sulfones

Summary

Top Publications

  1. ncbi TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial
    Charles F Burant
    Department of Internal Medicine, University of Michigan, Ann Arbor, MI 48105, USA
    Lancet 379:1403-11. 2012
  2. ncbi Cellular characterization of a novel focal adhesion kinase inhibitor
    Jill K Slack-Davis
    Department of Microbiology and Cancer Center, Health Sciences System, University of Virginia, Charlottesville, Virginia 22908, USA
    J Biol Chem 282:14845-52. 2007
  3. ncbi PDE5 inhibition with sildenafil improves left ventricular diastolic function, cardiac geometry, and clinical status in patients with stable systolic heart failure: results of a 1-year, prospective, randomized, placebo-controlled study
    Marco Guazzi
    Cardiopulmonary Unit and Department of Cardiology, University of Milano, San Paolo Hospital, Via A Di Rudini 8, Milan, Italy
    Circ Heart Fail 4:8-17. 2011
  4. ncbi Dapsone and sulfones in dermatology: overview and update
    Y I Zhu
    Department of Dermatology, New York Presbyterian Medical Center, 161 Fort Washington Ave, New York, NY 10032, USA
    J Am Acad Dermatol 45:420-34. 2001
  5. pmc Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752
    Gromoslaw A Smolen
    Cancer Center and Department of Pathology, Molecular Pathology Research Unit, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA
    Proc Natl Acad Sci U S A 103:2316-21. 2006
  6. ncbi Chronic inhibition of cyclic GMP phosphodiesterase 5A prevents and reverses cardiac hypertrophy
    Eiki Takimoto
    Division of Cardiology, Department of Medicine, Johns Hopkins Medical Institutions, Ross 835, 720 Rutland Avenue, Baltimore, Maryland 21205, USA
    Nat Med 11:214-22. 2005
  7. ncbi Chronic treatment with sildenafil improves energy balance and insulin action in high fat-fed conscious mice
    Julio E Ayala
    Department of Molecular Physiology and Biophysics, Vanderbilt University Medical Center, 2200 Pierce Ave, 702 Light Hall, Nashville, TN 37232, USA
    Diabetes 56:1025-33. 2007
  8. ncbi Cardiovascular risk and inhibition of cyclooxygenase: a systematic review of the observational studies of selective and nonselective inhibitors of cyclooxygenase 2
    Patricia McGettigan
    Discipline of Clinical Pharmacology, School of Medicine and Public Health, The University of Newcastle, New South Wales, Australia
    JAMA 296:1633-44. 2006
  9. pmc Anti-inflammatory compounds parthenolide and Bay 11-7082 are direct inhibitors of the inflammasome
    Christine Juliana
    Department of Biochemistry and Molecular Biology, Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
    J Biol Chem 285:9792-802. 2010
  10. ncbi Sildenafil citrate therapy for pulmonary arterial hypertension
    Nazzareno Galie
    Institute of Cardiology, University of Bologna, Bologna, Italy
    N Engl J Med 353:2148-57. 2005

Research Grants

Detail Information

Publications368 found, 100 shown here

  1. ncbi TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial
    Charles F Burant
    Department of Internal Medicine, University of Michigan, Ann Arbor, MI 48105, USA
    Lancet 379:1403-11. 2012
    ..We aimed to assess whether selective pharmacological activation of this receptor by TAK-875 in patients with type 2 diabetes mellitus improved glycaemic control without hypoglycaemia risk...
  2. ncbi Cellular characterization of a novel focal adhesion kinase inhibitor
    Jill K Slack-Davis
    Department of Microbiology and Cancer Center, Health Sciences System, University of Virginia, Charlottesville, Virginia 22908, USA
    J Biol Chem 282:14845-52. 2007
    ....
  3. ncbi PDE5 inhibition with sildenafil improves left ventricular diastolic function, cardiac geometry, and clinical status in patients with stable systolic heart failure: results of a 1-year, prospective, randomized, placebo-controlled study
    Marco Guazzi
    Cardiopulmonary Unit and Department of Cardiology, University of Milano, San Paolo Hospital, Via A Di Rudini 8, Milan, Italy
    Circ Heart Fail 4:8-17. 2011
    ..In a cohort of systolic HF patients, we tested the effects of PDE5 inhibition (sildenafil) on LV ejection fraction, diastolic function, cardiac geometry, and clinical status...
  4. ncbi Dapsone and sulfones in dermatology: overview and update
    Y I Zhu
    Department of Dermatology, New York Presbyterian Medical Center, 161 Fort Washington Ave, New York, NY 10032, USA
    J Am Acad Dermatol 45:420-34. 2001
    In their 60-year history, dapsone and the sulfones have been used as both antibacterial and anti-inflammatory agents...
  5. pmc Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752
    Gromoslaw A Smolen
    Cancer Center and Department of Pathology, Molecular Pathology Research Unit, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA
    Proc Natl Acad Sci U S A 103:2316-21. 2006
    ..MET amplification may thus identify a subset of epithelial cancers that are uniquely sensitive to disruption of this pathway and define a patient group that is appropriate for clinical trials of targeted therapy using MET inhibitors...
  6. ncbi Chronic inhibition of cyclic GMP phosphodiesterase 5A prevents and reverses cardiac hypertrophy
    Eiki Takimoto
    Division of Cardiology, Department of Medicine, Johns Hopkins Medical Institutions, Ross 835, 720 Rutland Avenue, Baltimore, Maryland 21205, USA
    Nat Med 11:214-22. 2005
    ..PDE5A inhibition may provide a new treatment strategy for cardiac hypertrophy and remodeling...
  7. ncbi Chronic treatment with sildenafil improves energy balance and insulin action in high fat-fed conscious mice
    Julio E Ayala
    Department of Molecular Physiology and Biophysics, Vanderbilt University Medical Center, 2200 Pierce Ave, 702 Light Hall, Nashville, TN 37232, USA
    Diabetes 56:1025-33. 2007
    ..These results show that phosphodiesterase-5 is a potential target for therapies aimed at preventing diet-induced energy imbalance and insulin resistance...
  8. ncbi Cardiovascular risk and inhibition of cyclooxygenase: a systematic review of the observational studies of selective and nonselective inhibitors of cyclooxygenase 2
    Patricia McGettigan
    Discipline of Clinical Pharmacology, School of Medicine and Public Health, The University of Newcastle, New South Wales, Australia
    JAMA 296:1633-44. 2006
    ..Regulatory agencies have provided variable advice regarding the cardiovascular risks with older nonselective NSAIDs...
  9. pmc Anti-inflammatory compounds parthenolide and Bay 11-7082 are direct inhibitors of the inflammasome
    Christine Juliana
    Department of Biochemistry and Molecular Biology, Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
    J Biol Chem 285:9792-802. 2010
    ..Our results thus elucidate the molecular mechanism for the therapeutic anti-inflammatory activity of parthenolide and identify vinyl sulfones as a new class of potential therapeutics that target the NLRP3 inflammasome.
  10. ncbi Sildenafil citrate therapy for pulmonary arterial hypertension
    Nazzareno Galie
    Institute of Cardiology, University of Bologna, Bologna, Italy
    N Engl J Med 353:2148-57. 2005
    ....
  11. pmc Dysregulated proinflammatory and fibrogenic phenotype of fibroblasts in cystic fibrosis
    Francois Huaux
    Louvain Centre for Toxicology and Applied Pharmacology LTAP, Institute of Experimental and Clinical Research IREC, Universite Catholique de Louvain UCL, Brussels, Belgium
    PLoS ONE 8:e64341. 2013
    ..Proinflammatory and fibrogenic functions of fibroblasts are upregulated in CF and are reduced by vardenafil. This study provides compelling new support for targeting cGMP signaling pathway in CF pharmacotherapy...
  12. ncbi Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist
    Barry G Shearer
    Department of Metabolic Chemistry, Metabolic Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 53:1857-61. 2010
    ..Compound 3 is a PPARdelta antagonist with utility as a tool to elucidate PPARdelta cell biology and pharmacology...
