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In search of selective inhibitors of cysteine protease, cathepsin K

In English

Författare

Summary, in English

Two potential azapeptide inhibitors of cathepsin K were designed and synthesized. To analyze in detail interactions between these azainhibitors and the investigated cysteine protease, molecular dynamics simulations were performed. For the obtained compounds the equilibrium constants for dissociation of inhibitor-enzyme complex, K-i, were determined. The examined azapeptides proved to be not as potent inhibitors of cathepsin K as they were expected to be according to the results of simulations. However, these calculations provide valuable information about probable structures of this type of peptidomimetics in the catalytic pocket of cathepsin K, which could be useful in designing of more selective inhibitors of this cysteine protease.

Publiceringsår

2005

Språk

Engelska

Sidor

203-209

Publikation/Tidskrift/Serie

International Journal of Peptide Research and Therapeutics

Volym

11

Issue

3

Dokumenttyp

Artikel i tidskrift

Förlag

Springer

Ämne

  • Medicinal Chemistry
  • Pharmacology and Toxicology

Nyckelord

  • cysteine protease
  • azapeptide
  • cathepsin K
  • inhibitor
  • dynamics
  • molecular

Status

Published

ISBN/ISSN/Övrigt

  • ISSN: 1573-3904