enzyme inhibitors

Summary

Summary: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.

Top Publications

  1. ncbi Role of NF-kappaB and Akt/PI3K in the resistance of pancreatic carcinoma cell lines against gemcitabine-induced cell death
    Alexander Arlt
    1Laboratory of Molecular Gastroenterology and Hepatology, 1st Department of Medicine, University of Kiel, Germany
    Oncogene 22:3243-51. 2003
  2. ncbi Epigenetic programming by maternal behavior
    Ian C G Weaver
    Douglas Hospital Research Center, 6875 LaSalle Blvd, , , Canada
    Nat Neurosci 7:847-54. 2004
  3. ncbi EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy
    J Guillermo Paez
    Departments of Medical Oncology and Cancer Biology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Science 304:1497-500. 2004
  4. ncbi Requirement for glycogen synthase kinase-3beta in cell survival and NF-kappaB activation
    K P Hoeflich
    Ontario Cancer Institute Princess Margaret Hospital, Toronto, Canada
    Nature 406:86-90. 2000
  5. ncbi Transcriptional silencing and longevity protein Sir2 is an NAD-dependent histone deacetylase
    S Imai
    Department of Biology, Massachusetts Institute of Technology, Cambridge 02139, USA
    Nature 403:795-800. 2000
  6. ncbi Infections with oseltamivir-resistant influenza A(H1N1) virus in the United States
    Nila J Dharan
    Epidemic Intelligence Service, Office of Workforce and Career Development Assigned to Influenza Division, Centers for Disease Control and Prevention, 1600 Clifton Rd, MS A 32, Atlanta, GA 30333, USA
    JAMA 301:1034-41. 2009
  7. ncbi Transcriptional activation of the NF-kappaB p65 subunit by mitogen- and stress-activated protein kinase-1 (MSK1)
    Linda Vermeulen
    Department of Molecular Biology, University of Gent VIB, K L Ledeganckstraat 35, B 9000 Gent, Belgium
    EMBO J 22:1313-24. 2003
  8. ncbi Involvement of caspases in proteolytic cleavage of Alzheimer's amyloid-beta precursor protein and amyloidogenic A beta peptide formation
    F G Gervais
    Department of Pharmacology, Biochemistry, and Molecular Biology, Merck Frosst Centre for Therapeutic Research, Merck Research Laboratories, Kirkland, Quebec, Canada
    Cell 97:395-406. 1999
  9. ncbi A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells
    Edgar R Wood
    Department of Computational, Analytical and Structural Sciences, GlaxoSmithKline, Inc, Research Triangle Park, North Carolina 27709, USA
    Cancer Res 64:6652-9. 2004
  10. ncbi Inhibition of histone deacetylase 6 acetylates and disrupts the chaperone function of heat shock protein 90: a novel basis for antileukemia activity of histone deacetylase inhibitors
    Purva Bali
    Department of Interdisciplinary Oncology, H Lee Moffitt Cancer Center, Tampa, Florida 33612, USA
    J Biol Chem 280:26729-34. 2005

Research Grants

  1. An Aldosterone-Endothelin Feedback Mechanism on Sodium Homeostasis
    CHARLES S contact WINGO; Fiscal Year: 2010
  2. Nanoliter Lab-on-a-chip for Protein Crystallization
    Vamsee Pamula; Fiscal Year: 2007
  3. Pharmacogenetics and Cardiovascular Events
    Bruce Psaty; Fiscal Year: 2006
  4. Mechanism of Arsenic-Induced Diabetes
    Miroslav Styblo; Fiscal Year: 2002
  5. Improving Outcomes in Diabetic Nephropathy
    Robert Toto; Fiscal Year: 2003
  6. HE3 MR Diffusion & Low Dose CT Quantitation of Emphysema
    David Gierada; Fiscal Year: 2005
  7. Phase III Trial of Minocycline in ALS:I-Clinical Center
    Paul Gordon; Fiscal Year: 2006
  8. Phase III Trial of Minocycline in ALS:I-Clinical Center
    Paul Gordon; Fiscal Year: 2007
  9. REGULATION OF HEME OXYGENASE IN NEONATAL ANIMALS
    David Stevenson; Fiscal Year: 2001
  10. Flavoenzymes in Pyrimidine Metabolism
    Bruce A Palfey; Fiscal Year: 2010

Detail Information

Publications261 found, 100 shown here

  1. ncbi Role of NF-kappaB and Akt/PI3K in the resistance of pancreatic carcinoma cell lines against gemcitabine-induced cell death
    Alexander Arlt
    1Laboratory of Molecular Gastroenterology and Hepatology, 1st Department of Medicine, University of Kiel, Germany
    Oncogene 22:3243-51. 2003
    ....
  2. ncbi Epigenetic programming by maternal behavior
    Ian C G Weaver
    Douglas Hospital Research Center, 6875 LaSalle Blvd, , , Canada
    Nat Neurosci 7:847-54. 2004
    ..Thus we show that an epigenomic state of a gene can be established through behavioral programming, and it is potentially reversible...
  3. ncbi EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy
    J Guillermo Paez
    Departments of Medical Oncology and Cancer Biology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Science 304:1497-500. 2004
    ..These results suggest that EGFR mutations may predict sensitivity to gefitinib...
  4. ncbi Requirement for glycogen synthase kinase-3beta in cell survival and NF-kappaB activation
    K P Hoeflich
    Ontario Cancer Institute Princess Margaret Hospital, Toronto, Canada
    Nature 406:86-90. 2000
    ..Thus, GSK-3beta facilitates NF-kappaB function...
