indazoles

Summary

Top Publications

  1. ncbi Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results
    Hope S Rugo
    University of California, San Francisco Comprehensive Cancer Center, USA
    J Clin Oncol 23:5474-83. 2005
  2. doi Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study
    Ezra E W Cohen
    Section of Hematology Oncology, Department of Medicine, University of Chicago Division of Biological Sciences, 5801 S Ellis, Chicago, IL 60637, USA
    J Clin Oncol 26:4708-13. 2008
  3. doi Phase II study of axitinib in sorafenib-refractory metastatic renal cell carcinoma
    Brian I Rini
    Department of Solid Tumor Oncology and Urology, Cleveland Clinic Taussig Cancer Institute, 9500 Euclid Ave, Desk R35, Cleveland, OH 44195, USA
    J Clin Oncol 27:4462-8. 2009
  4. doi Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3
    Dana D Hu-Lowe
    Department of Cancer Biology, PGRD La Jolla, Pfizer, Inc, San Diego, California 92121, USA
    Clin Cancer Res 14:7272-83. 2008
  5. doi The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer
    Adrian J Folkes
    Piramed Pharma, 957 Buckingham Avenue, Slough, Berks SL1 4NL, United Kingdom
    J Med Chem 51:5522-32. 2008
  6. doi Effect of axitinib (AG-013736) on fatigue, thyroid-stimulating hormone, and biomarkers: a phase I study in Japanese patients
    Toru Mukohara
    National Cancer Center Hospital East, Oncology Hematology, Kashiwa, Japan
    Cancer Sci 101:963-8. 2010
  7. ncbi Axitinib treatment in patients with cytokine-refractory metastatic renal-cell cancer: a phase II study
    Olivier Rixe
    Pitie Salpetriere Hospital, University of Paris, Paris, France
    Lancet Oncol 8:975-84. 2007
  8. pmc Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
    Florence I Raynaud
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, UK
    Mol Cancer Ther 8:1725-38. 2009
  9. pmc Bindarit: an anti-inflammatory small molecule that modulates the NFκB pathway
    Eugenio Mora
    Center for Epigenetics and Metabolism, School of Medicine, University of California at Irvine, Irvine, CA, USA
    Cell Cycle 11:159-69. 2012
  10. doi Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and human cancer cell line panel JFCR39
    Dexin Kong
    Division of Molecular Pharmacology, Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, 3 10 6, Ariake, Koto ku, Tokyo 135 8550, Japan
    Eur J Cancer 46:1111-21. 2010

Detail Information

Publications241 found, 100 shown here

  1. ncbi Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results
    Hope S Rugo
    University of California, San Francisco Comprehensive Cancer Center, USA
    J Clin Oncol 23:5474-83. 2005
    ....
  2. doi Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study
    Ezra E W Cohen
    Section of Hematology Oncology, Department of Medicine, University of Chicago Division of Biological Sciences, 5801 S Ellis, Chicago, IL 60637, USA
    J Clin Oncol 26:4708-13. 2008
    ..This multi-institutional study assessed the activity and safety of axitinib, an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3 in patients with advanced thyroid cancer...
  3. doi Phase II study of axitinib in sorafenib-refractory metastatic renal cell carcinoma
    Brian I Rini
    Department of Solid Tumor Oncology and Urology, Cleveland Clinic Taussig Cancer Institute, 9500 Euclid Ave, Desk R35, Cleveland, OH 44195, USA
    J Clin Oncol 27:4462-8. 2009
    ....
  4. doi Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3
    Dana D Hu-Lowe
    Department of Cancer Biology, PGRD La Jolla, Pfizer, Inc, San Diego, California 92121, USA
    Clin Cancer Res 14:7272-83. 2008
    ..We provide a comprehensive description of its in vitro characteristics and activities, in vivo antiangiogenesis, and antitumor efficacy and translational pharmacology data...
  5. doi The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer
    Adrian J Folkes
    Piramed Pharma, 957 Buckingham Avenue, Slough, Berks SL1 4NL, United Kingdom
    J Med Chem 51:5522-32. 2008
    ..This work resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor of PI3K and is currently being evaluated in human clinical trials for the treatment of cancer...
  6. doi Effect of axitinib (AG-013736) on fatigue, thyroid-stimulating hormone, and biomarkers: a phase I study in Japanese patients
    Toru Mukohara
    National Cancer Center Hospital East, Oncology Hematology, Kashiwa, Japan
    Cancer Sci 101:963-8. 2010
    ..Axitinib 5 mg twice-daily is the recommended starting dose for Japanese patients. This trial is registered with ClinicalTrials.gov, identifier NCT00447005...
  7. ncbi Axitinib treatment in patients with cytokine-refractory metastatic renal-cell cancer: a phase II study
    Olivier Rixe
    Pitie Salpetriere Hospital, University of Paris, Paris, France
    Lancet Oncol 8:975-84. 2007
    ..We aimed to assess the activity and safety of axitinib in patients with metastatic renal-cell cancer who had failed on previous cytokine-based treatment...
  8. pmc Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
    Florence I Raynaud
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, UK
    Mol Cancer Ther 8:1725-38. 2009
    ..Together, these data support the development of GDC-0941 as a potent, orally bioavailable inhibitor of phosphatidylinositide 3-kinase. GDC-0941 has recently entered phase I clinical trials...
  9. pmc Bindarit: an anti-inflammatory small molecule that modulates the NFκB pathway
    Eugenio Mora
    Center for Epigenetics and Metabolism, School of Medicine, University of California at Irvine, Irvine, CA, USA
    Cell Cycle 11:159-69. 2012
    ..These findings pave the way for future applications of bindarit as modulator of the inflammatory response...
  10. doi Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and human cancer cell line panel JFCR39
    Dexin Kong
    Division of Molecular Pharmacology, Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, 3 10 6, Ariake, Koto ku, Tokyo 135 8550, Japan
    Eur J Cancer 46:1111-21. 2010
    ..The biological implication of the difference in molecular target specificity of these PI3K inhibitors is under investigation...
  11. pmc The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemic mice
    Gianluca Grassia
    Department of Experimental Pharmacology, University of Naples Federico II, Via Domenico Montesano, 49, 80131 Naples, Italy
    Cardiovasc Res 84:485-93. 2009
    ....
  12. pmc c-Yes regulates cell adhesion at the blood-testis barrier and the apical ectoplasmic specialization in the seminiferous epithelium of rat testes
    Xiang Xiao
    Center for Biomedical Research, Population Council, 1230 York Avenue, New York, NY 10065, USA
    Int J Biochem Cell Biol 43:651-65. 2011
    ..In summary, c-Yes regulates BTB and apical ES integrity by maintaining proper distribution of integral membrane proteins and actin filament organization at these sites...
