Interaction of kendomycin and semi-synthetic analogues with the anti-apoptotic protein Bcl-xl

  • Bioorg Med Chem Lett. 2008 Nov 1;18(21):5771-3. doi: 10.1016/j.bmcl.2008.09.071.
Christian O Janssen  1 ,  Stephanie Lim ,  Ee Peng Lo ,  Kah Fei Wan ,  Victor C Yu ,  May Ann Lee ,  Siew Bee Ng ,  Martin J Everett ,  Antony D Buss ,  David P Lane ,  Rustum S Boyce
Affiliations
  • 1. MerLion Pharmaceuticals Pte Ltd, Medicinal Chemistry, Singapore Science Park II, Singapore 117528, Singapore.
PMID: 18845435 DOI: 10.1016/j.bmcl.2008.09.071
Abstract

The cytotoxic Macrolide kendomycin was identified as a ligand of Bcl-xL, an anti-apoptotic member of the Bcl-2 protein family. Hydrolysis-stable and protonable semi-synthetic analogues have been obtained that retain cytotoxicity and Bcl-xL binding.