{"doi":"10.3390/cancers12020466","title":"Venetoclax, a BCL-2 Inhibitor, Enhances the Efficacy of Chemotherapeutic Agents in Wild-Type ABCG2-Overexpression-Mediated MDR Cancer Cells","abstract":"Previous studies have shown that small-molecule BCL-2 inhibitors can have a synergistic interaction with ABCG2 substrates in chemotherapy. Venetoclax is a potent and selective BCL-2 inhibitor, approved by the FDA in 2016 for the treatment of patients with chronic lymphocytic leukemia (CLL). This study showed that, at a non-toxic concentration, venetoclax at 10 µM significantly reversed multidrug resistance (MDR) mediated by wild-type ABCG2, without significantly affecting MDR mediated by mutated ABCG2 (R482G and R482T) and ABCB1, while moderate or no reversal effects were observed at lower concentrations (0.5 to 1 µM). The results showed that venetoclax increased the intracellular accumulation of chemotherapeutic agents, which was the result of directly blocking the wild-type ABCG2 efflux function and inhibiting the ATPase activity of ABCG2. Our study demonstrated that venetoclax potentiates the efficacy of wild-type ABCG2 substrate drugs. These findings may provide useful guidance in combination therapy against wild-type ABCG2-mediated MDR cancer in clinical practice.","journal":"Cancers","year":2020,"id":61862,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":54,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9482,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":327828,"name":"Jonathan Y. Li","orcid":null,"position":1,"is_corresponding":false},{"id":327829,"name":"Qiu‐Xu Teng","orcid":null,"position":2,"is_corresponding":false},{"id":326822,"name":"Zi‐Ning Lei","orcid":"0000-0003-1696-8385","position":3,"is_corresponding":false},{"id":326823,"name":"Ning Ji","orcid":"0009-0004-3200-9429","position":4,"is_corresponding":false},{"id":326824,"name":"Qingbin Cui","orcid":"0000-0003-2561-2962","position":5,"is_corresponding":false},{"id":326825,"name":"Leli Zeng","orcid":"0000-0002-3378-5241","position":6,"is_corresponding":false},{"id":326826,"name":"Yihang Pan","orcid":"0000-0002-6278-7051","position":7,"is_corresponding":false},{"id":326827,"name":"Dong‐Hua Yang","orcid":"0000-0001-8649-5531","position":8,"is_corresponding":false},{"id":253755,"name":"Zhe‐Sheng Chen","orcid":"0000-0002-8289-097X","position":9,"is_corresponding":false},{"id":326821,"name":"Jing‐Quan Wang","orcid":"0000-0003-4331-0482","position":0,"is_corresponding":true}],"reference_count":67,"raw_metadata":null,"created_at":"2026-07-18T21:09:47.114172Z","pmid":"32085398","pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}