  13. ncbi Tadalafil, a long-acting inhibitor of PDE5, improves pulmonary hemodynamics and survival rate of monocrotaline-induced pulmonary artery hypertension in rats
    Fusae Sawamura
    Lilly Research Laboratories Japan, Eli Lilly Japan K K, Japan
    J Pharmacol Sci 111:235-43. 2009
    ..Thus, it is expected that tadalafil may be an effective, once-daily treatment option in humans with PAH...
  14. ncbi Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of the GPR40 agonist TAK-875: results from a double-blind, placebo-controlled single oral dose rising study in healthy volunteers
    Himanshu Naik
    Takeda Global Research and Development Center, Inc, Deerfield, IL 60015, USA
    J Clin Pharmacol 52:1007-16. 2012
    ..The pharmacodynamic data support the notion that TAK-875, if effective in diabetic patients, may bear a low risk of hypoglycemia...
  15. ncbi GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes
    T Araki
    Pharmaceutical Development Division, Takeda Pharmaceutical Company Limited, Osaka, Japan
    Diabetes Obes Metab 14:271-8. 2012
    ..In this study, we present the first clinical data for TAK-875, a novel highly selective, orally bioavailable GPR40 agonist, in Japanese patients with type 2 diabetes insufficiently controlled by diet or exercise therapy...
  16. ncbi IL-33 is induced by amyloid-β stimulation and regulates inflammatory cytokine production in retinal pigment epithelium cells
    Xiao Cui Liu
    Department of Ophthalmology, Chinese PLA People s Liberation Army General Hospital, 28 Fuxing Road, Beijing, 100853, China
    Inflammation 35:776-84. 2012
    ..Greater understanding of the inflammatory effect of IL-33 and its role in RPE cells should aid the development of future clinical therapeutics and enable novel pharmacological approaches towards the prevention of AMD...
  17. ncbi Immunomodulatory activity of vardenafil on induced lung inflammation in cystic fibrosis mice
    Bob Lubamba
    Louvain Centre for Toxicology and applied Pharmacology, Universite Catholique de Louvain, Brussels, Belgium
    J Cyst Fibros 11:266-73. 2012
    ..We tested the hypothesis that vardenafil, a common drug used for improving erectile dysfunction and able to partially normalize transepithelial chloride transport in cystic fibrosis (CF), modulates CF lung inflammation...
  18. ncbi Effects of sildenafil on oxidative and inflammatory injuries of the kidney in streptozotocin-induced diabetic rats
    Kyung Hwan Jeong
    Department of Nephrology, School of Medicine, Kyung Hee University, Seoul, Korea
    Am J Nephrol 29:274-82. 2009
    ..Because sildenafil citrate (Viagra) has variable cardiovascular benefits, including antioxidative and immunomodulating effects, we investigated its influence on oxidative stress and inflammation in diabetic rat kidney...
  19. ncbi BAY 11-7082, a nuclear factor-κB inhibitor, reduces inflammation and apoptosis in a rat cardiac ischemia-reperfusion injury model
    Yong Sook Kim
    Heart Research Center, Chonnam National University Hospital, Gwangju, South Korea
    Int Heart J 51:348-53. 2010
    ..These data demonstrate that a currently available and well-tolerated inhibitor of NF-κB can decrease the risk of myocardial injury associated with I/R...
  20. ncbi Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist
    Barry G Shearer
    Research and Development, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Mol Endocrinol 22:523-9. 2008
    ..Here we describe the first report of a PPARbeta/delta small molecule antagonist ligand. This antagonist ligand will be a useful tool for elucidating the biological roles of PPARbeta/delta...
  21. ncbi Inhibition of phosphodiesterase-5 rescues age-related impairment of synaptic plasticity and memory
    Agostino Palmeri
    Department of Bio Medical Sciences Section of Physiology, University of Catania, Catania, 95125, Italy
    Behav Brain Res 240:11-20. 2013
    ..Our data suggest that inhibition of phosphodiesterase-5 may be beneficial to treat age-related cognitive dysfunction in a physiological mouse model of aging...
  22. ncbi Very-long-chain fatty acids have an essential role in plastid division by controlling Z-ring formation in Arabidopsis thaliana
    Takashi Nobusawa
    Graduate School of Biological Sciences, Nara Institute of Science and Technology, Takayama 8916 5, Ikoma, Nara 630 0192, Japan
    Genes Cells 17:709-19. 2012
    ..Our results indicate that VLCFAs or VLCFA-containing lipids have an essential role in plastid division by controlling Z-ring formation, showing a novel function of plant VLCFAs...
  23. ncbi Effect of sildenafil on the anticonvulsant action of classical and second-generation antiepileptic drugs in maximal electroshock-induced seizures in mice
    Dorota Nieoczym
    Department of Animal Physiology, Institute of Biology, Maria Curie Skłodowska University, Lublin, Poland
    Epilepsia 51:1552-9. 2010
    ....
  24. ncbi Prevalence of erectile dysfunction among Chinese men with type 2 diabetes mellitus
    G Yang
    Department of Endocrinology, Chinese PLA General Hospital, Beijing, China
    Int J Impot Res 22:310-7. 2010
    ..ED is a common complication in Chinese men with type 2 diabetes mellitus, and certain risk factors are associated with the presence of ED and severity. Sildenafil citrate is a safe and effective treatment for these patients...
  25. ncbi The anti-inflammatory effects of methylsulfonylmethane on lipopolysaccharide-induced inflammatory responses in murine macrophages
    Yoon Hee Kim
    Center for Efficacy Assessment and Development of Functional Foods and Drugs, Hallym University, Korea
    Biol Pharm Bull 32:651-6. 2009
    ..Collectively, theses results indicate that MSM inhibits LPS-induced release of pro-inflammatory mediators in murine macrophages through downregulation of NF-kappaB signaling...
  26. ncbi Sildenafil-mediated neovascularization and protection against myocardial ischaemia reperfusion injury in rats: role of VEGF/angiopoietin-1
    Srikanth Koneru
    Department of Surgery, Molecular Cardiology and Angiogenesis Laboratory, University of Connecticut Health Center, Farmington, CT 06030 1110, USA
    J Cell Mol Med 12:2651-64. 2008
    ....
  27. ncbi cGMP modulates stem cells differentiation to neurons in brain in vivo
    U Gomez-Pinedo
    Laboratorio de Morfologia Celular, Centro de Investigacion Principe Felipe, Avda Autopista del Saler, Valencia, Spain
    Neuroscience 165:1275-83. 2010
    ..These results support that cGMP modulates the fate of neural stem cells in brain in vivo and suggest that high cGMP levels promote its differentiation to neurons while reduced cGMP levels promote differentiation to non-neuronal cells...
  28. ncbi Effects of specific inhibition of cyclooxygenase-2 on sodium balance, hemodynamics, and vasoactive eicosanoids
    F Catella-Lawson
    University of Pennsylvania, School of Medicine, Philadelphia, Pennsylvania, USA
    J Pharmacol Exp Ther 289:735-41. 1999
    ..Our data suggest that acute sodium retention by nonsteroidal anti-inflammatory drugs in healthy elderly subjects is mediated by the inhibition of Cox-2, whereas depression of GFR is due to inhibition of Cox-1...
  29. ncbi Sildenafil inhibits the formation of superoxide and the expression of gp47 NAD[P]H oxidase induced by the thromboxane A2 mimetic, U46619, in corpus cavernosal smooth muscle cells
    Anthony J Koupparis
    Urology and Bristol Heart Institute, Bristol Royal Infirmary, Bristol, UK
    BJU Int 96:423-7. 2005
    ..To assess the effect of sildenafil on superoxide formation and p47(phox) (the active subunit of NADPH oxidase) expression in cultured corpus cavernosal smooth muscle cells (CVSMCs)...
  30. ncbi Estimating a minimally important difference in pulmonary arterial hypertension following treatment with sildenafil
    Claire Gilbert
    PGRD, Pfizer Ltd, Sandwich, UK
    Chest 135:137-42. 2009
    ..These analyses were undertaken to help define a minimally important difference (MID) in exercise capacity, measured by the 6-min walk distance (6MWD), and HRQoL, measured by the Short Form-36 (SF-36) questionnaire in patients with PAH...