  13. pmc Intracellular protein binding patterns of the anticancer ruthenium drugs KP1019 and KP1339
    Petra Heffeter
    Department of Medicine I, Institute of Cancer Research, Medical University Vienna, Austria
    J Biol Inorg Chem 15:737-48. 2010
    ..The different protein binding patterns as compared with those for cisplatin suggest specific protein targets and consequently a unique mode of action for the ruthenium drugs investigated...
  14. pmc Inhibition of reactive gliosis prevents neovascular growth in the mouse model of oxygen-induced retinopathy
    Michael Deniro
    Research Department, King Khaled Eye Specialist Hospital, Riyadh, Saudi Arabia
    PLoS ONE 6:e22244. 2011
    ..In addition, the study reveals that YC-1 may exert promising therapeutic effects in the treatment of retinal and neuronal pathologies...
  15. doi Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors
    Kyle A Edgar
    Cancer Signaling and Translational Oncology, Genentech, Inc, South San Francisco, California 94080, USA
    Cancer Res 70:1164-72. 2010
    ..Our results imply that patients with PTEN-negative tumors may preferentially benefit from treatment with a class I PI3K inhibitor that is capable of inhibiting the p110beta isoform...
  16. doi Antiproteinuric effect of chemokine C-C motif ligand 2 inhibition in subjects with acute proliferative lupus nephritis
    Alessandro Ble
    Angelini Research Center, Piazzale della Stazione, S Palomba, Pomezia, Italy
    Am J Nephrol 34:367-72. 2011
    ..To test the role of chemokine C-C motif ligand 2 (CCL2) in the pathogenesis of lupus nephritis (LN), we evaluated the effects of CCL2 inhibition by bindarit therapy in patients with systemic lupus and active renal disease...
  17. doi Axitinib--a selective inhibitor of the vascular endothelial growth factor (VEGF) receptor
    Ronan J Kelly
    National Cancer Institute, Medical Oncology Branch, Center for Cancer Research, Bethesda, MD 20892, USA
    Target Oncol 4:297-305. 2009
    ..Ongoing Phase III studies in pancreatic and metastatic renal cell carcinoma should help to determine the optimum utilization of these agents at the appropriate stage of disease...
  18. ncbi Inhibitory effect of YC-1 on the hypoxic induction of erythropoietin and vascular endothelial growth factor in Hep3B cells
    Y S Chun
    Department of Pharmacology and Heart Research Institute, BK21 Human Life Sciences, Seoul National University College of Medicine, 28 Yongon-dong, Chongno-gu, 110-799, Seoul, South Korea
    Biochem Pharmacol 61:947-54. 2001
    ..This observation implies that the inhibitory effects of YC-1 on hypoxic responses can be developed to suppress EPO-overproduction by tumor cells and tumor angiogenesis...
  19. doi Pleiotropic effects of YC-1 selectively inhibit pathological retinal neovascularization and promote physiological revascularization in a mouse model of oxygen-induced retinopathy
    M DeNiro
    Research Department, King Khaled Eye Specialist Hospital, Aruba Street, P O Box 7191, Riyadh 11462, Kingdom of Saudi Arabia
    Mol Pharmacol 77:348-67. 2010
    ..The pleiotropic effects of YC-1 allude to its possible use as a promising therapeutic iNOS inhibitor candidate for the treatment of retinal neovascularization...
  20. doi Efficacy of gemcitabine plus axitinib compared with gemcitabine alone in patients with advanced pancreatic cancer: an open-label randomised phase II study
    Jean Philippe Spano
    Hopital de la Pitie Salpetriere, Paris, France
    Lancet 371:2101-8. 2008
    ..The aim of this study was to assess the safety and efficacy of gemcitabine plus axitinib versus gemcitabine alone...
  21. doi Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML
    Jianbiao Zhou
    Department of Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore
    Blood 113:4052-62. 2009
    ....
  22. doi Key predictive factors of axitinib (AG-013736)-induced proteinuria and efficacy: a phase II study in Japanese patients with cytokine-refractory metastatic renal cell Carcinoma
    Yoshihiko Tomita
    Department of Urology, Yamagata University Faculty of Medicine, Yamagata, Japan
    Eur J Cancer 47:2592-602. 2011
    ..This phase II study investigated axitinib efficacy, safety and biomarkers in Japanese patients with cytokine-refractory metastatic renal cell carcinoma (mRCC)...
  23. ncbi Intrinsic and acquired forms of resistance against the anticancer ruthenium compound KP1019 [indazolium trans-[tetrachlorobis(1H-indazole)ruthenate (III)] (FFC14A)
    P Heffeter
    Institute of Cancer Research, Borschkegasse 8a, 1090 Vienna, Austria
    J Pharmacol Exp Ther 312:281-9. 2005
    ..In summary, the likeliness of acquiring insensitivity to KP1019 during therapy is expected to be low, and resistance should not be based on overexpression of drug efflux transporters...
  24. doi Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics
    Meghan Brennan
    Pfizer Research Center of Emphasis for DNA and Biofluids Biobank, Groton, CT, USA
    Eur J Clin Pharmacol 68:645-55. 2012
    ..The potential contribution of polymorphisms in genes encoding these enzymes and transporters to axitinib pharmacokinetic variability was assessed...
  25. ncbi YC-1-induced cyclooxygenase-2 expression is mediated by cGMP-dependent activations of Ras, phosphoinositide-3-OH-kinase, Akt, and nuclear factor-kappaB in human pulmonary epithelial cells
    Ming Shyan Chang
    Graduate Institute of Medical Sciences, College of Medicine, Taipei Medical University, 250 Wu Hsing Street, Taipei 110, Taiwan
    Mol Pharmacol 66:561-71. 2004
    ....
  26. pmc En route to osmium analogues of KP1019: synthesis, structure, spectroscopic properties and antiproliferative activity of trans-[Os(IV)Cl4(Hazole)2]
    Gabriel E Büchel
    University of Vienna, Institute of Inorganic Chemistry, Währinger Strasse 42, A 1090 Vienna, Austria
    Inorg Chem 50:7690-7. 2011
    ..Their antiproliferative acitivity in the human cancer cell lines CH1 (ovarian carcinoma), A549 (nonsmall cell lung carcinoma), and SW480 (colon carcinoma) is reported...
  27. doi Inhibition of in-stent stenosis by oral administration of bindarit in porcine coronary arteries
    Armando Ialenti
    Department of Experimental Pharmacology, University of Naples Federico II, Naples, Italy
    Arterioscler Thromb Vasc Biol 31:2448-54. 2011
    ..The aim of the current study was to evaluate the efficacy of bindarit on in-stent stenosis in the preclinical porcine coronary stent model...
