title: ABCG2/BCRP: Specific and Nonspecific Modulators.
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.
authors.affiliation: Grupo de Investigación en Macromoléculas, Departamento de Química, Universidad Nacional de Colombia-Sede Bogotá, 5997, Bogotá, Colombia.
authors.forename: Diana
authors.initials: D
authors.lastname: Peña-Solórzano
authors.affiliation: Institute of Organic Chemistry, University of Regensburg, 93040 Regensburg, Germany.
authors.forename: Simone Alexandra
authors.initials: SA
authors.lastname: Stark
authors.affiliation: Institute of Organic Chemistry, University of Regensburg, 93040 Regensburg, Germany.
authors.forename: Burkhard
authors.initials: B
authors.lastname: König
authors.affiliation: Grupo de Investigación en Macromoléculas, Departamento de Química, Universidad Nacional de Colombia-Sede Bogotá, 5997, Bogotá, Colombia.
authors.forename: Cesar Augusto
authors.initials: CA
authors.lastname: Sierra
authors.affiliation: Grupo de Investigación en Macromoléculas, Departamento de Química, Universidad Nacional de Colombia-Sede Bogotá, 5997, Bogotá, Colombia.
authors.forename: Cristian
authors.initials: C
authors.lastname: Ochoa-Puentes
mesh_terms: D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2 / Q000378:metabolism*; D000818:Animals; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology; D006801:Humans
chemical_list: D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D001688:Biological Products; D005419:Flavonoids
keywords: ABC inhibitor; ABC modulator; ABC transporter; ABCG2/BCRP; multidrug resistance