Apabetalone (BioDeep_00000172562)
human metabolite blood metabolite
代谢物信息卡片
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-1,4-dihydroquinazolin-4-one
化学式: C20H22N2O5 (370.1528642)
中文名称: 阿帕他隆
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2
InChI: InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24)
描述信息
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
COVID info from clinicaltrial, clinicaltrials, clinical trial, clinical trials
Corona-virus
Coronavirus
SARS-CoV-2
COVID-19
SARS-CoV
COVID19
SARS2
SARS
同义名列表
数据库引用编号
6 个数据库交叉引用编号
- PubChem: 135564749
- HMDB: HMDB0244312
- DrugBank: DB12000
- Wikipedia: Apabetalone
- chemspider: 25069708
- CAS: 1044870-39-4
分类词条
相关代谢途径
Reactome(0)
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代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
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1 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Dan Shu, Lin Cheng, Kefei Yuan, Dan Liu, He Wei. RVX-208, an inducer of Apolipoprotein A-I, inhibits the particle production of hepatitis B virus through activation of cGAS-STING pathway.
Antiviral therapy.
2023 12; 28(6):13596535231219639. doi:
10.1177/13596535231219639. [PMID: 38037795] - Sylwia Wasiak, Laura M Tsujikawa, Emily Daze, Dean Gilham, Stephanie C Stotz, Brooke D Rakai, Chris D Sarsons, Li Fu, Salman Azhar, Ravi Jahagirdar, Michael Sweeney, Jan O Johansson, Norman C W Wong, Ewelina Kulikowski. Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells.
Atherosclerosis.
2023 01; 364(?):10-19. doi:
10.1016/j.atherosclerosis.2022.11.015. [PMID: 36455344] - Li Fu, Sylwia Wasiak, Laura M Tsujikawa, Brooke D Rakai, Stephanie C Stotz, Norman C W Wong, Jan O Johansson, Michael Sweeney, Connie M Mohan, Aneal Khan, Ewelina Kulikowski. Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy.
Pharmacology research & perspectives.
2022 06; 10(3):e00949. doi:
10.1002/prp2.949. [PMID: 35417091] - Kamyar Kalantar-Zadeh, Gregory G Schwartz, Stephen J Nicholls, Kevin A Buhr, Henry N Ginsberg, Jan O Johansson, Ewelina Kulikowski, Kenneth Lebioda, Peter P Toth, Norman Wong, Michael Sweeney, Kausik K Ray. Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN.
2021 05; 16(5):705-716. doi:
10.2215/cjn.16751020. [PMID: 33906908] - Dean Gilham, Audrey L Smith, Li Fu, Dalia Y Moore, Abenaya Muralidharan, St Patrick M Reid, Stephanie C Stotz, Jan O Johansson, Michael Sweeney, Norman C W Wong, Ewelina Kulikowski, Dalia El-Gamal. Bromodomain and Extraterminal Protein Inhibitor, Apabetalone (RVX-208), Reduces ACE2 Expression and Attenuates SARS-Cov-2 Infection In Vitro.
Biomedicines.
2021 Apr; 9(4):. doi:
10.3390/biomedicines9040437. [PMID: 33919584] - Richard J Mills, Sean J Humphrey, Patrick R J Fortuna, Mary Lor, Simon R Foster, Gregory A Quaife-Ryan, Rebecca L Johnston, Troy Dumenil, Cameron Bishop, Rajeev Rudraraju, Daniel J Rawle, Thuy Le, Wei Zhao, Leo Lee, Charley Mackenzie-Kludas, Neda R Mehdiabadi, Christopher Halliday, Dean Gilham, Li Fu, Stephen J Nicholls, Jan Johansson, Michael Sweeney, Norman C W Wong, Ewelina Kulikowski, Kamil A Sokolowski, Brian W C Tse, Lynn Devilée, Holly K Voges, Liam T Reynolds, Sophie Krumeich, Ellen Mathieson, Dad Abu-Bonsrah, Kathy Karavendzas, Brendan Griffen, Drew Titmarsh, David A Elliott, James McMahon, Andreas Suhrbier, Kanta Subbarao, Enzo R Porrello, Mark J Smyth, Christian R Engwerda, Kelli P A MacDonald, Tobias Bald, David E James, James E Hudson. BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection.
Cell.
2021 04; 184(8):2167-2182.e22. doi:
10.1016/j.cell.2021.03.026. [PMID: 33811809] - Julio M Martinez-Moreno, Miguel Fontecha-Barriuso, Diego Martin-Sanchez, Juan Guerrero-Mauvecin, Elena Goma-Garces, Beatriz Fernandez-Fernandez, Sol Carriazo, Maria D Sanchez-Niño, Adrian M Ramos, Marta Ruiz-Ortega, Alberto Ortiz, Ana B Sanz. Epigenetic Modifiers as Potential Therapeutic Targets in Diabetic Kidney Disease.
