Tailored fragments of roseophilin selectively antagonize Mcl-1 .
作者信息
Bracken Jack D, Carlson Andrew D, Frederich James H, Nguyen Mai, Shore Gordon C, Harran Patrick G
机构信息
Department of Chemistry and Biochemistry, University of California at Los Angeles, 607 Charles E. Young Drive East, Los Angeles, CA 90095, United States.
Department of Biochemistry and Goodman Cancer Research Center, McGill University, Montréal, Québec, Canada.
出版信息
Tetrahedron Lett. 2015 Jun 3;56(23):3612-3616. doi: 10.1016/j.tetlet.2015.01.191.
Abstract
We have discovered a fragment of the natural product roseophilin, a member of the prodiginine family, that antagonizes Mcl-1 functions in a liposome-based assay for mitochondrial membrane permeabilization. By tailoring this substance such that it can participate in salt bridging with the protein surface, we have prepared the first prodiginine inspired structure that shows direct, saturable binding to a recombinant Bcl-2 family member .
摘要
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