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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Structure-Based Approach for the Discovery of Novel Selective Estrogen Receptor Modulators

Author(s): C. Rosano, E. Stec-Martyna, R. Lappano and M. Maggiolini

Volume 18 , Issue 8 , 2011

Page: [1188 - 1194] Pages: 7

DOI: 10.2174/092986711795029645

Price: $65


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.

Keywords: Structure based drug design, estrogen, estrogen receptor, lasofoxifene, raloxifene, tamoxifen, SERMs, ADME, DNA, ligand binding domain

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