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Structure-based design of potent retinoid X receptor alpha agonists.

Abstract：

:A series of tetrahydrobenzofuranyl and tetrahydrobenzothienyl propenoic acids that showed potent agonist activity against RXRalpha were synthesized via a structure-based design approach. Among the compounds studied, 46a,b showed not only very good potency against RXRalpha (K(i) = 6 nM) but was also found to be greater than 167-fold selective vs RARalpha (K(i) > 1000 nM). This compound profiled out as a full agonist in a cell-based transient transfection assay (EC(50) = 3 nM). The two antipodes were separated via chiral chromatography, and 46b was found to be 40-fold more potent than 46a. Interestingly, cocrystallization of 46a,b with the RXRalpha protein generated a liganded structure whereby the (S)-antipode was found in the binding pocket. Given orally in db/db mice or ZDF rats, 46a,b showed a significant glucose-lowering effect and an increase in liver mass. Triglycerides decreased significantly in db/db mice but increased in the ZDF rats. A dose-dependent decrease of nonesterified free fatty acids was seen in ZDF rats but not in db/db mice. These differences indicate a species specific effect of RXR agonists on lipid metabolism.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Haffner CD,Lenhard JM,Miller AB,McDougald DL,Dwornik K,Ittoop OR,Gampe RT Jr,Xu HE,Blanchard S,Montana VG,Consler TG,Bledsoe RK,Ayscue A,Croom D

doi

10.1021/jm030565g

keywords:

subject

Has Abstract

pub_date

2004-04-08 00:00:00

pages

2010-29

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

47

pub_type

杂志文章

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