Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes.

Akiko Masuda, Kazuhiro Irie, Yu Nakagawa, Hajime Ohigashi

Index: Biosci. Biotechnol. Biochem. 66(7) , 1615-7, (2002)

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Abstract

Two conformationally restricted analogues of (-)-indolactam-V (1) (cis and trans amides) were examined for their binding selectivity to the synthetic C1 peptides of all protein kinase C (PKC) isozymes. Although the binding constants of the cis amide-restricted analogue (2) were equal to those of 1, the trans amide-restricted analogue (3) bound significantly only to the novel PKC (delta, epsilon, eta, theta) isozymes.