Ruboxistaurin (BioDeep_00000738663)
代谢物信息卡片
RUBOXISTAURIN MESYLATE
化学式: C28H28N4O3 (468.2161298)
中文名称: 鲁伯斯塔
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CN(C)CC1CCN2C=C(C3=CC=CC=C32)C4=C(C5=CN(CCO1)C6=CC=CC=C65)C(=O)NC4=O
InChI: InChI=1S/C28H28N4O3/c1-30(2)15-18-11-12-31-16-21(19-7-3-5-9-23(19)31)25-26(28(34)29-27(25)33)22-17-32(13-14-35-18)24-10-6-4-8-20(22)24/h3-10,16-18H,11-15H2,1-2H3,(H,29,33,34)/t18-/m0/s1
描述信息
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C61074 - Serine/Threonine Kinase Inhibitor
D004791 - Enzyme Inhibitors
同义名列表
2 个代谢物同义名
数据库引用编号
5 个数据库交叉引用编号
- PubChem: 153999
- DrugBank: DB11829
- ChEMBL: CHEMBL432130
- ChEMBL: CHEMBL91829
- CAS: 169939-94-0
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。
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
- Alessandro Rimessi, Chiara Pavan, Elli Ioannidi, Federica Nigro, Claudia Morganti, Alberto Brugnoli, Francesco Longo, Chiara Gardin, Letizia Ferroni, Michele Morari, Vincenzo Vindigni, Barbara Zavan, Paolo Pinton. Protein Kinase C β: a New Target Therapy to Prevent the Long-Term Atypical Antipsychotic-Induced Weight Gain.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology.
2017 Jun; 42(7):1491-1501. doi:
10.1038/npp.2017.20. [PMID: 28128334] - Asma S Al-Onazi, Nouf M Al-Rasheed, Hala A Attia, Nawal M Al-Rasheed, Raeesa M Ahmed, Maha A Al-Amin, Coralie Poizat. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways.
The Journal of pharmacy and pharmacology.
2016 Feb; 68(2):219-32. doi:
10.1111/jphp.12504. [PMID: 26817709] - Katherine R Tuttle, Janet B McGill, Edward J Bastyr, Keri Kles Poi, Nazila Shahri, Pamela W Anderson. Effect of ruboxistaurin on albuminuria and estimated GFR in people with diabetic peripheral neuropathy: results from a randomized trial.
American journal of kidney diseases : the official journal of the National Kidney Foundation.
2015 Apr; 65(4):634-6. doi:
10.1053/j.ajkd.2014.11.024. [PMID: 25618186] - Radica Z Alicic, Katherine R Tuttle. Novel therapies for diabetic kidney disease.
Advances in chronic kidney disease.
2014 Mar; 21(2):121-33. doi:
10.1053/j.ackd.2014.01.007. [PMID: 24602462] - Maciej J Zamek-Gliszczynski, Trent L Abraham, Jeffrey J Alberts, Palaniappan Kulanthaivel, Kimberley A Jackson, Kay H Chow, Denis J McCann, Haitao Hu, Shelby Anderson, Nathan A Furr, Robert J Barbuch, Kenneth C Cassidy. Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure.
Drug metabolism and disposition: the biological fate of chemicals.
2013 Apr; 41(4):714-26. doi:
10.1124/dmd.112.048488. [PMID: 23305709] - Xiao Lu, James S Bean, Ghassan S Kassab, Mark D Rekhter. Protein kinase C inhibition ameliorates functional endothelial insulin resistance and vascular smooth muscle cell hypersensitivity to insulin in diabetic hypertensive rats.
Cardiovascular diabetology.
2011 Jun; 10(?):48. doi:
10.1186/1475-2840-10-48. [PMID: 21635764] - Akira Mima, Yuzuru Ohshiro, Munehiro Kitada, Motonobu Matsumoto, Pedro Geraldes, Chenzhong Li, Qian Li, Gregory S White, Christopher Cahill, Christian Rask-Madsen, George L King. Glomerular-specific protein kinase C-β-induced insulin receptor substrate-1 dysfunction and insulin resistance in rat models of diabetes and obesity.