  31. pmc Tumor necrosis factor alpha represses bone morphogenetic protein (BMP) signaling by interfering with the DNA binding of Smads through the activation of NF-kappaB
    Masato Yamazaki
    Departments of Biosciences, Center for Oral Biological Research, Kyushu Dental College, Kitakyushu shi, Fukuoka 803 8580
    J Biol Chem 284:35987-95. 2009
    ..Importantly, the specific NF-kappaB inhibitor, BAY11-7082, abolished these phenomena. These results suggest that TNFalpha inhibits BMP signaling by interfering with the DNA binding of Smads through the activation of NF-kappaB...
  32. ncbi Sildenafil prevents endothelial dysfunction induced by ischemia and reperfusion via opening of adenosine triphosphate-sensitive potassium channels: a human in vivo study
    Tommaso Gori
    Department of Internal, Cardiovascular, and Geriatric Medicine, Azienda Universitaria Ospedaliera Senese, Siena, Italy
    Circulation 111:742-6. 2005
    ..No study has investigated whether sildenafil can also prevent the impairment in endothelium-dependent vasodilatation induced by ischemia-reperfusion (IR) in humans...
  33. ncbi Prescribing pattern of drugs in the treatment of osteoarthritis in Italian general practice: the effect of rofecoxib withdrawal
    Marianna Alacqua
    University of Messina, Messina, Italy
    Arthritis Rheum 59:568-74. 2008
    ..The aim of the present study was to compare the trend of nonsteroidal antiinflammatory drug (NSAID) use and other analgesics in osteoarthritis (OA) treatment before and after rofecoxib withdrawal in Italian general practice...
  34. ncbi A randomized, double-blind, placebo-controlled, dose-ranging study of oral sildenafil citrate in treatment-naive children with pulmonary arterial hypertension
    Robyn J Barst
    Columbia University, New York, NY, USA
    Circulation 125:324-34. 2012
    ..Safe, effective therapy is needed for pediatric pulmonary arterial hypertension...
  35. ncbi Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins
    Guoping Wang
    Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan, 1500 E Medical Center Drive, Ann Arbor, Michigan 48109, USA
    J Med Chem 49:6139-42. 2006
    ..Compound 5 potently inhibits cell growth in PC-3 prostate cancer cells with an IC(50) value of 200 nM and effectively induces apoptosis in a dose-dependent manner...
  36. ncbi Sildenafil increases endothelial progenitor cell function and improves ischemia-induced neovascularization in hypercholesterolemic apolipoprotein E-deficient mice
    Sylvie Dussault
    Department of Cardiovascular Research, Centre Hospitalier de l Universite de Montreal, Montreal, Quebec, Canada
    Hypertension 54:1043-9. 2009
    ..Sildenafil could constitute a novel therapeutic strategy to reduce tissue ischemia in atherosclerotic diseases...
  37. ncbi Chronic administration of Sildenafil improves markers of endothelial function in men with Type 2 diabetes
    A Aversa
    Department of Medical Pathophysiology, Sapienza University of Rome, Rome, Italy
    Diabet Med 25:37-44. 2008
    ..The aim of this study was to determine the effects of chronic therapy with sildenafil on endothelial function in patients with Type 2 diabetes mellitus (DM2)...
  38. ncbi Versatile effects of sildenafil: recent pharmacological applications
    Subramaniam Uthayathas
    Division of Pharmacology and Toxicology, Depertment of Pharmacal Sciences, Harrison School of Pharmacy, Auburn University, Auburn, AL 36849, USA
    Pharmacol Rep 59:150-63. 2007
    ..The present review primarily focuses on the various pharmacological effects of sildenafil with regard to its influence on the nervous and pulmonary system...
  39. ncbi Heme oxygenase-1 gene activation by the NAD(P)H oxidase inhibitor 4-(2-aminoethyl) benzenesulfonyl fluoride via a protein kinase B, p38-dependent signaling pathway in monocytes
    Nastiti Wijayanti
    Institut für Klinische Immunologie und Transfusionsmedizin, Justus Liebig Universitat Giessen, Langhanstrasse 7, D 35392 Giessen, Germany
    J Biol Chem 280:21820-9. 2005
    ..The data suggest that the transcriptional induction of HO-1 gene expression by AEBSF is mediated via activation of a PKB, p38 MAPK signaling pathway...
  40. pmc Improvement of vascular function by acute and chronic treatment with the PDE-5 inhibitor sildenafil in experimental diabetes mellitus
    A Schafer
    Medizinische Klinik und Poliklinik I, Universitatsklinikum Wurzburg, Julius Maximilians Universitat Wurzburg, Wurzburg, Bavaria, Germany
    Br J Pharmacol 153:886-93. 2008
    ..Diabetes-associated vascular dysfunction contributes to increased cardiovascular risk. We investigated whether the phosphodiesterase-5 inhibitor sildenafil would improve vascular function in diabetic rats...
  41. pmc Vinyl sulfones as antiparasitic agents and a structural basis for drug design
    Iain D Kerr
    Department of Cellular and Molecular Pharmacology, University of California, San Francisco, California 94158 2550, USA
    J Biol Chem 284:25697-703. 2009
    ..of rhodesain, in complex with a class of potent, small molecule, cysteine protease inhibitors, the vinyl sulfones. These data, in conjunction with comparative inhibition kinetics, provide insight into the molecular mechanisms ..
  42. ncbi Hemodynamic and gas exchange effects of sildenafil in patients with chronic obstructive pulmonary disease and pulmonary hypertension
    Isabel Blanco
    Department of Pulmonary Medicine, Hospital Clinic Institut d Investigacions Biomediques August Pi i Sunyer, University of Barcelona, Barcelona
    Am J Respir Crit Care Med 181:270-8. 2010
    ..However, vasodilators may inhibit hypoxic pulmonary vasoconstriction and impair gas exchange in this condition...
  43. ncbi Cardiac phosphodiesterase 5 (cGMP-specific) modulates beta-adrenergic signaling in vivo and is down-regulated in heart failure
    H Senzaki
    Division of Cardiology, Department of Medicine, Johns Hopkins Medical Institutions, Baltimore, Maryland 21287, USA
    FASEB J 15:1718-26. 2001
    ....
  44. pmc The liberation of fractalkine in the dorsal horn requires microglial cathepsin S
    Anna K Clark
    Wolfson Centre for Age Related Diseases, King s College London, Guy s Campus, London SE1 1UL, United Kingdom
    J Neurosci 29:6945-54. 2009
    ....
  45. ncbi TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats
    Yoshiyuki Tsujihata
    Metabolic Disease Drug Discovery Unit, Takeda Pharmaceutical Company Limited, Osaka, Japan
    J Pharmacol Exp Ther 339:228-37. 2011
    ..TAK-875 enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia with a low risk of hypoglycemia and no evidence of β cell toxicity...
  46. ncbi Endoplasmic reticulum stress stimulates the expression of cyclooxygenase-2 through activation of NF-kappaB and pp38 mitogen-activated protein kinase
    Jui Hsiang Hung
    Department of Biochemistry, College of Medicine, National Cheng Kung University, Tainan 701, Taiwan, Republic of China
    J Biol Chem 279:46384-92. 2004
    ..Our results provide important insights into cellular carcinogenesis associated with latent endoplasmic reticulum stress...
  47. ncbi A highly specific inhibitor of matrix metalloproteinase-9 rescues laminin from proteolysis and neurons from apoptosis in transient focal cerebral ischemia
    Zezong Gu
    Center for Neuroscience and Aging, The Burnham Institute, La Jolla, California 92037, USA
    J Neurosci 25:6401-8. 2005
    ..We conclude that MMP-9 is a highly promising drug target and that SB-3CT derivatives have significant therapeutic potential in stroke patients...
  48. pmc Nuclear IKK activity leads to dysregulated notch-dependent gene expression in colorectal cancer
    V Fernández-Majada
    Centre Oncologia Molecular, Institut d Investigacio Biomedica de Bellvitge, Gran Via Km 2 7, Hospitalet, 08907 Barcelona, Spain
    Proc Natl Acad Sci U S A 104:276-81. 2007
    ..Finally, BAY11-7082 significantly reduces tumor size in colorectal cancer xenografts (CRC-Xs) implanted in nude mice...
