Novel Retinoid X Receptor Antagonists: Specific Inhibition of Retinoid Synergism in RXR-RAR Heterodimer Actions

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2002 Jul 26

PMID 12139443

Citations 18

Authors

Bitoku Takahashi

Kiminori Ohta

Emiko Kawachi

Hiroshi Fukasawa

Yuichi Hashimoto

Hiroyuki Kagechika

Affiliations

Soon will be listed here.

Abstract

Several 2-(arylamino)pyrimidine-5-carboxylic acids were designed as novel retinoid X receptor (RXR) antagonists. Compound 6a or 6b alone did not exhibit differentiation-inducing activity toward HL-60 cells and did not affect the activity of a retinoic acid receptor (RAR) agonist, Am80, but did inhibit the synergistic activity of an RXR agonist, PA024 (3), in the presence of Am80. The activity of 6 was ascribed to selective antagonism at the RXR site of RXR-RAR heterodimers.

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