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Breaking boundaries: Pan BETi disrupt 3D chromatin structure, BD2-selective BETi are strictly epigenetic transcriptional regulators.
Tsujikawa LM, Kharenko OA, Stotz SC, Rakai BD, Sarsons CD, Gilham D, Wasiak S, Fu L, Sweeney M, Johansson JO, Wong NCW, Kulikowski E. Tsujikawa LM, et al. Among authors: rakai bd. Biomed Pharmacother. 2022 Aug;152:113230. doi: 10.1016/j.biopha.2022.113230. Epub 2022 Jun 7. Biomed Pharmacother. 2022. PMID: 35687908 Free article.
Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism.
Tsujikawa LM, Fu L, Das S, Halliday C, Rakai BD, Stotz SC, Sarsons CD, Gilham D, Daze E, Wasiak S, Studer D, Rinker KD, Sweeney M, Johansson JO, Wong NCW, Kulikowski E. Tsujikawa LM, et al. Among authors: rakai bd. Clin Epigenetics. 2019 Jul 12;11(1):102. doi: 10.1186/s13148-019-0696-z. Clin Epigenetics. 2019. PMID: 31300040 Free PMC article.
Epigenetic Modulation by Apabetalone Counters Cytokine-Driven Acute Phase Response In Vitro, in Mice and in Patients with Cardiovascular Disease.
Wasiak S, Gilham D, Daze E, Tsujikawa LM, Halliday C, Stotz SC, Rakai BD, Fu L, Jahagirdar R, Sweeney M, Johansson JO, Wong NCW, Kulikowski E. Wasiak S, et al. Among authors: rakai bd. Cardiovasc Ther. 2020 Jul 21;2020:9397109. doi: 10.1155/2020/9397109. eCollection 2020. Cardiovasc Ther. 2020. PMID: 32821285 Free PMC article.
BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes.
Wasiak S, Dzobo KE, Rakai BD, Kaiser Y, Versloot M, Bahjat M, Stotz SC, Fu L, Sweeney M, Johansson JO, Wong NCW, Stroes ESG, Kroon J, Kulikowski E. Wasiak S, et al. Among authors: rakai bd. Clin Epigenetics. 2020 Nov 11;12(1):166. doi: 10.1186/s13148-020-00943-0. Clin Epigenetics. 2020. PMID: 33172487 Free PMC article.
Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy.
Fu L, Wasiak S, Tsujikawa LM, Rakai BD, Stotz SC, Wong NCW, Johansson JO, Sweeney M, Mohan CM, Khan A, Kulikowski E. Fu L, et al. Among authors: rakai bd. Pharmacol Res Perspect. 2022 Jun;10(3):e00949. doi: 10.1002/prp2.949. Pharmacol Res Perspect. 2022. PMID: 35417091 Free PMC article.
Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells.
Wasiak S, Tsujikawa LM, Daze E, Gilham D, Stotz SC, Rakai BD, Sarsons CD, Fu L, Azhar S, Jahagirdar R, Sweeney M, Johansson JO, Wong NCW, Kulikowski E. Wasiak S, et al. Among authors: rakai bd. Atherosclerosis. 2023 Jan;364:10-19. doi: 10.1016/j.atherosclerosis.2022.11.015. Epub 2022 Nov 23. Atherosclerosis. 2023. PMID: 36455344
Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation.
Fu L, Gilham D, Stotz SC, Sarsons CD, Rakai BD, Tsujikawa LM, Wasiak S, Johansson JO, Sweeney M, Wong NCW, Kulikowski E. Fu L, et al. Among authors: rakai bd. Int Immunopharmacol. 2023 Apr;117:109929. doi: 10.1016/j.intimp.2023.109929. Epub 2023 Feb 23. Int Immunopharmacol. 2023. PMID: 36857935 Free PMC article.
15 results