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

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

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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2

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 transcr

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3

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 u

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4

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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5

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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6

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

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7

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 compa

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8

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, secr

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9

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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10

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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11

Wilson, Kris. "Novel screening techniques for the discovery of human KMO inhibitors." Thesis, University of Edinburgh, 2014. http://hdl.handle.net/1842/18743.

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Kynurenine 3-monooxygenase (KMO) is an enzyme central to the kynurenine pathway of tryptophan degradation. KMO is emerging as an increasingly important target for drug development. The enzyme is implicated in the development and progression of several neurodegenerative disorders, in the regulation of the immune response and in sterile systemic inflammation. Production of recombinant human enzyme is challenging due to the presence of transmembrane domains, which localise KMO to the outer mitochondrial membrane and render KMO insoluble in many in vitro expression systems. Although several in vit

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12

Suhuai, Liu. "Novel C-linked antifreeze glycoprotein (AFGP) analogues as potent recrystallization inhibitors: Preparation, assessment and in vitro studies." Thesis, University of Ottawa (Canada), 2006. http://hdl.handle.net/10393/29359.

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Antifreeze glycoproteins (AFGPs) are a subclass of biological antifreezes found primarily in the plasma of Teleost fish inhabiting in sub-zero temperature environments. These compounds have the ability to inhibit the growth and recrystallization of ice, thus ensuring the survival of these organisms in subzero environments. This characteristic property is highly desirable for medical and commercial applications. However, the limited bioavailability and the inherent instability of native AFGPs have precluded their commercialization. Consequently, rationally designed C-linked AFGP analogues are v

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13

Stimac, Robert. "Macrocyclic Carbon Suboxide Derivatives Novel Potent Inhibitors of the Na,K-ATPase, and their Mechanism of Inhibition /." [S.l. : s.n.], 2005. http://www.bsz-bw.de/cgi-bin/xvms.cgi?SWB11729978.

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14

Di, Maria Salvatore. "Development of novel pyrazolo[3,4-d]pyrimidines as anticancer agents: synthesis of potent c-Src/Abl inhibitors." Doctoral thesis, Università di Siena, 2021. http://hdl.handle.net/11365/1140488.

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The interest in protein tyrosine kinases has increased in recent years, particularly since their oncogenicity in human cells has been recognized. Tyrosine kinases promote phosphorylation of many proteins involved in cellular signaling pathways and the deregulation of their normal activity leads to diseases, such as cancer. In this context, several pyrazolo[3,4-d]pyrimidines have been developed as Tyrosine Kinase Inhibitor (TKI) and some of them have revealed promising in vitro and in vivo antitumor activity. In this thesis I describe the work done during my three years of PhD, which conc

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15

Sekgota, Khethobole Cassius. "Design, development and evaluation of novel lead compounds as HIV-1 enzyme inhibitors." Thesis, Rhodes University, 2015. http://hdl.handle.net/10962/d1017926.

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This project has been concerned with the application of the Baylis-Hillman methodology to the synthesis of medicinally important diketo acid analogues (cinnamate ester-AZT conjugates and 3-hydroxy ester-AZT conjugates) as dual-action HIV-1 IN/RT inhibitors; and on exploratory studies in the preparation of 3-(amidomethyl)-(1H)-2-quinolones as PR inhibitors; and (1H)-2- quinolone-AZT conjugates as dual action IN/RT inhibitors. A series of Baylis-Hillman adducts has been prepared, typically in moderate to excellent yield, by reacting 2-nitrobenzaldehyde with methyl acrylate, ethyl acrylate and me

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16

Koizumi, Fumito. "Studies on the novel inhibitors of interleukin-1β converting enzyme from microbial sources". Kyoto University, 2005. http://hdl.handle.net/2433/144583.

