pyrroles

Summary

Summary: Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.

Top Publications

  1. pmc Overall survival and updated results for sunitinib compared with interferon alfa in patients with metastatic renal cell carcinoma
    Robert J Motzer
    Memorial Sloan Kettering Cancer Center, 1275 York Ave, New York, NY 10021, USA
    J Clin Oncol 27:3584-90. 2009
  2. ncbi Intensive lipid lowering with atorvastatin in patients with stable coronary disease
    John C LaRosa
    State University of New York Health Science Center, Brooklyn, NY 11203, USA
    N Engl J Med 352:1425-35. 2005
  3. ncbi Prognostic factors for overall survival in patients with metastatic renal cell carcinoma treated with vascular endothelial growth factor-targeted agents: results from a large, multicenter study
    Daniel Y C Heng
    FRCPC, Department of Medical Oncology, Tom Baker Cancer Center, University of Calgary, Calgary, Alberta, Canada
    J Clin Oncol 27:5794-9. 2009
  4. ncbi Sunitinib versus interferon alfa in metastatic renal-cell carcinoma
    Robert J Motzer
    Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA
    N Engl J Med 356:115-24. 2007
  5. ncbi Phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) or adalimumab monotherapy versus placebo in patients with active rheumatoid arthritis with an inadequate response to disease-modifying antirheumatic drugs
    Roy Fleischmann
    Metroplex Clinical Research Center and University of Texas Southwestern Medical Center, Dallas, TX 75231, USA
    Arthritis Rheum 64:617-29. 2012
  6. pmc Interleukin-8 mediates resistance to antiangiogenic agent sunitinib in renal cell carcinoma
    Dan Huang
    Laboratory of Cancer Genetics, Laboratory of Computational Biology, Van Andel Research Institute, Grand Rapids, Michigan 49503, USA
    Cancer Res 70:1063-71. 2010
  7. pmc Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis
    Mai Nguyen
    Department of Biochemistry and McGill Cancer Center, McGill University, Montreal, QC, Canada
    Proc Natl Acad Sci U S A 104:19512-7. 2007
  8. ncbi Intensive versus moderate lipid lowering with statins after acute coronary syndromes
    Christopher P Cannon
    Thrombolysis in Myocardial Infarction TIMI Study Group, Cardiovascular Division, Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    N Engl J Med 350:1495-504. 2004
  9. pmc Efficacy, safety, and potential biomarkers of sunitinib monotherapy in advanced hepatocellular carcinoma: a phase II study
    Andrew X Zhu
    Division of Hematology Oncology, Department of Radiology, Massachusetts General Hospital, Boston, MA 02114, USA
    J Clin Oncol 27:3027-35. 2009
  10. ncbi In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship
    Dirk B Mendel
    Preclinical Research and Exploratory Development, SUGEN, Inc, South San Francisco, California 94080, USA
    Clin Cancer Res 9:327-37. 2003

Research Grants

Detail Information

Publications322 found, 100 shown here

  1. pmc Overall survival and updated results for sunitinib compared with interferon alfa in patients with metastatic renal cell carcinoma
    Robert J Motzer
    Memorial Sloan Kettering Cancer Center, 1275 York Ave, New York, NY 10021, USA
    J Clin Oncol 27:3584-90. 2009
    ..Final survival analyses and updated results are reported...
  2. ncbi Intensive lipid lowering with atorvastatin in patients with stable coronary disease
    John C LaRosa
    State University of New York Health Science Center, Brooklyn, NY 11203, USA
    N Engl J Med 352:1425-35. 2005
    ..We prospectively assessed the efficacy and safety of lowering LDL cholesterol levels below 100 mg per deciliter (2.6 mmol per liter) in patients with stable coronary heart disease (CHD)...
  3. ncbi Prognostic factors for overall survival in patients with metastatic renal cell carcinoma treated with vascular endothelial growth factor-targeted agents: results from a large, multicenter study
    Daniel Y C Heng
    FRCPC, Department of Medical Oncology, Tom Baker Cancer Center, University of Calgary, Calgary, Alberta, Canada
    J Clin Oncol 27:5794-9. 2009
    ..There are no robust data on prognostic factors for overall survival (OS) in patients with metastatic renal cell carcinoma (RCC) treated with vascular endothelial growth factor (VEGF) -targeted therapy...
  4. ncbi Sunitinib versus interferon alfa in metastatic renal-cell carcinoma
    Robert J Motzer
    Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA
    N Engl J Med 356:115-24. 2007
    ..Since sunitinib malate has shown activity in two uncontrolled studies in patients with metastatic renal-cell carcinoma, a comparison of the drug with interferon alfa in a phase 3 trial is warranted...
  5. ncbi Phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) or adalimumab monotherapy versus placebo in patients with active rheumatoid arthritis with an inadequate response to disease-modifying antirheumatic drugs
    Roy Fleischmann
    Metroplex Clinical Research Center and University of Texas Southwestern Medical Center, Dallas, TX 75231, USA
    Arthritis Rheum 64:617-29. 2012
    ....
  6. pmc Interleukin-8 mediates resistance to antiangiogenic agent sunitinib in renal cell carcinoma
    Dan Huang
    Laboratory of Cancer Genetics, Laboratory of Computational Biology, Van Andel Research Institute, Grand Rapids, Michigan 49503, USA
    Cancer Res 70:1063-71. 2010
    ..Our results reveal IL-8 as an important contributor to sunitinib resistance in ccRCC and a candidate therapeutic target to reverse acquired or intrinsic resistance to sunitinib in this malignancy...
  7. pmc Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis
    Mai Nguyen
    Department of Biochemistry and McGill Cancer Center, McGill University, Montreal, QC, Canada
    Proc Natl Acad Sci U S A 104:19512-7. 2007
    ..In both cases, this resistance was overcome by obatoclax. These findings support a rational clinical development opportunity for the compound in cancer indications or treatments where MCL-1 contributes to resistance to cell killing...
  8. ncbi Intensive versus moderate lipid lowering with statins after acute coronary syndromes
    Christopher P Cannon
    Thrombolysis in Myocardial Infarction TIMI Study Group, Cardiovascular Division, Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    N Engl J Med 350:1495-504. 2004
    ..Lipid-lowering therapy with statins reduces the risk of cardiovascular events, but the optimal level of low-density lipoprotein (LDL) cholesterol is unclear...
  9. pmc Efficacy, safety, and potential biomarkers of sunitinib monotherapy in advanced hepatocellular carcinoma: a phase II study
    Andrew X Zhu
    Division of Hematology Oncology, Department of Radiology, Massachusetts General Hospital, Boston, MA 02114, USA
    J Clin Oncol 27:3027-35. 2009
    ..To assess the safety and efficacy of sunitinib in patients with advanced hepatocellular carcinoma (HCC) and explore biomarkers for sunitinib response...
  10. ncbi In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship
    Dirk B Mendel
    Preclinical Research and Exploratory Development, SUGEN, Inc, South San Francisco, California 94080, USA
    Clin Cancer Res 9:327-37. 2003
    ..The pharmacokinetic/pharmacodynamic relationship established for SU11248 in these preclinical studies has aided in the design, selection, and evaluation of dosing regimens being tested in human trials...
  11. ncbi SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types
    T A Fong
    SUGEN, Inc, South San Francisco, California 94080, USA
    Cancer Res 59:99-106. 1999
    ..These findings support that pharmacological inhibition of the enzymatic activity of the vascular endothelial growth factor receptor represents a novel strategy for limiting the growth of a wide variety of tumor types...
