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Heightman et al., “Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2”

Click link to view article https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.1c00905 Abstract Aberrant activation of the mitogen-activated protein kinase pathway frequently drives tumor growth, and the ERK1/2 kinases are positioned at a key node in this pathway, making them important targets for therapeutic intervention. Recently, a number of ERK1/2 inhibitors have been advanced to investigational clinical trials in patients with […]

Munck et al., “ASTX029, a Novel Dual-Mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK”

Click link to view article https://mct.aacrjournals.org/content/early/2021/07/30/1535-7163.MCT-20-0909#:~:text=ASTX029%20is%20a%20highly%20potent,not%20directly%20inhibiting%20MEK%20activity Abstract The MAPK signaling pathway is commonly upregulated in human cancers. As the primary downstream effector of the MAPK pathway, ERK is an attractive therapeutic target for the treatment of MAPK-activated cancers and for overcoming resistance to upstream inhibition. ASTX029 is a highly potent and selective dual-mechanism ERK inhibitor, […]