{"doi":"10.1073/pnas.2113536119","title":"Rearrangement of a unique Kv1.3 selectivity filter conformation upon binding of a drug","abstract":"Significance Voltage-gated potassium channels (Kv) open with membrane depolarization and allow the flow of K + ions. Ion flow is tightly governed by time-dependent entry into nonconducting inactivated states. Here, we focus on Kv1.3, a channel of physiological importance in immune cells. We used cryogenic electron microscopy to determine structures of human Kv1.3 alone and bound to dalazatide, a peptide inhibitor in human trials. In the unbound state, Kv1.3’s outer pore is rearranged compared to all other K + channels analyzed. Interaction of dalazatide with Kv1.3’s outer pore causes a dynamic rearrangement of the selectivity filter as Kv1.3 enters a drug-blocked state.","journal":"Proceedings of the National Academy of Sciences","year":2022,"id":238793,"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":52,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9638,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2022-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":301039,"name":"Tofayel Ahmed","orcid":"0000-0002-7214-1000","position":1,"is_corresponding":false},{"id":863991,"name":"Shi Jian","orcid":null,"position":2,"is_corresponding":false},{"id":863318,"name":"Saumya Bajaj","orcid":"0000-0002-7554-7655","position":3,"is_corresponding":false},{"id":863319,"name":"Seow Theng Ong","orcid":"0000-0001-6089-4745","position":4,"is_corresponding":false},{"id":863320,"name":"Stephanie Shee Min Goay","orcid":"0000-0003-1231-3410","position":5,"is_corresponding":false},{"id":863321,"name":"Yue Zhao","orcid":"0000-0003-1157-5101","position":6,"is_corresponding":false},{"id":48172,"name":"Igor Vorobyov","orcid":"0000-0002-4767-5297","position":7,"is_corresponding":false},{"id":715244,"name":"Changlin Tian","orcid":"0000-0001-9315-900X","position":8,"is_corresponding":false},{"id":863322,"name":"K. George Chandy","orcid":"0000-0002-0557-6143","position":9,"is_corresponding":false},{"id":270335,"name":"Shashi Bhushan","orcid":"0000-0002-8514-5959","position":10,"is_corresponding":false},{"id":863317,"name":"Anu Tyagi","orcid":"0000-0002-6914-7700","position":0,"is_corresponding":true}],"reference_count":51,"raw_metadata":null,"created_at":"2026-07-19T00:22:31.741535Z","pmid":"35091471","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":[]}