  12. ncbi Antitumor activity and biomarker analysis of sunitinib in patients with bevacizumab-refractory metastatic renal cell carcinoma
    Brian I Rini
    Department of Solid Tumor Oncology and Urology, Cleveland Clinic Taussig Cancer Institute, 9500 Euclid Avenue, Desk R35, Cleveland, OH 44195, USA
    J Clin Oncol 26:3743-8. 2008
    ..To assess the safety and efficacy of sunitinib in patients with bevacizumab-refractory metastatic renal cell carcinoma (mRCC) and explore biomarkers for sunitinib response...
  13. pmc Induction of autophagy-dependent necroptosis is required for childhood acute lymphoblastic leukemia cells to overcome glucocorticoid resistance
    Laura Bonapace
    Department of Oncology, University Children s Hospital, University of Zurich, Switzerland
    J Clin Invest 120:1310-23. 2010
    ..Together with evidence for a chemosensitizing activity of obatoclax in vivo, our data provide a compelling rationale for clinical translation of this pharmacological approach into treatments for patients with refractory ALL...
  14. ncbi Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial
    George D Demetri
    Ludwig Center at Dana Farber Cancer Institute and Harvard Medical School, Boston, MA 02115, USA
    Lancet 368:1329-38. 2006
    ....
  15. ncbi Sunitinib: from rational design to clinical efficacy
    Laura Q M Chow
    Department of Medical Oncology, University of Colorado Health Sciences Center, Aurora, CO 80045, USA
    J Clin Oncol 25:884-96. 2007
    ....
  16. ncbi Efficacy and safety of tofacitinib, an oral Janus kinase inhibitor, in the treatment of psoriasis: a Phase 2b randomized placebo-controlled dose-ranging study
    K A Papp
    Probity Medical Research, 135 Union Street East, Waterloo, ON N2J 1C4, Canada
    Br J Dermatol 167:668-77. 2012
    ..Tofacitinib is a novel, oral Janus kinase inhibitor under investigation as a potential treatment for plaque psoriasis...
  17. ncbi A phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) versus placebo in combination with background methotrexate in patients with active rheumatoid arthritis and an inadequate response to methotrexate alone
    Joel M Kremer
    Albany Medical College, Albany, New York 12206, USA
    Arthritis Rheum 64:970-81. 2012
    ....
  18. ncbi Statin therapy, LDL cholesterol, C-reactive protein, and coronary artery disease
    Steven E Nissen
    Department of Cardiovascular Medicine, Cleveland Clinic Foundation, Cleveland, OH 44195, USA
    N Engl J Med 352:29-38. 2005
    ..Intensive treatment produced greater reductions in both low-density lipoprotein (LDL) cholesterol and C-reactive protein (CRP), suggesting a relationship between these two biomarkers and disease progression...
  19. ncbi Atorvastatin pretreatment improves outcomes in patients with acute coronary syndromes undergoing early percutaneous coronary intervention: results of the ARMYDA-ACS randomized trial
    Giuseppe Patti
    Department of Cardiovascular Sciences, Campus Bio Medico University, Rome, Italy
    J Am Coll Cardiol 49:1272-8. 2007
    ..This study sought to investigate potential protective effects of atorvastatin in patients with acute coronary syndromes (ACS) undergoing percutaneous coronary intervention (PCI)...
  20. pmc Oxidative stress induces angiogenesis by activating TLR2 with novel endogenous ligands
    Xiaoxia Z West
    Department of Molecular Cardiology, J J Jacobs Center for Thrombosis and Vascular Biology, NB50, The Cleveland Clinic Foundation, 9500 Euclid Avenue, Cleveland, Ohio 44195, USA
    Nature 467:972-6. 2010
    ..Here we show that the end products of lipid oxidation, ω-(2-carboxyethyl)pyrrole (CEP) and other related pyrroles, are generated during inflammation and wound healing and accumulate at high levels in ageing tissues in mice and ..
  21. ncbi An overview of small-molecule inhibitors of VEGFR signaling
    S Percy Ivy
    Investigational Drug Branch, Cancer Therapy Evaluation Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Bethesda, MD, USA
    Nat Rev Clin Oncol 6:569-79. 2009
    ..The on-target effects seem to be mechanistically based and predicted by VEGFR inhibition. Small-molecule inhibitors of angiogenesis are active in a wide variety of malignancies and fill a unique niche for cancer therapeutics...
  22. ncbi Single nucleotide polymorphism associations with response and toxic effects in patients with advanced renal-cell carcinoma treated with first-line sunitinib: a multicentre, observational, prospective study
    Jesus Garcia-Donas
    Hospital Universitario Fundacion Alcorcon, Alcorcon, Spain
    Lancet Oncol 12:1143-50. 2011
    ..Because there are no validated molecular predictors of response or toxicity to sunitinib, we aimed to identify genetic markers predictive of outcome and toxic effects...
  23. ncbi Phase II study of sunitinib as first-line treatment of urothelial cancer patients ineligible to receive cisplatin-based chemotherapy: baseline interleukin-8 and tumor contrast enhancement as potential predictive factors of activity
    J Bellmunt
    Medical Oncology Service, University Hospital del Mar, Barcelona, Spain
    Ann Oncol 22:2646-53. 2011
    ..This trial was designed to assess the activity of sunitinib as first-line treatment in patients with metastatic urothelial cancer ineligible for cisplatin and to explore molecular and imaging variables predictive of clinical benefit...
  24. ncbi Development and characterization of clinically relevant tumor models from patients with renal cell carcinoma
    Jose A Karam
    Department of Urology, University of Texas MD Anderson Cancer Center, Houston, TX, USA
    Eur Urol 59:619-28. 2011
    ..Animal models are instrumental in understanding disease pathophysiology and mechanisms of therapy action and resistance in vivo...
  25. ncbi Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis
    William J Sandborn
    Division of Gastroenterology, University of California San Diego, 9500 Gilman Dr, La Jolla, CA 92093 0956, USA
    N Engl J Med 367:616-24. 2012
    ..These cytokines are integral to lymphocyte activation, function, and proliferation...
  26. ncbi Safety and efficacy of combining sunitinib with bevacizumab + paclitaxel/carboplatin in non-small cell lung cancer
    Mark A Socinski
    Lineberger Comprehensive Cancer Center, University of North Carolina, Chapel Hill, North Carolina, USA
    J Thorac Oncol 5:354-60. 2010
    ....
  27. pmc Phase III randomized trial of sunitinib versus capecitabine in patients with previously treated HER2-negative advanced breast cancer
    Carlos H Barrios
    PUCRS School of Medicine, Centro de Pesquisa em Oncologia, Jardim Botanico, Porto Alegre, RS, 90610 000, Brazil
    Breast Cancer Res Treat 121:121-31. 2010
    ..51%). The relative dose intensity was lower with sunitinib than capecitabine (73 vs. 95%). Based on these efficacy and safety results, sunitinib should not be used as monotherapy for patients with ABC...
  28. pmc Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor
    Michael C Heinrich
    Division of Hematology Oncology, Department of Medicine and Cell and Developmental Biology, Portland Veterans Affairs Medical Center and Oregon Health and Science University Cancer Institute, Portland, OR 97239, USA
    J Clin Oncol 26:5352-9. 2008
    ..We evaluated the impact of primary and secondary kinase genotype on sunitinib activity...
  29. ncbi Carboxyethylpyrrole protein adducts and autoantibodies, biomarkers for age-related macular degeneration
    Xiaorong Gu
    Department of Chemistry, Case Western Reserve University, 10900 Euclid Avenue, Cleveland, Ohio 44106, USA
    J Biol Chem 278:42027-35. 2003
    ..These results suggest that together CEP immunoreactivity and autoantibody titer may have diagnostic utility in predicting AMD susceptibility...
