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  • Title: Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions.
    Author: Takahashi B, Ohta K, Kawachi E, Fukasawa H, Hashimoto Y, Kagechika H.
    Journal: J Med Chem; 2002 Aug 01; 45(16):3327-30. PubMed ID: 12139443.
    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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