S.C. Nanobiotecnologie, Istituto Nazionale per la Ricerca sul Cancro, 16132 Genova, Italy.
Curr Med Chem. 2011;18(8):1188-94. doi: 10.2174/092986711795029645.
In the last twenty years the efforts to design and optimize new drugs have been based on the three dimensional structure of the selected target proteins. In this regard, useful information has been achieved mainly by protein crystallography, which has recently turned from a low into a high-throughput process thanks to the improvement in robot technologies, automation procedure and the use of synchrotron radiation facilities [1-3]. This review examines the impact of Structure Based Drug Design (SBDD) on the discovery of ligands as the selective estrogen receptor modulators (SERMs) of the Estrogen Receptor (ER)α, which is involved in the regulation of several physiological and pathological processes.
在过去的二十年中，设计和优化新药的努力一直基于选定靶蛋白的三维结构。在这方面，主要通过蛋白质晶体学获得了有用的信息，由于机器人技术、自动化程序和同步辐射设施的使用的改进，蛋白质晶体学最近已经从低通量转变为高通量过程[1-3]。这篇综述考察了基于结构的药物设计（SBDD）对配体发现的影响，这些配体是雌激素受体（ER）α的选择性雌激素受体调节剂（SERMs），参与了几种生理和病理过程的调节。
