The research work of the third year of PhD has been focused on the synthesis of a novel series of tubulin polymerization inhibitors, based on the 1-(3’,4’,5’-trimethoxyphenyl)-2-aryl-1H-imidazole scaffold, with the goal of evaluating the effects of various patterns of substitution on the phenyl at the 2-position of the imidazole ring on biological activity. A chloro and ethoxy group at the meta- and para-positions, respectively, produced the most active compound in the series (1-(3’,4’ ,5’ -trimethoxyfenyl)-2-(3’-Cl, 4’-Ethoxyfenyl)-1H-imidazole ,4o), with IC50 values of 0.4-3.8 nM against a panel of seven cancer cell lines. Except in HL-60 cells, 4o had greater antiproliferative than CA-4, indicating that the 3’-chloro-4’-ethoxyphenyl moiety was a good surrogate for the CA-4 B-ring. Experiments carried out in a mouse syngenic model demonstrated high antitumor activity of 4o, which significantly reduced the tumor mass at a dose thirty times lower than that required for CA-4P, which was used as a reference compound.

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Ekici, Özlem Doğan. "Design, synthesis, and evaluation of novel irreversible inhibitors for caspases." Available online, Georgia Institute of Technology, 2004:, 2003. http://etd.gatech.edu/theses/available/etd-04062004-164633/unrestricted/ekici%5Fozlem%5Fd%5F200312%5Fphd.pdf.

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Agarwal, Anil Kumar. "Design and synthesis of novel bacterial enzyme inhibitors as potential antituberculosis agents." Thesis, University of Leeds, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.445382.

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Books on the topic "Novel Potent Enzyme Inhibitors"

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Bojidor, Georgiev, and Markovski Sava, eds. Serpins and protein kinase inhibitors: Novel functions, structural features, and molecular mechanisms. Nova Science, 2009.

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Georgiev, Bojidor. Serpins and protein kinase inhibitors: Novel functions, structural features and molecular mechanisms. Nova Science Publishers, 2010.

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AlJaroudi, Wael. Risk Assessment in Acute Coronary Syndromes. Oxford University Press, 2015. http://dx.doi.org/10.1093/med/9780199392094.003.0013.

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Acute coronary syndromes (ACS) include unstable angina pectoris (UAP), non-ST elevation (NSTEMI), and ST elevation acute myocardial infarction (STEMI). Each year, more than 2 million people are hospitalized with ACS in the United States. The initial treatment has evolved over the last few decades from conservative management to early reperfusion therapy. Medical therapy has also significantly changed with the use of newer more potent antiplatelet agents, beta-blockers, angiotensin converting enzyme inhibitors, statins, and anti-anginal drugs, which have resulted in improvement of patient care and survival. There is no role for stress myocardial perfusion imaging (MPI) in the acute presentation; however, rest MPI may be used to identify the culprit lesion and risk stratify patients if injected during chest pain. In stable patients for ACS, submaximal exercise or vasodilator MPI can be performed as early as 48 hours after the event. Several gated MPI-derived variables such as left ventricular (LV) ejection fraction (EF), LV volumes, infarct size, mechanical dyssynchrony, and residual ischemic burden can risk stratify patients and provide prognostic data incremental to validated clinical risk scores such as GRACE (Global Registry of Acute Coronary Syndrome) and TIMI (Thrombolysis in Myocardial Infarction). Patients with depressed LVEF, remodeled LV, and large perfusion defects are at particularly high- risk for subsequent cardiac death or recurrent myocardial infarction. In such setting, MPI plays a pivotal role in the management of patients and guiding therapeutic decisions. The current chapter will review the clinical and MPI predictors of outcomes in patients presenting with ACS according to updated guidelines and a proposed algorithm integrating the role of MPI in guiding therapeutic decisions and management.

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Book chapters on the topic "Novel Potent Enzyme Inhibitors"

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Polat, Hakan, and Yavuz Onur Danacioglu. "Abiraterone Acetate Treatment in Metastatic Prostate Cancer." In Current Management of Metastatic Prostate Cancer. Nobel Tip Kitabevleri, 2024. http://dx.doi.org/10.69860/nobel.9786053359142.8.

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Prostate cancer is the frequently presented malignancy in men, and it is expected that nearly 300,000 people will be diagnosed with it in the United States in 2024. Generally, the five-year survival rate is quite positive at 97.5%, but this rate drops to around 30% in cases with advenced disease. Tumors arise from changes in the genetic material of the epithelial cells in the prostate gland and typically appear as adenocarcinomas. Adenocarcinoma of the prostate is found within the gland in a multifocal and heterogeneous manner. Metastases of prostate cancer are hormonally sensitive, the primary therapy became aimed at lowering testosterone levels to castration levels through surgical procedures or androgen deprivation therapy (ADT) via gonadotropin-releasing hormone.However, it is rarely used nowadays following the development of more potent and selective androgen synthesis inhibitors. Abiraterone acetate (AA) is a potent and selective inhibitor of cytochrome P17 (CYP17), a key enzyme in androgen synthesis, unlike ketoconazole, which inhibits various cytochrome P pathways. In this section, the effectiveness of Abiraterone Acetate treatment in metastatic prostate cancer aims to be explained, relying on the literature for support.

