triazoles

Summary

Top Publications

  1. ncbi The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes
    Daniel J Drucker
    Samuel Lunenfeld Research Institute, Mount Sinai Hospital, University of Toronto, Toronto, Ontario, Canada
    Lancet 368:1696-705. 2006
  2. pmc Targeting MYC dependence in cancer by inhibiting BET bromodomains
    Jennifer A Mertz
    Constellation Pharmaceuticals, Inc, Cambridge, MA 02142, USA
    Proc Natl Acad Sci U S A 108:16669-74. 2011
  3. pmc Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity
    Patrick Dorr
    Discovery Biology, Pfizer Global Research and Development Sandwich Laboratories, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 49:4721-32. 2005
  4. ncbi Voriconazole versus amphotericin B for primary therapy of invasive aspergillosis
    Raoul Herbrecht
    Département d Hématologie et d Oncologie, Hopital de Hautepierre, Strasbourg, France
    N Engl J Med 347:408-15. 2002
  5. ncbi Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy
    Weiwen Ying
    Synta Pharmaceuticals Corp, 45 Hartwell Avenue, Lexington, MA 02421, USA
    Mol Cancer Ther 11:475-84. 2012
  6. ncbi Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes
    James Mu
    Department of Metabolic Disorders, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Diabetes 55:1695-704. 2006
  7. ncbi Efficacy and safety of exenatide once weekly versus sitagliptin or pioglitazone as an adjunct to metformin for treatment of type 2 diabetes (DURATION-2): a randomised trial
    Richard M Bergenstal
    International Diabetes Center at Park Nicollet, Minneapolis, MN 55416, USA
    Lancet 376:431-9. 2010
  8. ncbi Adherence to initial adjuvant anastrozole therapy among women with early-stage breast cancer
    Ann H Partridge
    Dana Farber Cancer Institute, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02115, USA
    J Clin Oncol 26:556-62. 2008
  9. pmc Genetic deletion or pharmacological inhibition of dipeptidyl peptidase-4 improves cardiovascular outcomes after myocardial infarction in mice
    Meghan Sauvé
    Samuel Lunenfeld Research Institute, Mt Sinai Hospital, University of Toronto, Toronto, Ontario, Canada
    Diabetes 59:1063-73. 2010
  10. ncbi Liraglutide versus sitagliptin for patients with type 2 diabetes who did not have adequate glycaemic control with metformin: a 26-week, randomised, parallel-group, open-label trial
    Richard E Pratley
    Diabetes and Metabolism Translational Medicine Unit, University of Vermont College of Medicine, Burlington, VT, USA
    Lancet 375:1447-56. 2010

Detail Information

Publications293 found, 100 shown here

  1. ncbi The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes
    Daniel J Drucker
    Samuel Lunenfeld Research Institute, Mount Sinai Hospital, University of Toronto, Toronto, Ontario, Canada
    Lancet 368:1696-705. 2006
    ..However, long-term clinical studies are needed to determine the benefits of targeting the incretin axis for the treatment of type 2 diabetes...
  2. pmc Targeting MYC dependence in cancer by inhibiting BET bromodomains
    Jennifer A Mertz
    Constellation Pharmaceuticals, Inc, Cambridge, MA 02142, USA
    Proc Natl Acad Sci U S A 108:16669-74. 2011
    ..These findings demonstrate that pharmacologic inhibition of MYC is achievable through targeting BET bromodomains. Such inhibitors may have clinical utility given the widespread pathogenetic role of MYC in cancer...
  3. pmc Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity
    Patrick Dorr
    Discovery Biology, Pfizer Global Research and Development Sandwich Laboratories, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 49:4721-32. 2005
    ..Clinical trials are ongoing to further investigate the potential of using maraviroc for the treatment of HIV-1 infection and AIDS...
  4. ncbi Voriconazole versus amphotericin B for primary therapy of invasive aspergillosis
    Raoul Herbrecht
    Département d Hématologie et d Oncologie, Hopital de Hautepierre, Strasbourg, France
    N Engl J Med 347:408-15. 2002
    ..Voriconazole is a broad-spectrum triazole that is active against aspergillus species. We conducted a randomized trial to compare voriconazole with amphotericin B for primary therapy of invasive aspergillosis...
  5. ncbi Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy
    Weiwen Ying
    Synta Pharmaceuticals Corp, 45 Hartwell Avenue, Lexington, MA 02421, USA
    Mol Cancer Ther 11:475-84. 2012
    ....
  6. ncbi Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes
    James Mu
    Department of Metabolic Disorders, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Diabetes 55:1695-704. 2006
    ..These findings suggest that DPP-4 inhibitors may offer long-lasting efficacy in the treatment of type 2 diabetes by modifying the courses of the disease...
  7. ncbi Efficacy and safety of exenatide once weekly versus sitagliptin or pioglitazone as an adjunct to metformin for treatment of type 2 diabetes (DURATION-2): a randomised trial
    Richard M Bergenstal
    International Diabetes Center at Park Nicollet, Minneapolis, MN 55416, USA
    Lancet 376:431-9. 2010
    ....
  8. ncbi Adherence to initial adjuvant anastrozole therapy among women with early-stage breast cancer
    Ann H Partridge
    Dana Farber Cancer Institute, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02115, USA
    J Clin Oncol 26:556-62. 2008
    ..Previous research evaluating adherence to tamoxifen therapy among women with early-stage breast cancer has revealed adherence estimates ranging from 25% to 96%. No previous studies have focused on adherence to adjuvant aromatase inhibitors...
  9. pmc Genetic deletion or pharmacological inhibition of dipeptidyl peptidase-4 improves cardiovascular outcomes after myocardial infarction in mice
    Meghan Sauvé
    Samuel Lunenfeld Research Institute, Mt Sinai Hospital, University of Toronto, Toronto, Ontario, Canada
    Diabetes 59:1063-73. 2010
    ..We examined whether chemical inhibition or genetic elimination of DPP-4 activity affects cardiovascular function in normoglycemic and diabetic mice after experimental myocardial infarction...
  10. ncbi Liraglutide versus sitagliptin for patients with type 2 diabetes who did not have adequate glycaemic control with metformin: a 26-week, randomised, parallel-group, open-label trial
    Richard E Pratley
    Diabetes and Metabolism Translational Medicine Unit, University of Vermont College of Medicine, Burlington, VT, USA
    Lancet 375:1447-56. 2010
    ....
  11. ncbi Efficacy and safety of sitagliptin when added to insulin therapy in patients with type 2 diabetes
    T Vilsbøll
    Diabetes Research Division, Department of Internal Medicine F, Gentofte Hospital, University of Copenhagen, Copenhagen, Denmark
    Diabetes Obes Metab 12:167-77. 2010
    ..To evaluate the efficacy and tolerability of sitagliptin when added to insulin therapy alone or in combination with metformin in patients with type 2 diabetes...
  12. ncbi Maraviroc versus efavirenz, both in combination with zidovudine-lamivudine, for the treatment of antiretroviral-naive subjects with CCR5-tropic HIV-1 infection
    David A Cooper
    University of New South Wales, Sydney, Australia
    J Infect Dis 201:803-13. 2010
    ..The MERIT (Maraviroc versus Efavirenz in Treatment-Naive Patients) study compared maraviroc and efavirenz, both with zidovudine-lamivudine, in antiretroviral-naive patients with R5 human immunodeficiency virus type 1 (HIV-1) infection...
  13. ncbi Phase II randomized study of neoadjuvant everolimus plus letrozole compared with placebo plus letrozole in patients with estrogen receptor-positive breast cancer
    Jose Baselga
    Medical Oncology Department, Vall d Hebron University Hospital, P Vall d Hebron, Barcelona, Spain
    J Clin Oncol 27:2630-7. 2009
    ..This study explored whether sensitivity to letrozole was enhanced with the oral mTOR inhibitor, everolimus (RAD001)...
