Bioorganic & Medicinal Chemistry Letters 2006-10-15

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

Sang-Jip Nam, Hyunsil Ko, Mihee Shin, Jungyeob Ham, Jungwook Chin, Youngshin Kim, Heeyoung Kim, Kyoungjin Shin, Hyukjae Choi, Heonjoong Kang

Index: Bioorg. Med. Chem. Lett. 16 , 5398-402, (2006)

Full Text: HTML

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.

Related Compounds

  • Z-Guggulsterone

Related Articles:

Chemical genetics reveals a complex functional ground state of neural stem cells.

2007-05-01

[Nat. Chem. Biol. 3(5) , 268-273, (2007)]

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

2009-10-01

[Nat. Chem. Biol. 5 , 765-71, (2009)]

Conformational dynamics of human FXR-LBD ligand interactions studied by hydrogen/deuterium exchange mass spectrometry: insights into the antagonism of the hypolipidemic agent Z-guggulsterone.

2014-09-01

[Biochim. Biophys. Acta 1844(9) , 1684-93, (2014)]

Effect of guggulsterone and cembranoids of Commiphora mukul on pancreatic phospholipase A(2): role in hypocholesterolemia.

2009-01-01

[J. Nat. Prod. 72 , 24-8, (2009)]

Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.

2007-04-01

[Bioorg. Med. Chem. 15 , 2587-600, (2007)]

More Articles...