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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: fu l. 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: fu l. 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: fu l. Clin Epigenetics. 2020 Nov 11;12(1):166. doi: 10.1186/s13148-020-00943-0. Clin Epigenetics. 2020. PMID: 33172487 Free PMC article.
BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection.
Mills RJ, Humphrey SJ, Fortuna PRJ, Lor M, Foster SR, Quaife-Ryan GA, Johnston RL, Dumenil T, Bishop C, Rudraraju R, Rawle DJ, Le T, Zhao W, Lee L, Mackenzie-Kludas C, Mehdiabadi NR, Halliday C, Gilham D, Fu L, Nicholls SJ, Johansson J, Sweeney M, Wong NCW, Kulikowski E, Sokolowski KA, Tse BWC, Devilée L, Voges HK, Reynolds LT, Krumeich S, Mathieson E, Abu-Bonsrah D, Karavendzas K, Griffen B, Titmarsh D, Elliott DA, McMahon J, Suhrbier A, Subbarao K, Porrello ER, Smyth MJ, Engwerda CR, MacDonald KPA, Bald T, James DE, Hudson JE. Mills RJ, et al. Among authors: fu l. Cell. 2021 Apr 15;184(8):2167-2182.e22. doi: 10.1016/j.cell.2021.03.026. Epub 2021 Mar 16. Cell. 2021. PMID: 33811809 Free PMC article.
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: fu l. Biomed Pharmacother. 2022 Aug;152:113230. doi: 10.1016/j.biopha.2022.113230. Epub 2022 Jun 7. Biomed Pharmacother. 2022. PMID: 35687908 Free 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: fu l. Atherosclerosis. 2023 Jan;364:10-19. doi: 10.1016/j.atherosclerosis.2022.11.015. Epub 2022 Nov 23. Atherosclerosis. 2023. PMID: 36455344
8,054 results