  5. ncbi Transcriptional silencing and longevity protein Sir2 is an NAD-dependent histone deacetylase
    S Imai
    Department of Biology, Massachusetts Institute of Technology, Cambridge 02139, USA
    Nature 403:795-800. 2000
    ..These findings provide a molecular framework of NAD-dependent histone deacetylation that connects metabolism, genomic silencing and ageing in yeast and, perhaps, in higher eukaryotes...
  6. ncbi Infections with oseltamivir-resistant influenza A(H1N1) virus in the United States
    Nila J Dharan
    Epidemic Intelligence Service, Office of Workforce and Career Development Assigned to Influenza Division, Centers for Disease Control and Prevention, 1600 Clifton Rd, MS A 32, Atlanta, GA 30333, USA
    JAMA 301:1034-41. 2009
    ..Early surveillance data suggest that the prevalence of oseltamivir resistance among A(H1N1) viruses will most likely be higher during the 2008-2009 season...
  7. ncbi Transcriptional activation of the NF-kappaB p65 subunit by mitogen- and stress-activated protein kinase-1 (MSK1)
    Linda Vermeulen
    Department of Molecular Biology, University of Gent VIB, K L Ledeganckstraat 35, B 9000 Gent, Belgium
    EMBO J 22:1313-24. 2003
    ..This effect represents, together with phosphorylation of nucleosome components such as histone H3, an essential step leading to selective transcriptional activation of NF-kappaB-dependent gene expression...
  8. ncbi Involvement of caspases in proteolytic cleavage of Alzheimer's amyloid-beta precursor protein and amyloidogenic A beta peptide formation
    F G Gervais
    Department of Pharmacology, Biochemistry, and Molecular Biology, Merck Frosst Centre for Therapeutic Research, Merck Research Laboratories, Kirkland, Quebec, Canada
    Cell 97:395-406. 1999
    ..Caspases thus appear to play a dual role in proteolytic processing of APP and the resulting propensity for A beta peptide formation, as well as in the ultimate apoptotic death of neurons in Alzheimer's disease...
  9. ncbi A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells
    Edgar R Wood
    Department of Computational, Analytical and Structural Sciences, GlaxoSmithKline, Inc, Research Triangle Park, North Carolina 27709, USA
    Cancer Res 64:6652-9. 2004
    ..The differences in the off-rates of these drugs and the ability of GW572016 to inhibit ErbB-2 can be explained by the enzyme-inhibitor structures...
  10. ncbi Inhibition of histone deacetylase 6 acetylates and disrupts the chaperone function of heat shock protein 90: a novel basis for antileukemia activity of histone deacetylase inhibitors
    Purva Bali
    Department of Interdisciplinary Oncology, H Lee Moffitt Cancer Center, Tampa, Florida 33612, USA
    J Biol Chem 280:26729-34. 2005
    ..Depletion of HDAC6 sensitized human leukemia cells to HAA-HDIs and proteasome inhibitors...
  11. ncbi Acetylation of the C terminus of Ku70 by CBP and PCAF controls Bax-mediated apoptosis
    Haim Y Cohen
    Department of Pathology, Harvard Medical School, 77 Avenue Louis Pasteur, Boston, MA 02115 USA
    Mol Cell 13:627-38. 2004
    ..We demonstrate that increased acetylation of Ku70 disrupts the Ku70-Bax interaction and coincides with cytoplasmic accumulation of CBP. These results shed light on the role of acetyltransferases as tumor suppressors...
  12. ncbi SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase
    B L Bennett
    Signal Research Division, Celgene Corporation, 5555 Oberlin Drive, San Diego, CA 92121 USA
    Proc Natl Acad Sci U S A 98:13681-6. 2001
    ..Our study supports targeting JNK as an important strategy in inflammatory disease, apoptotic cell death, and cancer...
  13. ncbi New insights on the use of desipramine as an inhibitor for acid ceramidase
    Saeed Elojeimy
    Department of Microbiology and Immunology, Medical University of South Carolina, P.O. Box 250504, 173 Ashley Avenue, Charleston, SC 29425, USA
    FEBS Lett 580:4751-6. 2006
    ..This study reveals a new mechanism of action for desipramine...
  14. ncbi ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models
    Cherrie K Donawho
    Abbott Laboratories, Abbott Park, Illinois 60064 6074, USA
    Clin Cancer Res 13:2728-37. 2007
    ..To evaluate the preclinical pharmacokinetics and antitumor efficacy of a novel orally bioavailable poly(ADP-ribose) polymerase (PARP) inhibitor, ABT-888...
  15. ncbi Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells
    P A Marks
    Cell Biology Program, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA
    J Natl Cancer Inst 92:1210-6. 2000
    ..The hydroxamic acid-based HPCs are potentially effective agents for cancer therapy and, possibly, cancer chemoprevention...
  16. ncbi The specificities of protein kinase inhibitors: an update
    Jenny Bain
    Division of Signal Transduction Therapy, School of Life Sciences, MSI/WTB Complex, University of Dundee, Dow Street, Dundee DD1 5EH, Scotland, UK
    Biochem J 371:199-204. 2003
    ..33 microM) and p38-regulated/activated kinase (PRAK; IC(50)=1.0 microM)...
