Article
Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib.
Cancer research - 1 Nov 2020
Sun Yuting, Meyers Brooke A, Czako Barbara, Leonard Paul, Mseeh Faika, Harris Angela L, Wu Qi, Johnson Sarah, Parker Connor A, Cross Jason B, Di Francesco Maria Emilia, Bivona Benjamin J, Bristow Christopher A, Burke Jason P, Carrillo Caroline C, Carroll Christopher L, Chang Qing, Feng Ningping, Gao Guang, Gera Sonal, Giuliani Virginia, Huang Justin K, Jiang Yongying, Kang Zhijun, Kovacs Jeffrey J, Liu Chiu-Yi, Lopez Anastasia M, Ma Xiaoyan, Mandal Pijus K, McAfoos Timothy, Miller Meredith A, Mullinax Robert A, Peoples Michael, Ramamoorthy Vandhana, Seth Sahil, Spencer Nakia D, Suzuki Erika, Williams Christopher C, Yu Simon S, Zuniga Andy M, Draetta Giulio F, Marszalek Joseph R, Heffernan Timothy P, Kohl Nancy E, Jones Philip
Abstract excerpt
Src homology 2 domain-containing phosphatase (SHP2) is a phosphatase that mediates signaling downstream of multiple receptor tyrosine kinases (RTK) and is required for full activation of the MAPK pathway. SHP2 inhibition has demonstrated tumor growth inhibition in RTK-activated cancers in preclinical studies. The long-term effectiveness of tyrosine kinase inhibitors such as the EGFR inhibitor (EGFRi),...
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