RAR ligands

Beta-cryptoxanthin, a novel natural RAR ligand, induces ATP-binding cassette transporters in macrophages. Biochem Pharmacol 74, 256-264. 

A paper has been published that discusses the structural basis for isotype selectivity of the RARs [30]. This paper reported structures of three RAR ligands bound to RAR-y, BMS184394 (PDB entry IFCX), an RAR-y-selective agonist, CD564 (PDB entry IFCY), an RAR-y9/y co-agonist and BMS181156 (PDB entry ... 

The doses of retinol that are protective in animals are in the toxic range (Section 2.5.1) and are unlikely to be useful in cancer therapy or prevention. A number of synthetic retinoids have been developed, in a search for compounds that show anticancer activity, but are metabolized, stored, and transported differently, or bind to different subtypes of retinoid receptor and are less toxic. RXR-selective ligands are less toxic and more active in animal cancer models than RAR ligands (Lippman and Lotan, 2000). Fenretinamide, and possibly other retinoids that have antitumor activity, exerts at least part of its action by induction of apoptosis by a receptor-independent mechanism (Wu et al., 2001). 

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