  17. ncbi 11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response
    Jeremy W Tomlinson
    Endocrinology, Division of Medical Sciences, University of Birmingham, Queen Elizabeth Hospital, Edgbaston, Birmingham, B15 2TH, UK
    Endocr Rev 25:831-66. 2004
    ..Therapeutic inhibition of 11beta-HSD1 reductase activity in patients with obesity and the metabolic syndrome, as well as in glaucoma and osteoporosis, remains an exciting prospect...
  18. ncbi Role of phosphatidylinositol 3-kinase and Rab5 effectors in phagosomal biogenesis and mycobacterial phagosome maturation arrest
    R A Fratti
    Department of Microbiology and Immunology, University of Michigan Medical School, Ann Arbor, MI 48109, USA
    J Cell Biol 154:631-44. 2001
    ..tuberculosis. This study also identifies mycobacterial phosphoinositides as products with specialized toxic properties, interfering with discrete trafficking stages in phagosomal maturation...
  19. ncbi Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors
    Roberto T Bossi
    Nerviano Medical Sciences S r l, Viale Pasteur 10, 20014 Nerviano MI, Italy
    Biochemistry 49:6813-25. 2010
    ..Finally, mapping of the activating mutations associated with neuroblastoma onto our structures may explain the roles these residues have in the activation process...
  20. ncbi High level soluble production of functional ribonuclease inhibitor in Escherichia coli by fusing it to soluble partners
    Wanhua Guo
    Department of Nuclear Medicine, Nanjing University, Nanjing 210008, People s Republic of China
    Protein Expr Purif 77:185-92. 2011
    ..And a convenient two-step immobilized metal affinity chromatography (IMAC) method has been implemented in our study, comparing with the traditional RNase A affinity chromatography method...
  21. ncbi Activity of any class IA PI3K isoform can sustain cell proliferation and survival
    Lazaros C Foukas
    Centre for Cell Signalling, Institute of Cancer, Queen Mary University of London, London EC1M 6BQ, United Kingdom
    Proc Natl Acad Sci U S A 107:11381-6. 2010
    ..Such functional redundancy of class IA PI3K isoforms upon sustained PI3K inhibition has implications for the development and use of PI3K inhibitors in cancer...
  22. ncbi Gilenya (FTY720) inhibits acid sphingomyelinase by a mechanism similar to tricyclic antidepressants
    Glyn Dawson
    Department of Pediatrics, University of Chicago, Chicago, IL 60637, USA
    Biochem Biophys Res Commun 404:321-3. 2011
    ....
  23. ncbi Histone deacetylase inhibitors induce remission in transgenic models of therapy-resistant acute promyelocytic leukemia
    L Z He
    Molecular Biology Program and Department of Pathology, Memorial Sloan-Kettering Cancer Center, Sloan-Kettering Division, Graduate School of Medical Sciences, Cornell University, New York, New York 10021, USA
    J Clin Invest 108:1321-30. 2001
    ..In vivo, HDACIs induced accumulation of acetylated histones in target organs. Strikingly, this combination of agents induced leukemia remission and prolonged survival, without apparent toxic side effects...
  24. ncbi Transcriptional repression by the methyl-CpG-binding protein MeCP2 involves a histone deacetylase complex
    X Nan
    Institute of Cell and Molecular Biology, University of Edinburgh, UK
    Nature 393:386-9. 1998
    ..The data suggest that two global mechanisms of gene regulation, DNA methylation and histone deacetylation, can be linked by MeCP2...
  25. ncbi Pharmacological inhibition of glucosylceramide synthase enhances insulin sensitivity
    Johannes M Aerts
    Department of Medical Biochemistry, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands
    Diabetes 56:1341-9. 2007
    ....
  26. ncbi Curcumin, a novel p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription
    Karanam Balasubramanyam
    Transcription and Disease Laboratory, Molecular Biology and Genetics Unit, Jawaharlal Nehru Centre for Advanced Scientific Research, Jakkur, Bangalore, 560064, India
    J Biol Chem 279:51163-71. 2004
    ..Thus, non-toxic curcumin, which targets p300/CBP, may serve as a lead compound in combinatorial HIV therapeutics...
  27. ncbi HDAC6, at the crossroads between cytoskeleton and cell signaling by acetylation and ubiquitination
    C Boyault
    INSERM, U823, Equipe Epigénétique et Signalisation Cellulaire, Institut Albert Bonniot, Universite Joseph Fourier, Domaine de la Merci, Grenoble, La Tronche Cedex, France
    Oncogene 26:5468-76. 2007
    ....
  28. ncbi STIM1, an essential and conserved component of store-operated Ca2+ channel function
    Jack Roos
    Torrey Pines Therapeutics, Inc, La Jolla, CA 92037, USA
    J Cell Biol 169:435-45. 2005
    ..We propose that STIM1, a ubiquitously expressed protein that is conserved from Drosophila to mammalian cells, plays an essential role in SOC influx and may be a common component of SOC and CRAC channels...
  29. ncbi Chromatin-modifying agents permit human hematopoietic stem cells to undergo multiple cell divisions while retaining their repopulating potential
    Hiroto Araki
    Section of Hematology Oncology, Department of Medicine, University of Illinois at Chicago, 909 S Wolcott Avenue, Chicago, IL 60612, USA
    Blood 109:3570-8. 2007
    ..These data indicate that HSC treated with chromatin-modifying agents are capable of undergoing repeated cell divisions in vitro while retaining their marrow-repopulating potential...