  14. pmc Targeting MYCN in neuroblastoma by BET bromodomain inhibition
    Alexandre Puissant
    Department of Pediatric Oncology, Dana Farber Cancer Institute, Boston, Massachusetts 02215, USA
    Cancer Discov 3:308-23. 2013
    ..BET inhibition conferred a significant survival advantage in 3 in vivo neuroblastoma models, providing a compelling rationale for developing BET bromodomain inhibitors in patients with neuroblastoma...
  15. ncbi Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 10-year analysis of the ATAC trial
    Jack Cuzick
    Cancer Research UK, Centre for Epidemiology, Mathematics, and Statistics, Wolfson Institute of Preventive Medicine, Queen Mary School of Medicine and Dentistry, University of London, London, UK
    Lancet Oncol 11:1135-41. 2010
    ..In this analysis, we assess the long-term outcomes after a median follow-up of 120 months...
  16. pmc Small-molecule inhibition of BRDT for male contraception
    Martin M Matzuk
    Department of Pathology and Immunology, Baylor College of Medicine, Houston, TX 77030, USA
    Cell 150:673-84. 2012
    ..These data establish a new contraceptive that can cross the blood:testis boundary and inhibit bromodomain activity during spermatogenesis, providing a lead compound targeting the male germ cell for contraception...
  17. ncbi Efficacy and tolerability of sitagliptin monotherapy in elderly patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial
    Nir Barzilai
    Merck Research Laboratories, Rahway, NJ 07065 0900, USA
    Curr Med Res Opin 27:1049-58. 2011
    ..Type 2 diabetes in the elderly is an important and insufficiently studied public health problem. This study evaluated sitagliptin monotherapy in patients with type 2 diabetes aged ≥ 65 years...
  18. pmc HIV-1 escape from the CCR5 antagonist maraviroc associated with an altered and less-efficient mechanism of gp120-CCR5 engagement that attenuates macrophage tropism
    Michael Roche
    Centers for Virology, Monash University, Australia
    J Virol 85:4330-42. 2011
    ....
  19. ncbi Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels after an oral glucose tolerance test in patients with type 2 diabetes
    Gary A Herman
    Merck Research Laboratories, Experimental Medicine, Rahway, New Jersey 07065, USA
    J Clin Endocrinol Metab 91:4612-9. 2006
    ..The degree of DPP-4 inhibition and the level of active incretin augmentation required for glucose lowering efficacy after an oral glucose tolerance test (OGTT) were evaluated...
  20. ncbi DPP-4 inhibition by sitagliptin improves the myocardial response to dobutamine stress and mitigates stunning in a pilot study of patients with coronary artery disease
    Philip A Read
    Department of Medicine, Cardiovascular Medicine, University of Cambridge, Addenbrooke s Hospital, Cambridge, United Kingdom
    Circ Cardiovasc Imaging 3:195-201. 2010
    ....
  21. ncbi Interaction of A2A adenosine and D2 dopamine receptors modulates corticostriatal glutamatergic transmission
    Alessandro Tozzi
    Clinica Neurologia, Universita di Perugia, Ospedale S Maria della Misericordia, 06156 Perugia, Italy
    Neuropharmacology 53:783-9. 2007
    ..These results suggest that A2A and D2 receptors converge in the control of corticostriatal glutamatergic transmission by exerting an opposite function...
  22. ncbi European guidelines for antifungal management in leukemia and hematopoietic stem cell transplant recipients: summary of the ECIL 3--2009 update
    J Maertens
    Department of Hematology, Leukemia and Stem Cell Transplantation Unit, University Hospitals Leuven, Campus Gasthuisberg, Leuven, Belgium
    Bone Marrow Transplant 46:709-18. 2011
    ....
  23. pmc The oral dipeptidyl peptidase-4 inhibitor sitagliptin increases circulating endothelial progenitor cells in patients with type 2 diabetes: possible role of stromal-derived factor-1alpha
    Gian Paolo Fadini
    Department of Clinical and Experimental Medicine, School of Medicine, University of Padova, Padova, Italy
    Diabetes Care 33:1607-9. 2010
    ..Because SDF-1alpha is a substrate of dipeptidyl-peptidase-4 (DPP-4), we investigated whether the DPP-4 inhibitor sitagliptin modulates EPC levels in type 2 diabetic patients...
  24. ncbi Safety and efficacy of sitagliptin in patients with type 2 diabetes and chronic renal insufficiency
    J C N Chan
    Chinese University of Hong Kong, Shatin, Hong Kong, Special Administrative Region, China
    Diabetes Obes Metab 10:545-55. 2008
    ..The efficacy of sitagliptin in this patient population was also assessed...
  25. pmc Invasive aspergillosis in patients with acute myeloid leukemia: a SEIFEM-2008 registry study
    Livio Pagano
    M D Istituto di Ematologia, Universita Cattolica del Sacro Cuore, Largo Francesco Vito, 1 I 00168 Roma, Italia
    Haematologica 95:644-50. 2010
    ..The aim of this study was to evaluate prognostic factors, treatments and outcome of invasive aspergillosis in patients with acute myeloid leukemia based on data collected in a registry...
  26. ncbi Prognostic value of Ki67 expression after short-term presurgical endocrine therapy for primary breast cancer
    Mitch Dowsett
    Academic Department of Biochemistry, 4th Floor, Wallace Wing, The Royal Marsden Hospital, Fulham Road, London SW3 6 JJ, UK
    J Natl Cancer Inst 99:167-70. 2007
    ....
  27. ncbi Trastuzumab plus anastrozole versus anastrozole alone for the treatment of postmenopausal women with human epidermal growth factor receptor 2-positive, hormone receptor-positive metastatic breast cancer: results from the randomized phase III TAnDEM study
    Bella Kaufman
    Chaim Sheba Medical Center, Tel Hashomer, Israel
    J Clin Oncol 27:5529-37. 2009
    ..TAnDEM is the first randomized phase III study to combine a hormonal agent and trastuzumab without chemotherapy as treatment for human epidermal growth factor receptor 2 (HER2)/hormone receptor-copositive metastatic breast cancer (MBC)...
  28. ncbi Effects of exenatide versus sitagliptin on postprandial glucose, insulin and glucagon secretion, gastric emptying, and caloric intake: a randomized, cross-over study
    Ralph A DeFronzo
    University of Texas Health Science Center, Department of Medicine, Diabetes Division MSC 7886, 7703 Floyd Curl Drive, San Antonio, TX 78229 3900, USA
    Curr Med Res Opin 24:2943-52. 2008
    ..This study evaluated the effects of exenatide, a GLP-1 receptor agonist, and sitagliptin, a DPP-4 inhibitor, on 2-h postprandial glucose (PPG), insulin and glucagon secretion, gastric emptying, and caloric intake in T2D patients...
  29. pmc Randomized phase II neoadjuvant comparison between letrozole, anastrozole, and exemestane for postmenopausal women with estrogen receptor-rich stage 2 to 3 breast cancer: clinical and biomarker outcomes and predictive value of the baseline PAM50-based int
    Matthew J Ellis
    Siteman Cancer Center, Washington University in St Louis, 660 South Euclid Avenue, St Louis, MO 63110, USA
    J Clin Oncol 29:2342-9. 2011
    ..To study this treatment option, responses to three AIs were compared in a randomized phase II neoadjuvant trial designed to select agents for phase III investigations...
  30. ncbi Sitagliptin augments protective effects of GLP-1 against advanced glycation end product receptor axis in endothelial cells
    Y Ishibashi
    Department of Pathophysiology and Therapeutics of Diabetic Vascular Complications, Kurume University School of Medicine, Kurume, Japan
    Horm Metab Res 43:731-4. 2011
    ..Sitagliptin may work as a vasoprotecitve agent in diabetes by blocking the AGE-RAGE axis...
  31. ncbi The effect of initial therapy with the fixed-dose combination of sitagliptin and metformin compared with metformin monotherapy in patients with type 2 diabetes mellitus
    C Reasner
    Texas Diabetes Unit, University of Texas, San Antonio, TX 78260, USA
    Diabetes Obes Metab 13:644-52. 2011
    ..This study was conducted to compare the glycaemic efficacy and safety of initial combination therapy with the fixed-dose combination of sitagliptin and metformin versus metformin monotherapy in drug-naive patients with type 2 diabetes...