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Kyoto University (京都大学)<br>0048<br>新制・論文博士<br>博士(農学)<br>乙第11725号<br>論農博第2574号<br>新制||農||919(附属図書館)<br>学位論文||H17||N4087(農学部図書室)<br>23622<br>UT51-2005-K529<br>(主査)教授大東肇, 教授吉川正明, 教授村田幸作<br>学位規則第4条第2項該当

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17

Darkins, Paul Anthony. "Synthesis and enzyme inhibitory properties of novel proteinase inhibitors derived from enantiopure #alpha#-diazoketones." Thesis, Queen's University Belfast, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.318839.

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18

Holt-Martyn, James. "Novel and selective small molecule inhibitors and activators for the prolyl hydroxylase domain enzyme." Thesis, University of Oxford, 2018. http://ora.ox.ac.uk/objects/uuid:4b3613c5-5ff3-43b0-a07e-cf3116a37c1b.

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Hypoxia Inducible Factors (HIF) functions are master regulators of oxygen homeostasis and have a key role in the physiological responses to hypoxia including angiogenesis and erythropoiesis. Under hypoxia, levels of HIF-α subunits increase, they hetereodimerise with HIF-1β sub unit and promote the initiation of transcription of target genes. Under normoxia, oxygen dependent HIF-α degradation is promoted by hydroxylation of either of two proline residues (Pro402 and Pro564). The interaction of prolylhydroxylated HIF-α with the Von Hippel-Lindau protein (pVHL) promotes hydrolytic degradation of

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19

Lauria, S. "THE ENDOCANNABINOID ENZYME MONOACYLGLYCEROL LIPASE: DEVELOPMENT OF A NEW FLUORESCENT ASSAY AND NOVEL INHIBITORS." Doctoral thesis, Università degli Studi di Milano, 2015. http://hdl.handle.net/2434/336675.

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The endocannabinoid system (ECS), comprising CB1/CB2 receptors, endocannabinoids (ECs) and their metabolic enzymes, FAAH (fatty acid amide hydrolase) and MAGL (monoacylglycerol lipase), is responsible for maintaining the homeostatic balance, regulating and modulating the physiological responses to improve general well-being [1]. A dysregulation of ECS is connected to pathological conditions such as pain, inflammation, anxiety, and other disorders [2]. Pharmacological blockade of FAAH and MAGL has emerged as a potentially attractive strategy to augment EC signalling and retain the beneficial ef

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20

Watermeyer, Jean Margaret. "Structural determinants of the domain-selectivity of novel inhibitors of human testis angiotensin-converting enzyme." Doctoral thesis, University of Cape Town, 2008. http://hdl.handle.net/11427/3154.

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21

Mahasenan, Kiran V. "Discovery of novel small molecule enzyme inhibitors and receptor modulators through structure-based computational design." The Ohio State University, 2012. http://rave.ohiolink.edu/etdc/view?acc_num=osu1332367560.

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22

GALBIATI, ANDREA. "DESIGN AND SYNTHESIS OF NOVEL ENZYME INHIBITORS AS ANTIPROLIFERATIVE COMPOUNDS WITH ANTIPROTOZOAL AND ANTICANCER ACTIVITY." Doctoral thesis, Università degli Studi di Milano, 2021. http://hdl.handle.net/2434/827428.

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This dissertation describes the research carried out as part of a PhD program in Chemistry from the 1st October 2017 until 30th November 2020. The PhD project investigated the development of inhibitors of enzymes involved in important metabolic pathways, with the final aim to produce an antiproliferative effect. The present thesis combines the works performed at the University of Milan and Vrije Universiteit of Amsterdam. Part A describes the research performed in Amsterdam, NL during my period abroad from January to September 2019 in the research group of Professor Rob Leurs, at the Di

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23

Lee, Yi-Chen. "Studies towards the development of novel HIV-1 integrase inhibitors." Thesis, Rhodes University, 2010. http://hdl.handle.net/10962/d1005022.