Kidney international.
2011 Apr; 79(8):883-96. doi:
10.1038/ki.2010.526. [PMID: 21228767] - Saeid Golbidi, S Alireza Ebadi, Ismail Laher. Antioxidants in the treatment of diabetes.
Current diabetes reviews.
2011 Mar; 7(2):106-25. doi:
10.2174/157339911794940729. [PMID: 21294707] - R Komers, T T Oyama, D R Beard, S Anderson. Effects of systemic inhibition of Rho kinase on blood pressure and renal haemodynamics in diabetic rats.
British journal of pharmacology.
2011 Jan; 162(1):163-74. doi:
10.1111/j.1476-5381.2010.01031.x. [PMID: 20840471] - Sudhir V Shah. Progress toward novel treatments for chronic kidney disease.
Journal of renal nutrition : the official journal of the Council on Renal Nutrition of the National Kidney Foundation.
2010 Sep; 20(5 Suppl):S122-6. doi:
10.1053/j.jrn.2010.06.013. [PMID: 20797560] - Ronald P Danis, Matthew J Sheetz. Ruboxistaurin: PKC-beta inhibition for complications of diabetes.
Expert opinion on pharmacotherapy.
2009 Dec; 10(17):2913-25. doi:
10.1517/14656560903401620. [PMID: 19929710] - Darren J Kelly, Amanda J Edgley, Yuan Zhang, Kerri Thai, Sih Min Tan, Alison J Cox, Andrew Advani, Kim A Connelly, Catharine I Whiteside, Richard E Gilbert. Protein kinase C-beta inhibition attenuates the progression of nephropathy in non-diabetic kidney disease.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association.
2009 Jun; 24(6):1782-90. doi:
10.1093/ndt/gfn729. [PMID: 19155535] - M Meier, J Menne, H Haller. Targeting the protein kinase C family in the diabetic kidney: lessons from analysis of mutant mice.
Diabetologia.
2009 May; 52(5):765-75. doi:
10.1007/s00125-009-1278-y. [PMID: 19238353] - Dongcheng Wu, Fangfang Peng, Baifang Zhang, Alistair J Ingram, Darren J Kelly, Richard E Gilbert, Bo Gao, Joan C Krepinsky. PKC-beta1 mediates glucose-induced Akt activation and TGF-beta1 upregulation in mesangial cells.
Journal of the American Society of Nephrology : JASN.
2009 Mar; 20(3):554-66. doi:
10.1681/asn.2008040445. [PMID: 19211711] - David Z I Cherney, Ana Konvalinka, Bernard Zinman, Eleftherios P Diamandis, Anton Soosaipillai, Heather Reich, Joanne Lorraine, Vesta Lai, James W Scholey, Judith A Miller. Effect of protein kinase Cbeta inhibition on renal hemodynamic function and urinary biomarkers in humans with type 1 diabetes: a pilot study.
Diabetes care.
2009 Jan; 32(1):91-3. doi:
10.2337/dc08-1609. [PMID: 18945921] - Sundararaman Swaminathan, Sudhir V Shah. Novel approaches targeted toward oxidative stress for the treatment of chronic kidney disease.
Current opinion in nephrology and hypertension.
2008 Mar; 17(2):143-8. doi:
10.1097/mnh.0b013e3282f4e539. [PMID: 18277146] - Pamela W Anderson, Janet B McGill, Katherine R Tuttle. Protein kinase C beta inhibition: the promise for treatment of diabetic nephropathy.
Current opinion in nephrology and hypertension.
2007 Sep; 16(5):397-402. doi:
10.1097/mnh.0b013e3281ead025. [PMID: 17693752] - Katherine R Tuttle, Janet B McGill, Douglas J Haney, Toni E Lin, Pamela W Anderson. Kidney outcomes in long-term studies of ruboxistaurin for diabetic eye disease.
Clinical journal of the American Society of Nephrology : CJASN.