  30. pmc Phase I dose finding studies of obatoclax (GX15-070), a small molecule pan-BCL-2 family antagonist, in patients with advanced solid tumors or lymphoma
    Jimmy J Hwang
    Lombardi Cancer Center, Georgetown Medical Center, 3800 Reservoir Road NW, Washington, DC 20007 2113, USA
    Clin Cancer Res 16:4038-45. 2010
    ..The two studies, GX001 and GX005, evaluated the safety and tolerability of weekly 1-hour and 3-hour infusions of obatoclax, respectively...
  31. ncbi The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo
    Joel M Kremer
    Albany Medical College, Albany, New York, USA
    Arthritis Rheum 60:1895-905. 2009
    ....
  32. ncbi Primary prevention of cardiovascular disease with atorvastatin in type 2 diabetes in the Collaborative Atorvastatin Diabetes Study (CARDS): multicentre randomised placebo-controlled trial
    Helen M Colhoun
    EURODIAB, Department of Epidemiology and Public Health, Royal Free and University College Medical School, London, UK
    Lancet 364:685-96. 2004
    ..We aimed to assess the effectiveness of atorvastatin 10 mg daily for primary prevention of major cardiovascular events in patients with type 2 diabetes without high concentrations of LDL-cholesterol...
  33. ncbi Clinical evaluation of continuous daily dosing of sunitinib malate in patients with advanced gastrointestinal stromal tumour after imatinib failure
    S George
    Center for Sarcoma and Bone Oncology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Eur J Cancer 45:1959-68. 2009
    ....
  34. pmc Sunitinib inhibition of Stat3 induces renal cell carcinoma tumor cell apoptosis and reduces immunosuppressive cells
    Hong Xin
    Divisions of Cancer Immunotherapeutics and Tumor Immunology, Beckman Research Institute and City of Hope Comprehensive Cancer Center, Duarte, California, USA
    Cancer Res 69:2506-13. 2009
    ..These results suggest that Stat3 activity is important for RCC response to sunitinib, and Stat3 inhibition permits the direct proapoptotic activity of sunitinib on tumor cells and positive effects on tumor immunologic microenvironment...
  35. ncbi Randomized trial of atorvastatin for reduction of myocardial damage during coronary intervention: results from the ARMYDA (Atorvastatin for Reduction of MYocardial Damage during Angioplasty) study
    Vincenzo Pasceri
    Interventional Cardiology Unit, San Filippo Neri Hospital, Rome, Italy
    Circulation 110:674-8. 2004
    ..Observational studies have suggested that statins may lower the risk of procedural myocardial injury. The aim of our study was to confirm this hypothesis in a randomized study...
  36. ncbi Pyrrolobenzodiazepine dimers: novel sequence-selective, DNA-interactive, cross-linking agents with activity against Gram-positive bacteria
    Tsveta Hadjivassileva
    School of Pharmacy, 29 39 Brunswick Square, London WC1N 1AX, UK
    J Antimicrob Chemother 56:513-8. 2005
    ..We investigated the antibacterial activity of three dimers, SJG-136, DRG-16 and ELB-21, which differ in the structure of the PBD monomeric unit and the length of the linker region between the two identical PBD monomers...
  37. ncbi Safety and efficacy of sunitinib for metastatic renal-cell carcinoma: an expanded-access trial
    Martin E Gore
    Royal Marsden Hospital NHS Trust, London, UK
    Lancet Oncol 10:757-63. 2009
    ..The primary objective of this trial was to provide sunitinib on a compassionate-use basis to trial-ineligible patients with RCC from countries where regulatory approval had not been granted...
  38. ncbi Increase in circulating endothelial progenitor cells by statin therapy in patients with stable coronary artery disease
    M Vasa
    Division of Molecular Cardiology, Department of Internal Medicine IV, University of Frankfurt, Theodor-Stern-Kai 7, Frankfurt, Germany
    Circulation 103:2885-90. 2001
    ..Given the well-established role of EPCs of participating in repair after ischemic injury, stimulation of EPCs by statins may contribute to the clinical benefit of statin therapy in patients with CAD...
  39. pmc Genome-wide association of lipid-lowering response to statins in combined study populations
    Mathew J Barber
    Department of Human Genetics, University of Chicago, Chicago, Illinois, United States of America
    PLoS ONE 5:e9763. 2010
    ..To identify single nucleotide polymorphisms (SNPs) contributing to this variation, we performed a combined analysis of genome-wide association (GWA) results from three trials of statin efficacy...
  40. ncbi Phase I study of obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist, in patients with advanced chronic lymphocytic leukemia
    Susan M O'Brien
    M D Anderson Cancer Center, Houston, TX 77030 7305 USA
    Blood 113:299-305. 2009
    ..Further evaluation in less heavily pretreated patients and in combination with other therapeutic agents is warranted. This trial has been registered with http://clinicaltrials.gov under identifier NCT00600964...
  41. ncbi Molecular basis for sunitinib efficacy and future clinical development
    Sandrine Faivre
    Service Inter Hospitalier de Cancérologie SIHC Beaujon Bichat and RayLab, Hopital Beaujon, APHP and Denis Diderot University, 100 Boulevard du General Leclerc, 92118 Clichy Cedex, France
    Nat Rev Drug Discov 6:734-45. 2007
    ....
  42. ncbi Total synthesis of (+/-)-marinopyrrole A and its library as potential antibiotic and anticancer agents
    Chunwei Cheng
    Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education, West China School of Pharmacy, State Key Laboratory of Biotherapy, Sichuan University, Chengdu 610041, China
    J Comb Chem 12:541-7. 2010
    ..The method that we have developed has made it possible to generate diverse analogues based on structurally novel marinopyrroles for study of potential antibiotic and anticancer activities...
  43. ncbi Sequential FDG-PET/CT as a biomarker of response to Sunitinib in metastatic clear cell renal cancer
    Irfan Kayani
    Department of Nuclear Medicine, University College Hospital, London, UK
    Clin Cancer Res 17:6021-8. 2011
    ..Three sequential scans were conducted to determine whether the timing of the investigation was relevant...
  44. pmc Cyclic pyrrole-imidazole polyamides targeted to the androgen response element
    David M Chenoweth
    Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, California 91125, USA
    J Am Chem Soc 131:7182-8. 2009
    ..We find that cyclic Py-Im polyamides 1-3 bind DNA with exceptionally high affinities and regulate the expression of AR target genes in cell culture studies, from which we infer that the cycle is cell permeable...
  45. pmc Enhancing the cellular uptake of Py-Im polyamides through next-generation aryl turns
    Jordan L Meier
    Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA
    Nucleic Acids Res 40:2345-56. 2012
    ..Overall this provides a step forward for controlling the intracellular concentration of Py-Im polyamides that will prove valuable for future applications in which biological potency is essential...
  46. pmc Multicenter, phase II trial of sunitinib in previously treated, advanced non-small-cell lung cancer
    Mark A Socinski
    Multidisciplinary Thoracic Oncology Program, Lineberger Comprehensive Cancer Center, University of North Carolina, CB 7305, Chapel Hill, NC 27599, USA
    J Clin Oncol 26:650-6. 2008
    ....
  47. pmc Atorvastatin as a potential anti-malarial drug: in vitro synergy in combinational therapy with quinine against Plasmodium falciparum
    Véronique Parquet
    Unité de Recherche en Biologie et Epidémiologie Parasitaires Unité de Recherche pour les Maladies Infectieuses et Tropicales Emergentes UMR 6236, Institut de Medecine Tropicale du Service de Sante des Armees, Marseille, France
    Malar J 9:139. 2010
    ....
