Relevant bibliographies by topics / Inhibition covalente

Contents

  1. Journal articles
  2. Dissertations / Theses
  3. Book chapters
  4. Conference papers

Academic literature on the topic 'Inhibition covalente'

Author: Grafiati
Published: 8 June 2024
Last updated: 31 July 2025

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Journal articles on the topic "Inhibition covalente"

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Zimmer, Collin, Jan Brauer, Dorota Ferenc, et al. "Substitution-Induced Mechanistic Switching in SNAr-Warheads for Cysteine Proteases." Molecules 29, no. 11 (2024): 2660. http://dx.doi.org/10.3390/molecules29112660.

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The aim of this study was to investigate the transition from non-covalent reversible over covalent reversible to covalent irreversible inhibition of cysteine proteases by making delicate structural changes to the warhead scaffold. To this end, dipeptidic rhodesain inhibitors with different N-terminal electrophilic arenes as warheads relying on the SNAr mechanism were synthesized and investigated. Strong structure–activity relationships of the inhibition potency, the degree of covalency, and the reversibility of binding on the arene substitution pattern were found. The studies were complemented
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Ma, Xingchuan. "Abstract 4462: Covalent inhibition of eIF4E: A computational approach." Cancer Research 85, no. 8_Supplement_1 (2025): 4462. https://doi.org/10.1158/1538-7445.am2025-4462.

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Abstract Covalent docking has emerged as a promising strategy for targeting challenging protein residues. Specifically, lysine residues, which are often overlooked due to their lower nucleophilicity compared to cysteines, have shown potential in the development of covalent inhibitors for eukaryotic translation initiation factor 4E (eIF4E), a critical regulator of protein synthesis implicated in breast cancers. Leveraging aryl sulfonyl fluorides, recent studies had successfully docked to K162 within eIF4E and shown reduced protein activity, but the molecules had faced significant specificity an
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Aljoundi, Aimen, Ahmed El Rashedy, Patrick Appiah-Kubi та Mahmoud E. S. Soliman. "Coupling of HSP72 α-Helix Subdomains by the Unexpected Irreversible Targeting of Lysine-56 over Cysteine-17; Coevolution of Covalent Bonding". Molecules 25, № 18 (2020): 4239. http://dx.doi.org/10.3390/molecules25184239.

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Covalent inhibition has recently gained a resurgence of interest in several drug discovery areas. The expansion of this approach is based on evidence elucidating the selectivity and potency of covalent inhibitors when bound to particular amino acids of a biological target. The unexpected covalent inhibition of heat shock protein 72 (HSP72) by covalently targeting Lys-56 instead of Cys-17 was an interesting observation. However, the structural basis and conformational changes associated with this preferential coupling to Lys-56 over Cys-17 remain unclear. To resolve this mystery, we employed st
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Peng, Huayong, Chenliang Chu, Lu Jin, et al. "Study on Oleum cinnamomi Inhibiting Cutibacterium acnes and Its Covalent Inhibition Mechanism." Molecules 29, no. 13 (2024): 3165. http://dx.doi.org/10.3390/molecules29133165.

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Oleum cinnamomi (OCM) is a volatile component of the Cinnamomum cassia Presl in the Lauraceae family, which displays broad-spectrum antibacterial properties. It has been found that OCM has a significant inhibitory effect against Cutibacterium acnes (C. acnes), but the precise target and molecular mechanism are still not fully understood. In this study, the antibacterial activity of OCM against C. acnes and its potential effect on cell membranes were elucidated. Metabolomics methods were used to reveal metabolic pathways, and proteomics was used to explore the targets of OCM inhibiting C. acnes
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Liu, S. Q., and P. A. Knauf. "Lys-430, site of irreversible inhibition of band 3 Cl- flux by eosin-5-maleimide, is not at the transport site." American Journal of Physiology-Cell Physiology 264, no. 5 (1993): C1155—C1164. http://dx.doi.org/10.1152/ajpcell.1993.264.5.c1155.

