Design and synthesis of chromogenic thiopeptolide substrates as MetAPs active site probes

Yong Mei Cui, Jing Ya Li, Ling Ling Chen, Jia Li, Qi Zhuang Ye, Fa Jun Nan

Research output: Contribution to journalArticle

6 Scopus citations

Abstract

Twenty one chromogenic thiopeptolide substrates were designed and synthesized as the active site probes and analyzed with each S1 site of mutant residues and enzymes of wild-type MetAP1s. The preliminary enzymatic experiments indicate that cysteine 70 or 202, at either Escherichia coli or human MetAP1, played a crucial role in the methionine hydrolysis.

Original languageEnglish (US)
Pages (from-to)2853-2861
Number of pages9
JournalBioorganic and Medicinal Chemistry
Volume12
Issue number11
DOIs
StatePublished - Jun 1 2004

    Fingerprint

Keywords

  • Chromogenic thiopeptolide substrates
  • Methionine aminopeptidases

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this