{"doi":"10.1016/j.bioorg.2025.108847","title":"The LSD1/HDAC dual-target inhibitor for cancer therapy: Challenge and opportunity","abstract":null,"journal":"Bioorganic Chemistry","year":2025,"id":642431,"datarank":0.32958368660043297,"base_score":2.1972245773362196,"endowment":2.1972245773362196,"self_citation_contribution":0.32958368660043297,"citation_network_contribution":0.0,"self_endowment_contribution":0.32958368660043297,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":8,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1671016,"name":"Hao-Qian Zhang","orcid":null,"position":1,"is_corresponding":false},{"id":1671018,"name":"Chen-Chen Ren","orcid":null,"position":2,"is_corresponding":false},{"id":1671020,"name":"Yong-Xing Chen","orcid":null,"position":3,"is_corresponding":false},{"id":638330,"name":"Ying Xu","orcid":"0000-0001-7341-8676","position":4,"is_corresponding":false},{"id":1644683,"name":"Rui-Fang Li","orcid":null,"position":5,"is_corresponding":false},{"id":1671023,"name":"Yi-Ru Bai","orcid":null,"position":6,"is_corresponding":false},{"id":95593,"name":"Hong-Min Liu","orcid":null,"position":7,"is_corresponding":false},{"id":490463,"name":"Shuo Yuan","orcid":"0000-0003-1880-6611","position":8,"is_corresponding":false},{"id":108957,"name":"Li Yang","orcid":"0000-0002-2528-5087","position":9,"is_corresponding":false},{"id":1671014,"name":"Dan-Dan Shen","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"The LSD1/HDAC dual-target inhibitor for cancer therapy: Challenge and opportunity","abstract":"In recent years, the epigenetic regulation in tumor development has garnered significant attention. The lysine-specific demethylase 1 (LSD1) and histone deacetylase (HDAC), key enzymes involved in epigenetic modification, are overexpressed in various cancers and promote tumor cell proliferation and differentiation by modulating histone modifications. Although single-target inhibitors for LSD1 or HDAC exhibit efficacy in preclinical models, their clinical utility is hindered by compensatory signaling pathways and the emergence of drug resistance. The development of bifunctional inhibitors targeting both LSD1 and HDAC has emerged as a promising strategy to synergistically remodel chromatin structure, thereby enhancing anti-tumor effects. Furthermore, several dual-target inhibitors have been reported, showcasing potent tumor suppression with low toxicity and high selectivity. The advancement of dual-target inhibitors represents a novel direction for cancer therapy. However, further investigation is required to optimize pharmacokinetics, enhance target selectivity, elucidate resistance mechanisms, and conduct systematic validation for clinical translation. This review highlights recent progress in LSD1/HDAC dual-target inhibitors to stimulate future research and structural optimization.","is_dataset_classified":null,"base_score":1.9459101490553132,"endowment":1.9459101490553132,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"40782410","pmcid":null,"openalex_id":"https://openalex.org/W4413001856","authors":[],"funders":[{"funder_name":"Henan Provincial Science and Technology Research Project","grant_id":"252102311176","title":null},{"funder_name":"Henan Provincial Science and Technology Research Project","grant_id":"242102311236","title":null},{"funder_name":"China Postdoctoral Science Foundation","grant_id":"2024M750818","title":null},{"funder_name":"National Natural Science Foundation of China","grant_id":"82304286","title":null},{"funder_name":"National Natural Science Foundation of China","grant_id":"82303741","title":null}],"total_grants":5,"fwci":2.4028,"citation_percentile":0.89158204,"influential_citations":0,"citation_trend":[{"year":2026,"count":6}],"oa_status":"closed","license":"https://doi.org/10.15223/policy-004","oa_locations":[{"url":"https://api.elsevier.com/content/article/PII:S0045206825007278?httpAccept=text/xml","host_type":"publisher"},{"url":"https://api.elsevier.com/content/article/PII:S0045206825007278?httpAccept=text/plain","host_type":"publisher"},{"url":"https://doi.org/10.1016/j.bioorg.2025.108847","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/40782410","host_type":"repository"}],"fields_of_study":["Histone Deacetylase Inhibitors Research","Epigenetics and DNA Methylation","Protein Degradation and Inhibitors","Humans","Histone Demethylases","Neoplasms","Antineoplastic Agents","Histone Deacetylases","Histone Deacetylase Inhibitors","Molecular Structure","Animals","Cell Proliferation","Structure-Activity Relationship","Enzyme Inhibitors"],"mesh_terms":["Animals","Antineoplastic Agents","Enzyme Inhibitors","Histone Deacetylases","Humans","Neoplasms","Structure-Activity Relationship","Molecular Structure","Cell Proliferation","Histone Demethylases","Histone Deacetylase Inhibitors"],"keywords":["Chemistry","Cancer therapy","Dual (grammatical number)","Cancer","Cancer research","Internal medicine","Medicine","Hdac","Lsd1","Dual-target Inhibitor"],"sdg_mappings":[],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-07T22:43:22.210862Z","pmid":null,"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":[]}