- 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...
- 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...
- 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
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...
- Voriconazole versus amphotericin B for primary therapy of invasive aspergillosis
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...
- Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy
Synta Pharmaceuticals Corp, 45 Hartwell Avenue, Lexington, MA 02421, USA
Mol Cancer Ther 11:475-84. 2012
- 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
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...
- 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
- 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...
- Genetic deletion or pharmacological inhibition of dipeptidyl peptidase-4 improves cardiovascular outcomes after myocardial infarction in mice
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...
- 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
- Efficacy and safety of sitagliptin when added to insulin therapy in patients with type 2 diabetes
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...
- 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...
- Phase II randomized study of neoadjuvant everolimus plus letrozole compared with placebo plus letrozole in patients with estrogen receptor-positive breast cancer
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)...
- Targeting MYCN in neuroblastoma by BET bromodomain inhibition
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...
- Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 10-year analysis of the ATAC trial
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...
- 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...
- Efficacy and tolerability of sitagliptin monotherapy in elderly patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial
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...
- HIV-1 escape from the CCR5 antagonist maraviroc associated with an altered and less-efficient mechanism of gp120-CCR5 engagement that attenuates macrophage tropism
Centers for Virology, Monash University, Australia
J Virol 85:4330-42. 2011
- 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...
- 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
- Interaction of A2A adenosine and D2 dopamine receptors modulates corticostriatal glutamatergic transmission
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...
- European guidelines for antifungal management in leukemia and hematopoietic stem cell transplant recipients: summary of the ECIL 3--2009 update
Department of Hematology, Leukemia and Stem Cell Transplantation Unit, University Hospitals Leuven, Campus Gasthuisberg, Leuven, Belgium
Bone Marrow Transplant 46:709-18. 2011
- 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...
- 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...
- Invasive aspergillosis in patients with acute myeloid leukemia: a SEIFEM-2008 registry study
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...
- Prognostic value of Ki67 expression after short-term presurgical endocrine therapy for primary breast cancer
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
- 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
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)...
- 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...
- 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...
- Sitagliptin augments protective effects of GLP-1 against advanced glycation end product receptor axis in endothelial cells
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...
- 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
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...
- Comparison of vildagliptin twice daily vs. sitagliptin once daily using continuous glucose monitoring (CGM): crossover pilot study (J-VICTORIA study)
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...
- Efficacy and safety of sitagliptin and metformin as initial combination therapy and as monotherapy over 2 years in patients with type 2 diabetes
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...
- 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...
- V3 determinants of HIV-1 escape from the CCR5 inhibitors Maraviroc and Vicriviroc
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...
- 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...
- Gibberellin regulates Arabidopsis seed germination via RGL2, a GAI/RGA-like gene whose expression is up-regulated following imbibition
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...
- 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
- Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes
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...
- A dipeptidyl peptidase-4 inhibitor, des-fluoro-sitagliptin, improves endothelial function and reduces atherosclerotic lesion formation in apolipoprotein E-deficient mice
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)...
- 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...
- 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
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...
- 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
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...
- Efficacy of short-term monotherapy with maraviroc, a new CCR5 antagonist, in patients infected with HIV-1
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...
- Dual inhibition of mTOR and estrogen receptor signaling in vitro induces cell death in models of breast cancer
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...
- Reduced maximal inhibition in phenotypic susceptibility assays indicates that viral strains resistant to the CCR5 antagonist maraviroc utilize inhibitor-bound receptor for entry
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...
- 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
Tulane University Medical Center, New Orleans, LA, USA
J Diabetes Complications 27:177-83. 2013
..5% and ≤11%)...
- 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
- Design, synthesis and biological evaluation of mannosyl triazoles as FimH antagonists
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...
- 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...
- Identification of new agonists and antagonists of the insect odorant receptor co-receptor subunit
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...
- Safety and efficacy of treatment with sitagliptin or glipizide in patients with type 2 diabetes inadequately controlled on metformin: a 2-year study
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...
- Inhibition of opioid transmission at the μ-opioid receptor prevents both food seeking and binge-like eating
Behavioral and Clinical Neuroscience Institute and Department of Experimental Psychology, University of Cambridge, Cambridge, UK
Neuropsychopharmacology 37:2643-52. 2012
- 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...
- 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...
- 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
- 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...
- Dose-ranging efficacy of sitagliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus
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...
- Clomiphene citrate or letrozole for ovulation induction in women with polycystic ovarian syndrome: a prospective randomized trial
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)...
- Efficacy and safety of sitagliptin monotherapy in Japanese patients with type 2 diabetes
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...
- The myocardial infarct size-limiting effect of sitagliptin is PKA-dependent, whereas the protective effect of pioglitazone is partially dependent on PKA
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...
- 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
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...
- 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.
- Selective interaction of triazole derivatives with DWF4, a cytochrome P450 monooxygenase of the brassinosteroid biosynthetic pathway, correlates with brassinosteroid deficiency in planta
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...
- The effects of post-surgical administration of goserelin plus anastrozole compared to goserelin alone in patients with severe endometriosis: a prospective randomized trial
Department of Obstetrics and Gynecology, Pamukkale University Medical Center, 20100 Denizli, Turkey
Hum Reprod 19:160-7. 2004
- 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...
- 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...
- 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...
- In vitro effect of anti-human immunodeficiency virus CCR5 antagonist maraviroc on chemotactic activity of monocytes, macrophages and dendritic cells
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...
- Effect of body mass index on recurrences in tamoxifen and anastrozole treated women: an exploratory analysis from the ATAC trial
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)...
- 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...
- Possible environmental origin of resistance of Aspergillus fumigatus to medical triazoles
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...
- Efficacy and safety of sitagliptin in the treatment of patients with type 2 diabetes in China, India, and Korea
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...
- 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
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...
- 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...
- 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...
- 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
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...
- 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...
- 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...
- Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors
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...
- 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...
- Failure of posaconazole therapy in a renal transplant patient with invasive aspergillosis due to Aspergillus fumigatus with attenuated susceptibility to posaconazole
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...
- 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...
- Effect of adenosine A(2A) receptor antagonists on L-DOPA-induced hydroxyl radical formation in rat striatum
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...
- 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...
- 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 ..
- 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...
- 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...
- 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...
- 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...
- 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 ..
- 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
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...
- Pregnancy outcome after ovulation induction with aromatase inhibitors or clomiphene citrate in unexplained infertility
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)...
- Letrozole and norethisterone acetate in colorectal endometriosis
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...
- Letrozole combined with norethisterone acetate compared with norethisterone acetate alone in the treatment of pain symptoms caused by endometriosis
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...
- Efficacy and safety of deferasirox doses of >30 mg/kg per d in patients with transfusion-dependent anaemia and iron overload
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...
- 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...
- Clinical outcome in resistant HIV-2 infection treated with raltegravir and maraviroc
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...
- Letrozole and norethisterone acetate in rectovaginal endometriosis
Department of Obstetrics and Gynecology, San Martino Hospital and University of Genoa, Genoa, Italy
Fertil Steril 88:724-6. 2007
- Letrozole and desogestrel-only contraceptive pill for the treatment of stage IV endometriosis
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...
- 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...