  30. ncbi Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    ChemMedChem 5:1026-44. 2010
    ..Comparison of the publicly available X-ray crystal structures of human 11beta-HSD1 led to docking studies of the potent compounds, revealing how these molecules may interact with the enzyme and cofactor...
  31. ncbi Dichloroacetate induces apoptosis and cell-cycle arrest in colorectal cancer cells
    B M Madhok
    Section of Translational Anaesthesia and Surgery, University of Leeds, Level 7 Clinical Sciences Building, St James s University Hospital, Leeds, UK
    Br J Cancer 102:1746-52. 2010
    ..Our aim was to determine if switching metabolism from glycolysis towards mitochondrial respiration would reduce growth preferentially in colorectal cancer cells over normal cells, and to examine the underlying mechanisms...
  32. ncbi Endocrine resistance associated with activated ErbB system in breast cancer cells is reversed by inhibiting MAPK or PI3K/Akt signaling pathways
    Sandra E Ghayad
    Universite de Lyon, France
    Int J Cancer 126:545-62. 2010
    ..In conclusion, the combination of MAPK and PI3K inhibitors represents a promising strategy to overcome endocrine therapy resistance in ER+ breast cancer patients...
  33. ncbi Reactive oxygen species, antioxidants, and the mammalian thioredoxin system
    J Nordberg
    Medical Nobel Institute for Biochemistry, Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden
    Free Radic Biol Med 31:1287-312. 2001
    ..Dinitrohalobenzenes constitute a unique class of immunostimulatory TrxR inhibitors and we consider the immunomodulatory effects of dinitrohalobenzene compounds in view of their reactions with the Trx system...
  34. ncbi Antizyme inhibitor: mysterious modulator of cell proliferation
    U Mangold
    Program in Vascular Biology, Children s Hospital, Karp Family Building, 1 Blackfan Circle, Boston, Massachusetts 02115, USA
    Cell Mol Life Sci 63:2095-101. 2006
    ..AZI inactivates all members of the antizyme family, reactivates ODC and prevents the proteolytic degradation of ODC, which may suggest a role for AZI in tumor progression...
  35. ncbi Growth inhibition of human malignant glioma cells induced by the PI3-K-specific inhibitor
    Takashi Shingu
    Department of Biochemistry and Neurosurgery, Shimane Medical University, Izumo, Japan
    J Neurosurg 98:154-61. 2003
    ..The authors examined the effects of the PI3-K inhibitor 2-(4-morpholinyl)-8-phenylchromone (LY294002) on human malignant glioma cells, and compared these effects on PTEN-deficient cells with those on PTEN-wild-type (PTEN-wt) cells...
  36. ncbi Src is the kinase of the Helicobacter pylori CagA protein in vitro and in vivo
    Matthias Selbach
    , Abt. Molekulare Biologie, Schumannstrasse 20/21, D-10117 Berlin, Germany
    J Biol Chem 277:6775-8. 2002
    ....
  37. ncbi Apocynin is not an inhibitor of vascular NADPH oxidases but an antioxidant
    Sabine Heumüller
    Institut für Kardiovaskuläre Physiologie, Johann Wolfgang Goethe Universitat, Theodor Stern Kai 7, D 60596 Frankfurt am Main, Germany
    Hypertension 51:211-7. 2008
    ..These observations indicate that apocynin predominantly acts as an antioxidant in endothelial cells and vascular smooth muscle cells and should not be used as an NADPH oxidase inhibitor in vascular systems...
  38. ncbi Phase 1 and pharmacologic study of MS-275, a histone deacetylase inhibitor, in adults with refractory and relapsed acute leukemias
    Ivana Gojo
    University of Maryland Marlene and Stewart Greenebaum Cancer Center, Baltimore, MD 21201, USA
    Blood 109:2781-90. 2007
    ..No responses by classical criteria were seen. Our results show that MS-275 effectively inhibits HDAC in vivo in patients with advanced myeloid leukemias and should be further tested, preferably in patients with less-advanced disease...
  39. ncbi Histone deacetylase inhibitors arrest polyglutamine-dependent neurodegeneration in Drosophila
    J S Steffan
    Department of Psychiatry and Human Behavior, Gillespie 2121, University of California, Irvine, California 92697, USA
    Nature 413:739-43. 2001
    ..These findings raise the possibility that therapy with HDAC inhibitors may slow or prevent the progressive neurodegeneration seen in Huntington's disease and other polyglutamine-repeat diseases, even after the onset of symptoms...
  40. ncbi Targeting mitochondrial glutaminase activity inhibits oncogenic transformation
    Jian Bin Wang
    Department of Molecular Medicine, Cornell University, Ithaca, NY 14853, USA
    Cancer Cell 18:207-19. 2010
    ..These findings highlight a previously unappreciated connection between Rho GTPase activation and cellular metabolism and demonstrate that targeting glutaminase activity can inhibit oncogenic transformation...
  41. ncbi Induction of the mitochondrial permeability transition mediates the killing of HeLa cells by staurosporine
    M Tafani
    Department of Pathology, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
    Cancer Res 61:2459-66. 2001
    ..Phosphorylation of Bad prevents Bax translocation. Caspases participate in the events related to cell killing that occur subsequent to induction of the MPT...
  42. ncbi Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors
    Stanley F Barnett
    Department of Cancer Research, Merck and Company, Sumneytown Pike, West Point, PA 19454, USA
    Biochem J 385:399-408. 2005
    ....
