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The BET inhibitor apabetalone decreases neuroendothelial proinflammatory activation in vitro and in a mouse model of systemic inflammation.
Wasiak S, Fu L, Daze E, Gilham D, Rakai BD, Stotz SC, Tsujikawa LM, Sarsons CD, Studer D, Rinker KD, Jahagirdar R, Wong NCW, Sweeney M, Johansson JO, Kulikowski E. Wasiak S, et al. Among authors: sarsons cd. Transl Neurosci. 2023 Dec 31;14(1):20220332. doi: 10.1515/tnsci-2022-0332. eCollection 2023 Jan 1. Transl Neurosci. 2023. PMID: 38222824 Free PMC article.
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: sarsons cd. 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.
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: sarsons cd. Atherosclerosis. 2023 Jan;364:10-19. doi: 10.1016/j.atherosclerosis.2022.11.015. Epub 2022 Nov 23. Atherosclerosis. 2023. PMID: 36455344
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: sarsons cd. 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: sarsons cd. Clin Epigenetics. 2019 Jul 12;11(1):102. doi: 10.1186/s13148-019-0696-z. Clin Epigenetics. 2019. PMID: 31300040 Free PMC article.
Apabetalone downregulates factors and pathways associated with vascular calcification.
Gilham D, Tsujikawa LM, Sarsons CD, Halliday C, Wasiak S, Stotz SC, Jahagirdar R, Sweeney M, Johansson JO, Wong NCW, Kalantar-Zadeh K, Kulikowski E. Gilham D, et al. Among authors: sarsons cd. Atherosclerosis. 2019 Jan;280:75-84. doi: 10.1016/j.atherosclerosis.2018.11.002. Epub 2018 Nov 14. Atherosclerosis. 2019. PMID: 30476723 Free article.
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