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Article

Iterative optimization yields Mcl-1-targeting stapled peptides with selective cytotoxicity to Mcl-1-dependent cancer cells.

Proceedings of the National Academy of Sciences of the United States of America - 30 Jan 2018

Rezaei Araghi Raheleh, Bird Gregory H, Ryan Jeremy A, Jenson Justin M, Godes Marina, Pritz Jonathan R, Grant Robert A, Letai Anthony, Walensky Loren D, Keating Amy E

Abstract excerpt

Bcl-2 family proteins regulate apoptosis, and aberrant interactions of overexpressed antiapoptotic family members such as Mcl-1 promote cell transformation, cancer survival, and resistance to chemotherapy. Discovering potent and selective Mcl-1 inhibitors that can relieve apoptotic blockades is thus a high priority for cancer research. An attractive strategy for disabling Mcl-1 involves using designer peptides to...

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PMID: 29339518
DOI: 10.1073/pnas.1712952115
PMCID: PMC5798337

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