title: ABCG2: recent discovery of potent and highly selective inhibitors.
abstract: ABCG2 impacts oral availability, tissue distribution and excretion of its substrates, including anticancer and anti-infectious drugs. Highly expressed at physiological barriers, its secretion level significantly controls drug distribution. Furthermore, its increased content into many types of cancer may lead to cell chemoresistance. Owing to the clinical relevance of ABCG2 in the multidrug resistance phenomenon, ABCG2 constitutes an appealing therapeutic target to increase drug distribution. Development of ABCG2 inhibitors can be used in combination with anticancer drugs to block the drug secretion from cancer cells. Very recently, an alternative use of ABCG2 inhibitors in enhancing the bioavailability of ABCG2 substrates has emerged. Hence, it is important to investigate ABCG2 inhibitors with high selectivity, high potency and safety. New inhibitors discovered during the last 5 years will be presented and discussed.
authors.affiliation: Université Joseph Fourier, Grenoble 1, CNRS UMR 5063, Département de Pharmacochimie Moléculaire, Grenoble, France.
authors.forename: Florine
authors.initials: F
authors.lastname: Lecerf-Schmidt
authors.forename: Basile
authors.initials: B
authors.lastname: Peres
authors.forename: Glaucio
authors.initials: G
authors.lastname: Valdameri
authors.forename: Charlotte
authors.initials: C
authors.lastname: Gauthier
authors.forename: Evelyn
authors.initials: E
authors.lastname: Winter
authors.forename: Léa
authors.initials: L
authors.lastname: Payen
authors.forename: Attilio
authors.initials: A
authors.lastname: Di Pietro
authors.forename: Ahcène
authors.initials: A
authors.lastname: Boumendjel
mesh_terms: D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000970:Antineoplastic Agents / Q000627:therapeutic use; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D002867:Chromones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D006801:Humans; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013267:Stilbenes / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D000970:Antineoplastic Agents; D047188:Chalcones; D002867:Chromones; D009363:Neoplasm Proteins; D011804:Quinolines; D013267:Stilbenes; C402343:tariquidar