Enzastaurin (BioDeep_00000178721)

   

human metabolite blood metabolite


代谢物信息卡片


3-(1-methyl-1H-indol-3-yl)-4-(1-{1-[(pyridin-2-yl)methyl]piperidin-4-yl}-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione

化学式: C32H29N5O2 (515.2321134)
中文名称: 恩扎妥林
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=CN(C2CCN(CC3=CC=CC=N3)CC2)C2=CC=CC=C12
InChI: InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39)

描述信息

C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C61074 - Serine/Threonine Kinase Inhibitor

同义名列表

4 个代谢物同义名

3-(1-methyl-1H-indol-3-yl)-4-(1-{1-[(pyridin-2-yl)methyl]piperidin-4-yl}-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione; Enzastaurin(LY317615); LY-317615Sid137275839; Enzastaurin



数据库引用编号

8 个数据库交叉引用编号

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)

COVID-19 Disease Map(0)

PathBank(0)

PharmGKB(0)

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

  • Aneesha Polisety, Gauri Misra, Jyotika Rajawat, Amit Katiyar, Harpreet Singh, Anant Narayan Bhatt. Therapeutic natural compounds Enzastaurin and Palbociclib inhibit MASTL kinase activity preventing breast cancer cell proliferation. Medical oncology (Northwood, London, England). 2022 May; 39(5):100. doi: 10.1007/s12032-022-01701-3. [PMID: 35599277]
  • Yu-Si Cheng, Jie Chao, Chen Chen, Lin-Li Lv, Yu-Chen Han, Bi-Cheng Liu. The PKCβ-p66shc-NADPH oxidase pathway plays a crucial role in diabetic nephropathy. The Journal of pharmacy and pharmacology. 2019 Mar; 71(3):338-347. doi: 10.1111/jphp.13043. [PMID: 30417389]
  • Sarah J Nelson, Achuta K Kadambi, Ilwoo Park, Yan Li, Jason Crane, Marram Olson, Annette Molinaro, Ritu Roy, Nicholas Butowski, Soonmee Cha, Susan Chang. Association of early changes in 1H MRSI parameters with survival for patients with newly diagnosed glioblastoma receiving a multimodality treatment regimen. Neuro-oncology. 2017 03; 19(3):430-439. doi: 10.1093/neuonc/now159. [PMID: 27576874]
  • Pamela A Welch, Wee Teck Ng, Christelle L Darstein, Luna Musib, Thierry Lesimple. Effects of enzastaurin and its metabolites on the QT interval in cancer patients. Journal of clinical pharmacology. 2016 Jan; 56(1):101-8. doi: 10.1002/jcph.573. [PMID: 26096682]
  • G Lesyk, T Fong, P P Ruvolo, P Jurasz. The potential of enzastaurin to enhance platelet aggregation and growth factor secretion: implications for cancer cell survival. Journal of thrombosis and haemostasis : JTH. 2015 Aug; 13(8):1514-20. doi: 10.1111/jth.13010. [PMID: 25990653]
  • Lindsay B Kilburn, Mehmet Kocak, Rodney L Decker, Cynthia Wetmore, Murali Chintagumpala, Jack Su, Stewart Goldman, Anuradha Banerjee, Richard Gilbertson, Maryam Fouladi, Larry Kun, James M Boyett, Susan M Blaney. A phase 1 and pharmacokinetic study of enzastaurin in pediatric patients with refractory primary central nervous system tumors: a pediatric brain tumor consortium study. Neuro-oncology. 2015 Feb; 17(2):303-11. doi: 10.1093/neuonc/nou114. [PMID: 25431212]
  • Chia-Wen Hsu, Jinghua Zhao, Ruili Huang, Jui-Hua Hsieh, Jon Hamm, Xiaoqing Chang, Keith Houck, Menghang Xia. Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor. Scientific reports. 2014 Sep; 4(?):6437. doi: 10.1038/srep06437. [PMID: 25257666]
  • Simona Romano, Giovanna Nappo, Gaetano Calì, Samuel Y-S Wang, Stefania Staibano, Anna D'Angelillo, Gennaro Ilardi, Antonio Sorrentino, Anna Laura Di Pace, Maria Siano, Rita Bisogni, Maria Fiammetta Romano. Synergy between enzastaurin doxorubicin in inducing melanoma apoptosis. Pigment cell & melanoma research. 2013 Nov; 26(6):900-11. doi: 10.1111/pcmr.12144. [PMID: 23866034]
  • Nwabundo Nwankwo, Zhe Zhang, Ting Wang, Connie Collins, Lee Resta, Sabine Ermisch, Jeannette Day, Rodney Decker, Lori Kornberg, Steven Nicol, Donald Thornton, Deborah K Armstrong, Michael A Carducci. Phase I study of enzastaurin and bevacizumab in patients with advanced cancer: safety, efficacy and pharmacokinetics. Investigational new drugs. 2013 Jun; 31(3):653-60. doi: 10.1007/s10637-012-9850-6. [PMID: 22766773]