  43. ncbi Natural products as alpha-amylase and alpha-glucosidase inhibitors and their hypoglycaemic potential in the treatment of diabetes: an update
    R Tundis
    Department of Pharmaceutical Sciences, Faculty of Pharmacy, Nutrition and Health Sciences, University of Calabria, 87036 I Rende CS, Italy
    Mini Rev Med Chem 10:315-31. 2010
    ..This article reviews recent data on plant extracts and isolated natural compounds that are being tested for their hypglycaemic activity, highlights ongoing research and considers the future persepctives...
  44. ncbi The 11-beta-hydroxysteroid dehydrogenase type 1 inhibitor INCB13739 improves hyperglycemia in patients with type 2 diabetes inadequately controlled by metformin monotherapy
    Julio Rosenstock
    Dallas Diabetes and Endocrine Center at Medical City, Dallas, Texas, USA
    Diabetes Care 33:1516-22. 2010
    ..The efficacy and safety of the 11betaHSD1 inhibitor INCB13739 were assessed when added to ongoing metformin monotherapy in patients with type 2 diabetes exhibiting inadequate glycemic control (A1C 7-11%)...
  45. ncbi Nutrient sensor O-GlcNAc transferase regulates breast cancer tumorigenesis through targeting of the oncogenic transcription factor FoxM1
    S A Caldwell
    Department of Biochemistry and Molecular Biology, Drexel University College of Medicine, Philadelphia, PA, USA
    Oncogene 29:2831-42. 2010
    ..These findings identify O-GlcNAc as a novel mechanism through which alterations in glucose metabolism regulate cancer growth and invasion and suggest that OGT may represent novel therapeutic targets for breast cancer...
  46. ncbi Antizyme and antizyme inhibitor, a regulatory tango
    Chaim Kahana
    Department of Molecular Genetics, The Weizmann Institute of Science, 76100 Rehovot, Israel
    Cell Mol Life Sci 66:2479-88. 2009
    ....
  47. ncbi Characterization of the fatty acid amide hydrolase inhibitor cyclohexyl carbamic acid 3'-carbamoyl-biphenyl-3-yl ester (URB597): effects on anandamide and oleoylethanolamide deactivation
    Darren Fegley
    Department of Pharmacology, University of California, Irvine CA 92697-4625, USA
    J Pharmacol Exp Ther 313:352-8. 2005
    ..The results also suggest that an enzyme distinct from FAAH catalyzes OEA hydrolysis in the duodenum, where this lipid substance acts as a local satiety factor...
  48. ncbi Effects of chronic exposure to cocaine are regulated by the neuronal protein Cdk5
    J A Bibb
    Laboratory of Molecular and Cellular Neuroscience, The Rockefeller University, 1230 York Avenue, New York, New York 10021, USA
    Nature 410:376-80. 2001
    ..Our results suggest that changes in Cdk5 levels mediated by DeltaFosB, and resulting alterations in signalling involving D1 dopamine receptors, contribute to adaptive changes in the brain related to cocaine addiction...
  49. ncbi Discovery and evaluation of inhibitors of human sphingosine kinase
    Kevin J French
    Department of Pharmacology, Penn State College of Medicine, Hershey, Pennsylvania 17033, USA
    Cancer Res 63:5962-9. 2003
    ..These compounds are the first examples of nonlipid inhibitors of SK with in vivo antitumor activity and so provide leads for additional development of inhibitors of this important molecular target...
  50. ncbi Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes
    Christopher Fotsch
    Department of Medicinal Chemistry, Amgen Inc, Thousand Oaks, California 91320, USA
    J Med Chem 51:4851-7. 2008
  51. ncbi Phase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphoma
    Qin C Ryan
    Clinical Trials Unit, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Bethesda, MD, USA
    J Clin Oncol 23:3912-22. 2005
    ..Histone deacetylase inhibition was observed in peripheral-blood mononuclear-cells. Based on PK data from the q14-day schedule, a more frequent dosing schedule, weekly x 4, repeated every 6 weeks is presently being evaluated...
  52. ncbi Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors
    Giorgio Tarzia
    Istituto di Chimica Farmaceutica e Tossicologica, , Piazza del Rinascimento 6, Italy
    J Med Chem 46:2352-60. 2003
    ..URB524 (N-cyclohexylcarbamic acid biphenyl-3-yl ester, 9g) is the most potent compound of the series (IC(50) = 63 nM) and was therefore selected for further optimization...
  53. ncbi Long-term treatment with novel glycogen synthase kinase-3 inhibitor improves glucose homeostasis in ob/ob mice: molecular characterization in liver and muscle
    Oksana Kaidanovich-Beilin
    Department of Human Genetics and Molecular Medicine, Sackler School of Medicine, Tel-Aviv University, Tel-Aviv 69978, Israel
    J Pharmacol Exp Ther 316:17-24. 2006
    ..Our studies show that long-term treatment with GSK-3 inhibitor improves glucose homeostasis in ob/ob mice and demonstrates a novel role of GSK-3 in regulating hepatic CREB activity and expression of muscle GLUT4...
  54. ncbi Topoisomerase I inhibitors: camptothecins and beyond
    Yves Pommier
    Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland, 20892 4255, USA
    Nat Rev Cancer 6:789-802. 2006
    ....
  55. ncbi Regulation of Akt and glycogen synthase kinase-3 beta phosphorylation by sodium valproate and lithium
    Patrizia De Sarno
    Department of Psychiatry and Behavioral Neurobiology, Sparks Center 1057, University of Alabama at Birmingham, Birmingham, AL 35294-0017, USA
    Neuropharmacology 43:1158-64. 2002
    ....
