Design synthesis and biological evaluation of JNK1 inhibitors

Abstract

c-Jun NH2-terminal kinase (JNK) is a stress activated protein kinase which modulate cellular signaling that is implicated in a variety of diseases like type-2 diabetes, cancer, atherosclerosis, stroke, Alzheimer’s and Parkinson diseases. JNK Interacting Protein 1 (JIP1) is a scaffolding protein of JNK which enhances JNK signaling by integrating the modules of JNK signaling. A part of the scaffolding protein- JIP-1 containing 153- 163 AA residues - known as pepJIP1 acts as an inhibitor to JNK at an allosteric site. The present work aims in design, synthesis and biological activity of small molecule allosteric inhibitors of JNK1.