International journal of molecular sciences.
2020 Jun; 21(11):. doi:
10.3390/ijms21114113. [PMID: 32526941] - Sylwia Wasiak, Dean Gilham, Emily Daze, Laura M Tsujikawa, Christopher Halliday, Stephanie C Stotz, Brooke D Rakai, Li Fu, Ravi Jahagirdar, Michael Sweeney, Jan O Johansson, Norman C W Wong, Ewelina Kulikowski. Epigenetic Modulation by Apabetalone Counters Cytokine-Driven Acute Phase Response In Vitro, in Mice and in Patients with Cardiovascular Disease.
Cardiovascular therapeutics.
2020; 2020(?):9397109. doi:
10.1155/2020/9397109. [PMID: 32821285] - Mathias Haarhaus, Dean Gilham, Ewelina Kulikowski, Per Magnusson, Kamyar Kalantar-Zadeh. Pharmacologic epigenetic modulators of alkaline phosphatase in chronic kidney disease.
Current opinion in nephrology and hypertension.
2020 01; 29(1):4-15. doi:
10.1097/mnh.0000000000000570. [PMID: 31725015] - Mathias Haarhaus, Kausik K Ray, Stephen J Nicholls, Gregory G Schwartz, Ewelina Kulikowski, Jan O Johansson, Michael Sweeney, Christopher Halliday, Kenneth Lebioda, Norman Wong, Vincent Brandenburg, Srinivasan Beddhu, Marcello Tonelli, Carmine Zoccali, Kamyar Kalantar-Zadeh. Apabetalone lowers serum alkaline phosphatase and improves cardiovascular risk in patients with cardiovascular disease.
Atherosclerosis.
2019 11; 290(?):59-65. doi:
10.1016/j.atherosclerosis.2019.09.002. [PMID: 31568963] - Laura M Tsujikawa, Li Fu, Shovon Das, Christopher Halliday, Brooke D Rakai, Stephanie C Stotz, Christopher D Sarsons, Dean Gilham, Emily Daze, Sylwia Wasiak, Deborah Studer, Kristina D Rinker, Michael Sweeney, Jan O Johansson, Norman C W Wong, Ewelina Kulikowski. Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism.
Clinical epigenetics.
2019 07; 11(1):102. doi:
10.1186/s13148-019-0696-z. [PMID: 31300040] - Daisuke Shishikura, Yu Kataoka, Satoshi Honda, Kohei Takata, Susan W Kim, Jordan Andrews, Peter J Psaltis, Michael Sweeney, Ewelina Kulikowski, Jan Johansson, Norman C W Wong, Stephen J Nicholls. The Effect of Bromodomain and Extra-Terminal Inhibitor Apabetalone on Attenuated Coronary Atherosclerotic Plaque: Insights from the ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions.
2019 Feb; 19(1):49-57. doi:
10.1007/s40256-018-0298-8. [PMID: 30155718] - Ewelina Kulikowski, Christopher Halliday, Jan Johansson, Mike Sweeney, Kenneth Lebioda, Norman Wong, Mathias Haarhaus, Vincent Brandenburg, Srinivasan Beddhu, Marcello Tonelli, Carmine Zoccali, Kamyar Kalantar-Zadeh. Apabetalone Mediated Epigenetic Modulation is Associated with Favorable Kidney Function and Alkaline Phosphatase Profile in Patients with Chronic Kidney Disease.
Kidney & blood pressure research.
2018; 43(2):449-457. doi:
10.1159/000488257. [PMID: 29566379] - Sylwia Wasiak, Dean Gilham, Laura M Tsujikawa, Christopher Halliday, Cyrus Calosing, Ravi Jahagirdar, Jan Johansson, Michael Sweeney, Norman C Wong, Ewelina Kulikowski. Downregulation of the Complement Cascade In Vitro, in Mice and in Patients with Cardiovascular Disease by the BET Protein Inhibitor Apabetalone (RVX-208).
Journal of cardiovascular translational research.
2017 Aug; 10(4):337-347. doi:
10.1007/s12265-017-9755-z. [PMID: 28567671] - Gopal C Ghosh, Rajarshi Bhadra, Raktim K Ghosh, Kinjal Banerjee, Anjan Gupta. RVX 208: A novel BET protein inhibitor, role as an inducer of apo A-I/HDL and beyond.
