Abstract

Simple bisubstrate analogs, Ad-E1-Gn, Ad-E2-Gn, and Ad-E3-Gn, are designed to be proto-type adenine-arginine mimetic structures. Both Ad-E1-Gn and Ad-E2-Gn inhibit PKA with IC50 values similar to that of adenosine at 100 μM ATP and are more potent inhibitors than adenosine at physiologically relevant 2 mM ATP. Ad-E3-Gn is 10-fold less potent than the other two analogs.

Original languageEnglish (US)
Pages (from-to)899-902
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume6
Issue number7
DOIs
StatePublished - Apr 9 1996

ASJC Scopus subject areas

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

Fingerprint Dive into the research topics of 'Adenine-arginine mimetics as bisubstrate analog inhibitors of cAMP-dependent protein kinase'. Together they form a unique fingerprint.

  • Cite this