  49. ncbi Functional recovery in aged and young rats after embolic stroke: treatment with a phosphodiesterase type 5 inhibitor
    Li Zhang
    Department of Neurology, Henry Ford Health Sciences Center, Detroit, Mich, USA
    Stroke 36:847-52. 2005
    ..Here, we test the hypothesis that sildenafil provides restorative therapeutic benefit to the aged animal...
  50. pmc Regulator of G protein signaling 2 mediates cardiac compensation to pressure overload and antihypertrophic effects of PDE5 inhibition in mice
    Eiki Takimoto
    Division of Cardiology, Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
    J Clin Invest 119:408-20. 2009
    ..Thus, RGS2 is required for early myocardial compensation to pressure overload and mediates the initial antihypertrophic and cardioprotective effects of PDE5 inhibitors...
  51. ncbi Activation of the PI3-K/Akt pathway mediates cGMP enhanced-neurogenesis in the adult progenitor cells derived from the subventricular zone
    Lei Wang
    Department of Neurology, Henry Ford Health Sciences Center, Detroit, Michigan 48202, USA
    J Cereb Blood Flow Metab 25:1150-8. 2005
    ..Furthermore, LY 294002 blocked Sildenafil-increased SVZ cell proliferation. These data suggest that Sildenafil-enhanced neurogenesis likely occurs through activation of the PI3-K/Akt/GSK-3 pathway...
  52. ncbi Phosphodiesterase-5 inhibitor sildenafil preconditions adult cardiac myocytes against necrosis and apoptosis. Essential role of nitric oxide signaling
    Anindita Das
    Division of Cardiology, Department of Internal Medicine, Virginia Commonwealth University Medical Center, Richmond, Virginia 23298 0281, USA
    J Biol Chem 280:12944-55. 2005
    ..The results may have possible therapeutic potential in preventing myocyte cell death following ischemia/reperfusion...
  53. pmc In vivo evaluation of the biocompatibility of surface modified hemodialysis polysulfone hollow fibers in rat
    Ganpat J Dahe
    Department of Chemical Engineering, Indian Institute of Technology Bombay, Powai, Mumbai, India
    PLoS ONE 6:e25236. 2011
    ..Additionally, Psf/TPGS exhibit most favorable tissue response as compared with other HFMs making them the material of choice for HFM preparation for hemodialysis applications...
  54. ncbi Sildenafil improves six-minute walk distance in chronic obstructive pulmonary disease: a randomised, double-blind, placebo-controlled trial
    Ravinder Singh Rao
    Allergy and Pulmonary Division, SMS Medical College and Hospital, Jaipur Rajasthan, India
    Indian J Chest Dis Allied Sci 53:81-5. 2011
    ..Sildenafil has been found to improve exercise capacity and haemodynamic parameters in patients with various pulmonary disorders. This study was undertaken to evaluate its efficacy in severe chronic obstructive pulmonary disease (COPD)...
  55. ncbi Inhaled phosphodiesterase type 5 inhibitors restore chloride transport in cystic fibrosis mice
    B Lubamba
    Louvain Centre for Toxicology and applied Pharmacology, Universite Catholique de Louvain, Brussels, Belgium
    Eur Respir J 37:72-8. 2011
    ....
  56. pmc Sildenafil reduces respiratory muscle weakness and fibrosis in the mdx mouse model of Duchenne muscular dystrophy
    Justin M Percival
    Department of Physiology and Biophysics, University of Washington, Seattle, WA 98195, USA
    J Pathol 228:77-87. 2012
    ..This study provides new insights into the therapeutic utility of targeting defects in NO-cGMP signalling with PDE5 inhibitors in dystrophin-deficient muscle...
  57. ncbi Comparison of migration from polyethersulphone and polycarbonate baby bottles
    C Simoneau
    European Commission, Joint Research Centre, Institute for Health and Consumer Protection, Unit Chemical Assessment and Testing, T P 260, Ispra VA 21027, Italy
    Food Addit Contam Part A Chem Anal Control Expo Risk Assess 28:1763-8. 2011
    ..321/2011). This confirms that the likelihood of migration of BPA is very low and remains at very minute amounts. The results also suggest the absence of release from PES bottles based on the set of bottles investigated...
  58. ncbi Long-term continuous sildenafil treatment ameliorates corporal veno-occlusive dysfunction (CVOD) induced by cavernosal nerve resection in rats
    I Kovanecz
    LA Biomedical Research Institute at Harbor UCLA Medical Center, Urology Research Laboratory, Torrance, CA 90502 2064, USA
    Int J Impot Res 20:202-12. 2008
    ....
  59. ncbi Cardiovascular events associated with rofecoxib: final analysis of the APPROVe trial
    John A Baron
    Departments of Medicine, and of Community and Family Medicine, Dartmouth Medical School, Hanover, NH, USA
    Lancet 372:1756-64. 2008
    ..We report the cardiovascular outcomes of a long-term follow-up of participants in the trial...
  60. ncbi A multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel GPR40 agonist, TAK-875, in subjects with type 2 diabetes
    E Leifke
    Takeda Global Research and Development Center, Inc, Deerfield, Illinois, USA
    Clin Pharmacol Ther 92:29-39. 2012
    ..Consistent with preclinical data, TAK-875 apparently acts as a glucose-dependent insulinotropic agent with low hypoglycemic risk. Its PK is suitable for once-daily oral administration...
  61. ncbi Inhibition of the SHV-1 beta-lactamase by sulfones: crystallographic observation of two reaction intermediates with tazobactam
    A P Kuzin
    Department of Molecular and Cell Biology, The University of Connecticut, Storrs, CT 06269 3125, USA
    Biochemistry 40:1861-6. 2001
    ..Results are discussed in relation to the mechanism-based inhibition of class A beta-lactamases by the similar inhibitors sulbactam and clavulanic acid...
  62. ncbi Sildenafil citrate therapy for severe early-onset intrauterine growth restriction
    P von Dadelszen
    Department of Obstetrics and Gynaecology, University of British Columbia, Vancouver, BC, Canada
    BJOG 118:624-8. 2011
    ..3, 126; compared with institutional Sildenafil-naive early-onset IUGR controls]. Randomised controlled trial data are required to determine whether Sildenafil improves perinatal outcomes for early-onset IUGR-complicated pregnancies...
  63. ncbi Na+/H+ exchanger-1 inhibitors decrease myocardial superoxide production via direct mitochondrial action
    Carolina D Garciarena
    Centro de Investigaciones Cardiovasces, Facultad de Ciencias Medicas, UNLP 60 y 120, 1900 La Plata, Argentina
    J Appl Physiol (1985) 105:1706-13. 2008
    ..Further studies are needed to clarify the precise mechanism and site of action of these drugs in blunting MPTP formation and ROS release...
  64. pmc Hospitalization for pain in patients with sickle cell disease treated with sildenafil for elevated TRV and low exercise capacity
    Roberto F Machado
    University of Illinois, Chicago, IL, USA
    Blood 118:855-64. 2011
    ..703), TRV (P = .503), or N-terminal pro-brain natriuretic peptide (P = .410). Sildenafil appeared to increase hospitalization rates for pain in patients with SCD. This study is registered at www.clinicaltrials.gov as NCT00492531...
  65. ncbi Spinal cathepsin S and fractalkine contribute to chronic pain in the collagen-induced arthritis model
    Anna K Clark
    King s College London, London, UK
    Arthritis Rheum 64:2038-47. 2012
    ..The purpose of this study was to examine the development of pain in the rat model of collagen-induced arthritis (CIA) and to evaluate the contribution of neuroimmune interactions to established arthritis pain...
  66. ncbi Sildenafil decreased cardiac cell apoptosis in diabetic mice: reduction of oxidative stress as a possible mechanism
    Farzad Ebrahimi
    Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, P O Box 13145 784, Tehran, Iran
    Can J Physiol Pharmacol 87:556-64. 2009
    ..In conclusion, our study indicated that sildenafil was beneficial to hearts of diabetic mice by reducing cardiac cell apoptosis, partially because of its antioxidant effects in the heart...
