Cariprazine, A Dopamine D₂/D₃ Receptor Partial Agonist, Modulates ABCG2-Mediated Multidrug Resistance in Cancer.

ABSTRACT: Multidrug resistance (MDR) is a continuing clinical problem that limits the efficacy of chemotherapy in cancer. The over expression of the ATP-binding cassette (ABC) family G2 (ABCG2) transporter is one of the main mechanisms that mediates MDR in cancer. Molecular modeling data indicated that cariprazine, a dopamine D₂/D₃ receptor partial agonist, had a significant binding affinity for ABCG2 transporter with a Glide XP score of -6.515. Therefore, in this in vitro study, we determined the effect of cariprazine on MDR resulting from the overexpression of ABCG2 transporters. Alone, cariprazine, at concentrations up to 20 μM, did not significantly decrease cell viability. Cariprazine, at concentrations ranging from 1 to 10 μM, did not significantly alter the cytotoxicity of mitoxantrone (MX) i

SUBMITTER: Hussein N 

PROVIDER: S-EPMC6162716 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature