Exciting news! We've identified 36c with a (thiophen-3-yl)aminopyrimidine scaffold as a potent ERK1/2 inhibitor through structure-guided optimization. The RAS-RAF-MEK-ERK signaling cascade is abnormally activated in various tumors and plays a crucial role in tumor progression. As the key component at the terminal stage, ERK1/2 emerges as a potential antitumor target. In preclinical studies, 36c showed powerful inhibitory activities and potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations. It can directly inhibit ERK1/2, block the phosphorylation expression of downstream substrates, and induce cell apoptosis and incomplete autophagy-related cell death. This work has been published in J Med Chem. Looking forward to more progress in the future! 🎉#ERK1/2 inhibitor #J Med Chem #tumor treatment #drug discovery #RAS-RAF-MEK-ERK #preclinical #autophagy-related cell death #medicinal chemistry https://lnkd.in/ejvfZBAu
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Muhammad L.
5mo
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-Professor and Pharmaceutical Research
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