Synthetic Retinoids and Their Nuclear Receptors

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Synthetic Retinoids and Their Nuclear Receptors

Anti-Cancer Agents in Medicinal Chemistry, 4(3): 199-230.

Author(s): M I Dawson.

Affiliation: Cancer Center, The BurnhamInstitute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA


In addition to all-trans-retinoic acid and its 9 and 13-cis isomers, four synthetic retinoids are currently available to treat diseases of hyperproliferation, such as acne, psoriasis, and actinic keratosis, or cancers such as acute promelocytic leukemia, cutaneous T-cell lymphoma, and squamous or basal cell carcinoma. The retinoids extert their antiproliferative effects by interacting with their retinoic acid and retinoid X receptors that act as ligand-inducible transcription factors. These homologous receptors function either directly on retinoid response elements or indirectly by modifying the responses of other transcription factors. Their major domains for binding DNA and their ligands have been characterized by either nuclear magnetic resonance spectroscopy or X-ray crystallography. The identification and design of synthetic retinoids are overviewed, as are their selective interactions with specific retinoid receptor subtypes and their clinical effects against cancer. Emphasis is placed on the retinoid X receptors and their ligands.


retinoid, retinoic acid, retinoid nuclear receptor, rar, rxr, anticancer activity, receptor-selective.

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Article Details

Volume: 4
Issue Number: 3
First Page: 199
Last Page: 230
Page Count: 32
DOI: 10.2174/1568011043352975
Price: $58

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