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The project has focused on the preparation of several series of compounds designed as potential HIV-1 integrase inhibitors. Various 2-nitrobenzaldehydes have been reacted with two activated alkenes, methyl vinyl ketone (MVK) and methyl acrylate, under Baylis-Hillman conditions to afford α-methylene-β-hydroxylalkyl derivatives in moderate to excellent yields. The reactions were conducted using the tertiary amine catalysts, 1,4-diazabicyclo[2.2.2]octane(DABCO) or 3-hydroxyquinuclidine (3-HQ) with chloroform as solvent, and yields were optimised by varying the catalyst, reagent concentrations and

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24

Chee, Soo Mei. "Design, synthesis and biological evaluation of the novel inhibitors of enzymes NQO1 and NQO2." Thesis, University of Manchester, 2014. https://www.research.manchester.ac.uk/portal/en/theses/design-synthesis-and-biological-evaluation-of-the-novel-inhibitors-of-enzymes-nqo1-and-nqo2(14689fca-4a77-4102-8f55-49c90be6fa72).html.

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A range of novel and potent NQO1 and NQO2 inhibitors were synthesised. A series of 4-hydroxycoumarin analogues were prepared and assayed against NQO1. Furthermore, a more efficient synthetic route was developed by employing the “borrowing hydrogen” methodology. All the synthetic unsymmetrical dicoumarol analogues were novel and potent NQO1 inhibitors with IC50¬ values in the nanomolar range. The most potent analogues were non-toxic against the non-small cell lung cancer cell line, A549.The potential NQO2 inhibitors were classified in three different groups based on their core structure: 4-amin

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25

Bailey, Helen Victoria. "Drug design and novel anti-cancer therapeutics : inhibitors of 17β hydroxysteroid dehydrogenase type 3". Thesis, University of Bath, 2007. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.512267.

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Herein, we describe the design and synthesis of novel inhibitors of 17β-hydroxysteroid dehydrogenase type 3 which convert androstenedione into testosterone, which is then converted into dihydrotestosterone (DHT). This isozyme has been implicated in the growth of prostate cancer. Using an in silico pharmacophore model initial targets were planned, based around a diphenylether hydrophobic head linked to a 4-substituted piperidine ring. Over 45 compounds were synthesised and many show significant biological activity when evaluated in a 17β-HSD type 3 biological assay. The most potent compound in

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26

Bourgeois, Karine. "Towards in vitro Pharmacokinetic Assessment of Novel Targeted Covalent Inhibitors for Human Tissue Transglutaminase." Thesis, Université d'Ottawa / University of Ottawa, 2019. http://hdl.handle.net/10393/39472.

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Human tissue transglutaminase (TG2) is a calcium-dependent multifunctional enzyme that natively catalyzes the post-translational modification of proteins, namely by the formation of isopeptide bonds between protein- or peptide-bound glutamine and lysine residues. This ubiquitously expressed enzyme plays important roles in cellular differentiation, extracellular matrix stabilization, and apoptosis, to name a few. However, its unregulated activity has been associated with many pathologies such as fibrosis, cancer, neurodegenerative disorders and celiac disease. Most of these disorders are associ

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27

Sachdeva, Sarbjot Singh. "Interactions of mtFabH with its Substrates and Inhibitors Reveal Novel Mechanistic Insights." VCU Scholars Compass, 2007. http://scholarscompass.vcu.edu/etd/1483.

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Tuberculosis emerged from its grave to be one of the deadliest diseases of the present time after recently developing a synergy with AIDS. A fatty acid condensing enzyme-mtFabH has been proposed to connect the key processes involved in biosynthesis of mycolic acids, an important component of mycobacterial cell wall. It condenses long acyl Coenzymes A (CoA; up to C20CoA) with malonyl Acyl Carrier Protein (ACP) to form the elongated β-ketoacyl-ACP which further undergoes rounds of elongation to form mero-mycolate branch of mature mycolic acids. Owing to its proposed central position in mycolic a

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28

Dotse, Anthony Kwabla. "Design, synthesis and evaluation of novel inhibitors of cysteine proteases, metalloproteases and the proteasome, a unique high molecular weight proteolytic enzyme." Diss., Georgia Institute of Technology, 1997. http://hdl.handle.net/1853/29979.