  • David Oleksyn, Mary Pulvino, Jiyong Zhao, Ravi Misra, Aram Vosoughi, Scott Jenks, Christopher Tipton, Frances Lund, George Schwartz, Bruce Goldman, Chandra Mohan, Kamal Mehta, Madhu Mehta, Michael Leitgets, Ignacio Sanz, Luojing Chen. Protein kinase Cβ is required for lupus development in Sle mice. Arthritis and rheumatism. 2013 Apr; 65(4):1022-31. doi: 10.1002/art.37825. [PMID: 23280626]
  • Manuela Schmidinger, Cezary Szczylik, Cora N Sternberg, Marek Kania, Claudia Sue Kelly, Rodney Decker, Oday Hamid, Taron Faelker, Bernard Escudier. Dose escalation and pharmacokinetics study of enzastaurin and sunitinib versus placebo and sunitinib in patients with metastatic renal cell carcinoma. American journal of clinical oncology. 2012 Oct; 35(5):493-7. doi: 10.1097/coc.0b013e31821cfc41. [PMID: 21654314]
  • A Sacco, I M Ghobrial, A M Roccaro. Anti-angiogenic therapies in the treatment of Waldenstrom's Macroglobulinemia. Current cancer drug targets. 2011 Nov; 11(9):1025-9. doi: 10.2174/156800911798073032. [PMID: 21933107]
  • R Stupp, A Tosoni, J E C Bromberg, P Hau, M Campone, J Gijtenbeek, M Frenay, L Breimer, H Wiesinger, A Allgeier, M J van den Bent, U Bogdahn, W van der Graaf, H J Yun, T Gorlia, D Lacombe, A A Brandes. Sagopilone (ZK-EPO, ZK 219477) for recurrent glioblastoma. A phase II multicenter trial by the European Organisation for Research and Treatment of Cancer (EORTC) Brain Tumor Group. Annals of oncology : official journal of the European Society for Medical Oncology. 2011 Sep; 22(9):2144-2149. doi: 10.1093/annonc/mdq729. [PMID: 21321091]
  • Daniela Molè, Teresa Gagliano, Erica Gentilin, Federico Tagliati, Claudio Pasquali, Maria Rosaria Ambrosio, Giancarlo Pansini, Ettore C Degli Uberti, Maria Chiara Zatelli. Targeting protein kinase C by Enzastaurin restrains proliferation and secretion in human pancreatic endocrine tumors. Endocrine-related cancer. 2011 Aug; 18(4):439-50. doi: 10.1530/erc-11-0055. [PMID: 21606156]
  • Lydia Usha, Michael W Sill, Kathleen M Darcy, Doris M Benbrook, Jean A Hurteau, David P Michelin, Robert S Mannel, Parviz Hanjani, Koen De Geest, Andrew K Godwin. A Gynecologic Oncology Group phase II trial of the protein kinase C-beta inhibitor, enzastaurin and evaluation of markers with potential predictive and prognostic value in persistent or recurrent epithelial ovarian and primary peritoneal malignancies. Gynecologic oncology. 2011 Jun; 121(3):455-61. doi: 10.1016/j.ygyno.2011.02.013. [PMID: 21414654]
  • Peng Cao, Xueting Cai, Wuguang Lu, Fei Zhou, Jiege Huo. Growth Inhibition and Induction of Apoptosis in SHG-44 Glioma Cells by Chinese Medicine Formula 'Pingliu Keli'. Evidence-based complementary and alternative medicine : eCAM. 2011; 2011(?):. doi: 10.1155/2011/958243. [PMID: 20953401]
  • Ze Tian, Jie Shen, Fengfei Wang, Peigen Xiao, Junshan Yang, Hetian Lei, Andrius Kazlauskas, Isaac S Kohane, Erxi Wu. Cambogin is preferentially cytotoxic to cells expressing PDGFR. PloS one. 2011; 6(6):e21370. doi: 10.1371/journal.pone.0021370. [PMID: 21712951]
  • Toru Mukohara, Shunji Nagai, Minori Koshiji, Kenichi Yoshizawa, Hironobu Minami. Phase I dose escalation and pharmacokinetic study of oral enzastaurin (LY317615) in advanced solid tumors. Cancer science. 2010 Oct; 101(10):2193-9. doi: 10.1111/j.1349-7006.2010.01677.x. [PMID: 20707806]
  • Chiharu Tanai, Nobuyuki Yamamoto, Yuichiro Ohe, Toshiaki Takahashi, Hideo Kunitoh, Haruyasu Murakami, Noboru Yamamoto, Yukiko Nakamura, Hiroshi Nokihara, Takehito Shukuya, John R Baldwin, Minori Koshiji, Tomohide Tamura. A phase I study of enzastaurin combined with pemetrexed in advanced non-small cell lung cancer. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2010 Jul; 5(7):1068-74. doi: 10.1097/jto.0b013e3181da3899. [PMID: 20453691]
