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PKC delta and epsilon in drug targeting and therapeutics

Tomo Yonezawa1, Riho Kurata, Minoru Kimura

  • 1Tokai University, Bohseidai, Ishehara, Kanagawa, Japan. yonet2301@yahoo.co.jp

Recent Patents on DNA & Gene Sequences
|June 13, 2009
PubMed

Insights

Novel drugs targeting Protein Kinase C (PKC) delta and epsilon isoforms show promise for treating conditions like acute myocardial infarction and insulin resistance. These therapies modulate PKC activity, offering new therapeutic avenues.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Protein Kinase C (PKC) is a family of serine/threonine kinases with diverse cellular roles.
  • At least ten PKC isoforms exist, grouped into classical, novel, and atypical categories.
  • Novel PKC isoforms delta and epsilon are key targets for therapeutic intervention due to their roles in various pathologies.

Purpose of the Study:

  • To review the development of novel therapeutic drugs targeting PKC delta and epsilon.
  • To highlight recent patents related to these PKC-targeted therapies.
  • To discuss the potential of PKC delta and epsilon modulation in treating diseases.

Main Methods:

  • Development of specific drugs (KAI-9803 and KAI-1678) targeting PKC delta and epsilon by KAI Pharmaceuticals.
  • Creation of PKC epsilon-inhibiting peptides (KCe-12 and KCe-16) using the KinAce() approach.
  • Evaluation of therapeutic efficacy in preclinical models of acute myocardial infarction, pain, and insulin resistance.

Main Results:

  • KAI-9803 and KAI-1678 ameliorate pathological conditions in acute myocardial infarction and reduce pain.
  • PKC epsilon-abrogating peptides effectively inhibit PKC epsilon and improve outcomes in a rodent insulin resistance model.
  • These findings demonstrate successful modulation of PKC delta and epsilon for therapeutic benefit.

Conclusions:

  • Targeted inhibition of PKC delta and epsilon represents a promising therapeutic strategy.
  • Developed drugs and peptides show potential for treating cardiovascular diseases and metabolic disorders.
  • Ongoing research and patent activity underscore the therapeutic significance of PKC delta and epsilon.

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