2007 Jul; 2(4):631-6. doi:
10.2215/cjn.00840207. [PMID: 17699475] - Richard E Gilbert, Sandra A Kim, Katherine R Tuttle, George L Bakris, Robert D Toto, Janet B McGill, Douglas J Haney, Darren J Kelly, Pamela W Anderson. Effect of ruboxistaurin on urinary transforming growth factor-beta in patients with diabetic nephropathy and type 2 diabetes.
Diabetes care.
2007 Apr; 30(4):995-6. doi:
10.2337/dc06-2079. [PMID: 17229944] - M Vaughn Emerson, Andreas K Lauer. Emerging therapies for the treatment of neovascular age-related macular degeneration and diabetic macular edema.
BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy.
2007; 21(4):245-57. doi:
10.2165/00063030-200721040-00005. [PMID: 17628122] - Jennifer L Burkey, Kristina M Campanale, Robert Barbuch, Douglas O'Bannon, James Rash, Charles Benson, David Small. Disposition of [14C]ruboxistaurin in humans.
Drug metabolism and disposition: the biological fate of chemicals.
2006 Nov; 34(11):1909-17. doi:
10.1124/dmd.106.009894. [PMID: 16896067] - Harold Lebovitz. Diabetes: assessing the pipeline.
Atherosclerosis. Supplements.
2006 Apr; 7(1):43-9. doi:
10.1016/j.atherosclerosissup.2006.01.007. [PMID: 16504599] - Robert J Barbuch, Kristina Campanale, Chad E Hadden, Milton Zmijewski, Ping Yi, Douglas D O'Bannon, Jennifer L Burkey, Palaniappan Kulanthaivel. In vivo metabolism of [14C]ruboxistaurin in dogs, mice, and rats following oral administration and the structure determination of its metabolites by liquid chromatography/mass spectrometry and NMR spectroscopy.
Drug metabolism and disposition: the biological fate of chemicals.
2006 Feb; 34(2):213-24. doi:
10.1124/dmd.105.007401. [PMID: 16258078] - Kwee Poo Yeo, Stephen L Lowe, Ming Tung Lim, James R Voelker, Jennifer L Burkey, Stephen D Wise. Pharmacokinetics of ruboxistaurin are significantly altered by rifampicin-mediated CYP3A4 induction.
British journal of clinical pharmacology.
2006 Feb; 61(2):200-10. doi:
10.1111/j.1365-2125.2005.02540.x. [PMID: 16433874] - Stephen Wise, Eunice Yuen, Clark Chan, Yeo Kwee Poo, Lorraine Teng, Titus Lau, James Voelker. Effects of chronic renal failure on the pharmacokinetics of ruboxistaurin and its active metabolite 338522.
Clinical pharmacokinetics.
2006; 45(3):297-303. doi:
10.2165/00003088-200645030-00005. [PMID: 16509761] - Mark E Williams. New potential agents in treating diabetic kidney disease: the fourth act.
Drugs.
2006; 66(18):2287-98. doi:
10.2165/00003495-200666180-00002. [PMID: 17181372] - Katherine R Tuttle, George L Bakris, Robert D Toto, Janet B McGill, Kuolung Hu, Pamela W Anderson. The effect of ruboxistaurin on nephropathy in type 2 diabetes.
Diabetes care.
2005 Nov; 28(11):2686-90. doi:
10.2337/diacare.28.11.2686. [PMID: 16249540] - Darren J Kelly, Anna Chanty, Renae M Gow, Yuan Zhang, Richard E Gilbert. Protein kinase Cbeta inhibition attenuates osteopontin expression, macrophage recruitment, and tubulointerstitial injury in advanced experimental diabetic nephropathy.
Journal of the American Society of Nephrology : JASN.
2005 Jun; 16(6):1654-60. doi:
10.1681/asn.2004070578. [PMID: 15843473] - Katherine R Tuttle. Linking metabolism and immunology: diabetic nephropathy is an inflammatory disease.
Journal of the American Society of Nephrology : JASN.
2005 Jun; 16(6):1537-8. doi:
10.1681/asn.2005040393. [PMID: 15872083] - Mark E Williams, Katherine R Tuttle. The next generation of diabetic nephropathy therapies: an update.
Advances in chronic kidney disease.
