{"doi":"10.7554/elife.94488","title":"ME3BP-7 is a targeted cytotoxic agent that rapidly kills pancreatic cancer cells expressing high levels of monocarboxylate transporter MCT1","abstract":"Nearly 30% of pancreatic ductal adenocarcinomas (PDACs) exhibit a marked overexpression of monocarboxylate transporter 1 (MCT1) offering a unique opportunity for therapy. However, biochemical inhibitors of MCT1 have proven unsuccessful in clinical trials. In this study, we present an alternative approach using 3-bromopyruvate (3BP) to target MCT1 overexpressing PDACs. 3BP is a cytotoxic agent that is known to be transported into cells via MCT1, but its clinical usefulness has been hampered by difficulties in delivering the drug systemically. We describe here a novel microencapsulated formulation of 3BP (ME3BP-7), which is effective against a variety of PDAC cells in vitro and remains stable in serum. Furthermore, systemically administered ME3BP-7 significantly reduces pancreatic cancer growth and metastatic spread in multiple orthotopic models of pancreatic cancer with manageable toxicity. ME3BP-7 is, therefore, a prototype of a promising new drug, in which the targeting moiety and the cytotoxic moiety are both contained within the same single small molecule.","journal":"eLife","year":2024,"id":490364,"datarank":0.11091635234068717,"base_score":0.6931471805599453,"endowment":0.6931471805599453,"self_citation_contribution":0.10397207708399181,"citation_network_contribution":0.0069442752566953566,"self_endowment_contribution":0.10397207708399181,"citer_contribution":0.0069442752566953566,"corpus_percentile":null,"corpus_rank":null,"citation_count":1,"citer_count":1,"citers_with_citation_signal":1,"citers_with_endowment":1,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9539,"is_data_producer":true,"deposit_databanks":{"Dryad":["10.5061/dryad.vhhmgqp5m"]},"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2024-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":294018,"name":"Marco Dal Molin","orcid":"0000-0003-1581-3576","position":1,"is_corresponding":false},{"id":615679,"name":"Brian J. Mog","orcid":"0000-0001-9988-7147","position":2,"is_corresponding":false},{"id":869270,"name":"Gyuri Han","orcid":null,"position":3,"is_corresponding":false},{"id":619583,"name":"Evangeline Watson","orcid":null,"position":4,"is_corresponding":false},{"id":732242,"name":"Nicolas Wyhs","orcid":"0000-0003-4252-4470","position":5,"is_corresponding":false},{"id":530912,"name":"Shun Ishiyama","orcid":null,"position":6,"is_corresponding":false},{"id":1176500,"name":"Taha Ahmedna","orcid":"0000-0003-4786-2292","position":7,"is_corresponding":false},{"id":420232,"name":"Il Minn","orcid":"0000-0002-7822-662X","position":8,"is_corresponding":false},{"id":62888,"name":"Nilofer S. Azad","orcid":"0000-0002-9613-3988","position":9,"is_corresponding":false},{"id":24634,"name":"Chetan Bettegowda","orcid":"0000-0001-9991-7123","position":10,"is_corresponding":false},{"id":2254,"name":"Nickolas Papadopoulos","orcid":"0000-0001-7135-7451","position":11,"is_corresponding":false},{"id":2256,"name":"Kenneth W. Kinzler","orcid":"0000-0001-5591-1176","position":12,"is_corresponding":false},{"id":62904,"name":"Shibin Zhou","orcid":"0000-0003-1941-4425","position":13,"is_corresponding":false},{"id":2255,"name":"Bert Vogelstein","orcid":"0000-0003-0766-3854","position":14,"is_corresponding":false},{"id":484337,"name":"Kathleen L. Gabrielson","orcid":"0000-0003-3901-4357","position":15,"is_corresponding":false},{"id":658685,"name":"Surojit Sur","orcid":"0000-0003-4536-7343","position":16,"is_corresponding":false},{"id":334511,"name":"Jordina Rincón-Torroella","orcid":"0000-0003-4798-8231","position":0,"is_corresponding":true}],"reference_count":59,"raw_metadata":null,"created_at":"2026-07-19T02:08:32.775003Z","pmid":"40391649","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":[]}