  48. pmc Hypertension as a biomarker of efficacy in patients with metastatic renal cell carcinoma treated with sunitinib
    Brian I Rini
    Department of Solid Tumor Oncology, Cleveland Clinic Taussig Cancer Institute, Cleveland, OH 44195, USA
    J Natl Cancer Inst 103:763-73. 2011
    ..We evaluated the association of sunitinib-induced HTN with antitumor efficacy and HTN-associated adverse events in patients with metastatic renal cell carcinoma...
  49. pmc Direct and differential suppression of myeloid-derived suppressor cell subsets by sunitinib is compartmentally constrained
    Jennifer S Ko
    Department of Immunology, Taussig Cancer Institute, and Glickman Urological Institute, Cleveland Clinic, Cleveland, Ohio, USA
    Cancer Res 70:3526-36. 2010
    ....
  50. ncbi Preclinical studies of the pan-Bcl inhibitor obatoclax (GX015-070) in multiple myeloma
    Suzanne Trudel
    Hematology Oncology, Princess Margaret Hospital, Toronto, ON, Canada
    Blood 109:5430-8. 2007
    ..Taken together, these studies describe a novel BH3 mimic with selectivity for Mcl-1, and support the therapeutic application of GX015-070 for diverse neoplasias including multiple myeloma...
  51. pmc Multiple circulating proangiogenic factors induced by sunitinib malate are tumor-independent and correlate with antitumor efficacy
    John M L Ebos
    Sunnybrook Health Sciences Centre, Molecular and Cellular Biology Research, 2075 Bayview Avenue, Toronto, Ontario, Canada
    Proc Natl Acad Sci U S A 104:17069-74. 2007
    ..They may also be relevant to drug-associated toxicities, drug resistance, and observed rapid tumor (re)growth seen after cessation of therapy...
  52. ncbi Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor
    Paul S Changelian
    Immunology Group, Department of Antibacterials and Immunology, Pfizer Global Researchand Development, Groton, CT 06340, USA
    Science 302:875-8. 2003
    ..On the basis of these preclinical results, we believe JAK3 blockade by CP-690,550 has potential for therapeutically desirable immunosuppression in human organ transplantation and in other clinical settings...
  53. ncbi Surgical management of advanced gastrointestinal stromal tumors after treatment with targeted systemic therapy using kinase inhibitors
    Chandrajit P Raut
    Department of Surgery, Brigham and Women s Hospital and Dana Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA
    J Clin Oncol 24:2325-31. 2006
    ..To assess the role of surgery in multimodality management of GISTs, we studied postoperative outcomes in patients treated with targeted kinase inhibitors for advanced GIST...
  54. ncbi SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models
    Aaron J Schueneman
    Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    Cancer Res 63:4009-16. 2003
    ..Moreover, inhibition of angiogenesis well beyond radiation therapy may be a promising treatment paradigm for refractory human neoplasms...
  55. pmc Next generation hairpin polyamides with (R)-3,4-diaminobutyric acid turn unit
    Christian Dose
    Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, California 91125, USA
    J Am Chem Soc 130:6859-66. 2008
    ....
  56. ncbi Antiangiogenic effect by SU5416 is partly attributable to inhibition of Flt-1 receptor signaling
    Takashi Itokawa
    Department of Medical Biochemistry, Graduate School of Medical Sciences, Kyushu University, Fukuoka 812 8582, Japan
    Mol Cancer Ther 1:295-302. 2002
    ..Cell migration of vascular endothelial cells and monocytic cells through Flt-1, thus, might play a key role in VEGF-induced tumor angiogenesis in concert with KDR/Flk-1...
  57. pmc The marinopyrroles, antibiotics of an unprecedented structure class from a marine Streptomyces sp
    Chambers C Hughes
    Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California San Diego, La Jolla, California 92093 0204, USA
    Org Lett 10:629-31. 2008
    ..The marinopyrroles possess potent antibiotic activities against methicillin-resistant Staphylococcus aureus...
  58. ncbi Molecular pathobiology of gastrointestinal stromal sarcomas
    Christopher L Corless
    Department of Pathology, Oregon Health and Science University Cancer Institute, Portland, OR 97239, USA
    Annu Rev Pathol 3:557-86. 2008
    ....
  59. ncbi Sunitinib plus paclitaxel versus bevacizumab plus paclitaxel for first-line treatment of patients with advanced breast cancer: a phase III, randomized, open-label trial
    Nicholas J Robert
    Virginia Cancer Specialists, US Oncology, Fairfax, VA, USA
    Clin Breast Cancer 11:82-92. 2011
    ....
  60. ncbi Metastatic renal carcinoma: evaluation of antiangiogenic therapy with dynamic contrast-enhanced CT
    Laure S Fournier
    Department of Radiology, Assistance Publique Hopitaux de Paris, Hopital Europeen Georges Pompidou, 20 rue Leblanc, Paris 75015, France FR
    Radiology 256:511-8. 2010
    ....
  61. ncbi A riboswitch selective for the queuosine precursor preQ1 contains an unusually small aptamer domain
    Adam Roth
    Howard Hughes Medical Institute, USA
    Nat Struct Mol Biol 14:308-17. 2007
    ..Relatively compact RNA structures can therefore serve effectively as metabolite receptors to regulate gene expression...
  62. ncbi SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo
    Anne Marie O'Farrell
    Preclinical Research and Exploratory Development, SUGEN, South San Francisco, CA 94080, USA
    Blood 101:3597-605. 2003
    ..These results suggest that further exploration of SU11248 activity in AML patients is warranted...
  63. ncbi Atorvastatin in patients with type 2 diabetes mellitus undergoing hemodialysis
    Christoph Wanner
    Division of Nephrology, Department of Medicine, University of Wurzburg, Wurzburg, Germany
    N Engl J Med 353:238-48. 2005
    ..However, the benefit of statins in such patients receiving hemodialysis, who are at high risk for cardiovascular disease and death, has not been examined...
  64. pmc Phase II study of continuous daily sunitinib dosing in patients with previously treated advanced non-small cell lung cancer
    S Novello
    Department of Clinical and Biological Sciences, Thoracic Oncology Unit, University of Turin, Orbassano, Turin, Italy
    Br J Cancer 101:1543-8. 2009
    ..Sunitinib malate (SUTENT) has promising single-agent activity given on Schedule 4/2 (4 weeks on treatment followed by 2 weeks off treatment) in advanced non-small cell lung cancer (NSCLC)...
  65. ncbi Improved pain, physical functioning and health status in patients with rheumatoid arthritis treated with CP-690,550, an orally active Janus kinase (JAK) inhibitor: results from a randomised, double-blind, placebo-controlled trial
    J H Coombs
    Pfizer Inc, Ann Arbor, Michigan, USA
    Ann Rheum Dis 69:413-6. 2010
    ....
  66. pmc Vascular endothelial growth factor is a key mediator in the development of T cell priming and its polarization to type 1 and type 17 T helper cells in the airways
    You Sun Kim
    Department of Life Science, Postech Biotech Center, Pohang University of Science and Technology, Pohang, Republic of Korea
    J Immunol 183:5113-20. 2009
    ..These findings indicate that VEGF produced by LPS plays a key role in activation of naive T cells and subsequent polarization to Th1 and Th17 cells...
  67. pmc Lapatinib and obatoclax kill breast cancer cells through reactive oxygen species-dependent endoplasmic reticulum stress
    Nichola Cruickshanks
    Department of Neurosurgery, School of Medicne, Virginia Commonwealth University, Richmond, VA 23298 0035, USA
    Mol Pharmacol 82:1217-29. 2012
    ..Our data indicate that mitochondrial function plays an essential role in cell killing by lapatinib and obatoclax, as well as radiosensitization by this drug combination...