  56. ncbi Manipulation of alternative splicing by a newly developed inhibitor of Clks
    Michiko Muraki
    Laboratory of Gene Expression, School of Biomedical Science, Department of Functional Genomics, Medical Research Institute, Tokyo Medical and Dental University, Japan
    J Biol Chem 279:24246-54. 2004
    ....
  57. ncbi Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
    Jeffrey F Ohren
    Department of Discovery Technologies, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA
    Nat Struct Mol Biol 11:1192-7. 2004
    ..Thus, the structures reported here reveal a novel, noncompetitive mechanism for protein kinase inhibition...
  58. ncbi Phosphorylation of p38 MAPK induced by oxidative stress is linked to activation of both caspase-8- and -9-mediated apoptotic pathways in dopaminergic neurons
    Won Seok Choi
    Department of Biology and Protein Network Research Center, Yonsei University College of Science, 134 Shinchon dong, Seodaemoon Gu, Seoul 120 749, Korea
    J Biol Chem 279:20451-60. 2004
    ....
  59. ncbi Ras family signaling: therapeutic targeting
    Adrienne D Cox
    University of North Carolina at Chapel Hill, North Carolina 27599, USA
    Cancer Biol Ther 1:599-606. 2002
    ..We review the current status of anti-Ras drug development, issues that have complicated their progression to the clinic, and possible future strategies for targeting Ras...
  60. ncbi Genetic knockout and pharmacologic inhibition of neuronal nitric oxide synthase attenuate nerve injury-induced mechanical hypersensitivity in mice
    Yun Guan
    Department of Anesthesiology and Critical Care Medicine, Johns Hopkins University School of Medicine, 355 Ross, 720 Rutland Ave, Baltimore, Maryland 21205, USA
    Mol Pain 3:29. 2007
    ..Our findings suggest that nNOS, especially in the dorsal root ganglion, may participate in the development and/or maintenance of mechanical hypersensitivity after nerve injury...
  61. ncbi Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?
    S Leclerc
    CNRS, Cell Cycle Group, Station Biologique, BP 74, Roscoff 29682 Cedex, Bretagne, France
    J Biol Chem 276:251-60. 2001
    ..Indirubins constitute the first family of low nanomolar inhibitors of GSK-3 beta to be described...
  62. ncbi Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death
    D A Cross
    Neurology Centre of Excellence in Drug Discovery, GlaxoSmithKline Pharmaceuticals, Harlow, Essex, UK
    J Neurochem 77:94-102. 2001
    ....
  63. ncbi Crystal structures of oseltamivir-resistant influenza virus neuraminidase mutants
    Patrick J Collins
    MRC National Institute for Medical Research, Mill Hill, London NW7 1AA, UK
    Nature 453:1258-61. 2008
    ..7) and H1N1 (ref. 8) viruses with neuraminidases carrying these mutations, our results indicate that it would be prudent for pandemic stockpiles of oseltamivir to be augmented by additional antiviral drugs, including zanamivir...
  64. ncbi Chitinases and chitinase-like proteins: potential therapeutic targets for the treatment of T-helper type 2 allergies
    T E Sutherland
    Ashworth Laboratories, Institute of Immunology and Infection Research, University of Edinburgh, Edinburgh, UK
    Clin Exp Allergy 39:943-55. 2009
    ..chitinase inhibition leads to an attenuated allergic response, several strategies are being used to develop enzyme inhibitors for therapeutic use in human diseases...
  65. ncbi Phase II open label study of valproic acid in spinal muscular atrophy
    Kathryn J Swoboda
    Departments of Neurology, Pediatrics, Neonatology and General Clinical Research Center, University of Utah School of Medicine, Salt Lake City, Utah, United States of America
    PLoS ONE 4:e5268. 2009
    ..TRIAL REGISTRATION: ClinicalTrials.gov...
  66. ncbi Phosphoinositide signalling in cancer: beyond PI3K and PTEN
    Tom D Bunney
    The Institute of Cancer Research, Section for Cell and Molecular Biology, Chester Beatty Laboratories, Fulham Road, London SW3 6JB, UK
    Nat Rev Cancer 10:342-52. 2010
    ..Studies of these enzymes are providing new insights into the mechanisms and the extent of their involvement in cancer, highlighting new potential targets for therapeutic intervention...
  67. ncbi 11beta-hydroxysteroid dehydrogenase type 1 and obesity
    Nicholas M Morton
    Endocrinology Unit, Centre for Cardiovascular Sciences, Queens Medical Research Institute, Edinburgh University, Edinburgh, UK
    Front Horm Res 36:146-64. 2008
    ....
  68. ncbi Poly(ADP-ribose) polymerase gene disruption renders mice resistant to cerebral ischemia
    M J Eliasson
    Department of Pharmacology and Molecular Science, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
    Nat Med 3:1089-95. 1997
    ....
  69. ncbi Radiation-induced cell cycle arrest compromised by p21 deficiency
    J Brugarolas
    Howard Hughes Medical Institute, Massachusetts Institute of Technology, Cambridge 02139, USA
    Nature 377:552-7. 1995
    ..However, p21-/- mouse embryo fibroblasts are impaired in their ability to undergo G1 arrest following DNA damage...