  • Teri N Kreisl, Svetlana Kotliarova, John A Butman, Paul S Albert, Lyndon Kim, Luna Musib, Donald Thornton, Howard A Fine. A phase I/II trial of enzastaurin in patients with recurrent high-grade gliomas. Neuro-oncology. 2010 Feb; 12(2):181-9. doi: 10.1093/neuonc/nop042. [PMID: 20150385]
  • C Meyer zum Büschenfelde, M Wagner, G Lutzny, M Oelsner, Y Feuerstacke, T Decker, C Bogner, C Peschel, I Ringshausen. Recruitment of PKC-betaII to lipid rafts mediates apoptosis-resistance in chronic lymphocytic leukemia expressing ZAP-70. Leukemia. 2010 Jan; 24(1):141-52. doi: 10.1038/leu.2009.216. [PMID: 19907441]
  • A-R Hanauske, M Lahn, L C Musib, K Weigang-Köhler, E Yilmaz, T Graefe, B Kuenen, D Thornton, P McNealy, G Giaccone. Phase Ib safety and pharmacokinetic evaluation of daily and twice daily oral enzastaurin in combination with pemetrexed in advanced/metastatic cancer. Annals of oncology : official journal of the European Society for Medical Oncology. 2009 Sep; 20(9):1565-1575. doi: 10.1093/annonc/mdp049. [PMID: 19487488]
  • Maria J Comin, Gabriella Czifra, Noemi Kedei, Andrea Telek, Nancy E Lewin, Sofiya Kolusheva, Julia F Velasquez, Ryan Kobylarz, Raz Jelinek, Peter M Blumberg, Victor E Marquez. Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths. Journal of medicinal chemistry. 2009 May; 52(10):3274-83. doi: 10.1021/jm900186m. [PMID: 19379015]
  • A Gonelli, C Mischiati, R Guerrini, R Voltan, S Salvadori, G Zauli. Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents. Mini reviews in medicinal chemistry. 2009 Apr; 9(4):498-509. doi: 10.2174/138955709787847967. [PMID: 19356127]
  • Donata Verdelli, Lucia Nobili, Katia Todoerti, Daniela Intini, Maria Cosenza, Monica Civallero, Jessika Bertacchini, Giorgio Lambertenghi Deliliers, Stefano Sacchi, Luigia Lombardi, Antonino Neri. Molecular targeting of the PKC-beta inhibitor enzastaurin (LY317615) in multiple myeloma involves a coordinated downregulation of MYC and IRF4 expression. Hematological oncology. 2009 Mar; 27(1):23-30. doi: 10.1002/hon.875. [PMID: 18759374]
  • Aldo M Roccaro, Irene M Ghobrial, Simona Blotta, Steven P Treon, Michele Malagola, Kenneth C Anderson, Paul G Richardson, Domenico Russo. Advances in the treatment of monoclonal gammopaties: The emerging role of targeted therapy in plasma cell dyscrasias. Biologics : targets & therapy. 2008 Sep; 2(3):419-31. doi: 10.2147/btt.s3088. [PMID: 19707373]
  • Klaus Podar, Marc S Raab, Jing Zhang, Douglas McMillin, Iris Breitkreutz, Yu-Tzu Tai, Boris K Lin, Nikhil Munshi, Teru Hideshima, Dharminder Chauhan, Kenneth C Anderson. Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl). Blood. 2007 Feb; 109(4):1669-77. doi: 10.1182/blood-2006-08-042747. [PMID: 17023575]
  • Michael A Carducci, Luna Musib, Merrill S Kies, Roberto Pili, Mylene Truong, Julie R Brahmer, Patricia Cole, Rana Sullivan, Jeanne Riddle, Jill Schmidt, Nathan Enas, Vikram Sinha, Donald E Thornton, Roy S Herbst. Phase I dose escalation and pharmacokinetic study of enzastaurin, an oral protein kinase C beta inhibitor, in patients with advanced cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2006 Sep; 24(25):4092-9. doi: 10.1200/jco.2005.05.3447. [PMID: 16943527]
  • Jeremy R Graff, Ann M McNulty, Kimberly Ross Hanna, Bruce W Konicek, Rebecca L Lynch, Spring N Bailey, Crystal Banks, Andrew Capen, Robin Goode, Jason E Lewis, Lillian Sams, Karen L Huss, Robert M Campbell, Philip W Iversen, Blake Lee Neubauer, Thomas J Brown, Luna Musib, Sandaruwan Geeganage, Donald Thornton. The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer research. 2005 Aug; 65(16):7462-9. doi: 10.1158/0008-5472.can-05-0071. [PMID: 16103100]