  32. pmc Comparison of vildagliptin twice daily vs. sitagliptin once daily using continuous glucose monitoring (CGM): crossover pilot study (J-VICTORIA study)
    Masaya Sakamoto
    Division of Diabetes, Metabolism and Endocrinology, Department of Internal Medicine, Jikei University School of Medicine, 3 25 8 Nishi shinbashi, Minato ku, Tokyo, Japan
    Cardiovasc Diabetol 11:92. 2012
    ..No previous studies have compared the DPP-4 inhibitors vildagliptin and sitagliptin in terms of blood glucose levels using continuous glucose monitoring (CGM) and cardiovascular parameters...
  33. ncbi Efficacy and safety of sitagliptin and metformin as initial combination therapy and as monotherapy over 2 years in patients with type 2 diabetes
    D Williams-Herman
    Merck Research Laboratories, Rahway, NJ 07065, USA debora
    Diabetes Obes Metab 12:442-51. 2010
    ..To assess the 104-week efficacy and safety of sitagliptin and metformin as initial combination therapy and as monotherapy in patients with type 2 diabetes and inadequate glycaemic control (HbA(1c) 7.5-11%) on diet and exercise...
  34. ncbi Deferasirox reduces iron overload significantly in nontransfusion-dependent thalassemia: 1-year results from a prospective, randomized, double-blind, placebo-controlled study
    Ali T Taher
    American University of Beirut, Beirut, Lebanon
    Blood 120:970-7. 2012
    ..8%), and diarrhea (n = 6; 3.6%). This is the first randomized study showing that iron chelation with deferasirox significantly reduces iron overload in NTDT patients with a frequency of overall adverse events similar to placebo...
  35. pmc V3 determinants of HIV-1 escape from the CCR5 inhibitors Maraviroc and Vicriviroc
    Reem Berro
    Department of Microbiology and Immunology, Weill Medical College of Cornell University, New York, NY 10065, USA
    Virology 427:158-65. 2012
    ..In summary, VVC and MVC trigger the evolution of distinct HIV-1 resistance patterns in V3...
  36. pmc Allosteric antagonism of insect odorant receptor ion channels
    Patrick L Jones
    Department of Biological Sciences, Vanderbilt University, Nashville, Tennessee, United States of America
    PLoS ONE 7:e30304. 2012
    ..In an effort to identify additional Orco modulators, we have investigated the structure/activity relationships around VUAA1...
  37. pmc Gibberellin regulates Arabidopsis seed germination via RGL2, a GAI/RGA-like gene whose expression is up-regulated following imbibition
    Sorcheng Lee
    Institute of Molecular Agrobiology, National University of Singapore, Singapore 117604
    Genes Dev 16:646-58. 2002
    ..Furthermore, as RGL2 expression is imbibition inducible, RGL2 may function as an integrator of environmental and endogenous cues to control seed germination...
  38. pmc A maraviroc-resistant HIV-1 with narrow cross-resistance to other CCR5 antagonists depends on both N-terminal and extracellular loop domains of drug-bound CCR5
    John C Tilton
    Department of Microbiology, University of Pennsylvania, 301C Johnson Pavilion, 3610 Hamilton Walk, Philadelphia, PA 19104, USA
    J Virol 84:10863-76. 2010
    ....
  39. ncbi Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes
    P Aschner
    Javeriana University and Colombian Diabetes Association, Bogota, Colombia
    Diabetes Obes Metab 12:252-61. 2010
    ..To compare the efficacy and safety of monotherapy with sitagliptin and metformin in treatment-naïve patients with type 2 diabetes...
  40. ncbi A dipeptidyl peptidase-4 inhibitor, des-fluoro-sitagliptin, improves endothelial function and reduces atherosclerotic lesion formation in apolipoprotein E-deficient mice
    Junichi Matsubara
    Department of Cardiovascular Medicine, Faculty of Life Sciences, Graduate School of Medical Sciences, Kumamoto University, Kumamoto, Japan
    J Am Coll Cardiol 59:265-76. 2012
    ..The aim of this study was to investigate the antiatherogenic effects of the dipeptidyl peptidase-4 inhibitor, des-fluoro-sitagliptin (DFS)...
  41. ncbi Population-based V3 genotypic tropism assay: a retrospective analysis using screening samples from the A4001029 and MOTIVATE studies
    Rachel A McGovern
    BC Centre for Excellence in HIV AIDS, St Paul s Hospital, Vancouver, British Columbia, Canada
    AIDS 24:2517-25. 2010
    ..This analysis retrospectively examined the performance of population-based sequence analysis of HIV-1 env V3-loop to predict coreceptor tropism...
  42. ncbi Phase III study of letrozole versus tamoxifen as first-line therapy of advanced breast cancer in postmenopausal women: analysis of survival and update of efficacy from the International Letrozole Breast Cancer Group
    Henning Mouridsen
    Rigshospitalet, Copenhagen, Denmark
    J Clin Oncol 21:2101-9. 2003
    ..To analyze overall survival (OS) and update efficacy data for letrozole versus tamoxifen as first-line therapy in postmenopausal women with locally advanced or metastatic breast cancer...
  43. ncbi Superior efficacy of letrozole versus tamoxifen as first-line therapy for postmenopausal women with advanced breast cancer: results of a phase III study of the International Letrozole Breast Cancer Group
    H Mouridsen
    Rigshospitalet, Copenhagen, Denmark
    J Clin Oncol 19:2596-606. 2001
    ..CONCLUSION: Letrozole was significantly superior to tamoxifen in TTP, TTF, ORR, and clinical benefit rate. Our results support its use as first-line endocrine therapy in postmenopausal women with advanced breast cancer...
  44. ncbi Efficacy of short-term monotherapy with maraviroc, a new CCR5 antagonist, in patients infected with HIV-1
    Gerd Fatkenheuer
    Department of Internal Medicine, Division of Infectious Diseases, Haus 11, University of Cologne, Joseph Stelzmann Strasse 9, D 50924 Cologne, Germany
    Nat Med 11:1170-2. 2005
    ..6 log(10) copies/ml at all twice daily doses >or=100 mg. These results provide proof of concept that CCR5 antagonism is a viable antiretroviral therapeutic approach...
  45. ncbi Dual inhibition of mTOR and estrogen receptor signaling in vitro induces cell death in models of breast cancer
    Anne Boulay
    Novartis Institutes for BioMedical Research Basel, Oncology Research, Novartis Pharma AG, Basel, Switzerland
    Clin Cancer Res 11:5319-28. 2005
    ..The role of the mTOR pathway in estrogen-driven proliferation and effects of combining RAD001 and letrozole were examined in vitro in two breast cancer models...
  46. pmc Reduced maximal inhibition in phenotypic susceptibility assays indicates that viral strains resistant to the CCR5 antagonist maraviroc utilize inhibitor-bound receptor for entry
    Mike Westby
    Globel Research and Development, Pfizer Ltd, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom
    J Virol 81:2359-71. 2007
    ..This hypothesis was further corroborated by the observation that a high concentration of maraviroc blocks the activity of aplaviroc against maraviroc-resistant virus...
  47. ncbi Efficacy and safety of sitagliptin added to ongoing metformin and pioglitazone combination therapy in a randomized, placebo-controlled, 26-week trial in patients with type 2 diabetes
    Vivian Fonseca
    Tulane University Medical Center, New Orleans, LA, USA
    J Diabetes Complications 27:177-83. 2013
    ..5% and ≤11%)...
  48. ncbi Tamoxifen and anastrozole as a sequencing strategy: a randomized controlled trial in postmenopausal patients with endocrine-responsive early breast cancer from the Austrian Breast and Colorectal Cancer Study Group
    Peter C Dubsky
    Medical University of Vienna, Austria
    J Clin Oncol 30:722-8. 2012
    ....
