MedicineOncologyPharmacologyCancer PharmacologyChemotherapyMolecular OncologyCellular Drug EffluxChemotherapy ResistanceEfflux-mediated ResistanceLysosomal TransportTherapeutic ResistanceTransporter PharmacologyAbc TransportersAdenosine Triphosphate-binding Cassette TransportersAnticancer Drug ResistanceAtp-binding Cassette TransportersMultidrug Resistance ModulationTherapeutic Resistance MechanismsTransporter-mediated Drug ResistanceTransporters
Human ABCG2 is a member of the ATP-binding cassette (ABC) transporter superfamily and is known to contribute to multidrug resistance (MDR) in cancer chemotherapy. Among ABC transporters that are known to cause MDR, ABCG2 is particularly interesting for its potential role in protecting cancer stem cells and its complex oligomeric structure. Recent studies have also revealed that the biogenesis of ABCG2 could be modulated by small molecule compounds. These modulators, upon binding to ABCG2, accelerate the endocytosis and trafficking to lysosome for degradation and effectively reduce the half-life of ABCG2. Hence, targeting ABCG2 stability could be a new venue for therapeutic discovery to sensitize drug resistant human cancers. In this report, we review recent progress on understanding the structure, function, biogenesis, as well as physiological and pathophysiological functions of ABCG2.
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