Lipid-conjugated Smac analogues.
Ontology highlight
ABSTRACT:
SUBMITTER: Micewicz ED
PROVIDER: S-EPMC4592835 | biostudies-literature | 2015 Oct
REPOSITORIES: biostudies-literature
Publications
Lipid-conjugated Smac analogues.
Micewicz Ewa D ED Ratikan Josephine A JA Waring Alan J AJ Whitelegge Julian P JP McBride William H WH Ruchala Piotr P
Bioorganic & medicinal chemistry letters 20150908 20
A small library of monovalent and bivalent Smac mimics was synthesized based on 2 types of monomers, with general structure NMeAla-Xaa-Pro-BHA (Xaa=Cys or Lys). Position 2 of the compounds was utilized to dimerize both types of monomers employing various bis-reactive linkers, as well as to modify selected compounds with lipids. The resulting library was screened in vitro against metastatic human breast cancer cell line MDA-MB-231, and the two most active compounds selected for in vivo studies. T ...[more]
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