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Although eosin-5-maleimide (EM) covalently labels band 3 and has been thought to react at the external-facing anion transport site, EM reversibly inhibits Cl- exchange at 0 degrees C in a noncompetitive fashion, indicating that under these conditions it does not bind to the transport site [Knauf, P.A., N.M. Strong, J. Penikas, R.B. Wheeler, Jr., and S.J. Liu. Am. J. Physiol. 264 (Cell Physiol. 33): C1144-C1154 1993]. To see whether or not the covalent labeling by EM takes place at the same noncompetitive site as the reversible binding, we examined the dependence of reaction rate on EM concentr
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Yang, Jianhong, Yong Li, Wei Yan та ін. "Covalent modification of Cys-239 in β-tubulin by small molecules as a strategy to promote tubulin heterodimer degradation". Journal of Biological Chemistry 294, № 20 (2019): 8161–70. http://dx.doi.org/10.1074/jbc.ra118.006325.

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Clinical microtubule-targeting drugs are functionally divided into microtubule-destabilizing and microtubule-stabilizing agents. Drugs from both classes achieve microtubule inhibition by binding different sites on tubulin and inhibiting or promoting polymerization with no concomitant effects on the protein levels of tubulin heterodimers. Here, we have identified a series of small molecules with diverse structures potentially representing a third class of novel tubulin inhibitors that promote degradation by covalent binding to Cys-239 of β-tubulin. The small molecules highlighted in this study
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Maksimenko, A. V., and R. Sh Beabealashvili. "Theoretical Grounding and Formation of Experimental Approaches to Hyaluronidase Structure Consolidation due to Its Computational Interactions with Shortchain Glycosaminoglycan Ligands." Биоорганическая химия 49, no. 4 (2023): 369–83. http://dx.doi.org/10.31857/s0132342323020161.

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The computational study of 3D model hyaluronidase interaction with shortchain glycosaminoglycan ligands demonstrated the diversity and significance of their reaction on enzyme structure. It has been realized due to electrostatic noncovalent interactions (without specific coupling with active site) inducing the perceptible conformational alterations of biocatalyst molecule. As a result of this the inactivation and stabilization of enzyme globule are observed, change of inhibition of biocatalyst by heparin. The binding of chondroitin trimers (on centers cn6, cn3, cn1) to hyaluronidase molecular
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Bhatia, Sumeena, Steven C. Almo, Stanley G. Nathenson, and Richard J. Hodes. "Dynamic equilibrium of B7-1 dimers and monomers is important for regulation of TCR/CD28 – mediated T cell activation (33.28)." Journal of Immunology 182, no. 1_Supplement (2009): 33.28. http://dx.doi.org/10.4049/jimmunol.182.supp.33.28.

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Abstract Under steady state conditions, B7-1 is present as a mixed population of non-covalent dimers and monomers on the cell surface. Here we have examined the physiological significance of this unique dimer-monomer equilibrium state of B7-1. We demonstrate that altering B7-1 to uniformly covalent dimeric state results in increased frequency of CD28 mediated T cell-APC conjugates. This augmented T cell-APC conjugate formation correlates with persistent concentration of signaling molecules, PKC-θ and lck, at the immunological synapse (IS) and with a higher calcium flux in T cells. In contrast,
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Kuznetsova, Anastasiya, Philipp Klein, and Till Opatz. "Halogenated 2,1,3-benzoxadiazoles as Potential Fluorescent Warheads for Covalent Protease Inhibitors." Proceedings 9, no. 1 (2018): 54. http://dx.doi.org/10.3390/ecsoc-22-05670.

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Recently there has been a growing interest in covalent protease inhibitors in both industry and academia, caused by their longer residence times, their higher potency and their high ligand efficiency. Covalently reactive moieties which interact with activated amino acid residues such as serine or cysteine in enzymes like proteases or esterases mostly act through nucleophilic addition, substitution or ring opening. In contrast, nucleophilic aromatic substitution (SNAr) is rarely employed. In our previous work, we prepared and investigated electrophilic “warheads”, which contain aromatic, hetero
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Bisconte, Angelina, Ronald Hill, Michael Bradshaw, et al. "Efficacy in collagen induced arthritis models with a selective, reversible covalent Bruton’s tyrosine kinase inhibitor PRN473 is driven by durable target occupancy rather than extended plasma exposure (THER5P.904)." Journal of Immunology 194, no. 1_Supplement (2015): 139.6. http://dx.doi.org/10.4049/jimmunol.194.supp.139.6.

