Evaluation of series of isobenzofuranone dimers as PKCalpha ligands: implication for the distance between the two ligand binding sites |
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| Authors: | Baba Yoshiyasu Mayumi Satoshi Hirai Go Kawasaki Hidekazu Ogoshi Yosuke Yanagisawa Takeshi Hashimoto Yuichi Sodeoka Mikiko |
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| Affiliation: | Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan. |
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| 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 C10-C12 linker and for the C7 dimers having a C14-C16. |
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