Multiple Targeting by the Antitumor Drug Tamoxifen: A Structure-Activity Study

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

Download PDF Flyer

Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

This journal supports open access

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 27th of 59 in Chemistry, Medicinal

Submit Abstracts Online Submit Manuscripts Online

Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.722
5 - Year: 2.849

Multiple Targeting by the Antitumor Drug Tamoxifen: A Structure-Activity Study

Anti-Cancer Agents in Medicinal Chemistry, 4(6): 491-508.

Author(s): Philippe de Medina, Gilles Favre and Marc Poirot.

Affiliation: INSERM U 563, C.P.T.P.,Departement Innovation Therapeutique et Oncologie Moleculaire, InstitutClaudius Regaud, 20-24 rue du Pont Saint Pierre, 31052 Toulouse Cedex; France.


Tamoxifen is a well-known antiestrogen used for the hormonotherapy of estrogen receptor positive breast cancer. In addition to its high affinity binding to the estrogen receptor (ER), tamoxifen binds with comparable affinity to the microsomal antiestrogen binding site (AEBS), and inhibits with a micromolar efficiency, protein kinase C (PKC), calmodulin (CaM)-dependent enzymes and Acyl CoenzymeA: Cholesterol Acyl Transferase (ACAT). Each of these tamoxifen targets might explain the genomic as well as non-genomic effects of tamoxifen. In this review, we will report current knowledge about the structural features of tamoxifen involved in this multiple targeting. These data provide a useful guide for the conception of selective ligands of ERs, AEBS, PKC, CaM or ACAT based on the chemical structure of tamoxifen.


tamoxifen, antiestrogen, estrogen receptor, pkc, calmodulin, acat, aebs, cancer.

Purchase Online Order Reprints Order Eprints Rights and Permissions

Article Details

Volume: 4
Issue Number: 6
First Page: 491
Last Page: 508
Page Count: 18
DOI: 10.2174/1568011043352696
Price: $58
Global Biotechnology Congress 2017Drug Discovery and Therapy World Congress 2017

Related Journals

Related eBooks

Webmaster Contact: Copyright © 2017 Bentham Science