  68. ncbi Assessing tumor response and detecting recurrence in metastatic renal cell carcinoma on targeted therapy: importance of size and attenuation on contrast-enhanced CT
    Andrew Dennis Smith
    Imaging Institute, Cleveland Clinic, 9500 Euclid Ave, Hb6, Cleveland, OH 44195, USA
    AJR Am J Roentgenol 194:157-65. 2010
    ....
  69. ncbi Sorafenib as third- or fourth-line treatment of advanced gastrointestinal stromal tumour and pretreatment including both imatinib and sunitinib, and nilotinib: A retrospective analysis
    M Montemurro
    Centre Pluridisciplinaire d Oncologie, University Hospital Lausanne, Lausanne, Switzerland
    Eur J Cancer 49:1027-31. 2013
    ..Smaller trials in this setting suggested activity for sorafenib, a multikinase inhibitor of receptor tyrosine kinases and RAF serine/threonine kinases...
  70. ncbi Inhibition of activated receptor tyrosine kinases by Sunitinib induces growth arrest and sensitizes melanoma cells to Bortezomib by blocking Akt pathway
    Andree Yeramian
    Pathology Group, Department of Pathology and Molecular Genetics, Hospital Universitari Arnau de Vilanova, University of Lleida, IRB Lleida, Lleida, Spain
    Int J Cancer 130:967-78. 2012
    ..Altogether, our results suggest that melanoma cells harboring an activated RTK may be clinically responsive to pharmacologic RTK inhibition by Sunitinib, and a strategy combining Sunitinib and Bortezomib, may provide therapeutic benefit...
  71. ncbi Preclinical evaluation of the tyrosine kinase inhibitor SU11248 as a single agent and in combination with "standard of care" therapeutic agents for the treatment of breast cancer
    Tinya J Abrams
    Preclinical Research and Experimental Development, SUGEN, Inc, South San Francisco, CA 94080, USA
    Mol Cancer Ther 2:1011-21. 2003
    ..05). These results demonstrate that SU11248 is effective in preclinical breast cancer models and suggest that it may be useful in the treatment of breast cancer in the clinic...
  72. pmc Single-dose pharmacokinetic and toxicity analysis of pyrrole-imidazole polyamides in mice
    Timothy W Synold
    Department of Molecular Pharmacology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
    Cancer Chemother Pharmacol 70:617-25. 2012
    ..In this study, two hairpin polyamides with demonstrated activity against androgen receptor signaling in cell culture were administered to mice to characterize their pharmacokinetic properties...
  73. pmc Surgery after treatment with imatinib and/or sunitinib in patients with metastasized gastrointestinal stromal tumors: is it worthwhile?
    Ronald Tielen
    Department of Surgical Oncology, Radboud University Nijmegen Medical Center, Nijmegen, The Netherlands
    World J Surg Oncol 10:111. 2012
    ..In other patients, surgery is performed to remove (focal) progressive or symptomatic lesions. The impact and long-term results of surgery after systemic therapy have not been clearly defined...
  74. pmc Consequence of dose scheduling of sunitinib on host immune response elements and vaccine combination therapy
    Benedetto Farsaci
    Laboratory of Tumor Immunology and Biology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MA 20892, USA
    Int J Cancer 130:1948-59. 2012
    ..In combination with immunotherapies, sunitinib treatment should precede vaccine, to precondition the immune system, to maximize the response to vaccine-mediated immune enhancement...
  75. ncbi Phase II trial of continuous once-daily dosing of sunitinib as first-line treatment in patients with metastatic renal cell carcinoma
    Carlos H Barrios
    PUCRS School of Medicine, Porto Alegre, Brazil
    Cancer 118:1252-9. 2012
    ..In this prospective, multicenter, phase II study, we evaluated the activity of continuous once-daily dosing with sunitinib 37.5 mg as first-line mRCC treatment...
  76. ncbi A phase I study of the pan bcl-2 family inhibitor obatoclax mesylate in patients with advanced hematologic malignancies
    Aaron D Schimmer
    Ontario Cancer Institute, Princess Margaret Hospital, Toronto, Ontario, Canada
    Clin Cancer Res 14:8295-301. 2008
    ..Therefore, we conducted a phase I clinical trial of the small-molecule pan-Bcl-2 inhibitor, obatoclax mesylate, in patients with refractory leukemia and myelodysplasia to assess its safety and define its optimal dose...
  77. ncbi Sunitinib enhances antitumor effects against chemotherapy-resistant bladder cancer through suppression of ERK1/2 phosphorylation
    Ario Takeuchi
    Department of Urology, Graduate School of Medical Sciences, Kyushu University, Fukuoka, Japan
    Int J Oncol 40:1691-6. 2012
    ..On the other hand, these findings provided the rationale for combination therapy with sunitinib and immune-based cancer therapy for advanced malignancies to prevent the occurrence of rebound phenomena...
  78. ncbi Inhibition of autophagy enhances sunitinib-induced cytotoxicity in rat pheochromocytoma PC12 cells
    Tatsuhiko Ikeda
    Department of Endocrine Surgery, Graduate School of Comprehensive Human Sciences, University of Tsukuba, Japan
    J Pharmacol Sci 121:67-73. 2013
    ..Inhibition of autophagy may be a promising therapeutic option for improving the anti-tumor effect of sunitinib...
  79. ncbi The novel role of tyrosine kinase inhibitor in the reversal of immune suppression and modulation of tumor microenvironment for immune-based cancer therapies
    Junko Ozao-Choy
    Departments of Gene and Cell Medicine, Mount Sinai School of Medicine, New York, New York, USA
    Cancer Res 69:2514-22. 2009
    ..These data suggest that sunitinib can be used to reverse immune suppression and as a potentially useful adjunct for enhancing the efficacy of immune-based cancer therapy for advanced malignancies...
  80. ncbi Sunitinib mediates reversal of myeloid-derived suppressor cell accumulation in renal cell carcinoma patients
    Jennifer S Ko
    Department of Immunology, Cleveland Clinic Lerner Research Institute, Cleveland, OH, USA
    Clin Cancer Res 15:2148-57. 2009
    ..Several factors pivotal to the accumulation of MDSC are targeted by the tyrosine kinase inhibitor, sunitinib. The effect of sunitinib on MDSC-mediated immunosuppression in RCC patients has been investigated...
  81. pmc Choi response criteria for early prediction of clinical outcome in patients with metastatic renal cell cancer treated with sunitinib
    A A M van der Veldt
    Department of Medical Oncology, VU University Medical Center, De Boelelaan 1117, Amsterdam, The Netherlands
    Br J Cancer 102:803-9. 2010
    ..Because sunitinib can induce extensive necrosis in metastatic renal cell cancer (mRCC), we examined whether criteria defined by Choi might be valuable to predict early sunitinib efficacy...
  82. ncbi Metastatic renal cell carcinoma treated with sunitinib: early evaluation of treatment response using dynamic contrast-enhanced ultrasonography
    Nathalie Lassau
    Imaging Department, Service of Biostatistics and Epidemiology, and Medical Department, Institut Gustave Roussy, Villejuif Cedex, France
    Clin Cancer Res 16:1216-25. 2010
    ....
  83. ncbi Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor
    Robert Roskoski
    Blue Ridge Institute for Medical Research, Horse Shoe, NC 28742, USA
    Biochem Biophys Res Commun 356:323-8. 2007
    ..Both sunitinib and imatinib bind reversibly to the ATP binding site of their target kinases and thereby inhibit their catalytic activity...
  84. pmc Modifications at the C-terminus to improve pyrrole-imidazole polyamide activity in cell culture
    Claire S Jacobs
    Division of Chemistry and Chemical Engineering, The California Institute of Technology, 1200 E California Boulevard, Mail Code 164 30, Pasadena, California 91125, USA
    J Med Chem 52:7380-8. 2009
    ....
