Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5398-402. doi: 10.1016/j.bmcl.2006.07.079. Epub 2006 Aug 14.

Abstract

Three novel (1-3) and two known (4-5) scalarane sesterterpenes were isolated from a marine sponge of the genus Spongia. The isolated compounds showed potent inhibition of transactivation for the nuclear hormone receptor, FXR (farnesoid X-activated receptor), which is a promising drug target to treat hypercholesterolemia in humans.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Cell Proliferation / drug effects
  • Chlorocebus aethiops
  • DNA-Binding Proteins / antagonists & inhibitors*
  • DNA-Binding Proteins / biosynthesis
  • DNA-Binding Proteins / genetics
  • Magnetic Resonance Spectroscopy / methods
  • Magnetic Resonance Spectroscopy / standards
  • Molecular Conformation
  • Porifera / chemistry*
  • Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*
  • Receptors, Cytoplasmic and Nuclear / biosynthesis
  • Receptors, Cytoplasmic and Nuclear / genetics
  • Reference Standards
  • Sesterterpenes
  • Stereoisomerism
  • Structure-Activity Relationship
  • Terpenes / chemistry
  • Terpenes / pharmacology*
  • Transcription Factors / antagonists & inhibitors*
  • Transcription Factors / biosynthesis
  • Transcription Factors / genetics
  • Transcriptional Activation / drug effects*
  • Transfection

Substances

  • DNA-Binding Proteins
  • Receptors, Cytoplasmic and Nuclear
  • Sesterterpenes
  • Terpenes
  • Transcription Factors
  • farnesoid X-activated receptor