Single Diastereomer of a Macrolactam Core Binds Specifically to Myeloid Cell Leukemia 1 (MCL1)
ACS Medicinal Chemistry Letters2014Vol. 5(12), pp. 1308–1312
Citations Over TimeTop 13% of 2014 papers
Chao Fang, Brendan D’Souza, Christopher F. Thompson, Matthew C. Clifton, J.W. Fairman, Ben Fulroth, Alison Leed, Patrick McCarren, Lili Wang, Yikai Wang, Clémentine Féau, Virendar K. Kaushik, Michelle Palmer, Guo Wei, Todd R. Golub, Brian K. Hubbard, Michael H. Serrano‐Wu
Abstract
A direct binding screen of 100 000 sp(3)-rich molecules identified a single diastereomer of a macrolactam core that binds specifically to myeloid cell leukemia 1 (MCL1). A comprehensive toolbox of biophysical methods was applied to validate the original hit and subsequent analogues and also established a binding mode competitive with NOXA BH3 peptide. X-ray crystallography of ligand bound to MCL1 reveals a remarkable ligand/protein shape complementarity that diverges from previously disclosed MCL1 inhibitor costructures.
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