  85. ncbi Efficacy of sunitinib and sorafenib in metastatic papillary and chromophobe renal cell carcinoma
    Toni K Choueiri
    Dana Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA
    J Clin Oncol 26:127-31. 2008
    ..The activity of sunitinib and sorafenib in non-clear cell histologies has not been evaluated...
  86. ncbi Sequential use of sorafenib and sunitinib in advanced renal-cell carcinoma (RCC): an Italian multicentre retrospective analysis of 189 patient cases
    Camillo Porta
    IRCCS San Matteo University Hospital Foundation, Pavia, Italy
    BJU Int 108:E250-7. 2011
    ..To conduct a retrospective, multicentre, cohort analysis to assess the sequential use of the tyrosine kinase inhibitors (TKIs) sorafenib and sunitinib...
  87. ncbi Inhibition of MMP-9 transcription and suppression of tumor metastasis by pyrrole-imidazole polyamide
    Xiaofei Wang
    Life Science, Advanced Research Institute for the Sciences and Humanities, Nihon University, Tokyo, Japan
    Cancer Sci 101:759-66. 2010
    ..Our results suggest that this PI polyamide, which targets the MMP-9 gene promoter, can be a novel MMP-9 down-regulating molecule for antimetastasis...
  88. ncbi Synthesis and biological properties of highly sequence-specific-alkylating N-methylpyrrole-N-methylimidazole polyamide conjugates
    Gengo Kashiwazaki
    Department of Chemistry, Graduate School of Science, Kyoto University, Kitashirakawa Oiwakecho, Sakyo ku, Kyoto 606 8502, Japan
    J Med Chem 55:2057-66. 2012
    ..The intravenous administration of each liposomal conjugate in water yielded tumor-suppressing effects specifically toward DU145 cells and not A549 cells, which was pertinent to cytotoxicity...
  89. ncbi An expeditious synthesis of N-substituted pyrroles via microwave-induced iodine-catalyzed reactions under solventless conditions
    Debasish Bandyopadhyay
    Department of Chemistry, The University of Texas Pan American, Edinburg, TX 78541, USA
    Molecules 15:2520-5. 2010
    An expeditious synthesis of N-substituted pyrroles has been developed by reacting 2,5-dimethoxy tetrahydrofuran and several amines using a microwave-induced molecular iodine-catalyzed reaction under solventless conditions.
  90. pmc Health-related quality of life in patients with metastatic renal cell carcinoma treated with sunitinib vs interferon-alpha in a phase III trial: final results and geographical analysis
    D Cella
    Robert H Lurie Comprehensive Cancer Center of Northwestern University, Chicago, IL 60611, USA
    Br J Cancer 102:658-64. 2010
    ..We report the final health-related quality of life (HRQoL) results...
  91. ncbi Identification of dual mTORC1 and mTORC2 inhibitors in melanoma cells: prodigiosin vs. obatoclax
    M Espona-Fiedler
    Cancer Cell Biology Research Group, Department of Pathology and Experimental Therapeutics, Faculty of Medicine, University of Barcelona, E 08907 Barcelona, Spain
    Biochem Pharmacol 83:489-96. 2012
    ..These results provide new data to understand the mechanism of action of these molecules, and provide new structural data that will allow the development of more specific mTOR inhibitors for cancer treatment...
  92. pmc Mechanisms of sunitinib resistance in gastrointestinal stromal tumors harboring KITAY502-3ins mutation: an in vitro mutagenesis screen for drug resistance
    Tianhua Guo
    Departments of Pathology, Medicine, and Surgery, Memorial Sloan Kettering Cancer Center, Sloan Kettering Institute, New York, NY 10021, USA
    Clin Cancer Res 15:6862-70. 2009
    ..The clinical benefit of sunitinib is genotype-dependent in regards to both primary and secondary mutations, with GIST patients harboring the KIT(AY502-3ins) exon 9 mutation being the most sensitive...
  93. ncbi Site-specific fluorescent probing of RNA molecules by unnatural base-pair transcription for local structural conformation analysis
    Yasushi Hikida
    TagCyx Biotechnologies, Yokohama, Kanagawa, Japan
    Nat Protoc 5:1312-23. 2010
    ..This is the first protocol for RNA transcript preparation with fluorescent labeling at a desired position. The procedure for s-containing RNA preparation takes about 2-3 d...
  94. ncbi First-line treatment of advanced breast cancer with sunitinib in combination with docetaxel versus docetaxel alone: results of a prospective, randomized phase III study
    Jonas Bergh
    Karolinska Institutet and University Hospital, 171 76 Stockholm, Sweden
    J Clin Oncol 30:921-9. 2012
    ..To investigate whether sunitinib plus docetaxel improves clinical outcomes for patients with human epidermal growth factor receptor 2 (HER2)/neu-negative advanced breast cancer (ABC) versus docetaxel alone...
  95. pmc Activation of Wnt signaling arrests effector differentiation in human peripheral and cord blood-derived T lymphocytes
    Sujatha Muralidharan
    Department of Pathology and Immunology, Baylor College of Medicine, Houston, TX 77030, USA
    J Immunol 187:5221-32. 2011
    ..The arrest in T cell differentiation induced by Wnt signaling might have relevant clinical applications such as to preserve the naive T cell compartment in Ag-specific T cells generated ex vivo for adoptive T cell immunotherapy...
  96. ncbi Comparison of RECIST and Choi criteria for computed tomographic response evaluation in patients with advanced gastrointestinal stromal tumor treated with sunitinib
    O Dudeck
    Department of Radiology, HELIOS Clinic Berlin Buch, Berlin, Germany
    Ann Oncol 22:1828-33. 2011
    ..Controversies exist about computed tomography (CT) response evaluation criteria for patients with gastrointestinal stromal tumor (GIST)...
  97. ncbi Effect of statin and fibrate treatment on inflammation in type 2 diabetes. A randomized, cross-over study
    Ana María Wagner
    Endocrinology Department, Hospital de la Santa Creu i Sant Pau, Barcelona, Spain
    Diabetes Res Clin Pract 93:e25-8. 2011
    ..Both lipid-lowering drugs had positive, complementary and additive effects on inflammatory markers, which were closely related to baseline inflammatory status...
  98. ncbi Lipid-altering efficacy and safety of ezetimibe/simvastatin versus atorvastatin in patients with hypercholesterolemia and the metabolic syndrome (from the VYMET study)
    Jennifer G Robinson
    University of Iowa College of Public Health, Iowa City, Iowa, USA
    Am J Cardiol 103:1694-702. 2009
    ..In conclusion, ezetimibe/simvastatin was more likely to result in lipid treatment end points than atorvastatin and was generally well tolerated at the doses compared in our patients...
  99. ncbi Reduction of low-density lipoprotein cholesterol in patients with coronary heart disease and metabolic syndrome: analysis of the Treating to New Targets study
    Prakash Deedwania
    Veterans Affairs Central California Healthcare System and University of California San Francisco School of Medicine, San Francisco, CA, USA
    Lancet 368:919-28. 2006
    ....
  100. ncbi Rapid, direct effects of statin treatment on arterial redox state and nitric oxide bioavailability in human atherosclerosis via tetrahydrobiopterin-mediated endothelial nitric oxide synthase coupling
    Charalambos Antoniades
    Department of Cardiovascular Medicine, University of Oxford, John Radcliffe Hospital OX3 9DU, Oxford, UK
    Circulation 124:335-45. 2011
    ..We examined the direct effects of atorvastatin on tetrahydrobiopterin-mediated endothelial nitric oxide (NO) synthase coupling in patients with coronary artery disease...
