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Protein kinase C inhibitors: a patent review (2008 - 2009)
M Elizabeth Sobhia1, Baljinder K Grewal, Stanly Paul Ml
1National Institute of Pharmaceutical Education and Research (NIPER), Department of Pharmacoinformatics , Sector 67, SAS Nagar (Mohali), Punjab , India mesophia@niper.ac.in.
Introduction:
The protein kinase C (PKC) is a family of multifunctional isoenzymes involved in apoptosis, migration, adhesion, tumorgenesis, cardiac hypertrophy, angiogenesis, platelet function and inflammation. It also plays a vital role in the regulation of signal transduction, cell proliferation and differentiation through positive and negative regulation of the cell cycle. In this work, we reviewed the existing PKC inhibitors and several patents linked to PKC inhibitors.
Areas Covered:
Thorough survey on the PKC inhibitors having clinical importance and patents filed for these inhibitors from 2008 - 2009 is reported.
Expert Opinion:
PKCs are highly potential therapeutic targets for treating diabetic complications, oncological, inflammatory, immunological and dermatological disorders. The clinical trial candidates of PKCs mainly target the catalytic domain, which is highly conserved throughout the PKC family making it difficult to target a particular isoform selectively. Relatively less chemical space and fewer bisubstrate inhibitors targeting both ATP and regulatory domain are explored for PKCs, more research in these areas will be helpful in overcoming existing problems.
Insights
Protein kinase C (PKC) inhibitors are reviewed, highlighting their therapeutic potential for various diseases. Research gaps exist in selectively targeting PKC isoforms and exploring novel inhibitor designs.
Area of Science:
- Biochemistry
- Pharmacology
- Medicinal Chemistry
Background:
- Protein kinase C (PKC) is a family of multifunctional enzymes crucial for cell signaling, proliferation, and differentiation.
- PKC dysregulation is implicated in numerous diseases, including cancer, inflammation, and diabetes.
Purpose of the Study:
- To review existing protein kinase C (PKC) inhibitors with clinical relevance.
- To analyze patents filed for PKC inhibitors between 2008 and 2009.
Main Methods:
- Comprehensive literature and patent survey.
- Focus on clinically significant PKC inhibitors and recent patent filings.
Main Results:
- Identified key PKC inhibitors and their associated patents.
- Highlighted the therapeutic potential of PKCs in various disorders.
Conclusions:
- PKCs represent promising therapeutic targets for diabetic, oncological, inflammatory, immunological, and dermatological conditions.
- Challenges remain in selective isoform targeting due to conserved catalytic domains.
- Further research is needed on bisubstrate inhibitors and exploring chemical space for PKCs.
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