SAR Study on CN17p a Potent and Selective CaMKII Peptide Inhibitor

摘要

Ca~(2+)/Calmodulin-dependent protein kinase II (CaMKII) constitutes a family of kinases that transduces elevated Ca~+ signals in cells to a number of targets [1]. CaMKII regulates diverse cellular functions, including Ca~(2+) homeostasis [2]. Misregulation of this enzyme is involved in cardiovascular diseases including hypertrophy and other types of ischemia/reperfusion injury [3], obesity and diabetes [4]. A natural inhibitor of CaMKII, protein CaM-KIIN and a 27-residue peptide derived from it, (CaM-KNtide, Table 1), are highly selective for inhibition of CaMKII [5]. We have recently demonstrated that a 17-mer peptide (named CN17P) derived from CaM-KNtide still retained useful inhibitory potency (Table 1) [6].