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Abstract Bruton’s Tyrosine Kinase (BTK) is an essential signaling element downstream of the B-cell receptor (BCR). Inhibition of BTK activity in B cells produces phenotypic changes consistent with blockade of the BCR, including inhibition of cell proliferation, differentiation, maturation, and survival. A selective BTK inhibitor has the potential to treat diseases involving inflammation and autoimmunity. Using Principia Biopharma’s proprietary Tailored Covalency™ technology, we discovered PRN473, a reversible covalent BTK inhibitor that selectively binds BTK with a slow off-rate as assessed in
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Dissertations / Theses on the topic "Inhibition covalente"

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Fındık, Volkan. "Simulations atomistiques de la réaction d’acétylation d’amines et de l’inhibition covalente de l’enzyme Phosphoinositide 3-kinase (PI3K)." Electronic Thesis or Diss., Université de Lorraine, 2022. http://www.theses.fr/2022LORR0266.

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Les inhibiteurs covalents ciblés (TCI) sont très prometteurs pour la recherche de nouveaux médicaments. Ils offrent un certain nombre d’avantages par rapport aux inhibiteurs réversibles traditionnels, comme un temps de séjour prolongé, une puissance accrue et la possibilité d’apporter des modifications pour une conception efficace. Les inhibiteurs de kinases sont les exemples les plus courants d’ITC. Les enzymes phosphoinositide 3-kinase (PI3K) sont des cibles médicamenteuses importantes en oncologie car elles sont impliquées dans la voie de signalisation de nombreuses fonctions cellulaires te
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Akbar, Abdullah. "Design, Synthesis and Evaluation of Covalent Inhibitors for Tissue Transglutaminase and Factor XIIIa." Thesis, Université d'Ottawa / University of Ottawa, 2019. http://hdl.handle.net/10393/39645.

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Transglutaminases are a family of enzymes expressed in various tissues of our body. Some are expressed ubiquitously while others are specific to a tissue. Their primary catalytic activity is to crosslink substrates via an isopeptidic bond. The work described in this thesis focuses on two of these transglutaminases; human tissue transglutaminase (hTG2) and human factor XIIIa (FXIIIa). Divided into two projects for each enzyme, the main objective of this thesis was directed towards the discovery of potent and selective covalent inhibitors for each isozyme, namely hTG2 and hFXIIIa. The first proj
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Belghazi, Maya. "Etude de modifications covalentes de protéines par spectrométrie de masse Maldi-Tof et Esi-Tof." Palaiseau, Ecole polytechnique, 2001. http://www.theses.fr/2001EPXX0030.

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La spectrométrie de masse MALDI-TOF (matrix-assisted laser desorption/ionization- time of flight) et ESI-TOF (electrospray ionization- time of flight) permettent d'accéder à des méthodologies performantes pour l'étude de la structure primaire des protéines. Ce travail a mis en oeuvre ces deux modes d'ionisation pour étudier les modifications covalentes de trois protéines impliquées dans des contextes biologiques différents. En premier lieu, les modifications post-traductionnelles de deux nitrile hydratases (NHases), métalloenzymes bactériennes catalysant l'hydrolyse de nitriles en amides, ont
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Erdmann, Alexandre. "Conception, synthèse et caractérisation de nouveaux inhibiteurs de méthyltranférases d'ADN à visée anticancéreuse." Thesis, Toulouse 3, 2015. http://www.theses.fr/2015TOU30270.

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Le domaine de l'épigénétique couvre l'ensemble des phénomènes héritables et transmissibles qui interviennent dans l'expression du génome sans modifier la séquence nucléotidique. L'information épigénétique est régulée par les modifications de la chromatine impliquant les histones et l'ADN. La méthylation de l'ADN est un phénomène réversible jouant un rôle crucial dans l'expression des gènes puisque la méthylation des promoteurs de gènes empêche leur transcription. La modulation aberrante de cette marque épigénétique est associée à diverses pathologies telles que le cancer. Cette méthylation éta
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Ueda, Tsuyoshi. "Development of Covalent Inhibitors and Drug Screening using Ligand-Directed NASA Chemistry." Doctoral thesis, Kyoto University, 2020. http://hdl.handle.net/2433/253248.

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京都大学<br>0048<br>新制・課程博士<br>博士(工学)<br>甲第22412号<br>工博第4673号<br>新制||工||1729(附属図書館)<br>京都大学大学院工学研究科合成・生物化学専攻<br>(主査)教授 浜地 格, 教授 森 泰生, 教授 生越 友樹<br>学位規則第4条第1項該当<br>Doctor of Philosophy (Engineering)<br>Kyoto University<br>DGAM
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Vermeer, Lydia Maria Mexas. "Covalent modification and inhibition of tyrosine hydroxylase by 3,4-dihydroxyphenylacetaldehyde, an endogenously produced neurotoxin relevant to Parkinson's disease." Diss., University of Iowa, 2012. https://ir.uiowa.edu/etd/1923.

