NDLI: Inhibitors of human heart chymase based on a peptide library.

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Inhibitors of human heart chymase based on a peptide library.

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Inhibitors of human heart chymase based on a peptide library.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Abeles, R. H. Bastos, M. Maeji, N. J.
Description	Author Affiliation: Bastos M ( Brandeis University Graduate Department of Biochemistry, Waltham, MA 02254, USA.);
Abstract	We have synthesized two sets of noncleavable peptide-inhibitor libraries to map the S and S' subsites of human heart chymase. Human heart chymase is a chymotrypsin-like enzyme that converts angiotensin I to angiotensin II. The first library consists of peptides with 3-fluorobenzylpyruvamides in the P1 position. (Amino acid residues of substrates numbered P1, P2, etc., are toward the N-terminal direction, and P'1, P'2, etc., are toward the C-terminal direction from the scissile bond.) The P'1 and P'2 positions were varied to contain each one of the 20 naturally occurring amino acids and P'3 was kept constant as an arginine. The second library consists of peptides with phenylalanine keto-amides at P1, glycine in P'1, and benzyloxycarbonyl (Z)-isoleucine in P4. The P2 and P3 positions were varied to contain each of the naturally occurring amino acids, except for cysteine and methionine. The peptides of both libraries are attached to a solid support (pins). The peptides are evaluated by immersing the pins in a solution of the target enzyme and evaluating the amount of enzyme absorbed. The pins with the best inhibitors will absorb most enzyme. The libraries select the best and worst inhibitors within each group of peptides and provide an approximate ranking of the remaining peptides according to Ki. Through this library, we determined that Z-Ile-Glu-Pro-Phe-CO2Me and (F)-Phe-CO-Glu-Asp-ArgOMe should be the best inhibitors of chymase in this collection of peptide inhibitors. We synthesized the peptides and found Ki values were 1 nM and 1 microM, respectively. The corresponding Ki values for chymotrypsin were 10 nM and 100 microM. The use of libraries of inhibitors has advantages over the classical method of synthesis of potential inhibitors in solution: the libraries are reusable, the same libraries can be used with a variety of different serine proteases, and the method allows the screening of hundreds of compounds in short periods of time.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	15
Volume Number	92
Language	English
Publisher	National Academy of Sciences
Publisher Date	1995-08-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Myocardium Enzymology Peptides Pharmacology Serine Endopeptidases Serine Proteinase Inhibitors Amino Acid Sequence Binding Sites Drug Effects Chymases Evaluation Studies As Topic Isoleucine Analogs & Derivatives Molecular Sequence Data Phenylalanine Pyruvates Chemistry Reproducibility Of Results Comparative Study Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S. Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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