期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 5, 期 12, 页码 1308-1312出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml500388q
关键词
MCL1; myeloid cell leukemia 1; sp(3)-rich; biophysical validation
资金
- Carlos Slim Health Institute in Mexico
- Robertson Foundation
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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