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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: gilham d. 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.
RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease.
Gilham D, Wasiak S, Tsujikawa LM, Halliday C, Norek K, Patel RG, Kulikowski E, Johansson J, Sweeney M, Wong NC, Gordon A, McLure K, Young P. Gilham D, et al. Atherosclerosis. 2016 Apr;247:48-57. doi: 10.1016/j.atherosclerosis.2016.01.036. Epub 2016 Jan 22. Atherosclerosis. 2016. PMID: 26868508 Free article.
Downregulation of the Complement Cascade In Vitro, in Mice and in Patients with Cardiovascular Disease by the BET Protein Inhibitor Apabetalone (RVX-208).
Wasiak S, Gilham D, Tsujikawa LM, Halliday C, Calosing C, Jahagirdar R, Johansson J, Sweeney M, Wong NC, Kulikowski E. Wasiak S, et al. Among authors: gilham d. J Cardiovasc Transl Res. 2017 Aug;10(4):337-347. doi: 10.1007/s12265-017-9755-z. Epub 2017 May 31. J Cardiovasc Transl Res. 2017. PMID: 28567671 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. Atherosclerosis. 2019 Jan;280:75-84. doi: 10.1016/j.atherosclerosis.2018.11.002. Epub 2018 Nov 14. Atherosclerosis. 2019. PMID: 30476723 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: gilham d. 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: gilham d. Cardiovasc Ther. 2020 Jul 21;2020:9397109. doi: 10.1155/2020/9397109. eCollection 2020. Cardiovasc Ther. 2020. PMID: 32821285 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: gilham d. Biomed Pharmacother. 2022 Aug;152:113230. doi: 10.1016/j.biopha.2022.113230. Epub 2022 Jun 7. Biomed Pharmacother. 2022. PMID: 35687908 Free article.
Data on gene and protein expression changes induced by apabetalone (RVX-208) in ex vivo treated human whole blood and primary hepatocytes.
Wasiak S, Gilham D, Tsujikawa LM, Halliday C, Norek K, Patel RG, McLure KG, Young PR, Gordon A, Kulikowski E, Johansson J, Sweeney M, Wong NC. Wasiak S, et al. Among authors: gilham d. Data Brief. 2016 Jul 29;8:1280-8. doi: 10.1016/j.dib.2016.07.047. eCollection 2016 Sep. Data Brief. 2016. PMID: 27570805 Free PMC article.
111 results