Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases

Autor: Chen, Ying-Nan P., LaMarche, Matthew J., Chan, Ho Man, Fekkes, Peter, Garcia-Fortanet, Jorge, Acker, Michael G., Antonakos, Brandon, Chen, Christine Hiu-Tung, Chen, Zhouliang, Cooke, Vesselina G., Dobson, Jason R., Deng, Zhan, Fei, Feng, Firestone, Brant, Fodor, Michelle, Fridrich, Cary, Gao, Hui, Grunenfelder, Denise, Hao, Huai-Xiang, Jacob, Jaison, Ho, Samuel, Hsiao, Kathy, Kang, Zhao B., Karki, Rajesh, Kato, Mitsunori, Larrow, Jay, La Bonte, Laura R., Lenoir, Francois, Liu, Gang, Liu, Shumei, Majumdar, Dyuti, Meyer, Matthew J., Palermo, Mark, Perez, Lawrence, Pu, Minying, Price, Edmund, Quinn, Christopher, Shakya, Subarna, Shultz, Michael D., Slisz, Joanna, Venkatesan, Kavitha, Wang, Ping, Warmuth, Markus, Williams, Sarah, Yang, Guizhi, Yuan, Jing, Zhang, Ji-Hu, Zhu, Ping, Ramsey, Timothy, Keen, Nicholas J., Sellers, William R., Stams, Travis, Fortin, Pascal D.
Zdroj: Nature; July 2016, Vol. 535 Issue: 7610 p148-152, 5p
Abstrakt: SHP099, a selective inhibitor of signalling meditator SHP2 with drug-like properties, has an allosteric mechanism of action whereby it stabilizes SHP2 in an auto-inhibited conformation, and suppresses RAS–ERK signalling and proliferation in receptor-tyrosine-kinase-driven cancer cell lines and mouse tumour xenograft models.
Databáze: Supplemental Index
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