  70. ncbi Development of anaplastic lymphoma kinase (ALK) small-molecule inhibitors for cancer therapy
    Rongshi Li
    High Throughput Medicinal Chemistry, ChemBridge Research Laboratories, 16981 Via Tazon, Suites K, San Diego, California 92127, USA
    Med Res Rev 28:372-412. 2008
    ....
  71. ncbi Protective effects of the urocortin homologues stresscopin (SCP) and stresscopin-related peptide (SRP) against hypoxia/reoxygenation injury in rat neonatal cardiomyocytes
    A Chanalaris
    Medical Molecular Biology Unit, Institute of Child Health, University College London, 30 Guilford Street, London WC1N 1EH, UK
    J Mol Cell Cardiol 35:1295-305. 2003
    ..In addition, we showed that SCP and UCN are potent activators of the p42/44 MAPK pathway, with SRP able to induce phosphorylation of p42/44 MAPK as well, albeit not as pronounced...
  72. ncbi Calcium/calmodulin-dependent protein kinase II binds to Raf-1 and modulates integrin-stimulated ERK activation
    Maddalena Illario
    Dipartimento di Biologia e Patologia Cellulare e Molecolare, Universita Federico II, Napoli, 80131 Italy
    J Biol Chem 278:45101-8. 2003
    ..These findings also provide evidence supporting the possible existence of cross-talk between other intracellular pathways involving CaMKII and Raf-1...
  73. ncbi Nitric oxide-mediated promotion of mammary tumour cell migration requires sequential activation of nitric oxide synthase, guanylate cyclase and mitogen-activated protein kinase
    Lorraine C Jadeski
    Department of Anatomy and Cell Biology, The University of Western Ontario, London, Ontario, Canada
    Int J Cancer 106:496-504. 2003
    ..Since NOS activity is positively associated with human breast cancer progression, the present results are relevant for development of therapeutic modalities for this disease...
  74. ncbi LPS regulate ERK1/2-dependent signaling in cardiac fibroblasts via PKC-mediated MKP-1 induction
    Philipp Stawowy
    Department of Medicine/Cardiology, Deutsches Herzzentrum Berlin, Augustenburger Platz 1, D-13353 Berlin, Germany
    Biochem Biophys Res Commun 303:74-80. 2003
    ..This might be relevant with regard to the decreased MAPK activity and increased levels in MKPs reported during chronic heart failure in humans...
  75. ncbi Olanzapine produces trophic effects in vitro and stimulates phosphorylation of Akt/PKB, ERK1/2, and the mitogen-activated protein kinase p38
    Xiao-Hong Lu
    Department of Pharmacology, LSU Health Sciences Center, Shreveport, LA 71130, USA
    Brain Res 1011:58-68. 2004
    ..Other antipsychotic drugs stimulated phosphorylation of a subset of the kinase panel, but not all three kinases. The present findings demonstrate that olanzapine has both mitogenic and neuroprotective effects in neuronal cells...
  76. ncbi Transforming growth factor-alpha attenuates N-methyl-D-aspartic acid toxicity in cortical cultures by preventing protein synthesis inhibition through an Erk1/2-dependent mechanism
    Valerie Petegnief
    Departament de Farmacologia i Toxicologia, Institut d Investigacions Biomediques de Barcelona, CSIC IDIBAPS, Spain
    J Biol Chem 278:29552-9. 2003
    ....
  77. ncbi NMDA-induced phosphorylation of the microtubule-associated protein MAP-2 is mediated by activation of nitric oxide synthase and MAP kinase
    M Llansola
    Laboratory of Neurobiology, Instituto de Investigaciones Citologicas, , Amadeo de Saboya, 4. 46010 Valencia, Spain
    Eur J Neurosci 13:1283-91. 2001
    ..The interplay between NMDA receptors-associated signal transduction pathways and MAP-2 may be involved in the modulation of neuronal responses to extracellular signals and in the regulation of neuronal function...
  78. ncbi Ouabain is a potent promoter of growth and activator of ERK1/2 in ouabain-resistant rat renal epithelial cells
    Renata I Dmitrieva
    Institute of Molecular Medicine, University of Texas Health Science Center at Houston, Houston, Texas 77030, USA
    J Biol Chem 278:28160-6. 2003
    ..These results indicate that renal epithelial cells may be a sensitive target of the ERK1/2-activating and growth-promoting effects of ouabain even in the presence of ouabain-resistant Na+, K+-ATPase...
  79. ncbi Regulation of insulin gene transcription by ERK1 and ERK2 in pancreatic beta cells
    Shih Khoo
    Department of Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    J Biol Chem 278:32969-77. 2003
    ..Phosphorylation increases their functional activity and results in a cumulative transactivation of the promoter. Thus, ERK1/2 act at multiple points to transduce a glucose signal to insulin gene transcription...
  80. ncbi Bombesin and substance P analogues differentially regulate G-protein coupling to the bombesin receptor. Direct evidence for biased agonism
    A C MacKinnon
    Rayne Laboratory, Centre for Inflammation Research, Respiratory Medicine Unit, University of Edinburgh Medical School, Teviot Place, Edinburgh, EH8 9AG, United Kingdom
    J Biol Chem 276:28083-91. 2001
    ..This validation of the concept of biased agonism has important implications in the development of novel pharmacological agents to dissect receptor-mediated signal transduction and of highly selective drugs to treat human disease...
