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

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.

• Authors: Sang-Jip Nam, Hyunsil Ko, Mihee Shin, Jungyeob Ham, Jungwook Chin, Youngshin Kim, Heeyoung Kim, Kyoungjin Shin, Hyukjae Choi, Heonjoong Kang
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 16 Issue 20 Pg. 5398-402 (Oct 15 2006) ISSN: 0960-894X [Print] England
• PMID: 16905319 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

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

Topics

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