Binding Selectivity of Conformationally Restricted Analogues of (−)-Indolactam-V to the C1 Domains of Protein Kinase C Isozymes

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 (δ, ε, η, θ) isozymes.