Importance of interaction between C1 domain and lipids in protein kinase Cα activation: Hydrophobic side chain direction in isobenzofuranone ligands controls enzyme activation level

Go Hirai, Adashi Shimizu, Toru Watanabe, Yosuke Ogoshi, Megumi Ohkubo, Mikiko Sodeoka

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Substituent direction is important: Type A-D isobenzofuranone derivatives were synthesized with differently directed hydrophobic alkyl side chains. These ligands bind in a similar conformation to protein kinase Cα but have contrasting activation abilities, possibly owing to different interaction of the side chain with the membrane lipid. (Chemical Equation Presented)

Original languageEnglish
Pages (from-to)1006-1009
Number of pages4
JournalChemMedChem
Volume2
Issue number7
DOIs
Publication statusPublished - Jul 9 2007
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

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