{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["14(2)"],"submitter":["Mamai A"],"funding":["Ontario Institute for Cancer Research","Johnson and Johnson Research and Development team","Ministry of Research and Innovation"],"pubmed_abstract":["B cell lymphoma 6 (BCL6), a highly regulated transcriptional repressor, is deregulated in several forms of non-Hodgkin lymphoma (NHL), most notably in diffuse large B-cell lymphoma (DLBCL). The activities of BCL6 are dependent on protein-protein interactions with transcriptional co-repressors. To find new therapeutic interventions addressing the needs of patients with DLBCL, we initiated a program to identify BCL6 inhibitors that interfere with co-repressor binding. A virtual screen hit with binding activity in the high micromolar range was optimized by structure-guided methods, resulting in a novel and highly potent inhibitor series. Further optimization resulted in the lead candidate <b>58</b> (OICR12694/JNJ-65234637), a BCL6 inhibitor with low nanomolar DLBCL cell growth inhibition and "],"journal":["ACS medicinal chemistry letters"],"pagination":["199-210"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9923840"],"repository":["biostudies-literature"],"pubmed_title":["Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor."],"pmcid":["PMC9923840"],"pubmed_authors":["Watson ID","Aman A","Connolly P","Marcellus R","Kiyota T","Du Jardin M","Al-Awar R","Undzys E","Poda G","Mohammed M","Pomroy NC","Phillippar U","Attar R","Uehling DE","Abibi A","Prakesch MA","Theriault B","Wilson BJ","Joseph BB","O'Meara J","Subramaniam R","Chan M","Subramanian PR","Edwards J","Nguyen K","Packman K","Isaac MB","Mamai A","Morin JA","Kuntz DA","Strathdee G","Prive GG","Chau AM","Morshed MM","Winston J","Lu T","Austin N"],"additional_accession":[]},"is_claimable":false,"name":"Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.","description":"B cell lymphoma 6 (BCL6), a highly regulated transcriptional repressor, is deregulated in several forms of non-Hodgkin lymphoma (NHL), most notably in diffuse large B-cell lymphoma (DLBCL). The activities of BCL6 are dependent on protein-protein interactions with transcriptional co-repressors. To find new therapeutic interventions addressing the needs of patients with DLBCL, we initiated a program to identify BCL6 inhibitors that interfere with co-repressor binding. A virtual screen hit with binding activity in the high micromolar range was optimized by structure-guided methods, resulting in a novel and highly potent inhibitor series. Further optimization resulted in the lead candidate <b>58</b> (OICR12694/JNJ-65234637), a BCL6 inhibitor with low nanomolar DLBCL cell growth inhibition and ","dates":{"release":"2023-01-01T00:00:00Z","publication":"2023 Feb","modification":"2025-04-19T22:30:02.675Z","creation":"2025-04-19T22:30:02.675Z"},"accession":"S-EPMC9923840","cross_references":{"pubmed":["36793435"],"doi":["10.1021/acsmedchemlett.2c00502"]}}