Protein kinase C intervention: the state of play

Jon Roffey; Carine Rosse; Mark Linch; Andrew Hibbert; Neil Q McDonald; Peter J Parker

doi:10.1016/j.ceb.2009.01.019

Protein kinase C intervention: the state of play

Curr Opin Cell Biol. 2009 Apr;21(2):268-79. doi: 10.1016/j.ceb.2009.01.019. Epub 2009 Feb 23.

Authors

Jon Roffey¹, Carine Rosse, Mark Linch, Andrew Hibbert, Neil Q McDonald, Peter J Parker

Affiliation

¹ Discovery Laboratory, Cancer Research Technology Limited, Wolfson Institute for Biomedical Research, London, UK.

PMID: 19233632
DOI: 10.1016/j.ceb.2009.01.019

Abstract

Intervention in protein kinase C (PKC) has a chequered history, partly because of the poor selectivity of many inhibitors and partly a reflection of the sometimes antagonistic action of related PKC isoforms. Recent advances in targeting PKC isoforms have come from structural work on isolated kinase domains that have provided opportunities to drive selectivity through structure-based avenues. The promise of isoform selective inhibitors and the rationale for their development are discussed in the broader context of the PKC inhibitor arsenal.

Publication types

Review

MeSH terms

Animals
Catalytic Domain
Clinical Trials as Topic
Enzyme Activation
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / therapeutic use
Humans
Isoenzymes / antagonists & inhibitors*
Isoenzymes / genetics
Isoenzymes / metabolism
Molecular Structure
Multigene Family
Neoplasms / drug therapy
Oligonucleotides, Antisense / therapeutic use
Protein Kinase C / antagonists & inhibitors*
Protein Kinase C / genetics
Protein Kinase C / metabolism
Signal Transduction / physiology

Substances

Enzyme Inhibitors
Isoenzymes
Oligonucleotides, Antisense
Protein Kinase C