PKC Delta and Epsilon in Drug Targeting and Therapeutics

Author(s): Tomo Yonezawa, Riho Kurata, Minoru Kimura, Hidetoshi Inoko

Journal Name: Recent Patents on DNA & Gene Sequences (Discontinued)

Volume 3 , Issue 2 , 2009


Protein kinase C (PKC) belongs to the serine and threonine kinase family. At least ten PKC isoforms have been identified and subdivided into three groups: classical (alpha, beta I, beta II and gamma), novel (delta, epsilon, theta and eta), and atypical (zeta and iota/lambda). Two calcium-insensitive isoforms of novel PKC, PKC delta and epsilon, have received particular attention as promising targets for new drugs. PKCs play a multifaceted role in cellular responses in a range of tissues. Professor Mochly-Rosens group and KAI Pharmaceuticals Inc. have developed drugs targeted against PKC delta (KAI-9803) and epsilon (KAI-1678). These drugs ameliorate pathological conditions in acute myocardial infarction and reduce pain via specific modulation of membrane-translocation of PKC delta or epsilon. Another research group has recently used the KinAceTM approach to produce PKC epsilon-abrogating peptides (KCe-12 and KCe-16) that are based on the catalytic domain of PKC. These peptides specifically inhibit PKC epsilon and ameliorate pathological conditions in a rodent insulin resistance model. This review describes the development of these therapeutic drugs targeting PKC delta and epsilon by two independent groups in the light of recent patents.

Keywords: Protein kinase C (PKC), selective peptide modulator, KAI-9803, KAI-1678, KCe-12, KCe-16

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2009
Page: [96 - 101]
Pages: 6
DOI: 10.2174/187221509788654205
Price: $58

Article Metrics

PDF: 7