Abstract
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
Current Medicinal Chemistry
Title: Structure-Based Approach for the Discovery of Novel Selective Estrogen Receptor Modulators
Volume: 18 Issue: 8
Author(s): C. Rosano, E. Stec-Martyna, R. Lappano and M. Maggiolini
Affiliation:
Keywords: Structure based drug design, estrogen, estrogen receptor, lasofoxifene, raloxifene, tamoxifen, SERMs, ADME, DNA, ligand binding domain
Abstract: 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.
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Cite this article as:
Rosano C., Stec-Martyna E., Lappano R. and Maggiolini M., Structure-Based Approach for the Discovery of Novel Selective Estrogen Receptor Modulators, Current Medicinal Chemistry 2011; 18 (8) . https://dx.doi.org/10.2174/092986711795029645
DOI https://dx.doi.org/10.2174/092986711795029645 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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