  67. pmc Strategic design of an effective beta-lactamase inhibitor: LN-1-255, a 6-alkylidene-2'-substituted penicillin sulfone
    Priyaranjan Pattanaik
    Department of Biochemistry, Case Western Reserve University School of Medicine, Cleveland, Ohio 44106, USA
    J Biol Chem 284:945-53. 2009
    ..The 2'-substituted penicillin sulfone, LN-1-255, is proving to be an important lead compound for novel beta-lactamase inhibitor design...
  68. ncbi Sildenafil accelerates liver regeneration after partial hepatectomy in rats
    S Yardimci
    Department of Gastrointestinal Surgery, Turkiye Yuksek Ihtisas Education and Research Hospital, Ankara, Turkey
    Transplant Proc 44:1747-50. 2012
    ..The aim of this study was to investigate the influence of sildenafil on liver regeneration in rats after partial hepatectomy...
  69. pmc Sildenafil restores endothelial function in the apolipoprotein E knockout mouse
    Camille M Balarini
    Dept, of Physiological Sciences, Health Sciences Center, Federal University of Espirito Santo, Vitoria, ES, Brazil
    J Transl Med 11:3. 2013
    ..The aim of this study was to investigate the influence of sildenafil on endothelial function and atherosclerosis progression in apolipoprotein E knockout (apoE-/-) mice...
  70. ncbi Endothelial antioxidant administration ameliorates the erectile response to PDE5 regardless of the extension of the atherosclerotic process
    Enzo Vicari
    Section of Endocrinology, Andrology and Internal Medicine, and Master in Andrological and Human Reproduction Sciences, Department of Biomedical Sciences, University of Catania, Catania, Italy
    J Sex Med 7:1247-53. 2010
    ....
  71. ncbi Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent
    Nobuyuki Negoro
    Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, 26 1 Muraoka Higashi 2 Chome, Fujisawa, Kanagawa 251 8555, Japan
    J Med Chem 55:3960-74. 2012
    ..Compound 16 (TAK-875) is being evaluated in human clinical trials for the treatment of type 2 diabetes...
  72. ncbi Suppression of NF-κB and NF-κB regulated oxidative stress and neuroinflammation by BAY 11-7082 (IκB phosphorylation inhibitor) in experimental diabetic neuropathy
    Ashutosh Kumar
    Molecular Neuropharmacology Laboratory, Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research, Sec 67, S A S Nagar, Mohali, Punjab 160062, India
    Biochimie 94:1158-65. 2012
    ....
  73. ncbi Metal-free synthesis of diaryl sulfones from arylsulfinic acid salts and diaryliodonium salts
    Natalie Umierski
    Department of Organic Chemistry and Chemical Biology, Goethe University Frankfurt, Frankfurt am Main, Germany
    Org Lett 15:188-91. 2013
    An efficient, high-yielding, and transition-metal-free synthesis of diaryl sulfones from arylsulfinic acid salts and diaryliodonium salts has been developed...
  74. ncbi Effects of protein kinase A and G inhibitors on hippocampal cholinergic markers expressions in rolipram- and sildenafil-induced spatial memory improvement
    Ali Hosseini-Sharifabad
    Department of Pharmacology, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran
    Pharmacol Biochem Behav 101:311-9. 2012
    ..However, we did not find evidence for a chronic increase of cholinergic activity in the observed PDE inhibitor-induced memory improvement...
  75. ncbi Bisphenol S in urine from the United States and seven Asian countries: occurrence and human exposures
    ChunYang Liao
    Wadsworth Center, New York State Department of Health, School of Public Health, State University of New York at Albany, Empire State Plaza, PO Box 509, Albany, New York 12201 0509, United States
    Environ Sci Technol 46:6860-6. 2012
    ..67, 0.339, 0.316, 0.292, 0.217, 0.122, 0.084, and 0.023 μg/person, respectively. This is the first study to report the occurrence of BPS in human urine...
  76. ncbi Administration of a low dose of sildenafil for 1 week decreases intrahepatic resistance in rats with biliary cirrhosis: the role of NO bioavailability
    Kuei Chuan Lee
    Division of Gastroenterology, Department of Medicine, Taipei Veterans General Hospital, Taipei, Taiwan
    Clin Sci (Lond) 119:45-55. 2010
    ..In contrast, sham rats did not produce any significant change in these measurements. In conclusion, sildenafil treatment improves endothelial dysfunction by augmenting NO bioavailability in the hepatic microcirculation...
  77. pmc Chronic treatment with sildenafil stimulates Leydig cell and testosterone secretion
    Karina Lidianne Alcântara Saraiva
    Laboratório de Ultraestrutura do Centro de Pesquisas Aggeu Magalhães FIOCRUZ, Recife, CEP 50670 420, Brazil
    Int J Exp Pathol 90:454-62. 2009
    ..Important clinical implications of hormonal disorders should be taken into account for patients with pulmonary hypertension...
  78. ncbi Effects of sildenafil in Nω-nitro-L-arginine methyl ester-induced intrauterine growth restriction in a rat model
    Anwar H Nassar
    Department of Obstetrics and Gynecology, American University of Beirut Medical Center, Beirut, Lebanon
    Am J Perinatol 29:429-34. 2012
    ..To assess the effect of sildenafil citrate in a rat model of Nω-nitro-l-arginine methyl ester (L-NAME)-induced intrauterine growth restriction (IUGR)...
  79. pmc Mitigation of the progression of heart failure with sildenafil involves inhibition of RhoA/Rho-kinase pathway
    Vinh Q Chau
    Div of Cardiology, Box 980204, Virginia Commonwealth Univ, 1101 E Marshall St, Rm 7 020A, Richmond, VA 23298, USA
    Am J Physiol Heart Circ Physiol 300:H2272-9. 2011
    ..Sildenafil may be a promising therapeutic tool for advanced HF in patients...
  80. ncbi Modulating effects of nonselective and selective phosphodiesterase inhibitors on lymphocyte subsets and humoral immune response in mice
    Marianna Szczypka
    Department of Biochemistry, Pharmacology and Toxicology, Faculty of Veterinary Medicine, Wrocław University of Environmental and Life Sciences, Norwida 31, PL 50 375 Wrocław, Poland
    Pharmacol Rep 62:1148-58. 2010
    ..No effect or slight influence of the drugs on anti-SRBC hemagglutinins was observed, but the number of plaque-forming splenocytes was increased. The drugs under investigation did not show a significant immunosuppressive effect...
  81. ncbi Sildenafil (Viagra) attenuates ischemic cardiomyopathy and improves left ventricular function in mice
    Fadi N Salloum
    Division of Cardiology, Department of Internal, Virginia Commonwealth University, Richmond, VA 23298, USA
    Am J Physiol Heart Circ Physiol 294:H1398-406. 2008
    ..05). Sildenafil attenuates ischemic cardiomyopathy in mice by limiting necrosis and apoptosis and by preserving left ventricular function possibly through a nitric oxide-dependent pathway...
  82. pmc Effects of sildenafil and tadalafil on intraocular pressure in sheep: implications for aqueous humor dynamics
    Rosana Gerometta
    Departamento de Oftalmologia, Facultad de Medicina, Universidad Nacional del Nordeste, Corrientes, Argentina
    Invest Ophthalmol Vis Sci 51:3139-44. 2010
    ....
  83. ncbi Synthesis of 9-acridinyl sulfur derivatives: sulfides, sulfoxides and sulfones. Comparison of their activity on tumour cells
    Christiane Santelli-Rouvier
    GERCTOP UMR CNRS 6009, Faculte de Pharmacie, Universite de la Mediterranee, 27, Boulevard Jean Moulin, 13385 Marseille 5, France
    Eur J Med Chem 39:1029-38. 2004
    ..The synthesis of several acridine thioethers is described. These compounds were oxidized to give new sulfoxides and sulfones. Among 23 compounds prepared, 19 were tested in vitro against the human cancer cell lines panel of NCI screening...
