Retinoids Selective for Retinoid X Receptor Response Pathways

Retinoids have a broad spectrum of biological activities and are useful therapeutic agents. Their physiological activities are mediated by two types of receptors, the retinoic acid receptors (RARs) and the retinoid X receptors (RXRs). RARs, as well as several related receptors, require heterodimeriz...

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Bibliographic Details
Published in:Science (American Association for the Advancement of Science) 1992-12, Vol.258 (5090), p.1944-1946
Main Authors: Lehmann, Jurgen M., Jong, Ling, Fanjul, Andrea, Cameron, James F., Lu, Xian Ping, Haefner, Pamela, Dawson, Marcia I., Pfahl, Magnus
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Cell Line
Cell lines
Chloramphenicol O-Acetyltransferase - genetics
Chloramphenicol O-Acetyltransferase - metabolism
Gels
Hep G2 cells
Kinetics
Ligands
Macromolecular Substances
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Physiological aspects
Receptors
Receptors, Cell Surface - drug effects
Receptors, Cell Surface - genetics
Receptors, Cell Surface - metabolism
Receptors, Retinoic Acid
Recombinant Fusion Proteins - metabolism
Reporter genes
Response elements
Retinoid X Receptors
Retinoids
Retinoids - chemistry
Retinoids - metabolism
Retinoids - pharmacology
Skin, nail, hair, dermoskeleton
Structure-Activity Relationship
Transcription Factors
Transcription, Genetic
Transfection
Tretinoin - metabolism
Tretinoin - pharmacology
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Summary:Retinoids have a broad spectrum of biological activities and are useful therapeutic agents. Their physiological activities are mediated by two types of receptors, the retinoic acid receptors (RARs) and the retinoid X receptors (RXRs). RARs, as well as several related receptors, require heterodimerization with RXRs for effective DNA binding and function. However, in the presence of 9-cis-retinoic acid, a ligand for both RARs and RXRs, RXRs can also form homodimers. A series of retinoids is reported that selectively activates RXR homodimers but does not affect RAR-RXR heterodimers and thus demonstrates that both retinoid response pathways can be independently activated.
ISSN:0036-8075
1095-9203
DOI:10.1126/science.1335166