Lehmann J M, Jong L, Fanjul A, Cameron J F, Lu X P, Haefner P, Dawson M I, Pfahl M
Cancer Center, La Jolla Cancer Research Foundation, La Jolla, CA 92037.
Science. 1992 Dec 18;258(5090):1944-6. doi: 10.1126/science.1335166.
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.
类视黄醇具有广泛的生物活性,是有用的治疗药物。它们的生理活性由两种类型的受体介导,即视黄酸受体(RARs)和类视黄醇X受体(RXRs)。RARs以及几种相关受体需要与RXRs异源二聚化才能有效地结合DNA并发挥功能。然而,在9-顺式视黄酸(一种RARs和RXRs的配体)存在的情况下,RXRs也可以形成同二聚体。据报道,一系列类视黄醇可选择性激活RXR同二聚体,但不影响RAR-RXR异二聚体,因此表明两种类视黄醇反应途径均可被独立激活。