  84. ncbi Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities
    Jose N Dominguez
    Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela, Caracas 1051, Venezuela
    Eur J Med Chem 44:1457-62. 2009
    ..Compounds were prepared via Claisen-Schmidt condensation from available chloromethylphenyl sulfones with substituted aldehydes. Antiplasmodial IC(50) activity of these compounds ranged between 0...
  85. pmc Comparative effects of the endogenous agonist glucagon-like peptide-1 (GLP-1)-(7-36) amide and the small-molecule ago-allosteric agent "compound 2" at the GLP-1 receptor
    Karen Coopman
    Department of Cell Physiology and Pharmacology, University of Leicester, Leicester, United Kingdom
    J Pharmacol Exp Ther 334:795-808. 2010
    ..Full assessment of the properties of compound 2 was potentially hampered by damaging effects that were particularly manifest in either longer term assays with intact cells or in acute assays with membranes...
  86. ncbi Effect of viagra on retinal vein diameter in AMD patients
    Tatyana I Metelitsina
    Scheie Eye Institute, Department of Ophthalmology, University of Pennsylvania, 51 North 39th Street, Philadelphia, PA 19104, USA
    Exp Eye Res 83:128-32. 2006
    ..Whether this vasodilatation is associated with changes in retinal blood flow needs to be further investigated...
  87. pmc Methyl sulfone induces loss of metastatic properties and reemergence of normal phenotypes in a metastatic cloudman S-91 (M3) murine melanoma cell line
    Joan McIntyre Caron
    Department of Cell Biology, School of Medicine, University of Connecticut Health Center, Farmington, Connecticut, USA
    PLoS ONE 5:e11788. 2010
    ..We sought to identify an effective and nontoxic agent against metastatic melanoma...
  88. pmc ERK phosphorylation mediates sildenafil-induced myocardial protection against ischemia-reperfusion injury in mice
    Anindita Das
    Division of Cardiology, Department of Internal Medicine, Box 980281, Virginia Commonwealth Univ Medical Center, 1101 East Marshall St, Rm 7 040, Richmond, VA 23298 0281, USA
    Am J Physiol Heart Circ Physiol 296:H1236-43. 2009
    ..We conclude that these studies provide first direct evidence that PKG-dependent ERK phosphorylation is indispensable for the induction of eNOS/iNOS and Bcl-2 and the resulting cardioprotection by sildenafil...
  89. ncbi Effects of nuclear factor-kappaB inhibitors and its implication on natural killer T-cell lymphoma cells
    Kihyun Kim
    Department of Medicine, Sungkyunkwan University School of Medicine, Seoul, Korea
    Br J Haematol 131:59-66. 2005
    ..Given that the chemoresistant NK-92 cells respond to NF-kappaB inhibitors but not to conventional drugs, BAY 11-7082 and curcumin could be potentially useful for achieving improved outcome in chemotherapy-refractory NKTL...
  90. ncbi ERG evaluation of daily, high-dose sildenafil usage
    Christopher I Zoumalan
    Department of Ophthalmology, Stanford University School of Medicine, Boswell Building, Stanford, CA 94305 5308, USA
    Doc Ophthalmol 118:225-31. 2009
    ..The purpose of our study is to investigate possible ERG changes in subjects using large doses of sildenafil on a chronic daily basis...
  91. ncbi Vinyl sulfone: a versatile function for simple bioconjugation and immobilization
    Julia Morales-Sanfrutos
    Departamento de Q Orgánica, Facultad de Ciencia, Instituto de Biotecnologia, Universidad de Granada, Granada, 18071 Spain
    Org Biomol Chem 8:667-75. 2010
    ....
  92. ncbi Effects of sildenafil on pentylenetetrazol-induced convulsions in mice and amygdala-kindled seizures in rats
    Dorota Nieoczym
    Department of Animal Physiology, Institute of Biology, Maria Curie Skłodowska University, Akademicka 19, PL 20 033 Lublin, Poland
    Pharmacol Rep 62:383-91. 2010
    ..Based on these data and in view of the clinical observations, sildenafil should be used in patients suffering from epilepsy with caution and only based on a careful individual risk/benefit evaluation...
  93. pmc Methylsulfonylmethane suppresses breast cancer growth by down-regulating STAT3 and STAT5b pathways
    Eun Joung Lim
    Department of Pathology, School of Medicine, and Institute of Biomedical Science and Technology, Konkuk University Glocal Campus, Seoul, South Korea
    PLoS ONE 7:e33361. 2012
    ..These are the major molecules involved in tumor development, progression, and metastasis. Thus, we strongly recommend the use of MSM as a trial drug for treating all types of breast cancers including triple-negative cancers...
  94. ncbi Preconditioning by phosphodiesterase-5 inhibition improves therapeutic efficacy of adipose-derived stem cells following myocardial infarction in mice
    Nicholas N Hoke
    Pauley Heart Center, Division of Cardiology, Department of Internal Medicine, Virginia Commonwealth University, Richmond, Virginia 23298, USA
    Stem Cells 30:326-35. 2012
    ..We conclude that preconditioning by inhibition of PDE-5 can be a powerful novel approach to improve stem cell therapy following myocardial infarction...
  95. pmc Matrix metalloproteinase-9 controls proliferation of NG2+ progenitor cells immediately after spinal cord injury
    Huaqing Liu
    Department of Anesthesiology at the University of California, San Diego, La Jolla, CA, USA
    Exp Neurol 231:236-46. 2011
    ..Collectively, these data establish a novel role for MMPs in regulation of NG2+ cell proliferation in the damaged CNS, and a long-term benefit of acute MMP-9 block after SCI...
  96. ncbi Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents
    Jean Damien Charrier
    Chemistry Department, Vertex Pharmaceuticals Europe Ltd, 88 Milton Park, Abingdon, Oxfordshire OX14 4RY, United Kingdom
    J Med Chem 54:2320-30. 2011
    ..This differential response between cancer and normal cells highlights the great potential for ATR inhibition as a novel mechanism to dramatically increase the efficacy of many established drugs and ionizing radiation...
  97. pmc Matrix metalloproteinase-9 and stromal cell-derived factor-1 act synergistically to support migration of blood-borne monocytes into the injured spinal cord
    Haoqian Zhang
    Department of Neurosurgery, University of California, San Francisco, California 94143 0110, USA
    J Neurosci 31:15894-903. 2011
    ..Collectively, these observations suggest a synergistic partnership between MMP-9 and SDF-1 in facilitating transmigration of monocytes into the injured spinal cord...
  98. ncbi Cigarette smoke-induced pulmonary endothelial dysfunction is partially suppressed by sildenafil
    Javier Milara
    Research Unit, University General Hospital Consortium, Valencia, Spain
    Eur J Pharm Sci 39:363-72. 2010
    ....
  99. ncbi Systematic review of the nutritional supplements dimethyl sulfoxide (DMSO) and methylsulfonylmethane (MSM) in the treatment of osteoarthritis
    S Brien
    Department of Primary Care, University of Southampton, UK
    Osteoarthritis Cartilage 16:1277-88. 2008
    ....
  100. ncbi Antiproliferative effects of phosphodiesterase type 5 inhibition in human pulmonary artery cells
    John Wharton
    Section on Experimental Medicine and Toxicology, Imperial College London, Hammersmith Campus, Du Cane Road, London W12 ONN, UK
    Am J Respir Crit Care Med 172:105-13. 2005
    ..Phosphodiesterase Type 5 (PDE5) inhibition represents a novel strategy for the treatment of pulmonary hypertension...
  101. ncbi Allosteric sites of phosphodiesterase-5 (PDE5). A potential role in negative feedback regulation of cGMP signaling in corpus cavernosum
    V K Gopal
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232-0615, USA
    Eur J Biochem 268:3304-12. 2001
    ..This introduces a new concept for cyclic nucleotide signaling...

Research Grants67

  1. Raman spectroscopic analysis of drug beta-lactamase interacteractions
    Paul R Carey; Fiscal Year: 2013
    ..Initially, our studies will use lead compounds that are 6-(pyridylmethylidene) penam sulfones possessing favorable IC50 values...
