Evaluation of series of isobenzofuranone dimers as PKCα ligands: Implication for the distance between the two ligand binding sites

Abstract Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. To examine the distance between the two ligand binding sites (C1A and C1B) of PKC, we designed and synthesized two series of isobenzofuranone dimers. Peak binding activities were observed for the C3-acyl chain dimers having a C 10 –C 12 linker and for the C7 dimers having a C 14 –C 16 .