  28. doi Modulation of the tumor microvasculature by phosphoinositide-3 kinase inhibition increases doxorubicin delivery in vivo
    Naseer Qayum
    Gray Institute for Radiation Oncology and Biology, Oxford University, Oxford, United Kingdom
    Clin Cancer Res 18:161-9. 2012
    ..On the basis of that result, we asked whether inhibition of PI3K would improve chemotherapy delivery...
  29. ncbi The anti-angiogenesis agent, AG-013736, has minimal activity in elderly patients with poor prognosis acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS)
    Francis J Giles
    Department of Leukemia, University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Box 428, Houston, TX 77030, USA
    Leuk Res 30:801-11. 2006
    ..AG-01736 had minimal biologic or clinical activity in this elderly patient population...
  30. ncbi YC-1 [3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole] inhibits endothelial cell functions induced by angiogenic factors in vitro and angiogenesis in vivo models
    Shiow Lin Pan
    Pharmacological Institute, College of Medicine, National Taiwan University, 1 Jen Ai Road, Section 1, Taipei, Taiwan
    J Pharmacol Exp Ther 314:35-42. 2005
    ..YC-1 may be useful for treating angiogenesis-dependent human diseases such as cancer...
  31. doi Benzotriazoles and indazoles are scaffolds with biological activity against Entamoeba histolytica
    Fabian López-Vallejo
    Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, FL 34987, USA
    J Biomol Screen 16:862-8. 2011
    ..The novel compounds have similar properties to approved drugs. Compounds with novel scaffolds represent promising starting points of an optimization program against E. histolytica...
  32. doi Amelioration of alphavirus-induced arthritis and myositis in a mouse model by treatment with bindarit, an inhibitor of monocyte chemotactic proteins
    Nestor E Rulli
    Faculty of Applied Science, University of Canberra, Canberra, ACT, Australia
    Arthritis Rheum 60:2513-23. 2009
    ..The aim of the present investigations was to determine whether bindarit, an inhibitor of monocyte chemotactic protein (MCP) synthesis, could ameliorate alphavirus-induced rheumatic disease in mice...
  33. doi CZE-ICP-MS as a tool for studying the hydrolysis of ruthenium anticancer drug candidates and their reactivity towards the DNA model compound dGMP
    Michael Groessl
    Institute of Inorganic Chemistry, University of Vienna, Waehringer Street 42, A 1090 Vienna, Austria
    J Inorg Biochem 102:1060-5. 2008
    ..RAPTA-C was found to hydrolyze fastest and showed the highest reactivity toward the DNA model compound, whereas KP418 was the most stable compound in both these respects...
  34. doi Amorphous solid dispersion enhances permeation of poorly soluble ABT-102: true supersaturation vs. apparent solubility enhancement
    Kerstin J Frank
    Institute of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK 5230 Odense M, Denmark
    Int J Pharm 437:288-93. 2012
    ..Overall, a good correlation between permeation rate and molecular solubility but not apparent solubility was seen...
  35. doi Multicenter, phase II study of axitinib, a selective second-generation inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, in patients with metastatic melanoma
    John Fruehauf
    University of California, Irvine, Orange, 92868, USA
    Clin Cancer Res 17:7462-9. 2011
    ....
  36. pmc YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase
    C C Wu
    Pharmacological Institute, College of Medicine, National Taiwan University, Taipei
    Br J Pharmacol 116:1973-8. 1995
    ..7. These results would suggest that YC-1 activates sGC of human platelets by a NO-dependent mechanism, and exerts its antiplatelet effects through the sGC/cyclic GMP pathway...
  37. ncbi Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor
    Daniel H Albert
    Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, R47J, Building AP9 2, 100 Abbott Park Road, Abbott Park, IL 60064 3500, USA
    Mol Cancer Ther 5:995-1006. 2006
    ..08 microg/mL, >or=7 hours) than with plasma area under the curve or Cmax. These results support clinical assessment of ABT-869 as a therapeutic agent for cancer...
  38. ncbi From bench to bedside--preclinical and early clinical development of the anticancer agent indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019 or FFC14A)
    Christian G Hartinger
    Institute of Inorganic Chemistry, University of Vienna, Waehringer Strasse 42, A 1090 Vienna, Austria
    J Inorg Biochem 100:891-904. 2006
    ..In this review, the preclinical and early clinical development of KP1019 - from bench to bedside - is recapitulated...
  39. doi Suppression of HER2/HER3-mediated growth of breast cancer cells with combinations of GDC-0941 PI3K inhibitor, trastuzumab, and pertuzumab
    Evelyn Yao
    Department of Cancer Signaling, Genentech, Inc, South San Francisco, California, USA
    Clin Cancer Res 15:4147-56. 2009
    ..We therefore investigated the combinatorial activity of GDC-0941, a novel class I PI3K inhibitor, with standard-of-care therapies for HER2-amplified breast cancer...
  40. doi A novel mode of action of YC-1 in HIF inhibition: stimulation of FIH-dependent p300 dissociation from HIF-1{alpha}
    Shan Hua Li
    Department of Pharmacology, Seoul National University College of Medicine, Seoul, Korea
    Mol Cancer Ther 7:3729-38. 2008
    ..Given these results, we suggest that the functional inactivation of HIF-alpha contributes to the YC-1-induced deregulation of hypoxia-induced genes...
  41. ncbi AG-013736, a novel inhibitor of VEGF receptor tyrosine kinases, inhibits breast cancer growth and decreases vascular permeability as detected by dynamic contrast-enhanced magnetic resonance imaging
    Lisa J Wilmes
    Department of Radiology, University of California San Francisco, San Francisco, CA 94143 1290, USA
    Magn Reson Imaging 25:319-27. 2007
    ..Furthermore, the correlative relationship between microvasculature changes and tumor growth inhibition supports DCE-MRI methods as a biomarker of VEGF receptor target inhibition with potential clinical utility...
  42. doi Pharmacokinetic-pharmacodynamic modeling of tumor growth inhibition and biomarker modulation by the novel phosphatidylinositol 3-kinase inhibitor GDC-0941
    Laurent Salphati
    Departments of Drug Metabolism and Pharmacokinetics, Genentech Inc, 1 DNA Way, South San Francisco, CA 94080, USA
    Drug Metab Dispos 38:1436-42. 2010
    ..1 xenograft...
