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  Bivalent inhibition of beta-tryptase: Distance scan of neighboring subunits by dibasic inhibitors

Schaschke, N., Dominik, A., Matschiner, G., & Sommerhoff, C. P. (2002). Bivalent inhibition of beta-tryptase: Distance scan of neighboring subunits by dibasic inhibitors. Bioorganic & Medicinal Chemistry Letters, 12(6), 985-988.

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Item Permalink: http://hdl.handle.net/11858/00-001M-0000-0010-6F88-5 Version Permalink: http://hdl.handle.net/11858/00-001M-0000-0010-6F89-3
Genre: Journal Article
Alternative Title : Bioorg. Med. Chem. Lett.

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 Creators:
Schaschke, N.1, Author              
Dominik, A., Author
Matschiner, G., Author
Sommerhoff, C. P., Author
Affiliations:
1Moroder, Luis / Bioorganic Chemistry, Max Planck Institute of Biochemistry, Max Planck Society, ou_1565160              

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 Abstract: Based on bifunctional diketopiperazines as templates and m- aminomethyl-phenylalanine as arginine mimetic, we have synthesized a new class of structurally related dibasic tryptase inhibitors with systematically increasing spacer length. These compounds were used to scan the distance between the active sites of two neighboring subunits of the beta- tryptase tetramer. The K-i-values obtained are a function of the distance between the terminal amino groups and indicate optimal binding of inhibitors with 29-31 bonds between the amino groups. These experimental data are in full agreement with predictions derived from a novel modeling program that allows the docking of bivalent ligands. (C) 2002 Elsevier Science Ltd. All rights reserved.

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Language(s): eng - English
 Dates: 2002-03-25
 Publication Status: Published in print
 Pages: -
 Publishing info: -
 Table of Contents: -
 Rev. Method: Peer
 Identifiers: eDoc: 39317
ISI: 000175291700036
 Degree: -

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Title: Bioorganic & Medicinal Chemistry Letters
  Alternative Title : Bioorg. Med. Chem. Lett.
Source Genre: Journal
 Creator(s):
Affiliations:
Publ. Info: -
Pages: - Volume / Issue: 12 (6) Sequence Number: - Start / End Page: 985 - 988 Identifier: ISSN: 0960-894X