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29

Lagerlund, Olof. "Design and Synthesis of Novel Glutamine Synthetase Inhibitors and Development of Palladium(0)-Catalyzed Aminocarbonylation." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis, Uppsala universitet, 2009. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-100377.

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30

Conibear, Anne Claire. "Synthesis and evaluation of novel inhibitors of 1-Deoxy-D-xylolose-5-phosphate reductoisomerase as potential antimalarials." Thesis, Rhodes University, 2013. http://hdl.handle.net/10962/d1008282.

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Malaria continues to be an enormous health-threat in the developing world and the emergence of drug resistance has further compounded the problem. The parasite-specific enzyme, 1-deoxY-D-xylulose-S-phosphate reductoisomerase (DXR), has recently been validated as a promising antimalarial drug target. The present study comprises a combination of synthetic, physical organic, computer modelling and bioassay techniques directed towards the development of novel DXR inhibitors. A range of 2-heteroarylamino-2-oxoethyl- and 2- heteroarylamino-2-oxopropyl phosphonate esters and their corresponding phosp

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31

Guest, Patrick. "The identification and characterisation of novel inhibitors of the 17β-HSD10 enzyme for the treatment of Alzheimer's disease". Thesis, University of St Andrews, 2016. http://hdl.handle.net/10023/10398.

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In 2015, an estimated 46.8 million people were living with dementia, a number predicted to increase to 74.7 million by 2030 and 131.5 million by 2050. Whilst there are numerous causes for the development of dementia, Alzheimer's disease is by far the most common, accounting for approximately 50-70% of all cases. Current therapeutic agents against Alzheimer's disease are palliative in nature, managing symptoms without addressing the underlying cause and thus disease progression and patient death remain a certainty. Whilst the main underlying cause for the development of Alzheimer's disease was

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Lee, Alison Frances Clare. "The renin angiotensin aldosterone axis : relationships with other hormone systems, and novel applications for angiotensin converting enzyme inhibitors." Thesis, University of Edinburgh, 2000. http://hdl.handle.net/1842/22401.

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The aim of this thesis was to look at the renin angiotensin system both in clinical heart failure, and in relation to other physiological systems where an interaction may exist. Furthermore, to address new areas where a potential for benefit with Angiotensin Converting Enzyme (ACE) inhibitors might occur. To this end there are five studies discussed within the thesis. It is shown that in a group of heart failure patients, stabilised on maximum tolerated dose of ACE inhibitor, mean levels of plasma neurohormones were remarkably stable over 18 months. Reactivation of aldosterone occurred in 13/9

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Kumar, Amit. "Synthesis and biochemical evaluation of novel enzyme inhibitors as potential anti-tumour agents in the treatment of breast cancer." Thesis, University of the West of Scotland, 2011. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.739948.

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Kaur, Gurpreet. "Synthesis of Boronic Acid Based Sensors for Glucose and Sialic Acid and Synthesis of Novel and Selective PDE4 Enzyme Inhibitors." Digital Archive @ GSU, 2006. http://digitalarchive.gsu.edu/chemistry_diss/9.

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The boronic acid functional group is known to bind compounds with the diol group tightly and reversibly in aqueous environment and has been used as a recognition moiety for the design of carbohydrate sensors. The first chapter of the dissertation studies the synthesis and substitution effect on the affinity and selectivity of a known boronic acid-based glucose sensor. In such a sensor design effort, the availability of a signaling event, whether it is fluorescence or UV, is crucial. The second chapter studies the detailed mechanism on how a well-known fluorescent boronic acid compound change

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35

Mohamed, Ebrahim. "Probing the HIV reverse-transcriptase enzyme with novel bifunctional HIV-1 RT inhibitors of the general formula (NRTI)-spacer-(NNRTI)." Doctoral thesis, University of Cape Town, 2009. http://hdl.handle.net/11427/12152.

