Protein kinase C, an elusive therapeutic target?

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Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach
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Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach

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Daria Mochly-Rosen1, Kanad Das, Kevin V Grimes

  • 1Department of Chemical and Systems Biology, Stanford University School of Medicine, Stanford, California 94305-5174, USA. mochly@stanford.edu

Nature Reviews. Drug Discovery
|December 1, 2012
PubMed

Insights

Protein kinase C (PKC) remains an elusive drug target despite decades of research. This review explores the challenges and opportunities in developing novel PKC modulators for various diseases.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Protein kinase C (PKC) identified in 1982 as a phorbol ester receptor.
  • PKC isozymes play roles in various physiological and pathological processes.
  • Therapeutic potential explored for cancer, diabetic complications, heart failure, pain, and bipolar disorder.

Purpose of the Study:

  • To review the historical efforts in developing PKC modulators.
  • To identify the challenges hindering PKC-targeted drug approval.
  • To discuss future opportunities for PKC-based therapeutics.

Main Methods:

  • Literature review of academic and pharmaceutical research on PKC.
  • Analysis of therapeutic strategies and clinical trial outcomes.
  • Examination of the biological roles of conventional and novel PKC isozymes.

Main Results:

  • Despite extensive research, no specific PKC-targeting drug has been approved.
  • Numerous PKC isozymes present complexity in drug development.
  • Understanding of PKC's role in disease has expanded significantly.

Conclusions:

  • PKC remains a challenging yet promising drug target.
  • Overcoming development hurdles requires innovative approaches.
  • Further research into PKC modulators could address unmet clinical needs.

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