RAR and RXR modulation in cancer and metabolic disease
Top Cited Papers
- 1 October 2007
- journal article
- review article
- Published by Springer Nature in Nature Reviews Drug Discovery
- Vol. 6 (10) , 793-810
- https://doi.org/10.1038/nrd2397
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.Keywords
This publication has 166 references indexed in Scilit:
- Opposing Effects of Retinoic Acid on Cell Growth Result from Alternate Activation of Two Different Nuclear ReceptorsCell, 2007
- Triterpenoids and rexinoids as multifunctional agents for the prevention and treatment of cancerNature Reviews Cancer, 2007
- Loss of acetylation at Lys16 and trimethylation at Lys20 of histone H4 is a common hallmark of human cancerNature Genetics, 2005
- Principles for modulation of the nuclear receptor superfamilyNature Reviews Drug Discovery, 2004
- Epigenetics in human disease and prospects for epigenetic therapyNature, 2004
- The history of cancer epigeneticsNature Reviews Cancer, 2004
- Structural basis for isotype selectivity of the human retinoic acid nuclear receptor 1 1Edited by T. RichmondJournal of Molecular Biology, 2000
- Preliminary Observations on the Use of Topical Tazarotene to Treat Basal-Cell CarcinomaNew England Journal of Medicine, 1999
- Identification of Highly Potent Retinoic Acid Receptor α-Selective AntagonistsJournal of Medicinal Chemistry, 1997
- Retinoid-interferon therapy of solid tumorsInternational Journal of Cancer, 1997