{"doi":"10.1021/acschembio.3c00548","title":"Selective and Potent PROTAC Degraders of c-Src Kinase","abstract":"Using dasatinib linked to E3 ligase ligands, we identified a potent and selective dual Csk/c-Src PROTAC degrader. We then replaced dasatinib, the c-Src-directed ligand, with a conformation-selective analogue that stabilizes the αC-helix-out conformation of c-Src. Using the αC-helix-out ligand, we identified a PROTAC that is potent and selective for c-Src. We demonstrated a high degree of catalysis with our c-Src PROTACs. Using our c-Src PROTACs, we identified pharmacological advantages of c-Src degradation compared to inhibition with respect to cancer cell proliferation.","journal":"ACS Chemical Biology","year":2023,"id":343735,"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":14,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9497,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2023-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":787495,"name":"Nathalie M. Vandecan","orcid":null,"position":1,"is_corresponding":false},{"id":1082193,"name":"C. Raymond Bingham","orcid":null,"position":2,"is_corresponding":false},{"id":1081771,"name":"Pui Ki Tsang","orcid":"0000-0003-2893-8247","position":3,"is_corresponding":false},{"id":321056,"name":"Peter Ulintz","orcid":"0000-0002-2037-8655","position":4,"is_corresponding":false},{"id":469420,"name":"Rachel Sexton","orcid":"0000-0002-0008-9629","position":5,"is_corresponding":false},{"id":209285,"name":"Daniel A. Bochar","orcid":null,"position":6,"is_corresponding":false},{"id":289066,"name":"Sofía D. Merajver","orcid":"0000-0002-6823-7130","position":7,"is_corresponding":false},{"id":718235,"name":"Matthew B. Soellner","orcid":"0000-0003-1394-8645","position":8,"is_corresponding":false},{"id":1081770,"name":"Wuxiang Mao","orcid":"0000-0001-7213-3062","position":0,"is_corresponding":true}],"reference_count":31,"raw_metadata":null,"created_at":"2026-07-19T01:11:26.556051Z","pmid":"38113191","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":[]}