title: Tailored fragments of roseophilin selectively antagonize Mcl-1in vitro.
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 memberin vitro.
authors.affiliation: Department of Chemistry and Biochemistry, University of California at Los Angeles, 607 Charles E. Young Drive East, Los Angeles, CA 90095, United States.
authors.forename: Jack D
authors.initials: JD
authors.lastname: Bracken
authors.affiliation: Department of Chemistry and Biochemistry, University of California at Los Angeles, 607 Charles E. Young Drive East, Los Angeles, CA 90095, United States.
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Carlson
authors.affiliation: Department of Chemistry and Biochemistry, University of California at Los Angeles, 607 Charles E. Young Drive East, Los Angeles, CA 90095, United States.
authors.forename: James H
authors.initials: JH
authors.lastname: Frederich
authors.affiliation: Department of Biochemistry and Goodman Cancer Research Center, McGill University, Montréal, Québec, Canada.
authors.forename: Mai
authors.initials: M
authors.lastname: Nguyen
authors.affiliation: Department of Biochemistry and Goodman Cancer Research Center, McGill University, Montréal, Québec, Canada.
authors.forename: Gordon C
authors.initials: GC
authors.lastname: Shore
authors.affiliation: Department of Chemistry and Biochemistry, University of California at Los Angeles, 607 Charles E. Young Drive East, Los Angeles, CA 90095, United States.
authors.forename: Patrick G
authors.initials: PG
authors.lastname: Harran
keywords: Bcl-2; Mcl-1; Obatoclax; Roseophilin; Tetrazole