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Parkinson's disease (PD) is a prevalent neurodegenerative disorder which affects over a million people in the United States. This disease is marked by the selective loss of dopaminergic neurons in the substantia nigra, leading to a decrease in the important neurotransmitter dopamine (DA), which is essential for the initiation and execution of coordinated movement. Currently, the pathogenesis behind PD is unknown, but there is evidence that both exogenous causes, such as pesticides and metals, as well as endogenous causes, such as reactive oxygen species or reactive metabolism intermediates, ma
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Tay, Sew Wah. "Factors affecting the thrombin inhibiting activity of heparin when immobilised to hydrogels by covalent bonding." Thesis, Massachusetts Institute of Technology, 1986. http://hdl.handle.net/1721.1/16490.

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Thesis (Sc. D.)--Massachusetts Institute of Technology, Dept. of Applied Biological Sciences, 1986.<br>MICROFICHE COPY AVAILABLE IN ARCHIVES AND SCIENCE.<br>Bibliography: leaves 157-166.<br>by Sew-Wah Tay.<br>Sc.D.
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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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CAMPANER, ELENA. "A new covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action." Doctoral thesis, Università degli Studi di Trieste, 2017. http://hdl.handle.net/11368/2908180.

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In the last decades targeted drugs have improved cancer treatment, but revealed to be ineffective mainly in the treatment of solid tumors, largely because of tumor heterogeneity, activation of redundant pathways, and drug resistance. A common and central signal transduction mechanism in many oncogenic pathways is the phosphorylation of proteins at serine or threonine residues followed by proline (S/T-P). Importantly, the phospho-S/T-P motifs of these proteins are recognized by the peptidyl-prolyl cis/trans isomerase (PPIase) PIN1, which catalyzes the cis-trans or trans-cis conformational chang
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Serrano, Aparicio Natalia. "Inhibition studies on the human 20S proteasome: molecular insights from a computational approach." Doctoral thesis, Universitat Jaume I, 2022. http://dx.doi.org/10.6035/14122.2022.684242.

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The human 20S proteasome activity and malfunction has been related to numerous diseases and validated as a protein target for inhibition in the treatment of cancer, with three proteasome inhibitors approved as a drug. But these compounds could be improved, since usually the molecular mechanism of action is unknown. Thus, computational studies can clarify the mode of action of proteasome inhibitors, helping to understand the system and improve the inhibition process The present thesis is devoted to understand the mode of action of two classes of covalent inhibitors of the 20S proteasome, α,β-ep
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Book chapters on the topic "Inhibition covalente"

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de Bruin, Gerjan, and Tjeerd Barf. "CHAPTER 4. Covalent Inhibition of Kinases." In Drug Discovery. Royal Society of Chemistry, 2018. http://dx.doi.org/10.1039/9781788013093-00061.

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Mehdi, Shujaath. "COVALENT ENZYME INHIBITION IN DRUG DISCOVERY AND DEVELOPMENT." In Enzyme Technologies. John Wiley & Sons, Inc, 2013. http://dx.doi.org/10.1002/9781118739907.ch3.

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Alexander, Patrick, and Andrew G. Stephen. "Affinity Measurement of Non-covalent Interactions of the Covalent KRAS G12C GDP Inhibitor MRTX849 to RAS Isoforms Using Surface Plasmon Resonance." In Methods in Molecular Biology. Springer US, 2024. http://dx.doi.org/10.1007/978-1-0716-3822-4_8.

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Potier, Noelle, Patrick Barth, Denis Tritsch, Jean-François Biellmann, and Alain Van Dorsselaer. "Study of Non-Covalent Enzyme-Inhibitor Complexes of Aldose Reductase by Electrospray Mass Spectrometry." In Advances in Experimental Medicine and Biology. Springer US, 1996. http://dx.doi.org/10.1007/978-1-4615-5871-2_51.

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Crawford, James J., and Haiming Zhang. "Discovery and Development of Non-Covalent, Reversible Bruton’s Tyrosine Kinase Inhibitor Fenebrutinib (GDC-0853)." In ACS Symposium Series. American Chemical Society, 2019. http://dx.doi.org/10.1021/bk-2019-1332.ch009.

