The selectivity of protein kinase inhibitors: a further update.
作者： Jenny Bain , Lorna Plater , Matt Elliott , Natalia Shpiro , C. James Hastie
DOI: 10.1042/BJ20070797
关键词: Biochemistry 、 Biology 、 Ribosomal s6 kinase 、 MAP kinase kinase kinase 、 Mitogen-activated protein kinase kinase 、 c-Raf 、 MAP2K7 、 ASK1 、 Wortmannin 、 Cell biology 、 Cyclin-dependent kinase 2
摘要: The specificities of 65 compounds reported to be relatively specific inhibitors protein kinases have been profiled against a panel 70–80 kinases. On the basis this information, effects that we studied in cells and other data literature, recommend use following small-molecule inhibitors: SB 203580/SB202190 BIRB 0796 used parallel assess physiological roles p38 MAPK (mitogen-activated kinase) isoforms, PI-103 wortmannin inhibit phosphatidylinositol (phosphoinositide) 3-kinases, PP1 or PP2 with Src-I1 (Src inhibitor-1) Src family members; PD 184352 0325901 MKK1 (MAPK kinase-1) plus MKK5, Akt-I-1/2 activation PKB (protein kinase B/Akt), rapamycin TORC1 [mTOR (mammalian target rapamycin)–raptor (regulatory associated mTOR) complex], CT 99021 GSK3 (glycogen synthase 3), BI-D1870 SL0101 FMK (fluoromethylketone) RSK (ribosomal S6 kinase), D4476 CK1 (casein 1), VX680 Aurora kinases, roscovitine as pan-CDK (cyclin-dependent inhibitor. We also identified harmine potent inhibitor DYRK1A (dual-specificity tyrosine-phosphorylated -regulated 1A) vitro. results further emphasized need for considerable caution using these enzymes. Despite being widely, many analysed were too non-specific useful conclusions made, than exclude involvement particular cellular processes.
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