Department of Chemistry, Columbia University, New York, New York 10027, USA.
Chirality. 2013 May;25(5):265-74. doi: 10.1002/chir.22145.
Selected examples of natural product and drug atropisomers that exhibit stereoselectivity towards receptor and enzyme targets are reviewed. The atropisomeric preference of the receptors and enzyme binding domains makes these agents attractive molecules for drug development in the treatment of various diseases. Included are commonly recognized atropisomers containing a chiral biaryl axis along with some less common examples of atropisomers without a biaryl axis. The biological targets include: antiapoptotic proteins; bacteria; microtubules; kinases; vasopressin receptors; a G-protein coupled receptor related to obesity; monocarboxylate transporters; tachykinin NK1 -receptors; cyclooxygenase-1 and squalene synthase.
本文综述了具有受体和酶靶点立体选择性的天然产物和药物差向异构体的一些实例。受体和酶结合结构域的对映体选择性使得这些药物成为治疗各种疾病的药物开发的有吸引力的分子。其中包括常见的含有手性联苯轴的对映异构体，以及一些较少见的没有联苯轴的对映异构体。生物靶标包括：抗凋亡蛋白；细菌；微管；激酶；血管加压素受体；与肥胖有关的 G 蛋白偶联受体；单羧酸转运蛋白；速激肽 NK1 受体；环加氧酶-1 和角鲨烯合酶。
