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Targeting Serine Proteases in Asthma
Current Topics in Medicinal Chemistry, 2006Leukocytes and lung structural cells contribute to the pathophysiology of asthma through the production of numerous mediators including serine proteases. Such proteases include mast cell tryptase and chymase; neutrophil elastase, cathepsin G and myeloblastin (proteinase 3); bronchial epithelial cell-derived transmembrane protease, serine 11D (human ...
Michel Laviolette +2 more
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On the stereochemistry of catalysis by serine proteases
Journal of Theoretical Biology, 1974Abstract From stereochemical considerations and model building the following conclusions were drawn for the stereochemistry of the catalytic steps of chymotrypsin and subtilisin. (1) In contrast to previous stereochemical investigations, rotation of 120° or more of the oxygen atom of the “reactive” serine residue is not possible in the course of the ...
László Polgár, Bence Asboth
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Inversion of enantioselectivity of serine proteases
Recueil des Travaux Chimiques des Pays-Bas, 1995AbstractThe enantioselectivity of serine proteases in the transesterification of N‐acetyl‐(D,L)‐ phenylalanine esters with propan‐1‐ol in cyclohexane is strongly influenced by the leaving ability of the alcoholate group. Moreover the enantioselectivity is greatly influenced by the addition of small amounts (0.33 M) of organic additives.
Willem Verboom +3 more
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Inhibition of serine proteases by steroids
Biochemical Pharmacology, 1982Proteolysis of 14C-labeled globin, as well as the hydrolysis of the specific substrate benzoyl tyrosine ethyl ester, by purified bovine chymotrypsin was found to be inhibited by several steroid hormones. The inhibition of chymotrypsin by the steroids was of a competitive nature, with Ki values of 9.9 x 10(-5) M for triamcinolone (9-fluoro-11 beta, 16 ...
Bilha Neufeld +2 more
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Hydrolysis of polyesters by serine proteases
Biotechnology Letters, 2005The substrate specificity of alpha-chymotrypsin and other serine proteases, trypsin, elastase, proteinase K and subtilisin, towards hydrolysis of various polyesters was examined using poly(L-lactide) (PLA), poly(beta-hydroxybutyrate) (PHB), poly(ethylene succinate) (PES), poly(ethylene adipate) (PEA), poly(butylene succinate) (PBS), poly(butylene ...
Yutaka Tokiwa, Hyun-A. Lim, Takao Raku
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Serine protease inhibitors (serpins)
Trends in Cardiovascular Medicine, 1991Inhibition of serine proteases by serpins (serpin: serine protease inhibitor) is a key mechanism for the control of proteolysis in thrombosis, shock, and inflammation. The various members of the serpin gene superfamily (α(1)-antitrypsin, ovalbumin, C1-inhibitor, antithrombin III, α(2)-antiplasmin, type-1 plasminogen-activator inhibitor, and so forth ...
Philip A. Patston, Marc Schapira
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Novel Serine Protease Inhibitors
Pharmaceutical Patent Analyst, 2012The pursuit of serine protease inhibitors as anticoagulants and anti-hepatitis C virus drugs continues to be an active area of research. Compounds such as P1-P3 macrocyclic peptides and linear peptides have been registered as potent hepatitis C virus protease inhibitors and compounds such as phenylglycinamide derivatives, substituted biaryls ...
Anilkumar R. Kore +1 more
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Serine Protease Mechanism and Specificity
ChemInform, 2002AbstractFor Abstract see ChemInform Abstract in Full Text.
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Strategies for the inhibition of serine proteases
Cellular and Molecular Life Sciences, 2001Serine proteases have been shown to play a multifarious role in health and disease. As a result, there has been considerable interest in the design and development of synthetic inhibitors of these enzymes. In view of their diverse roles in biological processing events, one of the great challenges in such endeavours has been the need to produce ...
Brian Walker, John F. Lynas
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Serine proteases and cardiac function
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, 2005The serine proteases of the trypsin superfamily are versatile enzymes involved in a variety of biological processes. In the cardiovascular system, the importance of these enzymes in blood coagulation, platelet activation, fibrinolysis, and thrombosis has been well established.
Gary Gang Deng, Hai-Chien Kuo, Qingyu Wu
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