  49. ncbi Design, synthesis and biological evaluation of mannosyl triazoles as FimH antagonists
    Oliver Schwardt
    Institute of Molecular Pharmacy, Pharmacenter, University of Basel, Klingelbergstrasse 50, CH 4056 Basel, Switzerland
    Bioorg Med Chem 19:6454-73. 2011
    ..Furthermore, to address the druglikeness of this new class of FimH antagonists, selected pharmacokinetic parameters, which are critical for oral bioavailability (lipophilicity, solubility, and membrane permeation), were determined...
  50. ncbi Regulation of ingestive behaviors in the rat by GSK1521498, a novel micro-opioid receptor-selective inverse agonist
    Diane M Ignar
    Metabolic Diseases Department, GlaxoSmithKline, Research Triangle Park, North Carolina, USA
    J Pharmacol Exp Ther 339:24-34. 2011
    ..In conclusion, GSK1521498 is a potent, MOR-selective inverse agonist that modulates the hedonic aspects of ingestion and, therefore, could represent a pharmacological treatment for obesity and binge-eating disorders...
  51. pmc Identification of new agonists and antagonists of the insect odorant receptor co-receptor subunit
    Sisi Chen
    Department of Molecular and Cellular Pharmacology, University of Miami Miller School of Medicine, Miami, Florida, United States of America
    PLoS ONE 7:e36784. 2012
    ..We have explored the chemical space around the VUAA1 structure in order to identify new Orco ligands...
  52. ncbi Safety and efficacy of treatment with sitagliptin or glipizide in patients with type 2 diabetes inadequately controlled on metformin: a 2-year study
    T Seck
    Merck Research Laboratories, Rahway, NJ, USA
    Int J Clin Pract 64:562-76. 2010
    ..To evaluate the 2-year safety and efficacy of adding sitagliptin or glipizide to ongoing metformin in patients with type 2 diabetes...
  53. pmc Inhibition of opioid transmission at the μ-opioid receptor prevents both food seeking and binge-like eating
    Chiara Giuliano
    Behavioral and Clinical Neuroscience Institute and Department of Experimental Psychology, University of Cambridge, Cambridge, UK
    Neuropsychopharmacology 37:2643-52. 2012
    ....
  54. ncbi Effect of sitagliptin on glucose control in adult patients with Type 1 diabetes: a pilot, double-blind, randomized, crossover trial
    S L Ellis
    Barbara Davis Center for Childhood Diabetes, University of Colorado Denver, Aurora, CO 80045, USA
    Diabet Med 28:1176-81. 2011
    ..This study evaluates the clinical implications of sitagliptin in adult patients with Type 1 diabetes...
  55. pmc Pharmacological differentiation of opioid receptor antagonists by molecular and functional imaging of target occupancy and food reward-related brain activation in humans
    E A Rabiner
    GSK Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, London, UK
    Mol Psychiatry 16:826-35, 785. 2011
    ..Pharmacological differentiation of these molecules suggests that they may have different therapeutic profiles for treatment of overeating and other disorders of compulsive consumption...
  56. ncbi Suppression of plasma estrogen levels by letrozole and anastrozole is related to body mass index in patients with breast cancer
    Elizabeth J Folkerd
    Royal Marsden Hospital, London, United Kingdom
    J Clin Oncol 30:2977-80. 2012
    ....
  57. pmc Cardiovascular safety of sitagliptin in patients with type 2 diabetes mellitus: a pooled analysis
    Samuel S Engel
    Merck Sharp and Dohme Corp, Whitehouse Station, NJ, USA
    Cardiovasc Diabetol 12:3. 2013
    ..To compare the incidence of cardiovascular events and mortality in patients with type 2 diabetes mellitus treated with sitagliptin or non-sitagliptin comparators...
  58. ncbi Dose-ranging efficacy of sitagliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus
    Yasuhiko Iwamoto
    Diabetes Center, Tokyo Women s Medical University, Tokyo, Japan
    Endocr J 57:383-94. 2010
    ..Treatment with sitagliptin for 12 weeks provided significant and clinically meaningful reductions in HbA(1c), FPG, and 2-hr PPG across the dose range studied and was generally well tolerated in Japanese patients with T2DM...
  59. ncbi Clomiphene citrate or letrozole for ovulation induction in women with polycystic ovarian syndrome: a prospective randomized trial
    Ahmed Badawy
    Department of Obstetrics and Gynecology, Mansoura University, Mansoura, Egypt
    Fertil Steril 92:849-52. 2009
    ..To compare the effects of letrozole (5 mg) and clomiphene citrate (100 mg) for ovulation induction in women with polycystic ovary syndrome (PCOS)...
  60. ncbi Efficacy and safety of sitagliptin monotherapy in Japanese patients with type 2 diabetes
    Kenji Nonaka
    Banyu Pharmaceutical Co Ltd, Tokyo, Japan
    Diabetes Res Clin Pract 79:291-8. 2008
    ..01) different relative to the placebo group (-0.7 kg). In this study, once-daily sitagliptin 100mg for 12 weeks improved fasting and postprandial glycemic control and was generally well tolerated in Japanese patients with type 2 diabetes...
  61. ncbi The myocardial infarct size-limiting effect of sitagliptin is PKA-dependent, whereas the protective effect of pioglitazone is partially dependent on PKA
    Yumei Ye
    John S Dunn Chair in Cardiology Research and Education, Department of Medicine, Section of Cardiology, Baylor College of Medicine, 1709 Dryden Road, Houston, TX 77030, USA
    Am J Physiol Heart Circ Physiol 298:H1454-65. 2010
    ..001). We found that SIT and PIO limit IS using different pathways. The protective effect of SIT is via cAMP-dependent PKA activation, whereas PIO mediates its effects via both PKA-dependent and -independent pathways...
  62. pmc Evaluation of the genotypic prediction of HIV-1 coreceptor use versus a phenotypic assay and correlation with the virological response to maraviroc: the ANRS GenoTropism study
    Patricia Recordon-Pinson
    Laboratoire de Virologie, CHU de Bordeaux, Bordeaux Cedex, France
    Antimicrob Agents Chemother 54:3335-40. 2010
    ..The baseline weighted genotypic sensitivity score was associated with VR at month 6. There were strong arguments in favor of using genotypic coreceptor use assays for determining which patients would respond to CCR5 antagonist...
  63. ncbi Voriconazole compared with liposomal amphotericin B for empirical antifungal therapy in patients with neutropenia and persistent fever
    Thomas J Walsh
    National Cancer Institute, Bethesda, MD 20892, USA
    N Engl J Med 346:225-34. 2002
    Patients with neutropenia and persistent fever are often treated empirically with amphotericin B or liposomal amphotericin B to prevent invasive fungal infections. Antifungal triazoles offer a potentially safer and effective alternative.
  64. ncbi Selective interaction of triazole derivatives with DWF4, a cytochrome P450 monooxygenase of the brassinosteroid biosynthetic pathway, correlates with brassinosteroid deficiency in planta
    T Asami
    RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    J Biol Chem 276:25687-91. 2001
    ..These results indicate that brassinazole inhibits the hydroxylation of the C-22 position of the side chain in BRs by direct binding to DWF4 and that DWF4 catalyzes this hydroxylation reaction...
  65. ncbi The effects of post-surgical administration of goserelin plus anastrozole compared to goserelin alone in patients with severe endometriosis: a prospective randomized trial
    Seyide Soysal
    Department of Obstetrics and Gynecology, Pamukkale University Medical Center, 20100 Denizli, Turkey
    Hum Reprod 19:160-7. 2004
    ....
  66. pmc Multifaceted intervention by the Hsp90 inhibitor ganetespib (STA-9090) in cancer cells with activated JAK/STAT signaling
    David A Proia
    Synta Pharmaceuticals Corp, Lexington, Massachusetts, United States of America
    PLoS ONE 6:e18552. 2011
    ..Overall, our findings support Hsp90 inhibition as a novel therapeutic approach for combating diseases dependent on JAK/STAT signaling, with the multimodal action of ganetespib demonstrating advantages over JAK-specific inhibitors...
