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 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.
Lehmann
J M
JM
Cancer Center, La Jolla Cancer Research Foundation, La Jolla, CA 92037.
Jong
L
L
Fanjul
A
A
Cameron
J F
JF
Lu
X P
XP
Haefner
P
P
Dawson
M I
MI
Pfahl
M
M
D000818:Animals; D002460:Cell Line; D015500:Chloramphenicol O-Acetyltransferase / Q000235:genetics / Q000378:metabolism; D007700:Kinetics; D046911:Macromolecular Substances; D015394:Molecular Structure; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D018168:Receptors, Retinoic Acid; D011993:Recombinant Fusion Proteins / Q000378:metabolism; D047488:Retinoid X Receptors; D012176:Retinoids / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014157:Transcription Factors; D014158:Transcription, Genetic; D014162:Transfection; D014212:Tretinoin / Q000378:metabolism / Q000494:pharmacology
D046911:Macromolecular Substances; D011956:Receptors, Cell Surface; D018168:Receptors, Retinoic Acid; D011993:Recombinant Fusion Proteins; D047488:Retinoid X Receptors; D012176:Retinoids; D014157:Transcription Factors; D014212:Tretinoin; D015500:Chloramphenicol O-Acetyltransferase