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Importance of Interaction between C1 Domain and Lipids in Protein Kinase Cα Activation: Hydrophobic Side Chain Direction in Isobenzofuranone Ligands Controls Enzyme Activation Level
Author(s) -
Hirai Go,
Shimizu Tadashi,
Watanabe Toru,
Ogoshi Yosuke,
Ohkubo Megumi,
Sodeoka Mikiko
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200700080
Subject(s) - side chain , substituent , chemistry , alkyl , enzyme , domain (mathematical analysis) , protein–protein interaction , stereochemistry , biochemistry , organic chemistry , polymer , mathematical analysis , mathematics
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.