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Penrose, John F., K. Frank Austen, and Bing K. Lam. "LTC4 synthase: A key enzyme in cysteinyl leukotriene formation." In Novel Inhibitors of Leukotrienes. Birkhäuser Basel, 1999. http://dx.doi.org/10.1007/978-3-0348-8703-8_2.

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Haeggström, Jesper Z., and Anders Wetterholm. "Leukotriene A4 hydrolase: A key enzyme in chemotactic leukotriene formation." In Novel Inhibitors of Leukotrienes. Birkhäuser Basel, 1999. http://dx.doi.org/10.1007/978-3-0348-8703-8_3.

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Magolda, Ronald L., William C. Ripka, William Galbraith, Paul R. Johnson, and Marla S. Rudnick. "Novel Synthesis of Potent Site-Specific Phospholipase A2 Inhibitors." In Prostaglandins, Leukotrienes, and Lipoxins. Springer US, 1985. http://dx.doi.org/10.1007/978-1-4684-4946-4_63.

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Leyssen, Pieter, Jacqueline Smadja, Philippe Rasoanaivo, et al. "Biodiversity as a Source of Potent and Selective Inhibitors of Chikungunya Virus Replication." In Novel Plant Bioresources. John Wiley & Sons, Ltd, 2014. http://dx.doi.org/10.1002/9781118460566.ch11.

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Loots, Melanie J., Michael C. Badia, David W. Cushman, et al. "Acyl lysinamido phosphonates: Potent, long-acting inhibitors of angiotensin-converting enzyme." In Peptides. Springer Netherlands, 1988. http://dx.doi.org/10.1007/978-94-010-9595-2_34.

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Gambhir, Lokesh, and Neha Kapoor. "Fungal Enzyme Inhibitors: Potent Repository of Lead Compounds to Curb Cancer." In Fungi Bioactive Metabolites. Springer Nature Singapore, 2024. http://dx.doi.org/10.1007/978-981-99-5696-8_13.

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Pandey, Divya, and Kuldeep K. Roy. "Identification of Novel Potent KRASG12D Inhibitors Through Target-Based Virtual Screening." In Global Trends in Health, Technology and Management. Springer Nature Switzerland, 2024. https://doi.org/10.1007/978-3-031-75457-9_14.

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Brands, B., C. A. Naranjo, J. W. Tighe, R. S. Collis, and E. M. Sellers. "Effects of Angiotensin Converting Enzyme Inhibitors on Free Choice Ethanol Consumption by Rats." In Novel Pharmacological Interventions for Alcoholism. Springer New York, 1992. http://dx.doi.org/10.1007/978-1-4612-2878-3_45.

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Grupp, L. A., G. Spinosa, and T. Lingham. "Management of Alcohol Consumption with Angiotensin Converting Enzyme Inhibitors: A Review of the Animal Findings." In Novel Pharmacological Interventions for Alcoholism. Springer New York, 1992. http://dx.doi.org/10.1007/978-1-4612-2878-3_16.

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Conference papers on the topic "Novel Potent Enzyme Inhibitors"

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Fujita, Hidenori, Yayoi Fujioka, Keiji Ishida, et al. "Abstract 3777: TAS4464, a novel and highly potent NEDD8 activating enzyme (NAE) inhibitor, causes apoptosis of sarcomas via cell cycle dysregulation." In Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA. American Association for Cancer Research, 2016. http://dx.doi.org/10.1158/1538-7445.am2016-3777.

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Muraoka, Hiromi, Chihoko Yoshimura, Shingo Tsuji та ін. "Abstract 1730: TAS4464, a novel highly potent NEDD8 activating enzyme inhibitor, demonstrates antitumor activity in multiple myeloma through the inactivation of NF-κB pathways". У Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1538-7445.am2015-1730.

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Yoshimura, Chihoko, Hiromi Muraoka, Hiroaki Ochiiwa, et al. "Abstract C176: TAS4464, a novel, highly potent, and selective inhibitor of NEDD8 activating enzyme demonstrates sustained target inhibition and antitumor activity in a preclinical model." In Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; November 5-9, 2015; Boston, MA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1535-7163.targ-15-c176.

