Single mechanism MAPK inhibitors bind phosphorylated MAPK

Stable Identifier
Reaction [binding]
Homo sapiens
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Single mechanism MAPK inhibitors such as ulixertinib and ravoxertinib bind to the activated forms of MAPK proteins and inhibit their intrinsic target-directed kinase activity (Germann et al, 2017; Blake et al, 2016; reviewed in Samatar and Poulikakos, 2014).
Literature References
PubMed ID Title Journal Year
28939558 Targeting the MAPK Signaling Pathway in Cancer: Promising Preclinical Activity with the Novel Selective ERK1/2 Inhibitor BVD-523 (Ulixertinib)

Namchuk, M, Germann, UA, Roix, JJ, Shapiro, P, Hoover, RR, Meshaw, K, Fitzgibbon, M, Emery, CM, Samadani, R, Furey, BF, Markland, W, Aronov, AM, Saha, S, Martinez-Botella, G, DeCrescenzo, G, Sorrell, DA, Wick, MJ, Hale, M, Groover, A, Welsch, DJ, Boucher, DM

Mol. Cancer Ther. 2017
27227380 Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development

Ren, L, Yin, J, Wang, W, Robarge, K, Liu, L, Moffat, J, Chan, J, Moreno, D, Chou, KJ, Chen, H, Merchant, M, Gaudino, JJ, Stults, J, Blake, JF, Grina, J, Gould, SE, Martinson, M, Qin, A, Belvin, M, Sullivan, F, Mueller, L, Schwarz, JB, Zhou, A, Burkard, M, Rasor, K, Dudley, DA, Diaz, D, Orr, C, Pacheco, P, Hunsaker, T, Shahidi-Latham, S

J. Med. Chem. 2016
25435214 Targeting RAS-ERK signalling in cancer: promises and challenges

Poulikakos, PI, Samatar, AA

Nat Rev Drug Discov 2014
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