Specificity and mechanism of action of some commonly used protein kinase inhibitors.

By S. Davies, Helen Reddy, M. Caivano, P. Cohen. Biochemical Journal, 2000

3,147 citations recorded by the source corpus.

View Paper: https://www.semanticscholar.org/paper/a03e7cd10181cfc1db6aeee9e93feb8da9a0ec5c

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Citations in the corpus

Activation of the PI3K/Akt pathway and chemotherapeutic resistance. (2002, background): “When tested in a large panel of protein kinases, wortmannin was found to have high selectivity for inhibiting PI3K (Davies et al., 2000).”
Rho Kinase Inhibition Enhances Axonal Regeneration in the Injured CNS (2003, background): “…protein kinases such as mitogen-and stress-activated protein kinase, mitogenactivated protein kinase-activated protein kinase 1b, and phosphorylase kinase can be inhibited by Y-27632 at high doses, this drug is a relatively specific ROCK inhibitor at low concentrations (Davies et al., 2000).”
Transient and Selective NF-κB p65 Serine 536 Phosphorylation Induced by T Cell Costimulation Is Mediated by IκB Kinase β and Controls the Kinetics of p65 Nuclear Import 1 (2004, methodology): “To investigate the importance of the PI3K/Akt pathway by a different experimental approach, costimulation-induced p65 phosphorylation was tested in the presence of wortmannin, a potent and specific PI3K inhibitor (49).”
GSK3 inhibitors: development and therapeutic potential (2004, background): “Indeed, lithium ions, which inhibit GSK3 relatively specifically in vitro”
Kinase-targeted cancer therapies: progress, challenges and future directions (2018, background): “Apart from this wide range of kinase-based drug targets, inhibition of distinct kinase signaling pathways can be less cytotoxic to non-cancerous cells, thus presenting the selective killing of tumor cells with considerably lower toxic manifestations [16, 17].”
The selectivity of protein kinase inhibitors: a further update. (2007, methodology): “Seven years ago we studied28commonlyusedproteinkinaseinhibitorsandexamined their specificities against a panel of 24 different protein kinases [ 1 ], and a few years later we extended this analysis to a further 14 compounds against a slightly larger panel [2].”
The Ancient Drug Salicylate Directly Activates AMP-Activated Protein Kinase (2012, methodology): “PKA was expressed and purified as described (9).”
TOR signaling in growth and metabolism. (2006, background): “FKBP12-rapamycin is probably the most potent and specific kinase inhibitor known (Davies et al., 2000).”
Exploiting the PI3K/AKT Pathway for Cancer Drug Discovery (2005, background): “Upon activation, PI3Ks phosphorylate phosphatidylinositol-4,5-bisphosphate (PtdIns(4,5)P2; FIG.”
Mitogen-activated protein kinase signaling in the heart: angels versus demons in a heart-breaking tale. (2010, background): “This is not a new concept, since for years the Cohen laboratory has performed detailed studies exposing the nonselectivity of reportedly selective inhibitors (20, 21, 92).”
Increased activation of the mammalian target of rapamycin pathway in liver and skeletal muscle of obese rats: possible involvement in obesity-linked insulin resistance. (2005, background): “Rapamycin is a very selective inhibitor of the mTOR pathway, with no inhibitory activity toward other known kinases even at concentrations in the high nanomolar range (35).”