  67. ncbi Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers
    Arthur J Bergman
    Merck and Co, Inc, Whitehouse Station, New Jersey 07065 0900, USA
    Clin Ther 28:55-72. 2006
    ..Sitagliptin is an orally active and selective DPP-IV inhibitor currently in Phase III development for the treatment of type 2 diabetes mellitus...
  68. ncbi Update in treatment of Chagas disease
    Guillaume Le Loup
    Service des Maladies Infectieuse et Tropicales, Hôpitaux Universitaires Paris Est Tenon, AP HP, Universite Pierre et Marie Curie, Paris, France
    Curr Opin Infect Dis 24:428-34. 2011
    ..This review discusses the recent data about the pathogenesis of Chagas disease, tolerance of drugs, and follow-up of patients impacting the treatment of Chagas disease in immunocompetent and immunocompromised patients...
  69. pmc In vitro effect of anti-human immunodeficiency virus CCR5 antagonist maraviroc on chemotactic activity of monocytes, macrophages and dendritic cells
    R Rossi
    Department of Public Health and Infectious Diseases, Istituto Pasteur Fondazione Cenci Bolognetti, Sapienza University, Rome
    Clin Exp Immunol 166:184-90. 2011
    ..The drug might have a potential role in the down-regulation of HIV-associated chronic inflammation by blocking the recirculation and trafficking of MO and MDC...
  70. ncbi Effect of body mass index on recurrences in tamoxifen and anastrozole treated women: an exploratory analysis from the ATAC trial
    Ivana Sestak
    Cancer Research UK UK, Queen Mary University of London, London, United Kingdom
    J Clin Oncol 28:3411-5. 2010
    ..As aromatase inhibitors work by inhibiting the conversion of androgens to estrogens in adipose tissue, we hypothesized that anastrozole may be more effective in women with a high body mass index (BMI)...
  71. ncbi Azole resistance in Aspergillus fumigatus: a side-effect of environmental fungicide use?
    Paul E Verweij
    Department of Medical Microbiology, Radboud University Nijmegen Medical Centre, Nijmegen, Netherlands
    Lancet Infect Dis 9:789-95. 2009
    ..Azoles are abundantly used in the environment and the presence of A fumigatus resistant to medical triazoles is a major challenge because of the possibility of worldwide spread of resistant isolates...
  72. pmc Possible environmental origin of resistance of Aspergillus fumigatus to medical triazoles
    Eveline Snelders
    Department of Medical Microbiology, Radboud University Nijmegen Medical Center, The Netherlands
    Appl Environ Microbiol 75:4053-7. 2009
    We reported the emergence of resistance to medical triazoles of Aspergillus fumigatus isolates from patients with invasive aspergillosis...
  73. ncbi Efficacy and safety of sitagliptin in the treatment of patients with type 2 diabetes in China, India, and Korea
    Viswanathan Mohan
    Madras Diabetes Research Foundation and Dr Mohan s Diabetes Specialities Centre, No 6B, Gopalapuram, Chennai 600086, India
    Diabetes Res Clin Pract 83:106-16. 2009
    ..No hypoglycemia was reported. In conclusion, in this study, sitagliptin monotherapy for 18 weeks significantly improved glycemic control and was well-tolerated in patients with type 2 diabetes from China, India, and Korea...
  74. pmc Emergence of CXCR4-using human immunodeficiency virus type 1 (HIV-1) variants in a minority of HIV-1-infected patients following treatment with the CCR5 antagonist maraviroc is from a pretreatment CXCR4-using virus reservoir
    Mike Westby
    Pfizer Global Research and Development, Sandwich, United Kingdom
    J Virol 80:4909-20. 2006
    ..Importantly, in all three patients, circulating virus reverted to predominantly CCR5 tropic following cessation of maraviroc...
  75. ncbi Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis
    Renee E Amori
    Division of Endocrinology, Diabetes and Metabolism, Tufts New England Medical Center, Boston, Massachusetts 02111, USA
    JAMA 298:194-206. 2007
    ..Pharmacotherapies that augment the incretin pathway have recently become available, but their role in the management of type 2 diabetes is not well defined...
  76. pmc A pièce de resistance: how HIV-1 escapes small molecule CCR5 inhibitors
    John P Moore
    Weill Medical College of Cornell University, New York, NY 10065, USA
    Curr Opin HIV AIDS 4:118-24. 2009
    ..We review what has been learned from in-vitro resistance studies, and how this relates to what is being seen, or can be anticipated, in clinical studies...
  77. ncbi The Patient's Anastrozole Compliance to Therapy (PACT) Program: a randomized, in-practice study on the impact of a standardized information program on persistence and compliance to adjuvant endocrine therapy in postmenopausal women with early breast cance
    P Hadji
    Department of Gynecology, Endocrinology and Oncology, Phillips University of Marburg, Marburg, Germany
    Ann Oncol 24:1505-12. 2013
    ..Compliance and persistence are often overlooked in adjuvant breast cancer treatment...
  78. pmc Synergistic activity of the Hsp90 inhibitor ganetespib with taxanes in non-small cell lung cancer models
    David A Proia
    Synta Pharmaceuticals Corp, Lexington, MA 02421, USA
    Invest New Drugs 30:2201-9. 2012
    ..Taken together, these findings provide preclinical evidence for the use of this combination to treat patients with advanced NSCLC...
  79. pmc Posaconazole exposure-response relationship: evaluating the utility of therapeutic drug monitoring
    Michael J Dolton
    Faculty of Pharmacy, University of Sydney, Sydney, Australia
    Antimicrob Agents Chemother 56:2806-13. 2012
    ..In patients with subtherapeutic posaconazole concentrations, increased dose frequency, administration with high-fat meals, and withdrawal of interacting medications from therapy are useful strategies to improve systemic absorption...
  80. pmc Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors
    Alexander Adibekian
    The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California, USA
    Nat Chem Biol 7:469-78. 2011
    ..These data indicate 1,2,3-triazole ureas are a pharmacologically privileged chemotype for serine hydrolase inhibition, combining broad activity across the serine hydrolase class with tunable selectivity for individual enzymes...
  81. ncbi Synthesis and polymerase chain reaction amplification of DNA strands containing an unnatural triazole linkage
    Afaf H El-Sagheer
    School of Chemistry, University of Southampton, Highfield, Southampton, SO17 1BJ, United Kingdom
    J Am Chem Soc 131:3958-64. 2009
    ..The remarkable ability of thermostable polymerases to reproducibly copy DNA templates containing such an unnatural backbone opens up intriguing possibilities in gene synthesis, genetic analysis, biology, and nanotechnology...
  82. pmc Failure of posaconazole therapy in a renal transplant patient with invasive aspergillosis due to Aspergillus fumigatus with attenuated susceptibility to posaconazole
    Saskia Kuipers
    Department of Medical Microbiology, Radboud University Nijmegen Medical Center, P O Box 9101, 6500 HB Nijmegen, Netherlands
    Antimicrob Agents Chemother 55:3564-6. 2011
    ..Posaconazole should be used with caution for invasive aspergillosis caused by strains with attenuated posaconazole susceptibility, as drug exposure may be inadequate, resulting in therapeutic failure...
  83. ncbi Polytriazoles as copper(I)-stabilizing ligands in catalysis
    Timothy R Chan
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 N Torrey Pines Road, La Jolla, California 92037, USA
    Org Lett 6:2853-5. 2004
    ..The C3-symmetric derivative, TBTA, was shown to be a powerful stabilizing ligand for copper(I), protecting it from oxidation and disproportionation, while enhancing its catalytic activity...
  84. ncbi Effect of adenosine A(2A) receptor antagonists on L-DOPA-induced hydroxyl radical formation in rat striatum
    Krystyna Gołembiowska
    Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, Kraków 31 343, Poland
    Neurotox Res 15:155-66. 2009
    ..Summing up, A(2A) antagonists, used as a supplement of L: -DOPA therapy, depending on the dose used, may have a beneficial or adverse effect on ongoing neurodegenerative processes and accompanying oxidative stress...
