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

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


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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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.

Abstract

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.

Keywords:

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



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Article Details

Volume: 4
Issue Number: 6
First Page: 491
Last Page: 508
Page Count: 18
DOI: 10.2174/1568011043352696
Price: $58
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