Tuesday, January 1, 2019

Live-Cell Imaging and Profiling of c-Jun N-Terminal Kinases with Covalent Inhibitor-Derived Probes

Linghui Qian,  Sijun Pan,  Jun-Seok Lee,  Jingyan Ge,  Lin Li  and  Shao Yao

Chem. Commun., 2018
DOI: 10.1039/C8CC09558B

c-Jun N-terminal kinases (JNKs) are involved in critical cellular functions. Herein, small-molecule JNK-targeting probes are reported based on a covalent inhibitor. Together with newly developed two-photon fluorescence Turn-ON reporters and chemoproteomic studies, we showed some probes may be suitable for live-cell imaging and profiling of JNKs.
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Covalent inhibitors of the RAS binding domain of PI3Ka impair tumor growth driven by RAS and HER2

Joseph E Klebba, Nilotpal Roy, Steffen M Bernard, Stephanie Grabow, Melissa A. Hoffman, Hui Miao, Junko Tamiya, Jinwei Wang, Cynthia Berry, ...