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Muraoka, Hiromi, Chihoko Yoshimura, Shingo Tsuji та ін. "Abstract C177: TAS4464, a novel and highly potent inhibitor of NEDD8 activating enzyme, overcomes insensitivity to BTK, PI3Kδ, and IRAK4 inhibitors in activated B-cell like diffuse large B-cell lymphoma via inactivation of the NF-κB pathway". У Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; November 5-9, 2015; Boston, MA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1535-7163.targ-15-c177.

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Cvijetić, Ilija, Petar Ristivojević, Maja Krstić-Ristivojević та Dušanka Milojković-Opsenica. "EXPLORING THE POTENTIAL OF Α-ARBUTIN AS THE INHIBITOR OF NEURODEGENERATIVE DISORDERS". У 1st INTERNATIONAL Conference on Chemo and BioInformatics. Institute for Information Technologies, University of Kragujevac, 2021. http://dx.doi.org/10.46793/iccbi21.292c.

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Tyrosinase is an enzyme involved in generation of dopamine-quinones, which has an important role in oxidative stress associated with the Parkinson’s disease. It is also a common molecular target for the design of novel anti-melanogenic agents. The inhibition of tyrosinase might be responsible for the experimentally observed intracellular antioxidant activity of α-arbutin. Moreover, intrinsic radical scavenging capacity of α-arbutin should also be considered. The binding mode of α-arbutin into the active site of Bacillus megaterium tyrosinase is predicted using AutoDock Vina 1.1. To map the thermodynamic feasibility of HAT and SET-PT mechanisms of the intrinsic antioxidant capacity α-arbutin, bond dissociation enthalpies (BDEs) and ionization potential (IP) are calculated using DFT with B3LYP functional and 6-31+g(d,p) basis set. α-Arbutin fitted well into the active site of tyrosinase, with the calculated binding affinity of -17.5 kcal/mol. The phenolic moiety is located deep into the binding pocket, interacting with His residues around Cu2+ ion. The binding mode of α-arbutin is stabilized via HBD interactions with His231, His42, His60, Arg209, Gly216, and Asn205, HBA interaction with Arg209 at the outer part of active site, and hydrophobic interactions with His208, Val218 and Ala221. The calculated IP of α-arbutin is 175.18 kcal/mol, and BDE of phenolic group is 79.85 kcal/mol. The spin densities of radical-cation and hydroxyl radical are delocalized on the aglycone moiety. The results of this study provide valuable structural insights into the molecular mechanisms of biological action of α-arbutin, and might be exploited for the design of more potent analogues.

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Zaman, Khair. "Chalcones: As Potent Α-Amylase Enzyme Inhibitors; Synthesis, In Vitro, And In Silico Studies." У International Conference on Biological Research and Applied Science. Jinnah University for Women, Karachi,Pakistan, 2022. http://dx.doi.org/10.37962/ibras/2022/83.

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Wengner, Antje Margret, Gerhard Siemeister, Marcus Koppitz, et al. "Abstract 3090: Novel Mps1 kinase inhibitors with potent anti-tumor activity." In Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1538-7445.am2015-3090.

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Callery, Patrick S., Wisut Wichitnithad, Elizabeth Borysiewicz, Gregory W. Konat, and Gregory W. Konat. "Abstract 3255: Tetrahydropyridine derivatives: Novel and potent histone demethylase LSD1 inhibitors." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-3255.

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Deryagina, V. P., N. I. Ryzhova, L. A. Savluchinskaya, I. S. Golubeva, L. V. Krivosheeva, and K. I. Kirsanov. "eNOS INVOLVEMENT IN CARCINOGENESIS AND PROSPECTS FOR THE USE OF ENZYME INHIBITORS." In NOVEL TECHNOLOGIES IN MEDICINE, BIOLOGY, PHARMACOLOGY AND ECOLOGY. Institute of information technology, 2022. http://dx.doi.org/10.47501/978-5-6044060-2-1.310-321.

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The review discusses the literature data and the results of our own research on the role of endothelial NO synthase (eNOS) in carcinogenesis. The antitumor potential of eNOS inhibi-tors and the molecular mechanisms of their action are analyzed.

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Vakkalanka, Swaroop, Meyyappan Muthuppalaniappan, Babu Govindarajulu, et al. "Abstract 1789: Preclinical profile of novel and potent c-Met kinase inhibitors." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-1789.

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Reports on the topic "Novel Potent Enzyme Inhibitors"

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Joel, Daniel M., John C. Steffens, and Alfred M. Mayer. Host-Elicited Germination and Mechanism of Penetration in Broomrape (Orobanche Spp.). United States Department of Agriculture, 1993. http://dx.doi.org/10.32747/1993.7568107.bard.