  101. ncbi Nilotinib in the treatment of advanced gastrointestinal stromal tumours resistant to both imatinib and sunitinib
    M Montemurro
    University Hospital Lausanne, Cancer Center, Lausanne, Switzerland
    Eur J Cancer 45:2293-7. 2009
    ..Nilotinib is active in GIST resistant to both imatinib and sunitinib. These results warrant further investigation of nilotinib in GIST...

Research Grants62

  1. PREPROSTAGLANDIN ENDOPEROXIDES
    ROBERT GERD SALOMON; Fiscal Year: 2013
    ..Some of these, e.g., carboxyethyl- pyrroles (CEPs), promote the angiogenesis involved in choroidal neovascularization, the primary cause of severe vision ..
  2. Au/Pt Catalysis in the Synthesis of Elaborate N-Heterocycles: Methodology Develop
    Liming Zhang; Fiscal Year: 2013
    ..g., pyridines, pyrroles, oxazoles, pyrroline and indoles)...
  3. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
    ..2-furanones, 2-pyrrolinones, benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and phenols...
  4. N-Heterocycles from Azides through Rhodium-Catalyzed Nitrenoid Transfer
    TOM GREGORY DRIVER; Fiscal Year: 2012
    ..that vinyl- and aryl azides are valuable precursors for the transition metal-catalyzed synthesis of indoles, pyrroles, and carbazoles...
  5. The Synthesis and Bioassay of Novel Pyrroles
    John T Gupton; Fiscal Year: 2012
    ..have established and are developing allows for rapid construction of highly substituted and highly functionalized pyrroles. This methodology also allows for great structural diversity for structure activity relationship (SAR) studies, ..
  6. Novel Direct Approaches Toward Bioactive Heterocycles
    Vladimir Gevorgyan; Fiscal Year: 2013
    ..to the investigation and development of novel cycloisomerization approaches toward monocyclic and fused furans, pyrroles, and thiophenes, and to the development of cascade migration/cyclization methodologies en route to highly ..
  7. Photoredox Catalysis Applications to Bioactive Compounds
    COREY STEPHENSON; Fiscal Year: 2013
    ..of a series of indolizidine alkaloids using photoredox- mediated, stereocontrolled radical cyclization onto pyrroles, and achieve the synthesis of actinophyllic acid using a photoredox-catalyzed fragment coupling strategy...
  8. GORDON RESEARCH CONFERENCE ON PYRROLES
    SAMUEL BEALE; Fiscal Year: 1990
    ..for a Conference Support Grant to support the Gordon Research Conference on the Chemistry and Biology of Pyrroles, which will be held on 23-28 July, 1990 at the Brewster Academy, Wolfeboro, New Hampshire...
  9. DEVELOPING AN UNDERSTANDING OF ASYMMETRIC INDUCTION
    Patrick J Walsh; Fiscal Year: 2010
    ..We have also developed several new routes to pyranones, furanosidic aldehydes, furans, and pyrroles. These medicinally important heterocycles can be prepared with high enantioselectivities using our methods...
  10. Alkynyliodonium Salts and Derived Diyls in Synthesis
    Ken Feldman; Fiscal Year: 2009
    ..chemistry with downstream olefin metathesis transformations for the efficient synthesis of highly functionalized pyrroles. Successful execution of this work will lead to assignment of the absolute stereochemistry of both species, and, ..
  11. FUSED HETEROCYCLES IN NATURAL PRODUCT SYNTHESIS
    Gordon Gribble; Fiscal Year: 2001
    ..and novel cycloaddition chemistry of these fused heterocyclic ring systems: furo[3,4-b]indoles, furo[3,4-b]pyrroles, and pyrrolo[3,4b]indoles, the second of which is an unknown ring system...
  12. TOXIC MODELS OF NEUROFIBRILLARY PATHOLOGY
    Douglas Anthony; Fiscal Year: 1991
    ..series the neurofibrillary pathology results from cyclization of the Gamma-diketone with lysyl residues to form pyrroles, autoxidation of the unstable pyrrolyl residues to form reactive intermediates, and subsequent attack of the ..
  13. POLYAMINES AND MONOCROTALINE PNEUMOTOXICITY
    JACK OLSON; Fiscal Year: 1992
    ..related to perivascular edema formation; (2) Cultured endothelial cells will be used to determine if MCT- derived pyrroles directly provoke polyamine dependent endothelial injury; and (3) Perfused lungs isolated from MCT-treated rats ..
  14. COLLAGEN CROSSLINKING BY THE MAILLARD REACTIOIN IN AGING
    Vincent Monnier; Fiscal Year: 2004
    ..establishing the structure of the first fluorescent cross- link of the Maillard reaction in vivo, the role of pyrroles in protein aging by glucose, the biological significance of glycoxidation in aging and age- related diseases, ..
  15. SYNTHESIS AND BIOASSAY OF HIGHLY FUNCTIONALIZED PYRROLES
    JOHN GUPTON; Fiscal Year: 1992
    ..One important class of compounds for which vinamidinium salts might serve as precursors are pyrroles and related compounds...
  16. SYNTHESIS AND EVALUATION OF NOVEL COCAINE ANALOGS
    Huw Davies; Fiscal Year: 2002
    ..A novel synthetic strategy to tropanes based on the reaction between vinylcarbenoids and pyrroles has led to a series of extremely potent cocaine analogs...
  17. Synthesis of Pyrrole-Based Non-traditional Cannabinoids
    LEA PADGETT; Fiscal Year: 2004
    ..observation that certain aminoalkylindoles exhibit cannabinoid receptor affinity, several series of indoles and pyrroles have been designed and tested...
  18. Total Synthesis of the Antitumor Agent Asparagamine A
    CHRISTOPHER SINZ; Fiscal Year: 2002
    ..MacMillan has recently developed the first organocatalytic, asymmetric Michael additions of pyrroles with alpha, beta- unsaturated aldehydes...
  19. Single Agents with Designed Combination Chemotherapy Potential
    Aleem Gangjee; Fiscal Year: 2010
    ..abstract_text> ..
  20. Antitumor Antimitotics That Reverse Tumor Resistance
    Aleem Gangjee; Fiscal Year: 2010
    ..The study will also further define the mechanism of action of the novel series and could afford agents for clinical use. ..
  21. Novel, P. jirovecii Specific Antipneumocystis Agents
    Aleem Gangjee; Fiscal Year: 2009
    ..These agents could be used alone or in combination to treat PCP thus providing novel agents against a new target. ..
  22. Alpha Folate Receptor Mediated GARFTase Inhibitors as Selective Antitumor Agents
    Aleem Gangjee; Fiscal Year: 2010
    ....
  23. Novel Single, Dual and Multitargeted Inhibitors of RTKs
    Aleem Gangjee; Fiscal Year: 2007
    ..abstract_text> ..
  24. Third Generation Antiopportunistic Agents
    Aleem Gangjee; Fiscal Year: 2003
    ..Screening against tuberculosis (NIAID) and tumor cells in culture (NCI) is also proposed. ..
  25. STRUCTURE BASED ANALOGS AS ANTIOPPORTUNISTIC AGENTS
    Aleem Gangjee; Fiscal Year: 2001
    ..The analogues synthesized will also be submitted for screening against tuberculosis (NIAID) parasitic diseases (WHO) and tumor cells in culture (NCI). ..
  26. NOVEL NONINDUCIBLE THYMIDYLATE SYNTHASE INHIBITORS
    Aleem Gangjee; Fiscal Year: 2004
    ....
