{"doi":"10.1007/s10549-023-07136-2","title":"Complete elimination of estrogen receptor α by PROTAC estrogen receptor α degrader ERD-148 in breast cancer cells","abstract":null,"journal":"Breast Cancer Research and Treatment","year":2024,"id":594983,"datarank":0.37273599746820013,"base_score":2.4849066497880004,"endowment":2.4849066497880004,"self_citation_contribution":0.37273599746820013,"citation_network_contribution":0.0,"self_endowment_contribution":0.37273599746820013,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":11,"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":1057151,"name":"Jiantao Hu","orcid":"0009-0007-4782-8779","position":1,"is_corresponding":false},{"id":775798,"name":"Biao Hu","orcid":"0000-0002-4691-6490","position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Complete elimination of estrogen receptor α by PROTAC estrogen receptor α degrader ERD-148 in breast cancer cells","abstract":"<h4>Purpose</h4>Estrogen Receptor α (ERα) is a well-established therapeutic target for Estrogen Receptor (ER)-positive breast cancers. Both Selective Estrogen Receptor Degraders (SERD) and PROTAC ER degraders are synthetic compounds suppressing the ER activity through the degradation of ER. However, the differences between SERD and PROTAC ER degraders are far from clear.<h4>Methods</h4>The effect of PROTAC ER degrader ERD-148 and SERD fulvestrant on protein degradation was evaluated by western blot analysis. The cell proliferation was tested by WST-8 assays and the gene expressions were assessed by gene microarray and real-time RT-PCR analysis after the compound treatment.<h4>Results</h4>ERD-148 is a potent and selective PROTAC ERα degrader. It degrades not only unphosphorylated ERα but also the phosphorylated ERα in the cells. In contrast, the SERD fulvestrant showed much-reduced degradation potency on the phosphorylated ERα. The more complete degradation of ERα by ERD-148 translates into a greater maximum cell growth inhibition. However, ERD-148 and fulvestrant share a similar gene regulation profile except for the variation of regulation potency. Further studies indicate that ERD-148 degrades the ERα in fulvestrant-resistant cells.<h4>Conclusion</h4>PROTAC ER degrader has a different mechanism of action compared to SERD which may be used in treating fulvestrant-resistant cancers.","is_dataset_classified":null,"base_score":2.4849066497880004,"endowment":2.4849066497880004,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"37847455","pmcid":null,"openalex_id":"https://openalex.org/W4387692979","authors":[],"funders":[{"funder_name":"University of Michigan Regional Comprehensive Metabolomics Resource Core","grant_id":"U24 DK097153","title":null},{"funder_name":"National Institutes of Health","grant_id":"5U24DK097153-03","title":"Data &amp; Information Tech Core - Athey"}],"total_grants":2,"fwci":1.0299,"citation_percentile":0.74804593,"influential_citations":0,"citation_trend":[{"year":2024,"count":4},{"year":2025,"count":5},{"year":2026,"count":2}],"oa_status":"closed","license":"Springer Nature TDM","oa_locations":[{"url":"https://link.springer.com/content/pdf/10.1007/s10549-023-07136-2.pdf","host_type":"publisher"},{"url":"https://link.springer.com/article/10.1007/s10549-023-07136-2/fulltext.html","host_type":"publisher"},{"url":"https://doi.org/10.1007/s10549-023-07136-2","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/37847455","host_type":"repository"},{"url":"http://deepblue.lib.umich.edu/bitstream/2027.42/192647/2/complete.pdf","host_type":"repository"},{"url":"https://dx.doi.org/10.7302/22463","host_type":""},{"url":"https://doi.org/https://doi.org/10.7302/22463","host_type":""},{"url":"https://doi.org/https://doi.org/10.1007/s10549-023-07136-2","host_type":""}],"fields_of_study":["Protein Degradation and Inhibitors","Estrogen and related hormone effects","Advanced Breast Cancer Therapies","03 medical and health sciences","0302 clinical medicine","Female","Humans","Breast Neoplasms","Estrogen Antagonists","Estrogen Receptor alpha","Fulvestrant","Selective Estrogen Receptor Modulators"],"mesh_terms":["Fulvestrant","Breast Neoplasms","Estrogen Antagonists","Female","Humans","Selective Estrogen Receptor Modulators","Estrogen Receptor alpha"],"keywords":["Fulvestrant","Estrogen receptor","Cancer research","Estrogen receptor alpha","Estrogen","Cell growth","Biology","Chemistry","Cancer","Breast cancer","Internal medicine","Endocrinology","Medicine","Biochemistry","Mcf7","Estrogen Receptor Α","Protac Er Degrader","Phosphorylated Erα","Selective Estrogen Receptor Modulators","Estrogen Antagonists","Breast Neoplasms","Humans","Female"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-07-27T16:08:20.297904Z","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":[]}