Cardiovascular therapeutics.
2017 Aug; 35(4):. doi:
10.1111/1755-5922.12265. [PMID: 28423226] - Andrew L Siebel, Si Khiang Trinh, Melissa F Formosa, Piyushkumar A Mundra, Alaina K Natoli, Medini Reddy-Luthmoodoo, Kevin Huynh, Anmar A Khan, Andrew L Carey, Gerrit van Hall, Claudio Cobelli, Chiara Dalla-Man, Jim D Otvos, Kerry-Anne Rye, Jan Johansson, Allan Gordon, Norman C W Wong, Dmitri Sviridov, Philip Barter, Stephen J Duffy, Peter J Meikle, Bronwyn A Kingwell. Effects of the BET-inhibitor, RVX-208 on the HDL lipidome and glucose metabolism in individuals with prediabetes: A randomized controlled trial.
Metabolism: clinical and experimental.
2016 Jun; 65(6):904-14. doi:
10.1016/j.metabol.2016.03.002. [PMID: 27173469] - Stephen J Nicholls, Rishi Puri, Kathy Wolski, Christie M Ballantyne, Philip J Barter, H Bryan Brewer, John J P Kastelein, Bo Hu, Kiyoko Uno, Yu Kataoka, Jean-Paul R Herrman, Bela Merkely, Marilyn Borgman, Steven E Nissen. Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions.
2016 Feb; 16(1):55-65. doi:
10.1007/s40256-015-0146-z. [PMID: 26385396] - Kapil Gadkar, James Lu, Srikumar Sahasranaman, John Davis, Norman A Mazer, Saroja Ramanujan. Evaluation of HDL-modulating interventions for cardiovascular risk reduction using a systems pharmacology approach.
Journal of lipid research.
2016 Jan; 57(1):46-55. doi:
10.1194/jlr.m057943. [PMID: 26522778] - Ravi Jahagirdar, Haiyan Zhang, Salman Azhar, Jennifer Tobin, Sarah Attwell, Raymond Yu, Jin Wu, Kevin G McLure, Henrik C Hansen, Gregory S Wagner, Peter R Young, Rai Ajit K Srivastava, Norman C W Wong, Jan Johansson. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Atherosclerosis.
2014 Sep; 236(1):91-100. doi:
10.1016/j.atherosclerosis.2014.06.008. [PMID: 25016363] - Yuri L Khmelnitsky, Vadim V Mozhaev, Ian C Cotterill, Peter C Michels, Sihem Boudjabi, Vladimir Khlebnikov, M Madhava Reddy, Gregory S Wagner, Henrik C Hansen. In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
European journal of medicinal chemistry.
2013 Jun; 64(?):121-8. doi:
10.1016/j.ejmech.2013.03.062. [PMID: 23644195] - Herman J Kempen, Daniel Bellus, Oleg Fedorov, Silke Nicklisch, Panagis Filippakopoulos, Sarah Picaud, Stefan Knapp. Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding.
Lipid insights.
2013; 6(?):47-54. doi:
10.4137/lpi.s13258. [PMID: 25278768] - Stephen J Nicholls, Allan Gordon, Jan Johannson, Christie M Ballantyne, Philip J Barter, H Bryan Brewer, John J P Kastelein, Norman C Wong, Marilyn R N Borgman, Steven E Nissen. ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies.
Cardiovascular drugs and therapy.
2012 Apr; 26(2):181-7. doi:
10.1007/s10557-012-6373-5. [PMID: 22349989] - Stephen J Nicholls, Allan Gordon, Jan Johansson, Kathy Wolski, Christie M Ballantyne, John J P Kastelein, Allen Taylor, Marilyn Borgman, Steven E Nissen. Efficacy and safety of a novel oral inducer of apolipoprotein a-I synthesis in statin-treated patients with stable coronary artery disease a randomized controlled trial.
Journal of the American College of Cardiology.
2011 Mar; 57(9):1111-9. doi:
10.1016/j.jacc.2010.11.015. [PMID: 21255957] - Dana Bailey, Ravi Jahagirdar, Allan Gordon, Anouar Hafiane, Steven Campbell, Safia Chatur, Gregory S Wagner, Henrik C Hansen, Fabrizio S Chiacchia, Jan Johansson, Larbi Krimbou, Norman C W Wong, Jacques Genest. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo.
Journal of the American College of Cardiology.
2010 Jun; 55(23):2580-9. doi:
10.1016/j.jacc.2010.02.035. [PMID: 20513599] - Eileen McNeill. RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases.
Current opinion in investigational drugs (London, England : 2000).
2010 Mar; 11(3):357-64. doi:
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