  27. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  28. CLINICAL TRIALS AND MENTORING IN ONCOLOGY RESEARCH
    Robert Motzer; Fiscal Year: 2003
    ..One recently joined staff at MSKCC in the Genito-urinary Section. Mentoring of clinical trials is extended beyond fellowship to junior faculty members. ..
  29. Molecular Basis Of Renal Cell Carcinoma Response to SU11428
    Robert J Motzer; Fiscal Year: 2011
    ..These tumor and cell line-based studies lay a foundation for further molecular studies aimed at understanding the sensitivity/resistance of RCC to SU11248. ..
  30. SARS-CoV S Protein Receptor-binding Domain-based Vaccines
    Shibo Jiang; Fiscal Year: 2010
    ..The long-term goal of this project is to develop highly effective and safe subunit vaccines for protecting at-risk populations from SARS-CoV infection or bioterrorism attack. ..
  31. ITEM BANKING AND CAT FOR QUALITY OF LIFE OUTCOMES
    David Cella; Fiscal Year: 2008
    ..We will also monitor treatment/management changes, and evaluate acceptability of computer assessments and the perceived benefits of the recommendations. ..
  32. Therapeutic Modulation of COX-2-induced Immunosuppression in Metastatic RCC
    Brian Rini; Fiscal Year: 2008
    ..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. [unreadable] [unreadable] [unreadable]..
  33. Rational Design of HIV Fusion Inhibitors Targeting gp41
    Shibo Jiang; Fiscal Year: 2010
    ..Therefore, this research is relevant to public health. ..
  34. Anti-HIV-1 Composite Cellulose Acetate Phthalate Film
    Shibo Jiang; Fiscal Year: 2008
    ....
  35. SYNTHESIS OF CANNABINOIDS, ANALOGUES AND METABOLITES
    John Huffman; Fiscal Year: 2009
    ..agonist properties and/or to provide additional insight into the manner in which cannabimimetic indoles and pyrroles interact with each receptor. Rigid indole analogues will be prepared and their pharmacology evaluated...
  36. NEW DEVELOPMENTS IN ORGANOCOPPER CHEMISTRY
    R Dieter; Fiscal Year: 2004
    ..The proposed synthetic routes to pyrrolidine aza sugars will develop the potential synthetic power of alpha-aminoalkylcuprate chemistry. ..
  37. Synthesis of Cannabinoid Receptor Ligands
    John Huffman; Fiscal Year: 2005
    ..agonist properties and/or provide additional insight into the manner in which cannabimimetic indoles and pyrroles interact with each receptor...
  38. HUMAN AND ANIMAL RETINAS--CELL BIOLOGY OF THE IPM
    Joe Hollyfield; Fiscal Year: 2001
    ....
  39. Inhibitors of Hedgehog Signaling For Brain Cancer Chemotherapy
    JEFFREY D contact WINKLER; Fiscal Year: 2010
    ..The studies outlined herein therefore hold the promise of developing important new tools in cancer biology and new drug candidates for the treatment of brain cancers. ..
  40. Oligopyrrole-based Anion Binding Agents
    Jonathan L Sessler; Fiscal Year: 2010
    ..abstract_text> ..
  41. ASYMMETRIC SYNTHESIS OF VANCOMYCIN ANTIBIOTICS
    David Evans; Fiscal Year: 2001
    ..During the course of this project we intend to confirm (correct) the absolute stereochemical assignments of the principal members of this family by total synthesis. ..
  42. Electronic Diary Assessment of Pain in Juvenile Arthritis
    Laura E Schanberg; Fiscal Year: 2010
    ..Finally, the study can serve as a catalyst for future research aimed at advancing medical and psychological knowledge of pain in other pediatric medical populations. ..
  43. Allenic [2 + 2 + 1] Reactions Enabling Syntheses of Natural Products with 7-Membe
    Kay M Brummond; Fiscal Year: 2010
    ..Grayanotoxin is an important molecular tool for deciphering the mechanism for gating functions of the sodium ion channels. ..
  44. IMAGING APOPTOSIS IN VIVO WITH TECHNETIUM 99M ANNEXIN
    Francis Blankenberg; Fiscal Year: 2001
    ..abstract_text> ..
  45. The Effect of Statins on Skeletal Muscle Function
    PAUL DAVIS THOMPSON; Fiscal Year: 2010
    ....
  46. Chemoprevention of Tobacco Related Cancer in Animals
    Michael Pereira; Fiscal Year: 2004
    ....
  47. Mechanisms of Stress-Induced Changes in Behavior
    Matthew Cooper; Fiscal Year: 2006
    ..The experiments in the current proposal will provide valuable information on the neurobiological mechanisms underlying stress-related disorders. [unreadable] [unreadable]..
  48. Novel Therapies for Resistant FSGS
    Howard Trachtman; Fiscal Year: 2006
    ..The infrastructure that is established for the performance of this R21/R33 project should prove useful for the efficient assessment of additional novel therapies that will be developed in the future for patients with primary FSGS. ..
  49. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
  50. IMAGING APOPTOSIS IN VIVO WITH TECHNETIUM 99M ANNEXIN
    Francis Blankenberg; Fiscal Year: 2007
    ..Completion of this proposal will aid in the design and planning of clinical trials that will study the use of serial annexin V imaging as a non-invasive marker of cellular injury and therapeutic efficacy. ..
  51. IGF-I and its binding proteins in vascular smooth muscle cells
    Cunming Duan; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  52. Vision Research Infrastructure Development Grant
    Joe Hollyfield; Fiscal Year: 2008
    ..Their research activities will be enhanced by these services and their collaborative interactions will be strengthened and extended through this program. [unreadable] [unreadable]..
  53. HSP27 in Kidney Epithelial to Mesenchymal Transformation
    Arjang Djamali; Fiscal Year: 2008
    ..Overexpression of HSP27 will be obtained by recombinant virus-mediated HSP27 gene transfer. This proposal would allow us to determine whether HSP27 overexpression can prevent/delay EMT. ..
  54. Human monoclonal antibody therapy for HUS
    Howard Trachtman; Fiscal Year: 2004
    ..abstract_text> ..
  55. Revision of ACR Classification Criteria for Systemic Lupus Erythematosus
    Michelle Petri; Fiscal Year: 2007
    ..This project will lead to updated, validated SLE classification criteria that can be immediately used by both industry and academic clinical trials. ..
  56. Phase II Study of 44Gy from 131I-81C6 for CNS Tumors
    David Reardon; Fiscal Year: 2004
    ..To further define the toxicity of this approach and Specific Aim 3.To determine the impact of this therapy on quality of life. ..
  57. Interferon Regulation in Systemic Lupus
    Lionel B Ivashkiv; Fiscal Year: 2010
    ..These experiments will yield insight into the molecular pathogenesis of SLE and identify novel therapeutic approaches to manipulatecytokine activity in SLE at the level of signal transduction. ..
  58. Biomarkers and Outcomes in the Diabetes Prevention Program
    Ronald B Goldberg; Fiscal Year: 2010
    ....
  59. Synthesis of Polyketides and Terpenes
    David A Evans; Fiscal Year: 2010
    ..As a consequence, organic synthesis is a critical discipline that continues to have an important impact on the fields of both medicine and biology. ..
  60. scVEGF Targeted Radiotherapy of Mammary and Colonic Cancer
    FRANCIS GERARD BLANKENBERG; Fiscal Year: 2010
    ..Successful completion of our proposal will give the needed preclinical data for pursuing scVEGF targeted radiotherapy in other models and ultimately clinical applications. ..
  61. LOWERING HOMOCYSTEINE TO REDUCE MYOCARDIAL ISCHEMIA
    Ahmed Tawakol; Fiscal Year: 2006
    ....