{"doi":"10.1111/jcpe.13887","title":"Selective <scp>BET</scp> inhibitor <scp>RVX</scp>‐208 ameliorates periodontal inflammation and bone loss","abstract":"AIM: To determine the effects of RVX-208, a selective bromodomain and extra-terminal domain (BET) inhibitor targeting bromodomain 2 (BD2), on periodontal inflammation and bone loss. MATERIALS AND METHODS: Macrophage-like cells (RAW264.7) and human gingival epithelial cells were challenged by Porphyromonas gingivalis (Pg) with or without RVX-208. Inflammatory gene expression and cytokine production were measured by reverse transcription polymerase chain reaction and enzyme-linked immunosorbent assay, respectively. RAW264.7 cells were induced to osteoclast differentiation. After RVX-208 treatment, osteoclast differentiation was evaluated by histology, tartrate-resistant-acid-phosphatase (TRAP) activity and the expression of osteoclast-specific genes. The effect of RVX-208 on osteoclast transcriptome was studied by RNA sequencing. Periodontitis was induced in rats by ligature and local RVX-208 treatment was administered every other day. Alveolar bone loss was measured by micro-computed tomography. RESULTS: RVX-208 inhibited inflammatory gene expression and cytokine production in Pg-infected cells. Osteoclast differentiation was inhibited by RVX-208, as evidenced by reduced osteoclast number, TRAP activity and osteoclast-specific gene expression. RVX-208 displayed a more selective and less profound suppressive impact on transcriptome compared with pan-BET inhibitor, JQ1. RVX-208 administration prevented the alveolar bone loss in vivo. CONCLUSIONS: RVX-208 regulated both upstream (inflammatory cytokine production) and downstream (osteoclast differentiation) events that lead to periodontal tissue destruction, suggesting that it may be a promising 'epi-drug' for the prevention of periodontitis.","journal":"Journal Of Clinical Periodontology","year":2023,"id":363020,"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":8,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9665,"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":1117021,"name":"Nicholas P. Clayton","orcid":"0000-0002-6314-8454","position":1,"is_corresponding":false},{"id":1117552,"name":"Sheikh Alam","orcid":null,"position":2,"is_corresponding":false},{"id":873600,"name":"Niels C. Asmussen","orcid":"0000-0002-0481-5464","position":3,"is_corresponding":false},{"id":1117022,"name":"Andrew Wong","orcid":"0000-0002-0902-3159","position":4,"is_corresponding":false},{"id":1117553,"name":"Jin Ha Kim","orcid":null,"position":5,"is_corresponding":false},{"id":1117554,"name":"Gary Luong","orcid":null,"position":6,"is_corresponding":false},{"id":1117555,"name":"Sasan Mokhtari","orcid":null,"position":7,"is_corresponding":false},{"id":1117556,"name":"David Pellei","orcid":null,"position":8,"is_corresponding":false},{"id":786776,"name":"Caroline K. Carrico","orcid":"0000-0001-9521-9854","position":9,"is_corresponding":false},{"id":452509,"name":"Zvi Schwartz","orcid":"0000-0003-1612-9223","position":10,"is_corresponding":false},{"id":452508,"name":"Barbara D. Boyan","orcid":"0000-0002-9642-0311","position":11,"is_corresponding":false},{"id":109673,"name":"William V. Giannobile","orcid":"0000-0002-7102-9746","position":12,"is_corresponding":false},{"id":509963,"name":"Sinem E. Sahingur","orcid":"0000-0001-6089-637X","position":13,"is_corresponding":false},{"id":731247,"name":"Lin Zhao","orcid":"0000-0003-2994-2387","position":14,"is_corresponding":false},{"id":1117020,"name":"Mingxu Sun","orcid":"0009-0003-5046-2086","position":0,"is_corresponding":true}],"reference_count":40,"raw_metadata":null,"created_at":"2026-07-19T01:14:28.054440Z","pmid":"37855275","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":[]}