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.

Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer

Benjamin C. Milgram, Deanna R. Borrelli, Natasja Brooijmans, Jack A. Henderson, Brendan J. Hilbert, Michael R. Huff, Takahiro Ito, Erica L. ...