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Liedtke, Harald, and Günter Legler. "Splenic Glucocerebrosidase and Its Cytosolic Activator Protein: Effects on Substrate Hydrolysis and Covalent Inhibition by Conduritol B Epoxides." In Lipid Storage Disorders. Springer US, 1988. http://dx.doi.org/10.1007/978-1-4613-1029-7_43.

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Surh, Y. J. "Chemopreventative Activity of Chlorophyllin: Inhibition of Mutagenicity and Covalent DNA Binding of Benzo[a]pyrene-7,8-dihydrodiol-9,10-epoxide." In Advances in Experimental Medicine and Biology. Springer US, 1994. http://dx.doi.org/10.1007/978-1-4899-0939-8_28.

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Kalgutkar, Amit S., Brenda C. Crews, Scott W. Rowlinson, Carlos Garner, and Lawrence J. Marnett. "Discovery of a New Class of Selective Cyclooxygenase-2 (COX-2) Inhibitor that Covalently Modifies the Isozyme." In Advances in Experimental Medicine and Biology. Springer US, 1999. http://dx.doi.org/10.1007/978-1-4615-4793-8_21.

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Yingsung, Wannarat, Lisheng Zhuo, Masahiko Yoneda, Naoki Ishiguro, Hisashi Iwata, and Koji Kimata. "The covalent complex formation of hyaluronan with heavy chains of inter-α-trypsin inhibitor family is important for its functions." In The Many Faces of Osteoarthritis. Birkhäuser Basel, 2002. http://dx.doi.org/10.1007/978-3-0348-8133-3_20.

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Zeller, Hans-Dieter, and Sandro Ghisla. "Inactivation of general acyl-CoA dehydrogenase from pig k i dney by the suicide substrate methylenecyclopropylacetyl - CoA. Stucture of one of the covalent flavin-inhibitor adducts." In Flavins and Flavoproteins 1987, edited by D. E. Edmondson and D. B. McCormick. De Gruyter, 1987. http://dx.doi.org/10.1515/9783110884715-027.

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Conference papers on the topic "Inhibition covalente"

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Holm, R., J. Eickmans, D. Holtkamp, H. J. Rother, A. Benninghoven, and Th Gantenfort. "Investigations on the Formation and Stability of Tolyltriazole and Butylbenzotriazole Inhibitor Layers on Copper with Tdms and Surface Analysis Methods." In CORROSION 1990. NACE International, 1990. https://doi.org/10.5006/c1990-90571.

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Abstract Corrosion inhibitors for copper from the triazole family strongly interact with the copper surface, leading to a layer highly resistant to many influences. Temperature Programmed Desorption Mass Spectrometry (TDMS) was applied to inhibitor layers formed under practical conditions, in order to quantify their stability. It was found that the films decompose at temperatures above 330°C. These desorption temperatures correspond to desorption energies of 40 - 45 kcal/mole, which are typical values for covalent bonds. There are no remarkable differences between benzotriazole, tolyltriazole,
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Santi, Claudio, Luca Sancineto, Francesca Mangiavacchi, Cecilia Scimmi, and Sougat Misra. "ELECTROPHILIC ORGANOSELENIUM COMPOUNDS AND SARS-COV-2: PRO-OXIDANT ACTIVITY AS A MORE PROMISING WAY TOWARDS THE DRUGGABILITY." In 1st INTERNATIONAL Conference on Chemo and BioInformatics. Institute for Information Technologies, University of Kragujevac,, 2021. http://dx.doi.org/10.46793/iccbi21.020s.

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Ebselent has been recently reported as the most efficient hinibitors of Sars-Cov-2 main protease (Mpro) thought the electrophilic covalent pro-oxidation of the reactive Cysteine 145. According to similar evidences in literature we can propose a general mechanism to explore a novel and promising application of mild organoselenium centered electrophiles in medicinal chemistry. New insights in the field of covalent and non-covalent inhibition of Mpro as well as the antiviral SARS-Cov2 activity of novel organoselenium compounds will be here discussed
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Venetsanakos, Eleni, Yan Xing, Natalie Loewenstein, et al. "Abstract 2091: PRN1371, an irreversible, covalent inhibitor of FGFR1-4 exhibits sustained pathway inhibition in cancer cell lines." In Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-2091.

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Koneti Rao, A., and Maria A. Kowalska. "ADP-INDUCED CYTOPLASMIC CALCIUM MOBILIZATION AND SHAPE CHANGE IN PLATELETS ARE MEDIATED BY DIFFERENT BINDING SITES." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644466.