  43. ncbi NO-independent stimulators of soluble guanylate cyclase
    A Straub
    Institute of Medicinal Chemistry, Pharma Research Centre, Bayer AG, Wuppertal, FRG
    Bioorg Med Chem Lett 11:781-4. 2001
    ..Several pyrazolopyridinylpyrimidines are shown to relax aortic rings and revealed a long-lasting blood pressure lowering effect in rats after oral application...
  44. doi Modulating the hypoxia-inducible factor signaling pathway as a therapeutic modality to regulate retinal angiogenesis
    M DeNiro
    Research Department, King Khaled Eye Specialist Hospital, Riyadh, Saudi Arabia
    Exp Eye Res 89:700-17. 2009
    ....
  45. doi [Os(IV)Cl(5)(Hazole)](-) complexes: synthesis, structure, spectroscopic properties, and antiproliferative activity
    Gabriel E Büchel
    University of Vienna, Institute of Inorganic Chemistry, Austria
    Inorg Chem 48:10737-47. 2009
    ..Replacement of azolium cations by sodium had significant effects; cytotoxicity increased in the case of the pyrazole system from 3 (A549) to the 5.5-fold (CH1)...
  46. ncbi YC-1: a potential anticancer drug targeting hypoxia-inducible factor 1
    Eun Jin Yeo
    Department of Pharmacology, BK21 Human Life Sciences, Seoul National University College of Medicine, Seoul, Korea
    J Natl Cancer Inst 95:516-25. 2003
    ..We tested whether YC-1 inhibits HIF-1 and tumor growth in vivo...
  47. pmc Epidermal growth factor receptor pathway substrate 8 (Eps8) is a novel regulator of cell adhesion and the blood-testis barrier integrity in the seminiferous epithelium
    Pearl P Y Lie
    Center for Biomedical Research, Population Council, 1230 York Ave, New York, NY 10065, USA
    FASEB J 23:2555-67. 2009
    ....
  48. pmc ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia
    Deepa B Shankar
    Division of Hematology Oncology, Department of Pediatrics, Gwynne Hazen Cherry Memorial Laboratories, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, CA, USA
    Blood 109:3400-8. 2007
    ..In tumors, ABT-869 inhibited FLT3 phosphorylation, induced apoptosis (transferase-mediated dUTP nick-end labeling [TUNEL]) and decreased proliferation (Ki67). ABT-869 is under clinical development for AML...
  49. ncbi Synergistic antileukemic effects between ABT-869 and chemotherapy involve downregulation of cell cycle-regulated genes and c-Mos-mediated MAPK pathway
    J Zhou
    Department of Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore
    Leukemia 22:138-46. 2008
    ..Thus, a clinical trial using sequence-dependent combination therapy with ABT-869 in AML is warranted...
  50. ncbi Phase II study of lonidamine and diazepam in the treatment of recurrent glioblastoma multiforme
    Stephane Oudard
    Department of Oncology, Hopital Europeen Georges Pompidou, Paris, France
    J Neurooncol 63:81-6. 2003
    ..LND plus diazepam may be interesting in the adjuvant setting or associated to chemotherapy to act on different targets and increase the therapeutic index...
  51. doi Does axitinib (AG-01376) have a future role in metastatic renal cell carcinoma and other malignancies?
    Robert Goldstein
    Department of Oncology, St George s Hospital, London, SW17 0QT, UK
    Expert Rev Anticancer Ther 10:1545-57. 2010
    ..It is now being investigated in two Phase III trials in metastatic renal cell carcinoma and in Phase II trials in a range of tumor types. These trials will determine whether axitinib is an effective and safe antiangiogenic therapy...
  52. pmc Inhibition of rat cerebellar nitric oxide synthase by 7-nitro indazole and related substituted indazoles
    R C Babbedge
    Biomedical Sciences Division, King s College, University of London
    Br J Pharmacol 110:225-8. 1993
    ..Indazole-based inhibitors of NOS may prove useful tools with which to evaluate the biological roles of nitric oxide in the central nervous system...
  53. pmc Adjudin-mediated Sertoli-germ cell junction disassembly affects Sertoli cell barrier function in vitro and in vivo
    Linlin Su
    Population Council, Center for Biomedical Research, New York, NY 10065, USA
    Int J Biochem Cell Biol 42:1864-75. 2010
    ..These results illustrate that a unique mechanism exists to maintain blood-testis barrier integrity at all costs, irrespective of the presence of germ cells in the seminiferous epithelium of the testis...
  54. ncbi Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists
    Anil Vasudevan
    Metabolic Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 15:5293-7. 2005
    ..Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice...
  55. ncbi Synthesis and antiproliferative activity of triazenoindazoles and triazenopyrazoles: a comparative study
    Giuseppe Daidone
    Dipartimento di Chimica e Tecnologie Farmaceutiche, Universita degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
    Eur J Med Chem 39:219-24. 2004
    ..The (1)H-NMR spectra showed that the rotational barrier around the N(2)-N(3) bond in the triazene group can be influenced both by the position of this group in the indazole nucleus and by the substitution pattern in the benzene moiety...
  56. ncbi Synthesis and biological evaluation of N-(7-indazolyl)benzenesulfonamide derivatives as potent cell cycle inhibitors
    L Bouissane
    Institut de Chimie Organique et Analytique, UMR CNRS 6005, Universite d Orleans, BP 6759, France
    Bioorg Med Chem 14:1078-88. 2006
    ..These compounds were evaluated for their antiproliferative activities toward L1210 murine leukemia cells. One of them, 4-methoxy-N-(3-chloro-7-indazolyl)benzenesulfonamide, was identified as the most potent with an IC(50) of 0.44 microM...
  57. ncbi Synthesis of furopyrazole analogs of 1-benzyl-3-(5-hydroxymethyl-2-furyl)indazole (YC-1) as novel anti-leukemia agents
    Li Chen Chou
    Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan
    Bioorg Med Chem 15:1732-40. 2007
    ..Therefore, compound 1 is identified here as a new lead compound of cell differentiating agent and apoptosis inducer for further development of new anti-leukemia agents...
  58. ncbi A new alkaloid and its artificial derivative with an indazole ring from Nigella glandulifera
    Yu Ming Liu
    Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Haidian District, PR China
    Chem Pharm Bull (Tokyo) 52:454-5. 2004
    ..Their structures were established by spectral analysis, including two-dimensional (2D)-NMR spectroscopy. Nigeglanine (1) is the third natural product determined to contain an indazole nucleus...
  59. ncbi YC-1 [3-(5'-Hydroxymethyl-2'-furyl)-1-benzyl Indazole] exhibits a novel antiproliferative effect and arrests the cell cycle in G0-G1 in human hepatocellular carcinoma cells
    Shih Wei Wang
    Pharmacological Institutes, College of Medicine, National Taiwan University, 1 Jen Ai Road, sect 1, Taipei, Taiwan
    J Pharmacol Exp Ther 312:917-25. 2005
    ..Because of this, YC-1 is a potential antitumor agent worthy of further investigation...
