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Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader

15 Nov 2019

Abstract excerpt

MEK1 and MEK2 (also known as MAP2K1 and MAP2K2) are the “gatekeepers” of the ERK signaling output with redundant roles in controlling ERK activity. Numerous inhibitors targeting MEK1/2 have been developed including three FDA-approved drugs. However, acquired resistance to MEK1/2 inhibitors has been observed in patients, and new therapeutic strategies are needed to overcome the resistance. Here, we report a...

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PMID: 31730343
DOI: 10.1021/acs.jmedchem.9b01528

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