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Platelet stimulation with ADP results in a number of responses including increase in cytoplasmic ionized calcium concentration [Ca2+]i, shape change, aggregation, secretion, and inhibition of cAMP accumulation caused by PGI2.5'-Fluorosulphonylbenzoyladenosine (FSBA), which covalently labels ADP binding site on platelets, blocks platelet shape change but not inhibition of cyclic AMP levels by ADP, while p-chloromercuribenzenesulfonate (pCMBS), a non-penetrating thiol reagent, blocks ADP-induced inhibition of adenylate cyclase but not shape change. We examined the effect of FSBA and pCMBS on ADP
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Poddutoori, Ramulu, Leena K. Satyam, Girish Daginakatte, et al. "Abstract C190: Potent and selective inhibition of CDK7 by novel covalent inhibitors." 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-c190.

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Satyam, Leena Khare, Ramulu Poddutoori, Subhendu Mukherjee, et al. "Abstract 3070: Potent and selective inhibition of CDK7 by novel covalent inhibitors." 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.am2016-3070.

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Yue, Zhiwei, Qiang Fu, Nancy Lang, and Chunfang Fan. "Liquid Scale Inhibitors for Metallic-Crosslinked Gel Fracturing Systems." In SPE International Oilfield Scale Conference and Exhibition. SPE, 2014. http://dx.doi.org/10.2118/spe-169806-ms.

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Abstract Scale inhibitors are important additives in fracturing fluids to help prevent mineral scale depositions during hydraulic fracturing, shut-in, and flowback stages. The inhibition mechanisms rely heavily on the interactions of certain functional groups from the inhibitor molecules and the lattice metals on the scale crystal surface. In stimulation using crosslinked gel fluids based on metallic crosslinkers, such as zirconium (Zr), titanium (Ti), or aluminum (Al), these metals form strong covalent bonds with guar and guar derivatives and therefore significantly increase overall gel stabi
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Niederst, P. N., M. Asbach, M. Ott, and R. E. Zimmermann. "IN VITRO REACTION MODELS OF THROMBIN AND ITS PHYSIOLOGICAL INHIBITOR ANTITHROMBIN III IN THE PRESENCE OF HEPARIN." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644356.

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Antithrombin III (AT III) neutralizes thrombin and other serine proteases of plasma coagulation system by forming a stable 1:1 covalent complex. The inhibition rates are greatly increased by the potent catalyst heparin. The catalytic mechanism of heparin was studied in the presence of dextran sulfate (DS), a thrombin-binding sulfated Polysaccharid. DS did not influence the reaction of AT III with heparin and the amidolytic activity of thrombin, but preincubation with thrombin could inhibit the catalytic activity of heparin in the reaction of thrombin with AT III. We conclude that the reaction
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Simone, E. R., T. A. Davies, N. A. Zabe, S. M. Greenberg-seperaky, and N. E. Larsen. "EARLY PLATELET-THROMBIN RECEPTORS AND THEIR FUNCTIONS." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643730.

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Human platelets possess less than 1000 high affinity [Kd=10-9]and 50-100,000 receptors of lower [Kd=10-7] affinity for o(α-thrombin. The selective derivatization of thrombin with the bifunctional crosslinking agent, DNCO, has enabled us to identify these receptorsvia covalent binding of either active siteinhibited tosyllyslmethylketothrombin (TLCK-T) or active Ctf-thrombin (T).Kinetic studies of the inhibition of the platelet-thrombin response by covalently and noncovalently bound TLCK-T have helped to elucidate the roles of the high and low affinity thrombin receptors. The activation paramete
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Kosmachevskaya, Olga, Elvira Nasybullina, Konstantin Shumaev, and Alexey Topunov. "HEMOGLOBIN-BOUND DYNITROSIL IRON COMPLEXES PROTECT IT FROM OXIDATIVE MODIFICATION." In NEW TECHNOLOGIES IN MEDICINE, BIOLOGY, PHARMACOLOGY AND ECOLOGY. Institute of information technology, 2021. http://dx.doi.org/10.47501/978-5-6044060-1-4.51.

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Abstract:
Under the action of peroxynitrite, DNICs associated with hemoglobin are dose-dependently destroyed, while inhibiting the oxidation of tryptophan and tyrosine residues, the formation of carbonyl derivatives, preventing the formation of covalent cross-links between subunits, and preventing the degradation of the heme group.
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