Structure-guided design, synthesis and in vitro evaluation of a series of pyrazole-based fatty acid binding protein (FABP) 3 ligands

Yoko Beniyama, Kenji Matsuno, Hiroyuki Miyachi

Research output: Contribution to journalArticlepeer-review

18 Citations (Scopus)

Abstract

We designed a series of pyrazole-based carboxylic acids as candidate ligands of heart fatty acid binding protein (H-FABP, or FABP3), based on a comparison of the X-ray crystallographic structures of adipocyte fatty acid binding protein (FABP4)-selective inhibitor (BMS309403) complex and FABP3-elaidic acid complex. Some of the synthesized compounds exhibited dual FABP3/4 ligand activity, and some exhibited selectivity for FABP3.

Original languageEnglish
Pages (from-to)1662-1666
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number6
DOIs
Publication statusPublished - Mar 15 2013
Externally publishedYes

Keywords

  • FABP3
  • Heart fatty acid binding protein
  • Pyrazole
  • Structural design

ASJC Scopus subject areas

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

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