{"doi":"10.1002/anie.202003342","title":"Activation of the G‐Protein‐Coupled Receptor Rhodopsin by Water","abstract":"Visual rhodopsin is an important archetype for G-protein-coupled receptors, which are membrane proteins implicated in cellular signal transduction. Herein, we show experimentally that approximately 80 water molecules flood rhodopsin upon light absorption to form a solvent-swollen active state. An influx of mobile water is necessary for activating the photoreceptor, and this finding is supported by molecular dynamics (MD) simulations. Combined force-based measurements involving osmotic and hydrostatic pressure indicate the expansion occurs by changes in cavity volumes, together with greater hydration in the active metarhodopsin-II state. Moreover, we discovered that binding and release of the C-terminal helix of transducin is coupled to hydration changes as may occur in visual signal amplification. Hydration-dehydration explains signaling by a dynamic allosteric mechanism, in which the soft membrane matter (lipids and water) has a pivotal role in the catalytic G-protein cycle.","journal":"Angewandte Chemie International Edition","year":2020,"id":100002,"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":29,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9498,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"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":491701,"name":"Suchithranga M.D.C. Perera","orcid":"0000-0002-7693-3224","position":1,"is_corresponding":false},{"id":360663,"name":"Steven D.E. Fried","orcid":"0000-0002-4826-2451","position":2,"is_corresponding":false},{"id":491702,"name":"Anna R. Eitel","orcid":"0000-0002-0050-9259","position":3,"is_corresponding":false},{"id":491703,"name":"Blake Mertz","orcid":"0000-0002-7677-0496","position":4,"is_corresponding":false},{"id":491704,"name":"Nipuna Weerasinghe","orcid":"0000-0002-9319-7353","position":5,"is_corresponding":false},{"id":492897,"name":"Michael C. Pitman","orcid":null,"position":6,"is_corresponding":false},{"id":491705,"name":"Andrey V. Struts","orcid":"0000-0002-1758-5151","position":7,"is_corresponding":false},{"id":229052,"name":"Michael F. Brown","orcid":"0000-0003-4154-0241","position":8,"is_corresponding":false},{"id":492896,"name":"Udeep Chawla","orcid":null,"position":0,"is_corresponding":true}],"reference_count":96,"raw_metadata":null,"created_at":"2026-07-18T22:38:35.493878Z","pmid":"32596956","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":[]}