Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo

Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo

The ERK signalling pathway is activated in many cancers, however ERK1 and ERK2 are difficult to target pharmacologically. Here, the authors identify a small molecule inhibitor that binds covalently to the D-recruitment site of ERK and induces cell death and reduces tumour growth in mice.

Bibliographic Details
Main Authors: Tamer S. Kaoud, William H. Johnson, Nancy D. Ebelt, Andrea Piserchio, Diana Zamora-Olivares, Sabrina X. Van Ravenstein, Jacey R. Pridgen, Ramakrishna Edupuganti, Rachel Sammons, Micael Cano, Mangalika Warthaka, Matthew Harger, Clint D. J. Tavares, Jihyun Park, Mohamed F. Radwan, Pengyu Ren, Eric V. Anslyn, Kenneth Y. Tsai, Ranajeet Ghose, Kevin N. Dalby
Format: Article
Language:English
Published: Nature Publishing Group 2019-11-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-019-12996-8

Internet

https://doi.org/10.1038/s41467-019-12996-8

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