Abstract

Retinoic acid receptors (RARs) are ligand-controlled transcription factors that function as heterodimers with retinoid X receptors (RXRs) to regulate cell growth and survival. The success of RAR modulation in the treatment of acute promyelocytic leukaemia (APL) has stimulated considerable interest in the development of RAR and RXR modulators. This has been aided by recent advances in the understanding of the biological role of RARs and RXRs and in the design of selective receptor modulators that might overcome the limitations of current drugs. Here, we discuss the challenges and opportunities for therapeutic strategies based on RXR and RAR modulators, with a focus on cancer and metabolic diseases such as diabetes and obesity.

Author affiliations

1. Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico Luigi de Crecchio 7, 80138 Napoli, Italy.
2. Ligand Pharmaceuticals Inc., Department of Pharmacology, 10275 Science Center Drive, San Diego, California 92121, USA.
3. Exelixis Inc., 4757 Nexus Center Drive, San Diego, California 92121, USA.
4. Universidade de Vigo, Departamento de Química Orgánica, Facultad de Química, 36310 Vigo, Spain.
5. Department of Cancer Biology, Institut de Génétique et de Biologie Moléculaire et Cellulaire, BP 10142, 67404 Illkirch Cedex, France.

Correspondence to: Hinrich Gronemeyer⁵ Email: hg@igbmc.u-strasbg.fr

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