Darapladib (BioDeep_00000858825)
代谢物信息卡片
Darapladib
化学式: C36H38F4N4O2S (666.2651456)
中文名称: 达普拉缔
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F
InChI: InChI=1S/C36H38F4N4O2S/c1-3-42(4-2)20-21-43(22-25-8-12-27(13-9-25)28-14-16-29(17-15-28)36(38,39)40)33(45)23-44-32-7-5-6-31(32)34(46)41-35(44)47-24-26-10-18-30(37)19-11-26/h8-19H,3-7,20-24H2,1-2H3
描述信息
C78276 - Agent Affecting Digestive System or Metabolism > C29703 - Antilipidemic Agent
D004791 - Enzyme Inhibitors > D064801 - Phospholipase A2 Inhibitors
Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer[1][2][3][4].
同义名列表
2 个代谢物同义名
数据库引用编号
6 个数据库交叉引用编号
- KEGGdrug: D03650
- PubChem: 9939609
- DrugBank: DB06311
- ChEMBL: CHEMBL204021
- CAS: 356057-34-6
- medchemexpress: HY-10521
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
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)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 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。
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文献列表
- Mihee Oh, Seo Young Jang, Ji-Yoon Lee, Jong Woo Kim, Youngae Jung, Jiwoo Kim, Jinho Seo, Tae-Su Han, Eunji Jang, Hye Young Son, Dain Kim, Min Wook Kim, Jin-Sung Park, Kwon-Ho Song, Kyoung-Jin Oh, Won Kon Kim, Kwang-Hee Bae, Yong-Min Huh, Soon Ha Kim, Doyoun Kim, Baek-Soo Han, Sang Chul Lee, Geum-Sook Hwang, Eun-Woo Lee. The lipoprotein-associated phospholipase A2 inhibitor Darapladib sensitises cancer cells to ferroptosis by remodelling lipid metabolism.
Nature communications.
2023 09; 14(1):5728. doi:
10.1038/s41467-023-41462-9. [PMID: 37714840] - Matthias Paulus Wagner, Pauline Formaglio, Olivier Gorgette, Jerzy Michal Dziekan, Christèle Huon, Isabell Berneburg, Stefan Rahlfs, Jean-Christophe Barale, Sheldon I Feinstein, Aron B Fisher, Didier Ménard, Zbynek Bozdech, Rogerio Amino, Lhousseine Touqui, Chetan E Chitnis. Human peroxiredoxin 6 is essential for malaria parasites and provides a host-based drug target.
Cell reports.
2022 06; 39(11):110923. doi:
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JAMA cardiology.
2021 12; 6(12):1440-1445. doi:
10.1001/jamacardio.2021.3079. [PMID: 34431970] - Pauline Morigny, Doris Kaltenecker, Julia Zuber, Juliano Machado, Lisa Mehr, Foivos-Filippos Tsokanos, Hanna Kuzi, Chris D Hermann, Michael Voelkl, German Monogarov, Christoph Springfeld, Victor Laurent, Bernd Engelmann, Helmut Friess, Inka Zörnig, Achim Krüger, Jeroen Krijgsveld, Olga Prokopchuk, Søren Fisker Schmidt, Maria Rohm, Stephan Herzig, Mauricio Berriel Diaz. Association of circulating PLA2G7 levels with cancer cachexia and assessment of darapladib as a therapy.
Journal of cachexia, sarcopenia and muscle.
2021 10; 12(5):1333-1351. doi:
10.1002/jcsm.12758. [PMID: 34427055] - Qing Li, Chunlei Feng, Lingyun Li, Guiliang Xu, Haijuan Gu, Shiqiang Li, Dali Li, Mingyao Liu, Shuhua Han, Biao Zheng. Lipid Receptor G2A-Mediated Signal Pathway Plays a Critical Role in Inflammatory Response by Promoting Classical Macrophage Activation.
Journal of immunology (Baltimore, Md. : 1950).
2021 05; 206(10):2338-2352. doi:
10.4049/jimmunol.2000231. [PMID: 33941654] - Shaoqiu Zhuo, Chong Yuan. Active site competition is the mechanism for the inhibition of lipoprotein-associated phospholipase A2 by detergent micelles or lipoproteins and for the efficacy reduction of darapladib.
Scientific reports.
2020 10; 10(1):17232. doi:
10.1038/s41598-020-74236-0. [PMID: 33057060] - Titin Andri Wihastuti, Fitria Nugraha Aini, Cholid Tri Tjahjono, Yuni Hendrati Sulfia, Zuhrotus Sholichah, Teuku Heriansyah. Lp-PLA2 Selective Inhibitor (Darapladib) Effect In Lowering The Expression Level Of IL-1B And IL-6 In The Renal At Type 2 Diabetes Mellitus.
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Journal of the American Heart Association.
2017 Oct; 6(10):. doi:
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Diabetes & vascular disease research.
2017 05; 14(3):200-213. doi:
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Journal of the American Heart Association.
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British journal of clinical pharmacology.
2015 Oct; 80(4):654-61. doi:
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PloS one.
2015; 10(10):e0139862. doi:
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British journal of clinical pharmacology.
2014 Nov; 78(5):1014-21. doi:
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The New England journal of medicine.
2014 May; 370(18):1702-11. doi:
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2014 Mar; 42(3):415-30. doi:
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PloS one.
2014; 9(2):e89034. doi:
10.1371/journal.pone.0089034. [PMID: 24586490] - Martin Koch, Michael Wiese. Gene expression signatures of angiocidin and darapladib treatment connect to therapy options in cervical cancer.
Journal of cancer research and clinical oncology.
2013 Feb; 139(2):259-67. doi:
10.1007/s00432-012-1317-9. [PMID: 23052694] - Hui Zhang, Jin-Ying Zhang, Tong-Wen Sun, De-Liang Shen, Fei He, Yu-Hua Dang, Ling Li. Amelioration of atherosclerosis in apolipoprotein E-deficient mice by inhibition of lipoprotein-associated phospholipase A2.
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2013 Feb; 36(1):E32-41. doi:
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Lancet (London, England).
2012 Mar; 379(9822):1205-13. doi:
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American journal of therapeutics.
2012 Mar; 19(2):115-20. doi:
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PloS one.
2012; 7(2):e29675. doi:
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Journal of parasitology research.
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Oncotarget.
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Acta pharmacologica Sinica.
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PloS one.
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