{"doi":"10.1128/mbio.03560-22","title":"The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function","abstract":"Despite the remarkable success of combination antiretroviral therapy, HIV-1 remains among the major causes of human suffering and loss of life in poor and developing nations. To prevail in this drawn-out battle with the pandemic, it is essential to continue developing advanced antiviral agents to fight drug resistant HIV-1 variants. Allosteric integrase inhibitors (ALLINIs) are an emerging class of HIV-1 antagonists that are orthogonal to the current antiretroviral drugs. These small molecules act as highly specific molecular glue, which triggers the aggregation of HIV-1 integrase. In this work, we present high-resolution crystal structures that reveal the crucial interactions made by two potent ALLINIs, namely, BI-D and Pirmitegravir, with HIV-1 integrase. Our results explain the mechanism of drug action and will inform the development of this promising class of small molecules for future use in antiretroviral regimens.","journal":"mBio","year":2023,"id":336883,"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":18,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9534,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2023-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":823436,"name":"Tung Dinh","orcid":"0000-0002-5141-3281","position":1,"is_corresponding":false},{"id":732590,"name":"Lev Levintov","orcid":"0000-0002-7950-9226","position":2,"is_corresponding":false},{"id":641039,"name":"Arun S. Annamalai","orcid":"0000-0003-4672-7283","position":3,"is_corresponding":false},{"id":1067837,"name":"Juan S. Rey","orcid":"0000-0003-2274-3748","position":4,"is_corresponding":false},{"id":860534,"name":"Lorenzo Briganti","orcid":"0000-0003-2237-6896","position":5,"is_corresponding":false},{"id":277723,"name":"Nicola Cook","orcid":"0000-0002-2738-7976","position":6,"is_corresponding":false},{"id":626565,"name":"Valerie E. Pye","orcid":"0000-0001-9616-2992","position":7,"is_corresponding":false},{"id":709717,"name":"Ian A. Taylor","orcid":"0000-0002-6763-3852","position":8,"is_corresponding":false},{"id":671354,"name":"Kyungjin Kim","orcid":"0000-0002-8271-7640","position":9,"is_corresponding":false},{"id":228712,"name":"Alan Engelman","orcid":"0000-0002-9709-2591","position":10,"is_corresponding":false},{"id":252056,"name":"Baek Kim","orcid":"0000-0001-7986-4335","position":11,"is_corresponding":false},{"id":298286,"name":"Juan R. Perilla","orcid":"0000-0003-1171-6816","position":12,"is_corresponding":false},{"id":324221,"name":"Mamuka Kvaratskhelia","orcid":"0000-0003-3800-0033","position":13,"is_corresponding":false},{"id":277729,"name":"Peter Cherepanov","orcid":"0000-0002-0634-538X","position":14,"is_corresponding":false},{"id":1068268,"name":"Matthew R. Singer","orcid":null,"position":0,"is_corresponding":true}],"reference_count":98,"raw_metadata":null,"created_at":"2026-07-19T01:10:21.947540Z","pmid":"36744954","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":[]}