  2. Raman Spectroscopic Analysis of Beta-Lactamase Drug Interactions
    Paul Carey; Fiscal Year: 2009
    ..Initially, our studies will use lead compounds that are 6- (pyridylmethylidene) penam sulfones possessing favorable IC50 values...
  3. Total Synthesis of Anticancer Agents Superstolides A & B
    Zhendong Jin; Fiscal Year: 2010
    ..A new efficient synthesis of allyl sulfones employing Negishi coupling between a-sulfonyl zinc chloride and vinyl halide;1b...
  4. Carbene-Catalyzed Reactions with Vinyl Sulfones
    ROXANNE L ATIENZA; Fiscal Year: 2012
    ....
  5. Mechanisms of Cutaneous Drug Reactions
    CRAIG SVENSSON; Fiscal Year: 2004
    ..Of particular interest are the delayed-type hypersensitivity reactions that occur with sulfonamides and sulfones. While most investigators have focused on the role of differences in hepatic bioactivation and detoxification in ..
  6. SULFONYL ANALOGUES OF SULFATES AND PHOSPHATES
    THEODORE WIDLANSKI; Fiscal Year: 1993
    ..e. viruses). This proposal details the synthesis of stable non-ionic oligonucleotides using sulfonates, sulfones and sulfonamides in the place of phosphate diesters...
  7. Arylation of weakly acidic sp3 hybridized C-H's
    Patrick J Walsh; Fiscal Year: 2013
    ..DCCP's of unactivated diarylmethanes, allylbenzenes, N,N-dialkylbenzylamines, sulfoxides, sulfonamides, and sulfones to generate novel arylated products...
  8. Biologic Ventricular Assist Device
    Robert Kloner; Fiscal Year: 2004
    ..Identification and characterization of transplants will be carried out with PCR analysis of the Y chromosome (male cells into female host), detailed histologic analysis and immunostaining for muscle cell markers. ..
  9. COLLABORATIVE R01-CARDIAC GRAFTS-FUNCTIONAL ANALYSES
    Robert Kloner; Fiscal Year: 2003
    ....
  10. Periodontal Assessment in RA Study (PARAS)
    Clifton Bingham; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  11. Molecular Control of cGMP Signaling by PKGs and PDEs
    Jackie Corbin; Fiscal Year: 2007
    ..A thorough physical and biochemical characterization of PDE11 will be carded out, and the likelihood of regulation of this enzyme by ligand binding to its GAF domains or by enzyme phosphorylation will be explored. ..
  12. ASYMMETRIC SYNTHESIS OF VANCOMYCIN ANTIBIOTICS
    David Evans; Fiscal Year: 2001
    ..During the course of this project we intend to confirm (correct) the absolute stereochemical assignments of the principal members of this family by total synthesis. ..
  13. ASYMMETRIC SYNTHESIS OF IONOPHORE/MACROLIDE ANTIBIOTICS
    David Evans; Fiscal Year: 2005
    ..Our goal has been to set in place all of the reactions necessary for the rapid assemblage of any polyketide target structure. ..
  14. N O S AND NEUROPATHIC AND ENDOTHELIAL INDUCED ED
    Kevin McVary; Fiscal Year: 2002
    ..Results of this research will aid in the understanding of how diabetic neuropathy contributes to sexual dysfunction and elucidate possible mechanisms to prevent them. ..
  15. Synthesis of Polyketides and Terpenes
    David A Evans; Fiscal Year: 2010
    ..As a consequence, organic synthesis is a critical discipline that continues to have an important impact on the fields of both medicine and biology. ..
  16. Molecular Mechanisms of PDE5 Regulation
    Jackie Corbin; Fiscal Year: 2005
    ..Results of these studies will provide a basis for understanding fundamental questions relating to cGMP signaling in many tissues. ..
  17. Dual Purpose b-Lactamase Inhibitors
    JOHN BUYNAK; Fiscal Year: 2004
    ..A group of scientists, including chemists, microbiologists, enzymologists, and crystallographers has been assembled to allow rapid optimization of SAR. ..
  18. PDE-5 Inhibition in HIV+ and HIV- Men
    Raymond Rosen; Fiscal Year: 2005
    ..Key personnel for the project are Raymond C. Rosen, Ph.D., Professor of Psychiatry and Medicine at UMDNJ, who will serve as PI, and Joseph Catania, PhD, co-PI, from the AIDS Research Institute at UCSF. ..
  19. The Efficacy of TUMT and Neoadjuvant Finasteride for BPH
    Kevin McVary; Fiscal Year: 2005
    ..We are proposing a 3-arm, placebo/sham controlled, randomized clinical trial using changes in symptoms as the primary ..
  20. Sexual Dysfunction and Diabetes:Look AHEAD Sub-Study
    Stephen Schneider; Fiscal Year: 2006
    ..iii) Finally, the proposed sub-study will investigate the relationship between changes in sexual function and quality of life outcomes. ..
  21. REGULATION OF PROSTATE GROWTH BY NEURAL FACTORS
    Kevin McVary; Fiscal Year: 2001
    ..Using this model allows one to explore the limits of understanding prostatic neuroregulation, to explore neurotrophic influences on exocrine gland development, and to possibly uncover novel methods to influence prostate disease. ..
  22. MINERALIZATION OF PRIMARY BONE
    JEFFREY GORSKI; Fiscal Year: 2008
    ..Results of this work should better define the differences between primariy and lamellar bone, as well as aid in the diagnosis and treatment of osteoporosis and atherosclerosis. ..
  23. Insulin Resistance and Hepatic Steatosis in Hepatitis C
    Charles F Burant; Fiscal Year: 2010
    ..abstract_text> ..
  24. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  25. BAG-75: UNIQUE MARKER OF PRIMARY BONE FORMATION
    JEFFREY GORSKI; Fiscal Year: 2003
    ..Stimulation of appositional formation by lamellar bone would not be expected to have the same effect. These future functional studies require determination of the BAG-75 cDNA sequence. ..
  26. Using Systems Biology to Understand Islet Adaptation and Failure Diabetes
    Charles F Burant; Fiscal Year: 2010
    ..The studies will also provide the first insights into the ways in which human islets react to specific nutrient challenges. ..
  27. Ethnic Differences in Media Response and Recruitment
    Deborah Bruner; Fiscal Year: 2008
    ..It would also serve as a potential model for improved information seeking and recruitment of AA men to be tested in other cancer control and treatment trials and potentially as a model for other minorities. ..
  28. LINKAGE ANALYSIS IN INTERSTITIAL CYSTITIS
    Jordan Dimitrakov; Fiscal Year: 2007
    ..Expand the analysis of the candidate gene(s) in families from the US. To validate our identification of a candidate IC gene, we will look for additional mutations in a select group of families from the US of non-Bulgarian ancestry. ..
  29. Assessment of Infant Outcomes After in Utero Exposure to Antiretroviral Therapy
    Sonia Hernandez diaz; Fiscal Year: 2010
    ..We propose to evaluate the risk of congenital malformations and other adverse pregnancy outcomes following antenatal exposure to ART in a prospective cohort of pregnant women. ..
  30. Novel Class of Phospholipases-Molecular Pathogenesis
    Michael Vasil; Fiscal Year: 2007
    ..Furthermore, it is likely that information we derive from our efforts will also provide additional insights about the biochemistry and biology of PLCs in general. ..
  31. Clinical and Molecular Evaluation of Cancer Therapy Induced Mucositis
    Sharon Gordon; Fiscal Year: 2007
    ..Demonstration of safety and tolerability will provide a basis to test further this route of administration. Hence, this proposal holds promise for clinical application in a relatively short period. [unreadable] [unreadable]..
  32. Telemonitoring to improve heart failure outcomes
    Harlan Krumholz; Fiscal Year: 2008
    ..abstract_text> ..
  33. Concurrent Immune Stimulation and Inhibition of Angiogenesis for Glioma Therapy
    JOHN OHLFEST; Fiscal Year: 2008
    ..The project has high impact potential because it may identify a new treatment approach for glioblastoma patients. [unreadable] [unreadable] [unreadable]..
