Lazertinib improves the efficacy of chemotherapeutic drugs in ABCB1 or ABCG2 overexpression cancer cells in vitro, in vivo, and ex vivo
Yingfang Fan, Tian Tao, Zhixing Guo, Kenneth K.W. To, Da Chen, Shaocong Wu, Chuan Yang, Jin-Sui Li, Min Luo, Fang Wang, Liwu Fu
Abstract
I-iodoarylazidoprazosin (IAAP). However, lazertinib neither changed the expression or locolization of ABCB1 and ABCG2 nor blocked the signal pathway of Akt or Erk1/2 at a drug concentration effective for MDR reversal. Overall, our results demonstrate that lazertinib effectively reverses ABCB1- or ABCG2-mediated MDR by competitively binding to the ATP-binding site and inhibiting drug efflux function. This is the first report demonstrating the novel combined use of lazertinib and conventional chemotherapeutical drugs to overcome MDR in ABCB1/ABCG2-overexpressing cancer cells.
Topics & Concepts
Ex vivoIn vivoAbcg2In vitroPharmacologyCancerCancer researchBiologyMedicineChemistryATP-binding cassette transporterTransporterInternal medicineBiochemistryGeneGeneticsDrug Transport and Resistance MechanismsPancreatic and Hepatic Oncology ResearchCholangiocarcinoma and Gallbladder Cancer Studies