1. Academic Validation
  2. Natural products reveal cancer cell dependence on oxysterol-binding proteins

Natural products reveal cancer cell dependence on oxysterol-binding proteins

  • Nat Chem Biol. 2011 Aug 7;7(9):639-47. doi: 10.1038/nchembio.625.
Anthony W G Burgett 1 Thomas B Poulsen Kittikhun Wangkanont D Ryan Anderson Chikako Kikuchi Kousei Shimada Shuichi Okubo Kevin C Fortner Yoshihiro Mimaki Minpei Kuroda Jason P Murphy David J Schwalb Eugene C Petrella Ivan Cornella-Taracido Markus Schirle John A Tallarico Matthew D Shair
Affiliations

Affiliation

  • 1 Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts, USA.
Abstract

Cephalostatin 1, OSW-1, ritterazine B and schweinfurthin A are Natural Products that potently, and in some cases selectively, inhibit the growth of cultured human Cancer cell lines. The cellular targets of these small molecules have yet to be identified. We have discovered that these molecules target oxysterol binding protein (OSBP) and its closest paralog, OSBP-related protein 4L (ORP4L)--proteins not known to be involved in Cancer cell survival. OSBP and the ORPs constitute an evolutionarily conserved protein superfamily, members of which have been implicated in signal transduction, lipid transport and lipid metabolism. The functions of OSBP and the ORPs, however, remain largely enigmatic. Based on our findings, we have named the aforementioned Natural Products ORPphilins. Here we used ORPphilins to reveal new cellular activities of OSBP. The ORPphilins are powerful probes of OSBP and ORP4L that will be useful in uncovering their cellular functions and their roles in human diseases.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-101213
    99.66%, ORP4拮抗剂