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

The isolation and structures of three novel scalarane sesterterpenes 1– 3 and their inhibition of FXR transactivation are reported. 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 inhibit...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-10, Vol.16 (20), p.5398-5402
Hauptverfasser:	Nam, Sang-Jip, Ko, Hyunsil, Shin, Mihee, Ham, Jungyeob, Chin, Jungwook, Kim, Youngshin, Kim, Heeyoung, Shin, Kyoungjin, Choi, Hyukjae, Kang, Heonjoong
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Cell Line Cell Proliferation - drug effects Cercopithecus aethiops DNA-Binding Proteins - antagonists & inhibitors DNA-Binding Proteins - biosynthesis DNA-Binding Proteins - genetics Farnesoid X-activated receptor General and cellular metabolism. Vitamins General pharmacology Guggulsterone Hypercholesterolemia Magnetic Resonance Spectroscopy - methods Magnetic Resonance Spectroscopy - standards Marine sponge Medical sciences Molecular Conformation Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Porifera - chemistry Receptors, Cytoplasmic and Nuclear - antagonists & inhibitors Receptors, Cytoplasmic and Nuclear - biosynthesis Receptors, Cytoplasmic and Nuclear - genetics Reference Standards Scalarane sesterterpene Sesterterpenes Spongia Stereoisomerism Structure-Activity Relationship Terpenes - chemistry Terpenes - pharmacology Transcription Factors - antagonists & inhibitors Transcription Factors - biosynthesis Transcription Factors - genetics Transcriptional Activation - drug effects Transfection
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The isolation and structures of three novel scalarane sesterterpenes 1– 3 and their inhibition of FXR transactivation are reported. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.07.079