{"doi":"10.17615/p2b6-9n53","title":"Decay of an active GPCR: Conformational dynamics govern agonist rebinding and persistence of an active, yet empty, receptor state","abstract":"G protein-coupled receptors (GPCRs) represent a major pharmaceutical drug target. However, one exception has been the visual photoreceptor rhodopsin, long considered “different” due to its covalently bound, light-sensitive retinal ligands. Here we demonstrate that, in contrast to prior assumptions, release of the agonist all-trans retinal (ATR) is not an irreversible process. Instead, during decay of the active species, ATR can rebind any rhodopsin remaining in an active-like conformation, and this active-like state can transiently persist even after agonist dissociation. These insights demonstrate rhodopsin behaves like other diffusible ligand-binding GPCRs and raise the possibility of treating rhodopsin by pharmaceutical agents.","journal":"UNC Libraries","year":2020,"id":144616,"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":0,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9454,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":613043,"name":"Jonathan F. Fay","orcid":"0000-0003-1822-2384","position":1,"is_corresponding":false},{"id":613044,"name":"Christopher T. Schafer","orcid":"0000-0001-9907-295X","position":2,"is_corresponding":false},{"id":613045,"name":"David Farrens","orcid":"0000-0003-2761-4769","position":3,"is_corresponding":false},{"id":613732,"name":"Jay M. Janz","orcid":null,"position":0,"is_corresponding":true}],"reference_count":0,"raw_metadata":null,"created_at":"2026-07-18T23:17:45.339291Z","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":[]}