Journal ArticleDOI
ABCG2/BCRP: Specific and Nonspecific Modulators.
Diana Peña-Solórzano,Simone Alexandra Stark,Burkhard König,Cesar A. Sierra,Cristian Ochoa-Puentes +4 more
TLDR
The aim of the present review is to describe and highlight specific and nonspecific modulators of ABCG2 reported to date based on the selectivity of the compounds, as many of them are effective against one or more ABC transport proteins.Abstract:
Multidrug resistance (MDR) in cancer cells is the development of resistance to a variety of structurally and functionally nonrelated anticancer drugs. This phenomenon has become a major obstacle to cancer chemotherapy seriously affecting the clinical outcome. MDR is associated with increased drug efflux from cells mediated by an energy-dependent mechanism involving the ATP-binding cassette (ABC) transporters, mainly P-glycoprotein (ABCB1), the MDR-associated protein-1 (ABCC1), and the breast cancer resistance protein (ABCG2). The first two transporters have been widely studied already and reviews summarized the results. The ABCG2 protein has been a subject of intense study since its discovery as its overexpression has been detected in resistant cell lines in numerous types of human cancers. To date, a long list of modulators of ABCG2 exists and continues to increase. However, little is known about the clinical consequences of ABCG2 modulation. This makes the design of novel, potent, and nontoxic inhibitors of this efflux protein a major challenge to reverse MDR and thereby increase the success of chemotherapy. The aim of the present review is to describe and highlight specific and nonspecific modulators of ABCG2 reported to date based on the selectivity of the compounds, as many of them are effective against one or more ABC transport proteins.read more
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Inhibitors of Human ABCG2: From Technical Background to Recent Updates With Clinical Implications.
TL;DR: This mini-review provides integrated information covering the technical backgrounds necessary to evaluate the ABCG2 inhibitory effects on the target compounds and a current update on theABCG2 inhibitors, as febuxostat is serendipitously identified as a well-used agent for hyperuricemia as a strong ABCG1 inhibitor that possesses some promising potentials.
Journal ArticleDOI
MicroRNA-145 exerts tumor-suppressive and chemo-resistance lowering effects by targeting CD44 in gastric cancer.
TL;DR: The results demonstrated that miR-145 regulated CD44 by targeting directly the CD44 3’-untranslated region (3‘-UTR), which plays critical roles in the regulation of tumor growth and chemo-resistance in gastric cancer.
Journal ArticleDOI
Defying Multidrug resistance! Modulation of Related Transporters by Flavonoids and Flavonolignans
Christopher S. Chambers,Jitka Viktorova,Kateřina Řehořová,David Biedermann,Lucie Turková,Tomas Macek,Vladimír Křen,Kateřina Valentová +7 more
TL;DR: Flavonoids and particularly flavonolignans are therefore highly prospective compounds for defying multidrug resistance.
Journal ArticleDOI
The Breast Cancer Stem Cells Traits and Drug Resistance
TL;DR: In this article, the authors summarize the principal BCSCs surface markers and signaling pathways, and list the BCSC-related drug resistance mechanisms in chemotherapy (CT), endocrine therapy (ET), and targeted therapy (TT).
References
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Journal ArticleDOI
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