Structure-based approach for the discovery of novel selective estrogen receptor modulators

C. Rosano, E. Stec-Martyna, R. Lappano, M. Maggiolini

Research output: Contribution to journalArticle

10 Citations (Scopus)

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), which is involved in the regulation of several physiological and pathological processes.

Original languageEnglish
Pages (from-to)1188-1194
Number of pages7
JournalCurrent Medicinal Chemistry
Volume18
Issue number8
DOIs
Publication statusPublished - Mar 2011

Fingerprint

Selective Estrogen Receptor Modulators
Physiological Phenomena
Crystallography
Synchrotrons
Drug Design
Automation
Pathologic Processes
Synchrotron radiation
Estrogen Receptors
Pharmaceutical Preparations
Proteins
Throughput
Robots
Radiation
Ligands
Technology

Keywords

  • Estrogen
  • Estrogen receptor
  • Lasofoxifene
  • Raloxifene
  • Structure based drug design
  • Tamoxifen

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

Cite this

Structure-based approach for the discovery of novel selective estrogen receptor modulators. / Rosano, C.; Stec-Martyna, E.; Lappano, R.; Maggiolini, M.

In: Current Medicinal Chemistry, Vol. 18, No. 8, 03.2011, p. 1188-1194.

Research output: Contribution to journalArticle

Rosano, C. ; Stec-Martyna, E. ; Lappano, R. ; Maggiolini, M. / Structure-based approach for the discovery of novel selective estrogen receptor modulators. In: Current Medicinal Chemistry. 2011 ; Vol. 18, No. 8. pp. 1188-1194.
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