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Inhibition of serine proteases by steroids

Biochemical Pharmacology, 1982
Proteolysis 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 ...
M, Mayer, B, Neufeld, Z, Finci
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Genomic overview of serine proteases

Biochemical and Biophysical Research Communications, 2003
Serine proteases (SP) are peptidases with a uniquely activated serine residue in the substrate-binding pocket. They represent about 0.6% of all proteins in the human genome. SP are involved in many vital functions such as digestion, blood clotting, fibrinolysis, fertilization, and complement activation and are related to many diseases including cancer,
George M, Yousef   +3 more
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Strategies for the inhibition of serine proteases

Cellular and Molecular Life Sciences, 2001
Serine 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 ...
B, Walker, J F, Lynas
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Serine proteases and cardiac function

Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, 2005
The 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.
Qingyu, Wu   +2 more
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The novel inhibitors of serine proteases

Amino Acids, 2009
Thirty optically active nonprotein alpha-amino acids and peptides based thereon have been screened for their ability to interact with bovine trypsin and proteinase K from Tritirachium album Limber, which belong to the group of serine proteases. Both structure-based drug design approach and determination of enzyme activity have been used to identify low
N, Hovhannisyan   +7 more
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Serine proteases of the complement system

Biochemical Society Transactions, 2000
The complement system in blood plasma is a major mediator of innate immune defence. The function of complement is to recognize, then opsonize or lyse, particulate materials, including bacteria, yeasts and other microrganisms, host cell debris and altered host cells.
R B, Sim, A, Laich
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Targeting Serine Proteases in Asthma

Current Topics in Medicinal Chemistry, 2006
Leukocytes 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 ...
Caroline, Guay   +2 more
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Serpins (Serine Protease Inhibitors)

Current Protocols in Protein Science, 2001
AbstractSerpins are a class of proteins involved in the regulation of serine and other types of proteases. In humans, the majority of serpins regulate the functions of proteases involved in the body's response to injury. This includes roles in coagulation, fibrinolysis, inflammation, wound healing, and tissue repair.
Susannah J, Bauman   +2 more
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Neutrophil serine proteases

Rare Disease and Orphan Drugs Journal, 2023
The identification and characterization of the four active neutrophil serine proteases (NSPs) have provided a better understanding of their roles in various physiological and pathological processes. The availability of appropriate tools such as substrates, inhibitors, and activity-based probes (ABPs) for studying their activity and functions in cells ...
Marcin Skoreński   +2 more
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On the stereochemistry of catalysis by serine proteases

Journal of Theoretical Biology, 1974
Abstract 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 ...
L, Polgár, B, Asbóth
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