  60. ncbi New anticancer strategies targeting HIF-1
    Eun Jin Yeo
    Department of Pharmacology, College of Medicine, Seoul National University, 28 Yongon Dong, Chongno Gu, 110 799, Republic of Korea
    Biochem Pharmacol 68:1061-9. 2004
    ..Moreover, it halted tumor growth in immunodeficient mice without serious toxicity during the treatment period. Thus, we propose that YC-1 is a good lead compound for the development of new anti-HIF-1, anticancer agents...
  61. ncbi YC-1 inhibits proliferation of human vascular endothelial cells through a cyclic GMP-independent pathway
    Hun Kung Hsu
    Graduate Institute of Medical Sciences, Taipei Medical University, 250 Wu Hsing Street, Taipei 110, Taiwan, ROC
    Biochem Pharmacol 66:263-71. 2003
    ..This YC-1-induced antiproliferation effect in HUVEC is via a cyclic GMP-independent pathway...
  62. ncbi Chromophore-modified bis-benzo[g]indole carboxamides: synthesis and antiproliferative activity of bis-benzo[g]indazole-3-carboxamides and related dimers
    Gerard A Pinna
    Dipartimento Farmaco Chimico Tossicologico, Universita di Sassari, via F Muroni 23 A, 07100 Sassari, Italy
    Farmaco 58:749-63. 2003
    ..Finally, viscosity measurement of 2f with poly(dA-dT)(2), confirmed that these promising compounds behaved as typical DNA-intercalating agents...
  63. pmc Axitinib for the management of metastatic renal cell carcinoma
    Bernard Escudier
    Institut Gustave Roussy, Villejuif, France
    Drugs R D 11:113-26. 2011
    ..These results will help to determine the place of axitinib in the mRCC treatment algorithm...
  64. ncbi Inhibition of hypoxia inducible factor 1α expression suppresses the progression of esophageal squamous cell carcinoma
    Hong Zhu
    Department of Gastroenterology, First Affiliated Hospital of Nanjing Medical University, Nanjing, China
    Cancer Biol Ther 11:981-7. 2011
    ..In conclusion, our results provide new insight into the potential role of HIF-1α in esophageal squamous cell carcinoma and open up the possibility of inhibiting HIF-1α for targeted therapy of esophageal squamous cell carcinoma...
  65. ncbi Synthesis of indazoles by the [3+2] cycloaddition of diazo compounds with arynes and subsequent acyl migration
    Zhijian Liu
    Department of Chemistry, Iowa State University, Ames, Iowa 50011, USA
    J Org Chem 73:219-26. 2008
    ..efficient approach to a wide range of potentially biologically and pharmaceutically interesting substituted indazoles in good to excellent yields under mild reaction conditions...
  66. doi The selective VEGFR1-3 inhibitor axitinib (AG-013736) shows antitumor activity in human neuroblastoma xenografts
    Jochen Rossler
    UPRES EA 3535, Pharmacology and New Anticancer Treatments, University Paris Sud, Institut Gustave Roussy, Villejuif, France
    Int J Cancer 128:2748-58. 2011
    ..Axitinib has potent antiangiogenic properties that may warrant further evaluation in neuroblastoma...
  67. doi Phase I and biomarker study of ABT-869, a multiple receptor tyrosine kinase inhibitor, in patients with refractory solid malignancies
    Chiung Ing Wong
    Department of Hematology Oncology, National University Hospital, National University of Singapore, Singapore 119074
    J Clin Oncol 27:4718-26. 2009
    ..To determine the safety and tolerability of ABT-869 at escalating doses and its effects on biomarkers relevant for antiangiogenic activity in patients with solid malignancies...
  68. pmc Zinc transporter 8 (ZnT8) expression is reduced by ischemic insults: a potential therapeutic target to prevent ischemic retinopathy
    Michael Deniro
    Research Department, King Khaled Eye Specialist Hospital Affiliate of the Wilmer Eye Institute of the Johns Hopkins Medicine, Riyadh, Saudi Arabia
    PLoS ONE 7:e50360. 2012
    ..Therefore, targeting ZnT8 provides a therapeutic strategy to combat neovascular eye diseases...
  69. ncbi Mitochondrial targeting drug lonidamine triggered apoptosis in doxorubicin-resistant HepG2 cells
    Y C Li
    Department of Biochemistry, The Chinese University of Hong Kong, Shatin, People s Republic of China
    Life Sci 71:2729-40. 2002
    ..Taken together, our results suggest a potential use of LND as an anti-cancer drug to bypass drug resistance and to trigger tumour destruction through apoptosis in HepG2 and R-HepG2 cells...
  70. doi Protective effects of YC-1 against glutamate induced PC12 cell apoptosis
    Xiaofan Yang
    College of Medicine, Nankai University, Tianjin, China
    Cell Mol Neurobiol 31:303-11. 2011
    ..These results revealed that YC-1 might attenuate glutamate-induced PC12 cell apoptosis via a sGC-cGMP involved pathway...
  71. pmc Effect of rifampin on the pharmacokinetics of Axitinib (AG-013736) in Japanese and Caucasian healthy volunteers
    Y K Pithavala
    Pfizer Oncology, Pfizer Global Research and Development, La Jolla Laboratories, 101646 Science Center Drive, San Diego, CA 92121, USA
    Cancer Chemother Pharmacol 65:563-70. 2010
    ..Equal numbers of Japanese and Caucasian subjects were enrolled to assess the potential differences in axitinib pharmacokinetics between the two ethnicities...
  72. ncbi Inhibitory mechanisms of YC-1 and PMC in the induction of iNOS expression by lipoteichoic acid in RAW 264.7 macrophages
    George Hsiao
    Graduate Institute of Pharmacology, Taipei Medical University, 250 Wu Shing Street, Taipei 110, Taiwan, ROC
    Biochem Pharmacol 67:1411-9. 2004
    ..YC-1 may be mediated by increasing cyclic GMP, followed by, at least partly, inhibition of JNK/SAPK and NF-kappaB activations, thereby leading to inhibition of iNOS expression...
  73. ncbi YC-1 inhibits HIF-1 expression in prostate cancer cells: contribution of Akt/NF-kappaB signaling to HIF-1alpha accumulation during hypoxia
    H L Sun
    Pharmacological Institute, College of Medicine, National Taiwan University, Taipei, Taiwan
    Oncogene 26:3941-51. 2007
    ..Overall, we identify a potential molecular mechanism whereby YC-1 serves to reduce HIF-1 expression...