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Includes abstract.<br>Includes bibliographical references (leaves 224-233).<br>The high levels of resistance elicited by both nucleoside (NRTI) and non-nucleoside (NNRTI) reverse transcriptase inhibitors have prompted the design of double-drugs combining these two entities with the aim of addressing the emergence of resistance as well as searching for synergism between the two drug target sites on HIV reverse transcriptase (RT). The strategy involves combining two different inhibitors into a single chemical entity via a linker, with the aim of developing a mixed-site inhibitor combining the in

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Nichols, Derek Allen. "Structure-Based Design of Novel Inhibitors and Ultra High Resolution Analysis of CTX-M Beta-Lactamase." Scholar Commons, 2014. https://scholarcommons.usf.edu/etd/5284.

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The emergence of CTX-M class-A extended-spectrum β-lactamases, which confer resistance to second and third-generation cephalosporins, poses a serious health threat to the public. CTX-M β-lactamases use a catalytic serine to hydrolyze the β-lactam ring. Specifically, the hydrolysis reaction catalyzed by CTX-M β-lactamase proceeds through a pre-covalent complex, a high-energy tetrahedral acylation intermediate, a low-energy acyl-enzyme complex, a high-energy tetrahedral deacylation intermediate after attack via a catalytic water, and lastly, the hydrolyzed β-lactam ring product which is released

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Hirsilä, M. (Maija). "Characterization of the novel human prolyl 4-hydroxylases and asparaginyl hydroxylase that modify the hypoxia-inducible factor." Doctoral thesis, University of Oulu, 2004. http://urn.fi/urn:isbn:9514275756.

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Abstract HIF prolyl 4-hydroxylases (HIF-P4Hs) and HIF asparaginyl hydroxylase (FIH) are novel members of the 2-oxoglutarate dioxygenase family that play key roles in the regulation of the hypoxia-inducible transcription factor (HIF). They hydroxylate specific proline and asparagine residues in HIF-α, leading to its proteasomal degradation and inhibition of its transcriptional activity, respectively. These enzymes are inhibited in hypoxia, and as a consequence HIF-α becomes stabilized, forms a dimer with HIF-β, attains its maximal transcriptional activity and induces expression of many genes th

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Srinivasan, Sheila. "The design and synthesis of novel heterocyclic inhibitors of the DNA-repair enzyme, poly(ADP-ribose) polymerase, as potential resistance-modifying agents." Thesis, University of Newcastle Upon Tyne, 1997. http://hdl.handle.net/10443/1022.

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The abundant nuclear enzyme, poly(ADP-ribose) polymerase (PARP) is activated by DNA strand breaks and catalyses the transfer of ADP-ribose moieties from its substrate, nicotinamide adenine dinucleotide (NAD), to various histone- or non-histone nuclear acceptor proteins. The net result is the formation of long, homopolymeric chains, the exact purpose of which is not clearly understood. Since this process is thought to facilitate DNA repair, the PARP enzyme represents a possible therapeutic target. A well known mechanism by which tumours become resistant to anticancer treatments is increased DNA

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Pirrie, Lisa. "Development of novel active site and allosteric inhibitors of enzymes associated with cancer, neurodegenerative diseases and bacterial infections." Thesis, University of St Andrews, 2013. http://hdl.handle.net/10023/3471.

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The sirtuins are a family of NAD⁺-dependent deacetylase enzymes which are implicated in various illnesses including cancer and neurodegenerative diseases. Part I of this thesis describes the synthesis and biological evaluation of inhibitors of the SIRT1 and SIRT2 isoforms of this important family of enzymes. Chapter 1 gives an overview of sirtuin biology and the physiological roles of these enzymes. In particular the link between SIRT1 and cancer and SIRT2 and its role in the onset of neurodegenerative diseases is discussed. A review of the most potent and selective inhibitors of SIRT1 and SIR

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Wilkinson, Brendan Luke. "Synthesis of Novel Carbohydrate Based Enzyme Inhibitor Libraries Utilising Click Chemistry." Thesis, Griffith University, 2007. http://hdl.handle.net/10072/366473.