2005 Apr; 12(2):212-22. doi:
10.1053/j.ackd.2005.01.011. [PMID: 15822057] - Munehiro Kitada, Daisuke Koya, Toshiro Sugimoto, Motohide Isono, Shin-ichi Araki, Atsunori Kashiwagi, Masakazu Haneda. Translocation of glomerular p47phox and p67phox by protein kinase C-beta activation is required for oxidative stress in diabetic nephropathy.
Diabetes.
2003 Oct; 52(10):2603-14. doi:
10.2337/diabetes.52.10.2603. [PMID: 14514646] - Katherine R Tuttle, Pamela W Anderson. A novel potential therapy for diabetic nephropathy and vascular complications: protein kinase C beta inhibition.
American journal of kidney diseases : the official journal of the National Kidney Foundation.
2003 Sep; 42(3):456-65. doi:
10.1016/s0272-6386(03)00741-8. [PMID: 12955673] - Toru Abiko, Atsuko Abiko, Allen C Clermont, Brett Shoelson, Naoichi Horio, Junichi Takahashi, Anthony P Adamis, George L King, Sven-Erik Bursell. Characterization of retinal leukostasis and hemodynamics in insulin resistance and diabetes: role of oxidants and protein kinase-C activation.
Diabetes.
2003 Mar; 52(3):829-37. doi:
10.2337/diabetes.52.3.829. [PMID: 12606527] - Darren J Kelly, Yuan Zhang, Claire Hepper, Renae M Gow, Kassie Jaworski, Bruce E Kemp, Jennifer L Wilkinson-Berka, Richard E Gilbert. Protein kinase C beta inhibition attenuates the progression of experimental diabetic nephropathy in the presence of continued hypertension.
Diabetes.
2003 Feb; 52(2):512-8. doi:
10.2337/diabetes.52.2.512. [PMID: 12540629] - J L Burkey, K M Campanale, D D O'Bannon, J W Cramer, N A Farid. Disposition of LY333531, a selective protein kinase C beta inhibitor, in the Fischer 344 rat and beagle dog.
Xenobiotica; the fate of foreign compounds in biological systems.
2002 Nov; 32(11):1045-52. doi:
10.1080/0049825021000012619. [PMID: 12487733] - G L Engel, N A Farid, M M Faul, L A Richardson, L L Winneroski. Salt form selection and characterization of LY333531 mesylate monohydrate.
International journal of pharmaceutics.
2000 Apr; 198(2):239-47. doi:
10.1016/s0378-5173(00)00350-1. [PMID: 10767572] - D Koya, M Haneda, H Nakagawa, K Isshiki, H Sato, S Maeda, T Sugimoto, H Yasuda, A Kashiwagi, D K Ways, G L King, R Kikkawa. Amelioration of accelerated diabetic mesangial expansion by treatment with a PKC beta inhibitor in diabetic db/db mice, a rodent model for type 2 diabetes.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
2000 Mar; 14(3):439-47. doi:
10.1096/fasebj.14.3.439. [PMID: 10698958] - R Efendiev, A M Bertorello, C H Pedemonte. PKC-beta and PKC-zeta mediate opposing effects on proximal tubule Na+,K+-ATPase activity.
FEBS letters.
1999 Jul; 456(1):45-8. doi:
10.1016/s0014-5793(99)00925-4. [PMID: 10452527] - D Koya, M R Jirousek, Y W Lin, H Ishii, K Kuboki, G L King. Characterization of protein kinase C beta isoform activation on the gene expression of transforming growth factor-beta, extracellular matrix components, and prostanoids in the glomeruli of diabetic rats.
The Journal of clinical investigation.
1997 Jul; 100(1):115-26. doi:
10.1172/jci119503. [PMID: 9202063] - H Ishii, M R Jirousek, D Koya, C Takagi, P Xia, A Clermont, S E Bursell, T S Kern, L M Ballas, W F Heath, L E Stramm, E P Feener, G L King. Amelioration of vascular dysfunctions in diabetic rats by an oral PKC beta inhibitor.
Science (New York, N.Y.).
1996 May; 272(5262):728-31. doi:
10.1126/science.272.5262.728. [PMID: 8614835]