  74. doi Human trabecular meshwork cell volume decrease by NO-independent soluble guanylate cyclase activators YC-1 and BAY-58-2667 involves the BKCa ion channel
    William M Dismuke
    Department of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, USA
    Invest Ophthalmol Vis Sci 50:3353-9. 2009
    ..This study investigated the effects of the nitric oxide (NO)-independent activators of soluble guanylate cyclase (sGC), YC-1, and BAY-58-2667 on TM cell volume and the signal transduction pathways and ion channel involved...
  75. doi Stable expression of HIF-1alpha in tubular epithelial cells promotes interstitial fibrosis
    Kuniko Kimura
    First Department of Internal Medicine, Nara Medical University, 840 Shijo, Kashihara, Nara 634 8522, Japan
    Am J Physiol Renal Physiol 295:F1023-9. 2008
    ..In conclusion, HIF-1alpha appears to be a critical contributor to the progression of renal fibrosis and could be a useful target for its treatment...
  76. ncbi YC-1 induces S cell cycle arrest and apoptosis by activating checkpoint kinases
    Eun Jin Yeo
    Department of Pharmacology, Seoul National University College of Medicine, Seoul, South Korea
    Cancer Res 66:6345-52. 2006
    ..These results imply that YC-1 does not promote the regrowth of hypoxic tumors because of its cell cycle arrest effect. Furthermore, YC-1 may induce the combined anticancer effects of HIF-1alpha inhibition and cell growth inhibition...
  77. ncbi Inhibition of hypoxia-induced increase of blood-brain barrier permeability by YC-1 through the antagonism of HIF-1alpha accumulation and VEGF expression
    Wei Lan Yeh
    Department of Pharmacology, College of Medicine, National Taiwan University, 1, Sec 1, Jen Ai Road, Taipei, Taiwan
    Mol Pharmacol 72:440-9. 2007
    ..Taken together, these results indicate that YC-1 may inhibit HIF-1alpha accumulation and VEGF production, which in turn protect BBB from injury caused by hypoxia...
  78. ncbi A domain responsible for HIF-1alpha degradation by YC-1, a novel anticancer agent
    Hye Lim Kim
    Department of Pharmacology, Seoul National University College of Medicine, Chongno Gu, Seoul 110 799, Korea
    Int J Oncol 29:255-60. 2006
    ..However, their binding to HIF-1alpha was not affected by YC-1, suggesting that they are not involved in the YC-1 action. It is also suggested that YC-1 targets a novel pathway regulating HIF-1alpha stability...
  79. ncbi Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor
    Yujia Dai
    Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6100, USA
    J Med Chem 50:1584-97. 2007
    ..In particular, compound 17p (ABT-869) was found to possess favorable pharmacokinetic profiles across different species and display significant tumor growth inhibition in multiple preclinical animal models...
  80. ncbi Hypoxia-inducible factor-1 inhibition in combination with temozolomide treatment exhibits robust antitumor efficacy in vivo
    Leiming Li
    Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    Clin Cancer Res 12:4747-54. 2006
    ..However, these hypotheses have not been rigorously tested in tumor models in vivo. The present study was carried out to evaluate the antitumor efficacy of combining HIF-1 inhibition with angiogenesis inhibitors or cytotoxic agents...
  81. ncbi Treatment with bindarit, a blocker of MCP-1 synthesis, protects mice against acute pancreatitis
    Madhav Bhatia
    Dept of Pharmacology, National Univ of Singapore, Faculty of Medicine, Bldg MD2, 18 Medical Dr, Singapore 117597
    Am J Physiol Gastrointest Liver Physiol 288:G1259-65. 2005
    ....
  82. doi ABT-869, a multi-targeted tyrosine kinase inhibitor, in combination with rapamycin is effective for subcutaneous hepatocellular carcinoma xenograft
    Viraj J Jasinghe
    Department of Medicine, Yong Loo Lin School of Medicine, National University of Singapore, 5 Lower Kent Ridge Road, Singapore 119074, Singapore
    J Hepatol 49:985-97. 2008
    ..Receptor tyrosine kinase inhibitors (RTKIs) and mTOR inhibitors are potential novel anticancer therapies for HCC. We hypothesized that combination targeted on distinctive signal pathways would provide synergistic therapeutics...
  83. doi Impact of the anti-inflammatory agent bindarit on the chemokinome: selective inhibition of the monocyte chemotactic proteins
    Massimiliano Mirolo
    Istituto Clinico Humanitas IRCCS, Rozzano, Italy
    Eur Cytokine Netw 19:119-22. 2008
    ..Here we report on the use of inhibition of synthesis as a potentially viable and selective approach to modify the chemokine system...
  84. ncbi N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics
    Paul Bamborough
    GlaxoSmithKline R and D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK
    Bioorg Med Chem Lett 17:4363-8. 2007
    ..Replacement of this substituent by 4-amino(5-methyl-1H-indazole) yielded compounds with comparable enzyme potency and improved pharmacokinetic properties...
  85. ncbi Involvement of nitric oxide-soluble guanylyl cyclase pathway in the control of maximal dentate gyrus activation in the rat
    P Sardo
    Dipartimento di Medicina Sperimentale, Sezione di Fisiologia umana G Pagano, Universita degli Studi di Palermo, Palermo, Italy
    J Neural Transm 113:1855-61. 2006
    ..Our results indicate that the nitrergic neurotransmission exerts a modulatory role in the proneness to the epileptogenic phenomena through the activation of sGC metabolic pathway...
  86. ncbi The discharge of subthalamic neurons is modulated by inhibiting the nitric oxide synthase in the rat
    Pierangelo Sardo
    Dipartimento di Medicina Sperimentale Sezione di Fisiologia umana, Universita degli Studi di Palermo, Corso Tukory, 129, Palermo 90134, Italy
    Neurosci Lett 396:252-6. 2006
    ..We hypothesize that nitric oxide neurotransmission could exert a tonic modulatory influence upon spontaneously discharging subthalamic neurons, with a prevalent excitatory effect...
  87. ncbi 7-Nitroindazole potentiates the anticonvulsant action of some second-generation antiepileptic drugs in the mouse maximal electroshock-induced seizure model
    J J Luszczki
    Department of Pathophysiology, Medical University of Lublin, Lublin, Poland
    J Neural Transm 113:1157-68. 2006
    ....
  88. ncbi Amelioration of rat adjuvant arthritis by therapeutic treatment with bindarit, an inhibitor of MCP-1 and TNF-alpha production
    A Guglielmotti
    Immunopharmacology Lab, ACRAF SpA Angelini Ricerche, Rome, Italy
    Inflamm Res 51:252-8. 2002
    ..This study was designed to evaluate therapeutic effects of bindarit, an indazolic derivative able to inhibit monocyte chemoattractant protein-1 (MCP-1) production, in adjuvant induced arthritis in rats...
