Beard Richard L, Duong Tien T, Teng Min, Klein Elliott S, Standevan Andrew M, Chandraratna Roshantha A S
Retinoid Research, Department of Chemistry, Allergan Inc., Irvine, CA 92623-9534, USA.
Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8. doi: 10.1016/s0960-894x(02)00647-9.
Retinoids are analogues of all-trans-retinoic acid, a powerful hormone that mediates many fundamental biological processes. Cancer and other serious hyperproliferative diseases are attractive therapeutic targets for retinoids, but the therapeutic use of retinoids is limited due to severe toxicity. We report here the design of retinoid receptor-alpha specific ligands with growth inhibitory activity in breast cancer cell lines, and which do not cause the cutaneous toxicity associated with the currently available nonselective retinoid agonists.
类视黄醇是全反式视黄酸的类似物，全反式视黄酸是一种强大的激素，介导许多基本的生物学过程。癌症和其他严重的过度增殖性疾病是类视黄醇有吸引力的治疗靶点，但由于严重的毒性，类视黄醇的治疗用途受到限制。我们在此报告了在乳腺癌细胞系中具有生长抑制活性且不会引起与目前可用的非选择性类视黄醇激动剂相关的皮肤毒性的类视黄醇受体α特异性配体的设计。
