Journal
ADVANCED DRUG DELIVERY REVIEWS
Volume 61, Issue 1, Pages 34-46Publisher
ELSEVIER
DOI: 10.1016/j.addr.2008.10.004
Keywords
QSAR; Pharmacophore; Inhibitor; Substrate; Multidrug resistance; ABCG2; Breast cancer resistance protein (BCRP); Flavonoids; Chemotherapy
Categories
Funding
- CNRS
- Universite Lyon 1 [UMR 5086]
- Agence Nationale de la Recherche [ANR-06-BLAN-0420]
- Association pour la Recherche sur le Cancer [ARC 3942]
- Ligue Nationale contre le Cancer
- Ministry of Higher Education from Mali
- French Ligue de la Loire contre le Cancer and Association pour la Recherche Sur le Cancer
- region Rhone-Alpes (Explora'Doc mobility program)
- Rhone-Alpes (Cluster program)
- Agence Nationale de la Recherche (ANR) [ANR-06-BLAN-0420] Funding Source: Agence Nationale de la Recherche (ANR)
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In addition to its critical role is controlling drug availability and protecting sensitive organs and stem cells through cellular detoxification. breast cancer resistance protein (BCRP/ABCG2) plays an important role in cancer cell resistance to chemotherapy, together with P-glycoprotein/ABCB1. A main approach to abolish multidrug resistance is to find out specific inhibitors of the drug-efflux activity, able to chemosensitize cancer cell proliferation. Many efforts have been primarily focused on ABCB1, discovered thirty years ago, whereas very few studies have concerned ABCG2, identified much more recently. This review describes the main types of inhibitors presently known for ABCG2, and how quantitative structure-activity relationship analysis among series of compounds may lead to build up molecular models and pharmacophores allowing to design lead inhibitors as future candidates for clinical trials. A special attention is drawn on flavonoids which constitute a structural ly-diverse class of compounds, well suited to identify potent ABCG2-specific inhibitors. (C) 2008 Elsevier B.V. All rights reserved.
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