  85. ncbi Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and pioglitazone on glycemic control and measures of β-cell function in patients with type 2 diabetes
    K H Yoon
    Catholic University of Korea, Kangnamgu Seoul, Korea
    Int J Clin Pract 65:154-64. 2011
    ..To assess the safety and efficacy of initial combination therapy with sitagliptin and pioglitazone compared with pioglitazone monotherapy in drug-naïve patients with type 2 diabetes...
  86. pmc Comparison of the broth microdilution (BMD) method of the European Committee on Antimicrobial Susceptibility Testing with the 24-hour CLSI BMD method for testing susceptibility of Candida species to fluconazole, posaconazole, and voriconazole by use of ep
    M A Pfaller
    Medical Microbiology Division, C606 GH, Department of Pathology, University of Iowa College of Medicine, Iowa City, IA 52242, USA
    J Clin Microbiol 49:845-50. 2011
    ..1% for C. krusei. We demonstrate high levels of EA and CA between the CLSI and EUCAST BMD methods for testing of triazoles against Candida when the MICs were determined after 24 h and ECVs were used to differentiate wild-type (WT) from ..
  87. pmc Biocompatible artificial DNA linker that is read through by DNA polymerases and is functional in Escherichia coli
    Afaf H El-Sagheer
    School of Chemistry, University of Southampton, Highfield, Southampton SO17 1BJ, United Kingdom
    Proc Natl Acad Sci U S A 108:11338-43. 2011
    ..The base sequences of the DNA strands containing this artificial linkage were copied during PCR with high fidelity and a gene containing the triazole linker was functional in Escherichia coli...
  88. pmc Maraviroc for previously treated patients with R5 HIV-1 infection
    Roy M Gulick
    Weill Cornell Medical College, New York, NY 10065, USA
    N Engl J Med 359:1429-41. 2008
    ..CC chemokine receptor 5 antagonists are a new class of antiretroviral agents...
  89. ncbi Iron chelation with deferasirox in adult and pediatric patients with thalassemia major: efficacy and safety during 5 years' follow-up
    M Domenica Cappellini
    Universita di Milano, Ca Granda Foundation Istituto di Ricovero e Cura a Carattere Scientifico corrected IRCCS, Milan, Italy
    Blood 118:884-93. 2011
    ..This trial was registered at www.clinicaltrials.gov as #NCT00171210...
  90. pmc Rapid induction of multiple resistance mechanisms in Aspergillus fumigatus during azole therapy: a case study and review of the literature
    Simone M T Camps
    Department of Medical Microbiology, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands
    Antimicrob Agents Chemother 56:10-6. 2012
    ..Furthermore, the median time between the last cultured wild-type isolate and the first azole-resistant isolate was 4 months (range, 3 weeks to 23 months), indicating a rapid induction of resistance...
  91. ncbi Echinocandin and triazole antifungal susceptibility profiles for Candida spp., Cryptococcus neoformans, and Aspergillus fumigatus: application of new CLSI clinical breakpoints and epidemiologic cutoff values to characterize resistance in the SENTRY Antimi
    Michael A Pfaller
    JMI Laboratories, North Liberty, IA 52317, USA
    Diagn Microbiol Infect Dis 69:45-50. 2011
    ..glabrata. The triazoles, with the exception of itraconazole, also exhibited excellent potency and low levels of resistance when tested ..
  92. ncbi Effect of a switch of aromatase inhibitors on musculoskeletal symptoms in postmenopausal women with hormone-receptor-positive breast cancer: the ATOLL (articular tolerance of letrozole) study
    Karine Briot
    Rheumatology Department, Cochin Hospital, Rheumatology Department, Paris Descartes University, 27 rue Faubourg Saint Jacques, 75014, Paris, France
    Breast Cancer Res Treat 120:127-34. 2010
    ..04). This study shows that in patients intolerant to one AI, switching to another agent allows a higher proportion of patients to continue the therapy and maximize hormonal adjuvant therapy and disease outcome benefits...
  93. ncbi Pregnancy outcome after ovulation induction with aromatase inhibitors or clomiphene citrate in unexplained infertility
    Ahmed Badawy
    Department of Obstetrics and Gynecology, Mansoura University, Egypt
    Acta Obstet Gynecol Scand 88:187-91. 2009
    ..To evaluate the pregnancy outcome after ovulation induction with aromatase inhibitors or clomiphene citrate (CC)...
  94. ncbi Letrozole and norethisterone acetate in colorectal endometriosis
    Simone Ferrero
    Department of Obstetrics and Gynaecology, San Martino Hospital and University of Genoa, Genoa, Italy
    Eur J Obstet Gynecol Reprod Biol 150:199-202. 2010
    ..This study evaluates the efficacy of aromatase inhibitors and norethisterone acetate in treating pain and gastrointestinal symptoms caused by bowel endometriosis...
  95. ncbi Letrozole combined with norethisterone acetate compared with norethisterone acetate alone in the treatment of pain symptoms caused by endometriosis
    S Ferrero
    Department of Obstetrics and Gynaecology, San Martino Hospital and University of Genoa, Largo R Benzi 1 16132, Genoa, Italy
    Hum Reprod 24:3033-41. 2009
    ..We compared the efficacy and tolerability of the aromatase inhibitor letrozole combined with norethisterone acetate versus norethisterone acetate alone in treating pain symptoms...
  96. pmc Efficacy and safety of deferasirox doses of >30 mg/kg per d in patients with transfusion-dependent anaemia and iron overload
    Ali Taher
    Department of Internal Medicine, Haematology Oncology Division, American University of Beirut, Medical Centre, Beirut, Lebanon
    Br J Haematol 147:752-9. 2009
    ..This has important implications for patients who are heavily transfused and may require higher doses to reduce body iron burden...
  97. ncbi Aromatase inhibitors in the treatment of severe endometriosis
    Noha A Mousa
    Institute of Medical Science, Samuel Lunenfeld Research Institute, Mount Sinai Hospital, University of Toronto, Toronto, Ontario, Canada
    Obstet Gynecol 109:1421-3. 2007
    ..Endometriosis-associated chronic pelvic pain unresponsive to surgical menopause is a difficult clinical problem...
  98. ncbi Clinical outcome in resistant HIV-2 infection treated with raltegravir and maraviroc
    Darius Armstrong-James
    Imperial College, St Stephens AIDS Trust, Chelsea and Westminster Hospital, London, UK
    Antiviral Res 86:224-6. 2010
    ..Further studies are required to assess the clinical efficacy of maraviroc in HIV-2 infection...
  99. ncbi Letrozole and norethisterone acetate in rectovaginal endometriosis
    Valentino Remorgida
    Department of Obstetrics and Gynecology, San Martino Hospital and University of Genoa, Genoa, Italy
    Fertil Steril 88:724-6. 2007
    ....
  100. ncbi Letrozole and desogestrel-only contraceptive pill for the treatment of stage IV endometriosis
    Valentino Remorgida
    Department of Obstetrics and Gynaecology, San Martino Hospital and University of Genoa, Genoa, Italy
    Aust N Z J Obstet Gynaecol 47:222-5. 2007
    ..It has recently been suggested that aromatase inhibitors may effectively reduce pain symptoms related to the presence of endometriosis both in postmenopausal women and in subjects of reproductive age...
  101. ncbi Aromatase inhibitors for female infertility: a systematic review of the literature
    Nikolaos P Polyzos
    PACMeR Panhellenic Association for Continual Medical Research, Section of Obstetrics and Gynaecology and Public Health, Athens 10438, Greece
    Reprod Biomed Online 19:456-71. 2009
    ..If solid data from future large adequately powered randomized trials support current evidence regarding efficacy and safety, AI might offer a new treatment choice for infertile women...