  89. pmc Human soluble guanylate cyclase: functional expression and revised isoenzyme family
    U Zabel
    Department of Pharmacology and Toxicology, Julius Maximilians University, 9 Versbacher St, D 97078 Wurzburg, Germany
    Biochem J 335:51-7. 1998
    ..Having access to the human key enzyme of NO signalling will now permit the study of novel sGC-modulating compounds with therapeutic potential...
  90. ncbi Changes in nitric oxide synthesis and epileptic activity in the contralateral hippocampus of rats following intrahippocampal kainate injection
    H Yasuda
    Department of Neurosurgery, Yamaguchi University School of Medicine 1144, Kogushi Ube, Yamaguchi 755-8505, Japan
    Epilepsia 42:13-20. 2001
    ..CONCLUSIONS: The results suggest that remote seizure activity caused by the transneuronal spread of kainate-induced discharges may be related to NO derived from neuronal NOS...
  91. ncbi Activators of soluble guanylate cyclase for the treatment of male erectile dysfunction
    J D Brioni
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    Int J Impot Res 14:8-14. 2002
    ..This type of sGC activators represent a new class of compounds with a different pharmacological profile in comparison to the classical NO-donors and they could be beneficial for the treatment of male erectile dysfunction...
  92. ncbi Adenine nucleotide translocator mediates the mitochondrial membrane permeabilization induced by lonidamine, arsenite and CD437
    A S Belzacq
    CNRS-UMR6022, , BP 20529, , France
    Oncogene 20:7579-87. 2001
    ..These results indicate that ANT is a target of lonidamine, arsenite, and CD437 and unravel an unexpected heterogeneity in the mode of action of these three compounds...
  93. ncbi Increased neuronal nitric oxide synthase (nNOS) activity triggers picrotoxin-induced seizures in rats and evidence for participation of nNOS mechanism in the action of antiepileptic drugs
    Karthik Rajasekaran
    Department of Pharmacology and Environmental Toxicology, Dr ALM Post Graduate Institute of Basic Medical Sciences, University of Madras, Taramani, 600 113, Chennai, India
    Brain Res 979:85-97. 2003
    ..The results of the present study provide evidence for a trigger role of neuronally produced NO in epileptogenesis induced by PCT and the participation of nNOS inhibitory mechanisms in the action of AEDs...
  94. ncbi NO-independent regulatory site on soluble guanylate cyclase
    J P Stasch
    Pharma Research Center, Bayer AG, Aprather Wey 18a, D 42096 Wuppertal, Germany
    Nature 410:212-5. 2001
    ..This results in antiplatelet activity, a strong decrease in blood pressure and an increase in survival in a low-NO rat model of hypertension, and as such may offer an approach for treating cardiovascular diseases...
  95. ncbi Purified soluble guanylyl cyclase expressed in a baculovirus/Sf9 system: stimulation by YC-1, nitric oxide, and carbon monoxide
    M Hoenicka
    DLR Institute of Aerospace Medicine, Cologne, Germany
    J Mol Med (Berl) 77:14-23. 1999
    ..The described method should help to facilitate the investigation of the new therapeutic principle of NO-independent guanylyl cyclase activators...
  96. ncbi In vivo activity of ABT-869, a multi-target kinase inhibitor, against acute myeloid leukemia with wild-type FLT3 receptor
    Jianbiao Zhou
    Department of Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore
    Leuk Res 32:1091-100. 2008
    ..ABT-869 also reduced the leukemia burden and prolonged survival. Our study supports the rationale for clinically testing an anti-angiogenesis agent in AML with wild-type FLT3...
  97. ncbi Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors
    Jun Guo
    Cancer Discovery Research R47J, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6121, USA
    Mol Cancer Ther 5:1007-13. 2006
    ..These results show the use of a cell-based assay to confirm the inhibitory activity of lead compounds and drug candidates, such as ABT-869, against the CSF-1R protein in situ...
  98. ncbi Synthesis and biological evaluation of novel pyrazoles and indazoles as activators of the nitric oxide receptor, soluble guanylate cyclase
    D L Selwood
    Biological and Medicinal Chemistry and Molecular and Cellular Biology, The Wolfson Institute for Biomedical Research, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, UK
    J Med Chem 44:78-93. 2001
    ..Furthermore 32 has an excellent selectivity profile notably showing no significant inhibition of phosphodiesterases or nitric oxide synthases...
  99. ncbi Contributions of nitric oxide synthase isozymes to exhaled nitric oxide and hypoxic pulmonary vasoconstriction in rabbit lungs
    David J Vaughan
    Department of Pediatrics, Children s Hospital and Regional Medical Center, Seattle 98105, USA
    Am J Physiol Lung Cell Mol Physiol 284:L834-43. 2003
    ..Our findings show virtually all exhaled NO in the rabbit lung is produced by eNOS, which is present throughout the airways, alveoli, and vessels. Both vascular and epithelial-derived NO modulate HPV...
  100. pmc YC-1 activation of human soluble guanylyl cyclase has both heme-dependent and heme-independent components
    E Martin
    Department of Integrative Biology and Pharmacology, Institute of Molecular Medicine, University of Texas Health Science Center at Houston, Houston, TX 77030, USA
    Proc Natl Acad Sci U S A 98:12938-42. 2001
    ..These findings indicate that YC-1 activation of sGC can occur independently of heme, but that activation is substantially increased when the heme moiety is present in the enzyme...
  101. pmc Modulatory effects of nitric oxide-active drugs on the anticonvulsant activity of lamotrigine in an experimental model of partial complex epilepsy in the rat
    Pierangelo Sardo
    Dipartimento di Medicina Sperimentale, Sezione di Fisiologia umana G, Pagano, Universita degli Studi di Palermo, C so Tukory, Palermo, Italy
    BMC Neurosci 8:47. 2007
    ..The epileptic activity of the dentate gyrus was obtained through the repetitive stimulation of the angular bundle and maximal dentate gyrus activation latency, duration and post-stimulus afterdischarge duration were evaluated...

Research Grants101 found, 100 shown here

  1. Therapeutic Modulation of COX-2-induced Immunosuppression in Metastatic RCC
    Brian Rini; Fiscal Year: 2007
    ..This project will have broad implications for the immunoregulation of cancer and how expression and modulation of COX-2 expression influences the immune response to cancer. ..