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Within a short timeframe, the CuI-catalysed 1,3-dipolar cycloaddition (1,3-DCR) of an organic azide to a terminal acetylene to form a 1,4-disubstituted-1,2,3-triazole, has emerged as a powerful synthetic transformation in combinatorial chemistry, organic synthesis and bioconjugation research. This synthetic methodology, now known as click chemistry, has had an appreciable impact in the drug discovery and biotechnology sectors and has shown broad scope and compatibility with small molecule and polymeric substrates. The application of this powerful synthetic transformation, specifically in carbo

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Salwiński, Aleksander. "Development of novel mass spectrometry-based approaches for searching for low-mass tyrosinase inhibitors in complex mixtures." Thesis, Orléans, 2014. http://www.theses.fr/2014ORLE2013/document.

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Ce manuscrit de thèse présente le développement de méthodes basées sur la spectrométrie de masse consacrées à la recherche d'inhibiteurs d'enzymes en milieux complexes, tels que les extraits de plantes. L’enzyme Tyrosinase a été utilisé comme principale cible biologique du fait de son implication dans les processus d’hyperpigmentation cutanée. De ce fait, la recherche d’inhibiteurs de cette enzyme, présente un grand intérêt pour l'industrie cosmétique. La première partie de ce manuscrit décrit la mise en place de la chromatographie d'affinité frontale (FAC), permettant d’obtenir le classement

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Daneshpour, Nooshin. "Local and systemic delivery of a novel group of inhibitors of transglutaminase enzyme : a potential approach for treating of catheter-related complications and liver fibrosis." Thesis, Aston University, 2010. http://publications.aston.ac.uk/13343/.

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The present thesis investigates targeted (locally and systemically) delivery of a novel group of inhibitors of enzyme transglutaminases (TGs). TGs are a widely distributed group of enzymes that catalyse the formation of isopeptide bonds between the y-carboxamide group of protein-bound glutamines and the a-amino group of protein-bound lysines or polyamines. The first group of the novel inhibitors tested were the tluorescently labelled inhibitors of Factor XIIIa (FXIIIa). These small, non-toxic inhibitors have the potential to prevent stabilisation of thrombi by FXIIIa and consequently increase

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Stimac, Robert. "Macrocyclic carbon suboxide derivates : novel potent inhibitors of the Na,K-ATPase, and their mechanism of inhibition = Makrozyklische Kohlensuboxid-Derivate : neuartige, besonders wirksame Inhibitoren der Na,K-ATPase und ihr Inhibitionsmechanismus /." Konstanz, 2004. http://deposit.ddb.de/cgi-bin/dokserv?idn=974308676.

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Shahid, Imran. "Synthesis and biochemical evaluation of novel non-steroidal inhibitors of the cytochrome P450 enzyme 17α-hydroxylase/17,20-lyase in the treatment of hormone-dependent prostate cancer". Thesis, Kingston University, 2008. http://eprints.kingston.ac.uk/20397/.

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A high proportion of prostate cancers have been shown to be androgen-dependent. The biosynthesis of the androgens is catalysed by the cytochrome P450 enzyme 17[alpha]-hydroxylase/17, 20-lyase (P450[sub]17[alpha]), which is responsible for the conversion of C[sub]21 steroids (for example pregnenolone and progesterone) to the androgens (for example dehydroepiandrosterone and androstenedione respectively). The inhibition of this enzyme would therefore lead to the overall reduction in the level of androgens and thus result in an overall decrease in the stimulation of androgen-dependent cancer cell

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Slynko, Inna [Verfasser], Wolfgang [Akademischer Betreuer] Sippl, Mike [Akademischer Betreuer] Schutkowski, and Gerhard [Akademischer Betreuer] Wolber. "Structural analysis and computer-based design of novel inhibitors for human protein-kinase-C-related enzyme PRK1 / Inna Slynko. Betreuer: Wolfgang Sippl ; MIke Schutkowski ; Gerhard Wolber." Halle, Saale : Universitäts- und Landesbibliothek Sachsen-Anhalt, 2015. http://d-nb.info/1076503179/34.