Research Grants69

  1. Triazole hypersensitivity in Candida albicans
    Neeraj Chauhan; Fiscal Year: 2009
    ..My preliminary results of MIC broth micro dilution assays indicate that the ssk1 mutant is hypersensitive to the triazoles, fluconazole and voriconazole compared to the wild type strain CAF2-1...
  2. A Structural Approach for Treating Drug Resistant Fungal Pathogens
    Mitchell W Mutz; Fiscal Year: 2013
    ..The emergence of fungal drug resistance to widely used antifungals including triazoles and echinocandins further compromises the efficacy of the limited armamentarium of antifungal therapeutics...
  3. A Combination Therapy Approach to Treating Drug Resistant Fungal Infections
    Mitchell W Mutz; Fiscal Year: 2011
    ..The emergence of fungal drug resistance to widely used antifungals including triazoles and echinocandins further compromises the efficacy of the limited armamentarium of antifungal therapeutics...
  4. Chemical Probes Targeting the Protein Arginine Deiminases
    Paul R Thompson; Fiscal Year: 2013
    ..replacement of the backbone amides in Cl-amidine, an inhibitor developed by the PI's lab, with libraries of triazoles and tetrazoles;and (i) a cyclic peptoid library approach...
  5. Myocotic Ulcer Treatment Trial
    Thomas M Lietman; Fiscal Year: 2013
    ..Our preliminary studies indicate that the newer triazoles are more effective than natamycin in vitro against filamentous fungi such as Fusarium and Aspergillus spp, the ..
  6. A Computer Modeling Approach to Create an Antifungal to Improve the Treatment of
    Mitchell W Mutz; Fiscal Year: 2013
    ..will have the potential to be employed as a single agent or in combination with AmB or orally available triazoles to improve survival rates and compliance with treatment regimens. Our Aims are: 1...
  7. Multi-center studies to improve diagnosis and treatment of pediatric candidiasis
    Theoklis Zaoutis; Fiscal Year: 2013
    ..invasive candidiasis to compare the effectiveness of current pediatric antifungal treatments (amphotericin B, triazoles, and echinocandins)...
  8. Dissecting triazole resistance and transcriptional regulation of ergosterol homeo
    Haoping Liu; Fiscal Year: 2013
    ..Treatment of candidiasis is hampered by the limited number of antifungal drugs. The triazoles are the largest class of antifungal drugs in clinical use. They inhibit lanosterol 14-demethylase (Erg11)...
  9. Novel antifungal therapeutics
    WILLIAM CONSTANTINE GROUTAS; Fiscal Year: 2012
    ..First, there are no new classes of anti- fungals;the new drugs are remodeled triazoles or echinocandins, many still not evaluated clinically...
  10. 1,2,3-Triazole nucleobases in antiviral nucleoside analogues
    ERLAND P STEVENS; Fiscal Year: 2010
    ..We hypothesize 1,4-disubstituted 1,2,3- triazoles should be able to serve as a nucleobase scaffold that will be useful for the discovery of new antiviral ..
  11. Oxime-Assisted Catalysis of Organophosphates and Reactivation of AChE
    PALMER WILLIAM TAYLOR; Fiscal Year: 2011
    ..to the development of reactivating agents using AChE-phosphonate conjugates as the template for synthesis of the triazoles. In addition to oxime assisted catalysis in plasma, new oximes and other nucleophiles will be developed as novel ..
  12. Synthetic Methodology to Access Novel Antivirals
    Mahesh K Lakshman; Fiscal Year: 2012
    ..azide- alkyne ligation chemistry to regiospecifically introduce a deuterium atom at the C-5 position of triazoles in the same step that leads to the formation of the triazole ring...
  13. Genetic Analysis of Echinocandin Sensitivity
    Santosh Katiyar; Fiscal Year: 2004
    ..available antifungals were limited by systemic toxicity (polyenes and imidazoles), lack of fungicidal activity (triazoles and flucytosine), or narrow spectrum (allylamines)...
  14. Carbon-Heteroatom Bond-Forming Reactions
    Valery V Fokin; Fiscal Year: 2013
    ..We begin with cycloaddition processes for the synthesis of azoles. 1,2,3-Triazoles have witnessed a resurgence of interest during the last several years...
  15. GENETIC & MOLECULAR BIOLOGY OF VIRULENCE IN C NEOFORMANS
    John Perfect; Fiscal Year: 2004
    ..neoformans causes a life threatening meningoencephalitis and despite treatments with amphotericin B and newer triazoles the management of this infection remains problematic...
  16. RESPONSE REGULATOR GENE (CASSK1) OF CANDIDA ALBICANS
    Richard Calderone; Fiscal Year: 2004
    ..In spite of the advent of triazoles as anti-fungals, management of AIDS patients with candidiasis is complicated by the development of drug-..
  17. Treatment of Fungal Infections with ATAK Cells
    Ashraf Ibrahim; Fiscal Year: 2004
    ..Furthermore, the genetic construct targeting ATAK cells to Candida can easily be adapted to any other pathogen against which a MAb has been raised. ..
  18. Innate Effectors of rAls3p-N Anti-Candida Vaccine
    Brad J Spellberg; Fiscal Year: 2010
    ..PNS 398/2590 (Rev. 11/07) Page - Continuation Format Page ..
  19. Adrenergic Antagonism During Murine Candidiasis
    Brad Spellberg; Fiscal Year: 2008
    ..For these reasons, the potential for adrenergic antagonism to act as an effective immunotherapy is highly meritorious of investigation in this training application. ..
  20. Anal Dysplasia in HIV+ and HIV- men
    Timothy Wilkin; Fiscal Year: 2006
    ..This study will help provide important new information on which groups of HIV+ men may benefit from screening and how HAART may modify this risk. ..
  21. The Role of TIMP-1 in Uterine Physiology
    Warren Nothnick; Fiscal Year: 2005
    ..These studies will broaden our understanding on the role of TIMP-1 in uterine physiology and may help to develop new strategies to treat uterine disorders such as infertility, endometriosis and uterine cancer. ..
  22. Estrogen regulation of uterine microRNAs: Novel factors in MMP-9 regulation
    Warren Nothnick; Fiscal Year: 2008
    ..Enhancing our understanding on the regulation of MMP-9 expression may lead to the establishment of novel approaches to counteract mis-expression of this protease and the diseases associated with it. [unreadable] [unreadable] [unreadable]..
  23. NMDA Receptor Dynamics After Brain Injury
    Anat Biegon; Fiscal Year: 2011
    ..The results may explain the failure of NMDAR antagonists in clinical trials and suggest novel strategies for treatment of brain injury. ..
  24. Cardiac Function and Cardiac iron (T2*) in Thalassemia
    John Wood; Fiscal Year: 2007
    ..These studies will provide the necessary groundwork for longitudinal studies of cardiac iron load on cardiac performance in thalassemia patients. ..
  25. Novel Antifungal Strategies for Lethal Mucormycosis
    Ashraf Ibrahim; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  26. The Effects of the Cannabinoid-1 Receptor Antagonist Rimonabant on Weight...
    Robert Buchanan; Fiscal Year: 2008
    ..There should be direct evidence of efficacy and safety in these patients in order to provide truly effective treatments and further understanding of these disorders. [unreadable] [unreadable] [unreadable]..
  27. Early Diagnosis of Neonatal Candidiasis
    Daniel Benjamin; Fiscal Year: 2008
    ..abstract_text> ..
  28. Quantitative methods for genetic linkage heterogeneity
    Daniel Schaid; Fiscal Year: 2008
    ..Aim 3. User-friendly software: User-friendly software that implements the proposed methods, including well-documented procedures and examples of their usage, will be provided free to the scientific community. ..
  29. Sterol Metabolism in Pneumocystis
    EDNA KANESHIRO; Fiscal Year: 2009
    ....
  30. First International Inflammatory Breast Cancer Conference
    Massimo Cristofanilli; Fiscal Year: 2008
    ..For project details please see "Conference Plan". [unreadable] [unreadable] [unreadable]..
