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)

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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.