  34. Complications of Surgery for Spinal Stenosis: A Clinical Prediction Rule
    Richard A Deyo; Fiscal Year: 2010
    ..PUBLIC HEALTH RELEVANCE: A new method for estimating surgical risk will improve patient safety and assist in surgical decision-making, informed consent, monitoring surgical products, &improving quality assessment. ..
  35. WGA Study to Identify Genetic Variants Associated with CV Events in CHS
    Bruce Psaty; Fiscal Year: 2009
    ..The proposed three-part study is efficient, has excellent power to detect small to modest-sized hazard ratios, provides a large sample of WG scans for aim 2, and includes an external replication. (End of Abstract) ..
  36. Serotonin-related genes in human brain
    Wolfgang Sadee; Fiscal Year: 2008
    ..Identifying genetic variants that regulate key serotonin-related genes will be a significant step toward developing new methods for the diagnosis, treatment and, possibly, prevention of these disorders. [unreadable] [unreadable]..
  37. LIPID MODULATORS OF PULMONARY VASCULAR TONE
    Elizabeth R Jacobs; Fiscal Year: 2010
    ....
  38. Folate in Schizophrenia
    Donald C Goff; Fiscal Year: 2010
    ..This will be the first adequately-powered study to assess efficacy and identify predictors of response. ..
  39. Pharmacogenomics in Pulmonary Arterial Hypertension
    Raymond Benza; Fiscal Year: 2008
    ..PAH = pulmonary arterial hypertension PA = pulmonary artery PPH = primary pulmonary hypertension ..
  40. Clinical & Molecular Studies of Drug Resistant Malaria
    Philip Rosenthal; Fiscal Year: 2008
    ..abstract_text> ..
  41. Estradiol Metabolites for Treatment of Pulmonary Hypertension
    Stevan Tofovic; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  42. IMAGING DOPAMINE/SEROTONIN MECHANISMS IN COCAINE CRAVING
    DEAN WONG; Fiscal Year: 2003
    ..Testing of these hypotheses will provide novel and fundamental answers to craving mechanisms. ..
  43. Chemopreventive Efficacy of Broccoli Sprouts in Humans
    Thomas Kensler; Fiscal Year: 2004
    ..abstract_text> ..
  44. ONCOGENE DIRECTED SYNTHESIS OF CEPHALOSTATIN CANCER DRUG
    Philip Fuchs; Fiscal Year: 2004
    ..This will be accomplished by systematic exploration of the potential of a previously unknown stereospecific dyatropic rearrangement of beta-hydroxyketones and beta-hydroxy lactones to accomplish this transformation. ..
  45. UTILIZATION AND COST OF HEALTH SERVICES BY CDUs
    W Bradford; Fiscal Year: 2003
    ....
  46. EXCITATORY AMINO ACIDS IN GLAUCOMA
    Alan Laties; Fiscal Year: 2004
    ..These experiments will help test the central hypothesis--for if one can block the effects of IOP elevation with glutamate antagonists, then elevated 10P may toxic glutamate levels ganglion cell loss. ..
  47. PHOSPHORYLATED ISONUCLEOSIDES: NEW ANTI-HIV AGENTS
    Vasu Nair; Fiscal Year: 2003
    ..Cellular combination drug studies, particularly those having the potential for synergistic inhibition of HIV infectivity, are also planned. ..
  48. MECHANISMS OF DOPAMINE & SEROTONIN IN TOURETTE SYNDROME
    DEAN WONG; Fiscal Year: 2003
    ..We propose to carry out experiments using PET to establish a more complete understanding of the neurotransmission in TS. This will also help establish new ationales for improved therapeutics in TS. ..
  49. EVALUATION OF FALCIPAIN AS AN ANTIMALARIAL DRUG TARGET
    Philip Rosenthal; Fiscal Year: 2003
    ..This evaluation is also likely to identify specific falcipain inhibitors with potent antimalarial activity that will be ready for initial testing against human malaria. ..
  50. MUTATIONS OF MUSCARINIC CHOLINERGIC RECEPTOR GENES
    Wolfgang Sadee; Fiscal Year: 2001
    ..The expected insights from the studies outlined in this proposal should assist in the design of cholinergic therapy for cognitive disorders. ..
  51. PROTEASE INHIBITOR ADHERENCE AMONG DRUG USERS
    Perry Halkitis; Fiscal Year: 2002
    ..Generalized linear, Markov regression, and structural equation modeling will be used to achieve the study's goals. ..
  52. GENETIC DETERMINATION OF ALLOGRAFT VASCULOPATHY
    Raymond Benza; Fiscal Year: 2002
    ..If his faculty mentor were to leave the institution, a new mentor will be appointed and his continued development toward becoming a independent physician scientist supported and encouraged. ..
  53. Targeted Intervention Against EphA2 on Cancer Cells
    DEBORAH KNAPP; Fiscal Year: 2004
    ..Upon conclusion of our studies, we will have validated EphA2 as a molecular target for cancer treatment and will have generated the reagents and expertise to exploit a critical vulnerability on malignant cells. ..
  54. ANTIHYPERTENSIVE DRUG/GENE INTERACTIONS AND CV EVENTS
    Bruce Psaty; Fiscal Year: 2004
    ..58 (the difference between an odds ratio of 0.46 and 0.79 in subjects with and without the variant, respectively). Power for other primary aims is excellent; power for secondary aims is good to excellent. ..
  55. Iron and O2 in the Regulation of P. aeruginosa Virulence
    Michael Vasil; Fiscal Year: 2003
    ..This project will investigate the role of PA-Fur and PA-Fur regulated genes in the pathogenesis of P. aeruginosa infections for the ultimate goal or developing novel antimicrobial agents against this formidable opportunist. ..
  56. High End Computing for PET/SPECT
    DEAN WONG; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  57. Synthesis through N-Acylnitrenium Ion Cyclization
    DUNCAN WARDROP; Fiscal Year: 2006
    ..abstract_text> ..
  58. Immortalized Human Cavernosal Endothelial Cells
    Hunter Wessells; Fiscal Year: 2005
    ..abstract_text> ..
  59. Hormone Replacement Therapy and Prothrombotic Variants
    Bruce Psaty; Fiscal Year: 2005
    ..Power for primary and secondary aims is excellent. Information from this project may help physicians counsel women about HRT to maximize either effectiveness, or safety, or both. ..
  60. CLUB DRUG USE AND MEN'S HEALTH--A COMMUNITY STUDY
    Perry Halkitis; Fiscal Year: 2003
    ....
  61. THE ROLE OF MYCOBACTERIA IN CROHN'S DISEASE
    David Graham; Fiscal Year: 2005
    ..The results of this study should either confirm or refute the proposed etiologic association of M. paratuberculosis and Crohn's disease as well as the identification of patients with Crohn's disease and M. paratuberculosis. ..
  62. 2004 Barriers of CNS
    MARTHA O DONNELL; Fiscal Year: 2004
    ..Two open workshops/debates to occur during the meeting are also planned. The maximum permitted attendance at this meeting is 150 scientists. ..
  63. OPIOID RECEPTOR REGULATION
    Wolfgang Sadee; Fiscal Year: 2003
    ..Considered together, these hypotheses may yield important insights into the mechanisms underlying tolerance and dependence, providing the opportunity to develop effective therapies of narcotic addiction. ..
  64. NEUROPSYCHIATRIC EFFECTS OF TESTOSTERONE IN MEN
    Stuart Seidman; Fiscal Year: 2004
    ..abstract_text> ..
  65. Diet, Colon Cancer, and Cancer Communications
    Jessie Satia; Fiscal Year: 2005
    ..Obtaining this award will greatly broaden and strengthen the candidate's focus on cancer prevention and control. ..
  66. Antioxidant nutrients and Oxidative DNA Damage in Afric*
    Jessie Satia; Fiscal Year: 2005
    ..In addition, this work would potentially provide investigators with a validated instrument for assessing antioxidant nutrient exposure in population-based studies in the U.S. ..
  67. Dietary Supplements and Lung & Colorectal Cancer Risk
    Jessie Satia; Fiscal Year: 2006
    ..abstract_text> ..