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Orobanche is an important parasitic weed. For developing novel methods for its control, a thorough understanding of crucial stages of its development is needed. Therefore, the objectives of this project were characterization of Orobanche germination stimulants, analysis of mechanisms of haustorial penetration, and characterization and isolation of penetration enzymes. The first highly potent natural germination stimulant for Orobanche was isolated from sunflower and identified by high-field 1D (1H and 13C), 2D (1H-1H COSY, HMQC, HMBC)-NMR, GC.FT-IR, and GC.MS as costuslactone, a guaiane type sesquiterpene lactone that resembles strigol only in possessing a lactone moiety that is required for activity. The first direct in situ evidence for the enzymatic nature of the infection process of a parasitic angiosperm was established. Pectin deesterification and depletion of pectins in host cell walls were shown adjacent to haustorial cells. Pectin methyl esterase and polygalacturonase were immunocytochemically detected in intrusive cells and in adjacent host apoplast. Orobanche tissues contain inhibitors of PGase activity. PME and three PGases were isolated from Orobanche calli. PME was characterized and purified, and antibodies were prepared against it. This study presents novel findings regarding parasitism in Orobanche, which may help to open up new approaches for controlling broomrapes.

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Simeonova, Rumiana, Vessela Vitcheva, Ivanka Kostadinova, et al. In Vivo Studies on Novel Potent Acetylcholinesterase Inhibitors with Dual-site Binding for Treatment of Alzheimer’s Disease. "Prof. Marin Drinov" Publishing House of Bulgarian Academy of Sciences, 2021. http://dx.doi.org/10.7546/crabs.2021.06.13.

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Blumwald, Eduardo, and Avi Sadka. Sugar and Acid Homeostasis in Citrus Fruit. United States Department of Agriculture, 2012. http://dx.doi.org/10.32747/2012.7697109.bard.

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Citrus fruit quality standards have been determined empirically, depending on species and on the particular growing regions. In general, the TSS (total soluble solids) to total acidity (TA) ratio determines whether citrus fruit can be marketed. Soluble sugars account for most of the TSS during harvest while TA is determined almost solely by the citric acid content, which reaches levels of 1-5% by weight in many cultivated varieties. Acid and sugar homeostasis in the fruit is critical for the management of existing cultivars, the development of new cultivars, the improvement of pre- and post-harvest strategies and the control of fruit quality and disorders. The current proposal (a continuation of a previous proposal) aimed at: (1) completing the citrus fruit proteome and metabolome, and establish a citrus fruit functional database, (2) further characterization of the control of fruit acidity by studying the regulation of key steps affecting citrate metabolism, and determine the fate of citrate during acid decline stage, and (3) Studying acid and sugar homeostasis in citrus fruits by characterizing transport mechanisms across membranes. These aims were completed as the following: (1) Our initial efforts were aimed at the characterization and identification of citric acid transporters in citrus juice cells. The identification of citrate transporters at the vacuole of the citrus juice cell indicated that the steady-state citrate cytosolic concentration and the action of the cytosolic aconitase were key elements in establishing the pH homeostat in the cell that regulates the metabolic shift towards carbon usage in the fruit during the later stages of fruit development. We focused on the action of aconitase, the enzyme mediating the metabolic use of citric acid in the cells, and identified processes that control carbon fluxes in developing citrus fruits that control the fruit acid load; (2) The regulation of aconitase, catalyzing a key step in citrate metabolism, was further characterized by using two inhibitors, citramalte and oxalomalte. These compounds significantly increased citrate content and reduced the enzyme’s activity. Metabolite profiling and changes of amino-acid metabolizing enzymes in oxalomalate- treated cells suggested that the increase in citrate, caused by aconitase inhibition, induces amino acid synthesis and the GABA shunt, in accordance with the suggested fate of citrate during the acid decline stage in citrus fruit. (3) We have placed a considerable amount of time on the development of a citrus fruit proteome that will serve to identify all of the proteins in the juice cells and will also serve as an aid to the genomics efforts of the citrus research community (validating the annotation of the fruit genes and the different ESTs). Initially, we identified more than 2,500 specific fruit proteins and were able to assign a function to more than 2,100 proteins (Katz et al., 2007). We have now developed a novel Differential Quantitative LC-MS/MS Proteomics Methodology for the identification and quantitation of key biochemical pathways in fruits (Katz et al., 2010) and applied this methodology to identify determinants of key traits for fruit quality (Katz et al., 2011). We built “biosynthesis maps” that will aid in defining key pathways associated with the development of key fruit quality traits. In addition, we constructed iCitrus (http://wiki.bioinformatics.ucdavis.edu/index.php/ICitrus), a “functional database” that is essentially a web interface to a look-up table that allows users to use functional annotations in the web to identify poorly annotated citrus proteins. This resource will serve as a tool for growers and field extension specialists.

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