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Paper | Special issue | Vol 73, No. 1, 2007, pp.289-302
Published online, 22nd May, 2007
DOI: 10.3987/COM-07-S(U)3
Binding Selectivity of 1- or 12-Substituted Indolactam Derivatives for Protein Kinase C Isozymes

Ryo C. Yanagita, Keiji Torii, Yu Nakagawa, and Kazuhiro Irie*

*Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Kyoto 606-8502, Japan


The selectivity with which 1- or 12-substituted analogues of indolactam-V (1) bind protein kinase C (PKC) isozymes was examined. Moderate selectivity for novel PKC isozymes over conventional PKC isozymes was observed in the case of indolactam-nV (13) and indolactam-L (14) without an α-branched side chain at position 12. The introduction of a bulky isopropyl group to position 1 of 1 drastically increased the selectivity for novel PKC isozymes.