PMID- 1335166 OWN - NLM STAT- MEDLINE DCOM- 19930125 LR - 20190618 IS - 0036-8075 (Print) IS - 0036-8075 (Linking) VI - 258 IP - 5090 DP - 1992 Dec 18 TI - Retinoids selective for retinoid X receptor response pathways. PG - 1944-6 AB - 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. FAU - Lehmann, J M AU - Lehmann JM AD - Cancer Center, La Jolla Cancer Research Foundation, La Jolla, CA 92037. FAU - Jong, L AU - Jong L FAU - Fanjul, A AU - Fanjul A FAU - Cameron, J F AU - Cameron JF FAU - Lu, X P AU - Lu XP FAU - Haefner, P AU - Haefner P FAU - Dawson, M I AU - Dawson MI FAU - Pfahl, M AU - Pfahl M LA - eng GR - CA50676/CA/NCI NIH HHS/United States GR - P01 CA51993/CA/NCI NIH HHS/United States PT - Comparative Study PT - Journal Article PT - Research Support, U.S. Gov't, P.H.S. PL - United States TA - Science JT - Science (New York, N.Y.) JID - 0404511 RN - 0 (Macromolecular Substances) RN - 0 (Receptors, Cell Surface) RN - 0 (Receptors, Retinoic Acid) RN - 0 (Recombinant Fusion Proteins) RN - 0 (Retinoid X Receptors) RN - 0 (Retinoids) RN - 0 (Transcription Factors) RN - 5688UTC01R (Tretinoin) RN - EC 2.3.1.28 (Chloramphenicol O-Acetyltransferase) SB - IM MH - Animals MH - Cell Line MH - Chloramphenicol O-Acetyltransferase/genetics/metabolism MH - Kinetics MH - Macromolecular Substances MH - Molecular Structure MH - Receptors, Cell Surface/drug effects/genetics/*metabolism MH - *Receptors, Retinoic Acid MH - Recombinant Fusion Proteins/metabolism MH - Retinoid X Receptors MH - Retinoids/chemistry/*metabolism/pharmacology MH - Structure-Activity Relationship MH - *Transcription Factors MH - Transcription, Genetic MH - Transfection MH - Tretinoin/metabolism/pharmacology EDAT- 1992/12/18 00:00 MHDA- 1992/12/18 00:01 CRDT- 1992/12/18 00:00 PHST- 1992/12/18 00:00 [pubmed] PHST- 1992/12/18 00:01 [medline] PHST- 1992/12/18 00:00 [entrez] AID - 10.1126/science.1335166 [doi] PST - ppublish SO - Science. 1992 Dec 18;258(5090):1944-6. doi: 10.1126/science.1335166.