The selectivity of protein kinase inhibitors: a further update.

By J. Bain, Lorna Plater, M. Elliott, N. Shpiro, J. Hastie, Hilary, Mclauchlan, Iva Klevernic, S. Arthur, D. Alessi and 1 more. Biochemical Journal, 2007

2,647 citations recorded by the source corpus.

Subfields: Cell Biology, Molecular Biology, Oncology

View Paper: https://www.semanticscholar.org/paper/624125b014b08897ba0fa72ebe71e6258fe85fd0

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Cell Biology

1. Philippe P Roux
2. J. Blenis
3. J. Avruch
4. R. Anjum
5. J. Kyriakis

In Molecular Biology

1. Jennifer Nichols
2. Austin G Smith
3. José C. R. Silva
4. J. Blenis
5. Philippe P Roux
6. Qi-Long Ying
7. M. Roode
8. R. Anjum

In Oncology

1. J. Avruch
2. M. Sliwkowski
3. Philippe P Roux
4. J. Blenis
5. J. Kyriakis
6. M. Lacouture

Citations in the corpus

• Suppression of Erk signalling promotes ground state pluripotency in the mouse embryo (2009, methodology): “RESULTS Inhibition of Erk activity in early embryos eliminates hypoblast and expands epiblast We previously demonstrated that ES cells can be maintained in an undifferentiated state in the presence of the Mek inhibitor PD184352 and the FGF receptor inhibitor SU5402, but that survival and expansion a”
• Targeting the cancer kinome through polypharmacology (2010, neutral): “In 2007, the same group published a follow-up paper that analysed the specificity of 65 common kinase inhibitors against 70 kinases (approximately 4,500 kinase–drug pairs) 90 .”
• Capture of authentic embryonic stem cells from rat blastocysts. (2008, positive): “Accordingly we omitted SU5402 and switched to a two inhibitor (2i) formulation comprised of the more potent MEK inhibitor PD0325901 (Bain et al., 2007) with the GSK3 inhibitor.”
• 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).”
• The RSK family of kinases: emerging roles in cellular signalling (2008, methodology): “These inhibitors have been profiled against a panel of 70–80 protein kinases and were found to be RSK-selectiv”
• Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941. (2009, background): “Several properties that are critical for therapeutic agents differentiate GDC-0941 from previously tested PI3K inhibitors, including wortmannin and LY294002 (Bain et al., 2007; Hennessy et al., 2005; Nagata et al., 2004).”
• Activation and Function of the MAPKs and Their Substrates, the MAPK-Activated Protein Kinases (2011, background): “However, a recent study indicated that this compound was a relatively weak inhibitor of MNKs, with 50% inhibitory concentrations (IC50s) in the low-micromolar range (18).”