Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study

Masato Komoda, Hiroki Kakuta, Hiroyasu Takahashi, Yasuyuki Fujimoto, Shizuo Kadoya, Fuminori Kato, Yuichi Hashimoto

Research output: Contribution to journalArticle

60 Citations (Scopus)

Abstract

2-(2,6-Diethylphenyl)-1,2,3,4-tetrahydroisoquinoline-1,3-dione (2: PIQ-22) was found to be a potent and specific inhibitor of puromycin-sensitive aminopeptidase (PSA). Lineweaver-Burk plot analysis showed that PSA is inhibited by PIQ-22 in a non-competitive manner. Structure-activity relationship studies indicated that tautomerism of the imidobenzoylketone group in the cyclic imide moiety of the PIQ-22 skeleton is important for the inhibitory activity.

Original languageEnglish
Pages (from-to)121-131
Number of pages11
JournalBioorganic and Medicinal Chemistry
Volume9
Issue number1
DOIs
Publication statusPublished - Jan 8 2001
Externally publishedYes

ASJC Scopus subject areas

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

Fingerprint Dive into the research topics of 'Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study'. Together they form a unique fingerprint.

  • Cite this