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Pont, Masanet Caterina. "Multitarget strategies in search of novel drug candidates against Alzheimer’s disease." Doctoral thesis, Universitat de Barcelona, 2020. http://hdl.handle.net/10803/668672.

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Alzheimer’s disease (AD) is the most common form of dementia and one of the most important health-care problems in the world, due to its high prevalence and unaffordable personal and economic impact. Moreover, current commercialised treatments are only symptomatic, but are not capable of preventing, curing or even delaying the disease progression. Because AD arises from a complex network of pathological events, such as dysfunction in neurotransmitter systems (mainly cholinergic and glutamatergic), β-amyloid and tau proteins disorders, oxidative stress or neuroinflammation, amongst others, the

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Evitt, Andrew. "Design, Synthesis & Evaluation of Inhibitors & Substrates of the Enzyme L-Aspartate-/B-Semialdehyde Dehydrogenase AND A Novel Synthetic Route to Deoxyxylulose-5-Phosphate - a Substrate of Deoxyxyluiose-5-Phosphate Reductase." Thesis, University of Bristol, 2009. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.520640.

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Yang, Chou-Chih, and 楊宙芝. "Structure-based screening on novel potent inhibitors for Prephenate Dehydratase (PDT) of Buchnera aphidicola." Thesis, 2009. http://ndltd.ncl.edu.tw/handle/69909665781183100620.

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碩士<br>國立彰化師範大學<br>生物學系<br>97<br>Aphids are insect vectors which transmit virus and damage agricultural economy. Aphids feed strictly on the nutritionally poor diet of phloem sap by piercing-sucking mouthparts, and thus maintain an obligate endosymbiotic association with Buchnera aphidicola, a member of the class -Proteobacteria closely related to Escherichia coli. It is commonly accepted that Buchnera provides essential nutrients to aphids. The enzyme prephenate dehydratase (PDT) is encoded by pheA, and is a terminal and committed enzyme in the biosynthesis of L-Phe in the shikimate pathway.

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Teng, Lead-Well, and 鄧力瑋. "Virtual screening and 3D-QSAR study on novel potent inhibitors for nuclear factor kappa B." Thesis, 2008. http://ndltd.ncl.edu.tw/handle/27473293793089737205.

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碩士<br>國立彰化師範大學<br>生物技術研究所<br>96<br>NF-κB (nuclear factor-kappa B) is an important transcription factor. It is found in almost all animal cell types and is involved in cellular responses to stimuli such as stress, ultraviolet irradiation, and bacterial or viral antigens. NF-κB plays a key role in regulating the immune response to infection. Consistent with this role, incorrect regulation of NF-κB has been linked to cancer, inflammatory and autoimmune diseases, septic shock, viral infection, and improper immune development. Therefore, we report selective inhibitor of NF-κB activation expected wa

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Bhuyan, Bhaskar Jyoti. "Design And Synthesis Of Novel Angiotensin Converting Enzyme (ACE) Inhibitors Having Antioxidant Activity." Thesis, 2010. https://etd.iisc.ac.in/handle/2005/1339.

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Angiotensin converting enzyme (ACE) catalyzes the conversion of angiotensin I (Ang I) to angiotensin II (AngII). ACE also cleaves the terminal dipeptide of vasodilating hormone bradykinin (a nonapeptide) to its inactive form. Therefore, inhibition of ACE is one of the treatments of hypertension. A number of ACE inhibitory antihypertensive drugs are known. ‘Oxidative stress’ is another disease state caused by an imbalance in the production of oxidants and antioxidants in the body. A number of studies suggest that hypertension and oxidative stress are interdependent. Therefore, ACE inhibitors ha

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