Protein kinase C inhibitors: a patent review (2008 - 2009)

• Published in: Expert opinion on therapeutic patents Vol. 23; no. 10; p. 1297
• Main Authors: Sobhia, M Elizabeth, Grewal, Baljinder K, Ml, Stanly Paul, Patel, Jigneshkumar, Kaur, Amandeep, Haokip, Thongtinlal, Kokkula, Alekhya
• Format: Journal Article
• Language: English
• Published: England 01.10.2013
• Subjects: Animals; Drug Design; Drug Discovery; Humans; Isoenzymes - antagonists & inhibitors; Patents as Topic; Protein Kinase C - antagonists & inhibitors; Protein Kinase Inhibitors - classification; Protein Kinase Inhibitors - pharmacology; Protein Kinase Inhibitors - therapeutic use
• ISSN: 1744-7674
• DOI: 10.1517/13543776.2013.805205

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. Thorough survey on the PKC inhibitors having clinical importance and patents filed for these inhibitors from 2008 - 2009 is reported. 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.