  2. NO MEDIATED MODIFICATION OF NMDA RECEPTOR DURING HYPOXIA
    Om Mishra; Fiscal Year: 2001
    ..The elucidation of molecular mechanisms of NMDA receptor modification in response to hypoxia will aid in the development of novel preventive strategies for hypoxia-induced brain dysfunction in the newborn. ..
  3. NO-MEDIATED MODIFICATION OF NMDA RECEPTOR DURING HYPOXIA
    Om Mishra; Fiscal Year: 2006
    ..abstract_text> ..
  4. Reconsolidation and extinction processes in the treatment of drug addiction
    Yossef Itzhak; Fiscal Year: 2010
    ..abstract_text> ..
  5. Adolescent Exposure to Psychostimulants: Role of nNOS
    Yossef Itzhak; Fiscal Year: 2007
    ..Results of these studies would provide new information on mechanisms that underlie the development of hypersensitivity to these drugs from adolescence through adulthood. ..
  6. Substituted Amphetamines: NO-Dependent Mechanisms
    Yossef Itzhak; Fiscal Year: 2005
    ....
  7. ITEM BANKING AND CAT FOR QUALITY OF LIFE OUTCOMES
    David Cella; Fiscal Year: 2004
    ..abstract_text> ..
  8. Development of cAMP Biosensor, High Content Imaging, and Functional GLP-1R aSSAYS
    Philip LoGrasso; Fiscal Year: 2010
    ....
  9. Development of cAMP Biosensor, High Content Imaging, and Functional GLP-1R aSSAYS
    Philip LoGrasso; Fiscal Year: 2009
    ....
  10. TUMOR OXYGENATION, VASCULARIZATION, AND RADIORESPONSE
    Bruce Fenton; Fiscal Year: 2007
    ..These results with lead to the more rational and optimal design of effective combined therapies, thereby ultimately accelerating their implementation into clinical protocols. ..
  11. Cannabinoid Regulation of Basal Ganglia Glutamate and GABA
    SCOTT RAWLS; Fiscal Year: 2007
    ..Our outcomes will be a first step in determining whether blocking endocannabinoid inactivation offers any therapeutic advantage over direct activation of cannabinoid receptors with marijuana. ..
  12. Interdisciplinary Center for Male Contraceptive Research and Drug Development
    JOSEPH TASH; Fiscal Year: 2007
    ....
  13. TUMOR OXYGENATION, VASCULARIZATION, AND RADIORESPONSE
    Bruce Fenton; Fiscal Year: 2009
    ..These results with lead to the more rational and optimal design of effective combined therapies, thereby ultimately accelerating their implementation into clinical protocols. ..
  14. TUMOR OXYGENATION, HYPOXIA, AND RADIATION RESPONSE
    Bruce Fenton; Fiscal Year: 1999
    ..A final goal will be to combine oxygen manipulative agents with fractionated radiotherapy, in order to better understand the combined physiological effects and to provide a basis for selecting optimal time points. ..
  15. CO POISONING IN THE CONTEXT OF A REPERFUSION INJURY
    Stephen Thom; Fiscal Year: 1999
    ..Impaired cGMP synthesis will be investigated as a possible mechanism for inhibition of B2 integrin function caused by both nitric oxide and hyperbaric oxygen treatment of CO-poisoned rats. ..
  16. TUMOR OXYGENATION AND RADIATION RESPONSE
    Bruce Fenton; Fiscal Year: 1993
    ....
  17. CO POISONING IN THE CONTEXT OF A REPERFUSION INJURY
    Stephen Thom; Fiscal Year: 2003
    ..The research plan is aimed to test the hypothesis that immune responses and the associated oxidative stress cause neurological injuries. ..
  18. TUMOR OXYGENATION, VASCULARIZATION, AND RADIORESPONSE
    Bruce Fenton; Fiscal Year: 2003
    ..In summary, our primary goals are to determine the fundamental relationships between molecular and pathophysiological changes in disparate tumor models and whether observed differences can be therapeutically exploited. ..
  19. Vascular adhesion protein-1 (VAP-1) as a therapeutic target in stroke
    DALE ALAN PELLIGRINO; Fiscal Year: 2010
    ..The present project utilizes a selective pharmacologic approach that targets a novel protein which appears to be important in the trafficking of all leukocyte subsets and, therefore, may prove to have wide-ranging clinical efficacy. ..
  20. Rapamycin as an Antineoplastic Agent
    Ezra Cohen; Fiscal Year: 2006
    ..At the conclusion of the trial RAPA toxicity and effect on p-S6K will be defined over a range of doses as well as the MTD for use in future studies that will develop this agent. ..
  21. ITEM BANKING AND CAT FOR QUALITY OF LIFE OUTCOMES
    David Cella; Fiscal Year: 2007
    ..We will also monitor treatment/management changes, and evaluate acceptability of computer assessments and the perceived benefits of the recommendations. ..
  22. MID CAREER INVESTIGATOR AWARD
    Joan Schiller; Fiscal Year: 2004
    ....
  23. Nano-Structure Surfaces and Liquid Crystal Analysis
    Joan Schiller; Fiscal Year: 2005
    ..abstract_text> ..
  24. Functional Infrared Imaging Predicts Radiation Mucositis
    Ezra Cohen; Fiscal Year: 2007
    ..Such a tool would have wide applicability in this patient population and would have tremendous impact on their treatment. ..
  25. MECHANISMS OF CUTANEOUS ACTIVE VASODILATION
    Dean Kellogg; Fiscal Year: 2003
    ..In addition intradermal microdialysis will be combined with measurements of bioavailable NO by hemoglobin-trapping to define further how the NO system functions in cutaneous active vasodilation. ..
  26. CCNU in NSCLC Patients with Methylation of the MGMT Gene
    Joan Schiller; Fiscal Year: 2003
    ..abstract_text> ..
  27. Phase I Clinical Trials of Anti-Cancer Agents
    Francis Giles; Fiscal Year: 2007
    ..abstract_text> ..
  28. NO-independent cGMP regulation of vascular remodeling
    DAVID TULIS; Fiscal Year: 2007
    ....
  29. MECHANISMS OF CUTANEOUS ACTIVE VASODILATION
    Dean Kellogg; Fiscal Year: 2007
    ..In addition, intradermal microdialysis will be combined with measurements of bioavailable NO by NO-selective amperometric electrode to define further how the NO system functions in cutaneous active vasodilation. ..
  30. NM-404 A Novel Imaging Agent in Lung Cancer
    Joan Schiller; Fiscal Year: 2002
    ..The results of this exploratory study will provide the preliminary data for a larger study designed to more accurately estimate the predictive power of NM-404 for staging and/or following response to therapy in NSCLC. ..