title: Protein kinase C intervention: the state of play.
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.
authors.affiliation: Discovery Laboratory, Cancer Research Technology Limited, Wolfson Institute for Biomedical Research, London, UK.
authors.forename: Jon
authors.initials: J
authors.lastname: Roffey
authors.forename: Carine
authors.initials: C
authors.lastname: Rosse
authors.forename: Mark
authors.initials: M
authors.lastname: Linch
authors.forename: Andrew
authors.initials: A
authors.lastname: Hibbert
authors.forename: Neil Q
authors.initials: NQ
authors.lastname: McDonald
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Parker
mesh_terms: D000818:Animals; D020134:Catalytic Domain; D002986:Clinical Trials as Topic; D004789:Enzyme Activation; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D015394:Molecular Structure; D005810:Multigene Family; D009369:Neoplasms / Q000188:drug therapy; D016376:Oligonucleotides, Antisense / Q000627:therapeutic use; D011493:Protein Kinase C / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D015398:Signal Transduction / Q000502:physiology
chemical_list: D004791:Enzyme Inhibitors; D007527:Isoenzymes; D016376:Oligonucleotides, Antisense; D011493:Protein Kinase C