  31. Functional active-site models of cytochrome c oxidase
    JAMES COLLMAN; Fiscal Year: 2009
    ..The role that the copper ion (CuB) and a phenolic group, in the amino acid tyrosine (Tyr244) play in the catalytic function of CcO are of particular interest. ..
  32. Application of C-H Activation to Natural Product Synthesis
    HUW M DAVIES; Fiscal Year: 2010
    ....
  33. Design of New Treatment Agents for Drug Abuse
    HUW M DAVIES; Fiscal Year: 2010
    ..This will be achieved through a multidisciplinary research program combining organic synthesis, medicinal chemistry, pharmacology and behavioral physiology, exploring the efficacy of a new class of 5HT2A receptor antagonists. ..
  34. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  35. Modulation of Iron Deposition in SCD and Other Hemoglobinopathies
    ELLIOTT P contact VICHINSKY; Fiscal Year: 2010
    ....
  36. Glycomimetics of S. aureus CP Aminosugars
    Peter Norris; Fiscal Year: 2003
    ..aureus type 5 CP and the corresponding J3-DManAcA-(1,3)-alpha-L-FucNAc linkage in the type 8 CP. ..
  37. CVN-12p1 Chimeras and Combinations for AIDS Microbiocides
    Irwin Chaiken; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  38. Advanced Centers for Interventions and Services Research
    Robert Buchanan; Fiscal Year: 2007
    ....
  39. Cryptococcus gatti mating 1oci; mapping and gene study
    Vishnu Chaturvedi; Fiscal Year: 2004
    ..abstract_text> ..
  40. Pharmacogenomics/natural products + antifungal activity
    John Cleary; Fiscal Year: 2004
    ..Probing this array with eukaryotic mRNA from cells exposed to novel antifungals would predict common mechanism of action and likelihood of toxicity, activity and resistance. ..
  41. Anti-Inflammatory PAF Acetylhydrolase in Lung Injury
    Katherine Howard; Fiscal Year: 2004
    ..Through the logical design of the proposed studies, novel and important information will be gained that will significantly advance our understanding of the cell biology of this important anti-inflammatory enzyme. ..
  42. Biomarker modulation/COX-2 inhibitor/Breast Cancer
    Banu Arun; Fiscal Year: 2003
    ..Ultimately, the development of non-hormonal chemoprevention agents, and identification of surrogate markers will allow us to plan large-scale, phase III chemoprevention studies with the endpoint of cancer incidence. ..
  43. MOTOR EFFECTS OF ATYPICAL ANTIPSYCHOTICS
    John Salamone; Fiscal Year: 2003
    ..Taken together, the results of these experiments will help to identify the pharmacological characteristics and brain circuits that underlie the motor effects of clozapine. ..
  44. Clinical Predictors of Antiretroviral Failure
    Daniel Benjamin; Fiscal Year: 2003
    ..abstract_text> ..
  45. E/BETA THALASSEMIA--NATURAL HISTORY & RESPONSE TO CHEMO
    Elliott Vichinsky; Fiscal Year: 2002
    ..In summary, if this study is successful, it will change the approach to Hb E/B worldwide and result in improved quality of life and decreased mortality. (End of Abstract) ..
  46. REGULATION OF HUMAN ALDOSTERONE SYNTHASE
    Perrin White; Fiscal Year: 2002
    ..These studies should provide insight into mechanisms underlying a genetic risk factor for cardiovascular disease. ..
  47. SYNTHESIS AND EVALUATION OF NOVEL COCAINE ANALOGS
    Huw Davies; Fiscal Year: 2002
    ..The proposed studies will ensure that a greater structural diversity is brought into the types of compounds that will be considered as potential medications for the treatment of cocaine addiction. ..
  48. Pneumocystis Biochemistry: Ubiquinones
    EDNA KANESHIRO; Fiscal Year: 2002
    ..carinii CoQ biosynthesis and growth in axenic cultures, and (4) develop atovaquone-resistant P. carinii populations to evaluate CoQ synthesis in sensitive and resistant organisms. ..
  49. CARDIOPROTECTIVE EFFECT--NEW CHELATORS FOR THALASSEMIA
    Chaim Hershko; Fiscal Year: 2001
    ..abstract_text> ..
  50. Effect of Continuous vs. Sequential Oral Contraception
    RICHARD LEGRO; Fiscal Year: 2004
    ..Therefore, the risks and benefits of a CCOCP regimen are an important women's health issue that warrant investigation. ..
  51. Structural Mechanism of IL5-Receptor Subunit Recruitment
    Irwin Chaiken; Fiscal Year: 2004
    ....
  52. Eighth Cooley's Anemia Symposium
    Elliott Vichinsky; Fiscal Year: 2005
    ....
  53. Biochemical Basis of Cortisone Reductase Deficiency
    Perrin White; Fiscal Year: 2007
    ..Subsets of the genotyping data will be analyzed as an association study, as an affected sib pair study, and by transmission disequilibrium testing. Additional polymorphisms in these genes will be sought in PCOS subjects. ..
  54. Biomimetic Studies of NO-binding Respiratory Chain Hemes
    JAMES COLLMAN; Fiscal Year: 2008
    ..An emphasis will be placed on kinetic and mechanistic studies to elucidate the putitive reaction pathways of CcO and NOR. ..
  55. Prognosis in BRCA1 Associated Breast Cancer
    Pamela Goodwin; Fiscal Year: 2007
    ..Because this research is nested within the CFRBCS, the objectives can be addressed in a timely and cost effective manner. ..
  56. c-Kit Mutations and Their Role in Tumor Biology
    Cheryl London; Fiscal Year: 2005
    ..abstract_text> ..
  57. NINTH INTERNATIONAL WORKSHOPS ON OPPORTUNISTIC PEOTISTS (IWOP-9)
    EDNA KANESHIRO; Fiscal Year: 2006
    ..As in several IWOP meetings in the past, the 2006 Workshops will be held jointly with the annual meetings of the International Society of Protistologists ( formerly Society of Protozoologists). ..
  58. CGRP CONTROL IN TRIGEMINAL NEURONS IN VITRO AND IN VIVO
    Paul Durham; Fiscal Year: 2006
    ..abstract_text> ..
  59. Optimizing Foamy Virus Vectors for Gene Therapy & Vaccine Applications
    WILLAM HARDY; Fiscal Year: 2006
    ..I am seeking a KO8 grant to allow me to expand my HIV clinical research career with basic science training to enable me to undertake translational studies directed at HIV therapeutics. ..
  60. Cytokine-Augmented DNA Vaccine-Elicited Immunity to HIV
    DAN BAROUCH; Fiscal Year: 2005
    ..Raphael Dolin, Dean for Clinical Programs, Harvard Medical School, will guide Dr. Barouch's development as an independent investigator. In addition, a committee of distinguished scientists will oversee his progress toward independence. ..
  61. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  62. Radioimmunotherapy: An Anti-Neoplastic Strategy
    Andres Forero; Fiscal Year: 2006
    ..The follow-up trial will be a phase II study to determine the efficacy of 131I-HuCC49ACH2 in resistant/refractory EOC patients. [unreadable] [unreadable] [unreadable] [unreadable] [unreadable]..
  63. PROGESTERONE THERAPY FOR WOMEN WITH EPILEPSY
    Andrew Herzog; Fiscal Year: 2008
    ..30 x .35) 100,000 women with catamenial epilepsy and perhaps many more women with no a priori demonstrated hormonal sensitivity to seizure occurrence. ..
  64. Physiological regulation of FGF-23 by dietary phosphate
    SHERRI ANN BURNETT; Fiscal Year: 2004
    ..We anticipate that male and female participants will show different physiology. Finally, we anticipate that there will be a diurnal variation in FGF-23 that mirrors the diurnal variation in phosphate. ..
  65. Analysis of 5'UTR-Mediated Regulation of p53 Expression
    Philip Lazarus; Fiscal Year: 2006
    ..abstract_text> ..
  66. Functional Analysis of GABAerglc Sedative/Anxiolytics
    NANCY ATOR; Fiscal Year: 2007
    ..abstract_text> ..