  81. ncbi Role of p38 mitogen-activated protein kinase (p38 MAPK) in cytokine-induced rat islet cell apoptosis
    J Saldeen
    Department of Medical Cell Biology, Uppsla University, Biomedicum, P O Box 571, S 751 23 Uppsala, Sweden
    Biochem Pharmacol 61:1561-9. 2001
    ..In conclusion, cytokine-induced p38 activation participates in beta-cell apoptosis, possibly by a nitric oxide-independent mechanism or by enhancing the sensitivity to nitric oxide...
  82. ncbi Activation of the pro-survival phosphatidylinositol 3-kinase/AKT pathway by transforming growth factor-beta1 in mesenchymal cells is mediated by p38 MAPK-dependent induction of an autocrine growth factor
    Jeffrey C Horowitz
    Department of Medicine, University of Michigan Medical Center, Ann Arbor, Michigan 48109, USA
    J Biol Chem 279:1359-67. 2004
    ....
  83. ncbi Temporal control of NF-kappaB activation by ERK differentially regulates interleukin-1beta-induced gene expression
    Bingbing Jiang
    Whitaker Cardiovascular Institute, Department of Medicine, Boston University School of Medicine, Boston, Massachusetts 02118, USA
    J Biol Chem 279:1323-9. 2004
    ..These results reveal a novel functional role for ERK as an important temporal regulator of NF-kappaB activation and NF-kappaB-dependent gene expression...
  84. ncbi Chronic stimulation of D1 dopamine receptors in human SK-N-MC neuroblastoma cells induces nitric-oxide synthase activation and cytotoxicity
    Jun Chen
    Department of Pediatrics, Georgetown University, Washington, DC 20007, USA
    J Biol Chem 278:28089-100. 2003
    ..These data demonstrate a novel pathway of dopamine-mediated postsynaptic oxidative stress and cell death through direct activation of NOS enzymes by D1 dopamine receptors and its associated signaling pathways...
  85. ncbi Insulin receptor substrate-1/SHP-2 interaction, a phenotype-dependent switching machinery of insulin-like growth factor-I signaling in vascular smooth muscle cells
    Ken ichiro Hayashi
    Department of Neuroscience D13, Osaka University Graduate School of Medicine, Yamadaoka 2 2, Suita, Osaka 565 0871, Japan
    J Biol Chem 279:40807-18. 2004
    ....
  86. ncbi A novel role of lactosylceramide in the regulation of lipopolysaccharide/interferon-gamma-mediated inducible nitric oxide synthase gene expression: implications for neuroinflammatory diseases
    Ravinder Pannu
    Department of Pediatrics, Medical University of South Carolina, Charleston, South Carolina 29425, USA
    J Neurosci 24:5942-54. 2004
    ..To our knowledge this is the first report of a role of LacCer in iNOS expression and the advantage of GSL depletion in attenuating post-SCI inflammation to improve the outcome of SCI...
  87. ncbi Phospholipase D isozymes mediate epigallocatechin gallate-induced cyclooxygenase-2 expression in astrocyte cells
    Shi Yeon Kim
    Department of Physiology, College of Medicine, The Catholic University of Korea, Seoul 137 701, Korea
    J Biol Chem 279:38125-33. 2004
    ..Collectively, our results demonstrate for the first time that PLD isozymes mediate EGCG-induced COX-2 expression through PKC and p38 in immortalized astroglial line and normal astrocyte cells...
  88. ncbi Erk1/2 phosphorylation and reactive oxygen species formation via nitric oxide and Akt-1/Raf-1 crosstalk in cultured rat cerebellar granule cells exposed to the organic solvent 1,2,4-trimethylcyclohexane
    Oddvar Myhre
    Norwegian Defence Research Establishment, Division for Protection and Materiel, P O Box 25, N 2027 Kjeller, Norway
    Toxicol Sci 80:296-303. 2004
    ....
  89. ncbi Effect of erythropoietin axotomy-induced apoptosis in rat retinal ganglion cells
    Jochen H Weishaupt
    Department of Neurology, , , Germany
    Invest Ophthalmol Vis Sci 45:1514-22. 2004
    ....
  90. ncbi Focal adhesion kinase in netrin-1 signaling
    Xiu Rong Ren
    Department of Pathology, University of Alabama, Birmingham, Alabama 35294, USA
    Nat Neurosci 7:1204-12. 2004
    ..Taken together, these results indicate a new signaling mechanism for DCC, in which FAK is activated upon netrin-1 stimulation and mediates netrin-1 function; they also identify a critical role for FAK in axon navigation...
  91. ncbi Arginine and Leucine regulate p70 S6 kinase and 4E-BP1 in intestinal epithelial cells
    Hidetoshi Ban
    Department of Gastroenterological Surgery, Transplant, and Surgical Oncology, Graduate School of Medicine and Dentistry, Okayama University, Okayama 700 8558, Japan
    Int J Mol Med 13:537-43. 2004
    ..In conclusion, l-Arginine regulates p70 S6 kinase activity and phosphorylation of 4E-BP1 through mTOR signaling pathway, which involves system y(+), cationic amino acid transporters...
  92. ncbi Angiotensin II differentially regulates interleukin-1-beta-inducible NO synthase (iNOS) and vascular cell adhesion molecule-1 (VCAM-1) expression: role of p38 MAPK
    Bingbing Jiang
    Whitaker Cardiovascular Institute, Vascular Biology Unit, Department of Medicine, Boston University School of Medicine, Boston, MA 02118, USA
    J Biol Chem 279:20363-8. 2004
    ....
  93. ncbi Antioxidants N-acetylcysteine (NAC) and 2-mercaptoethanol (2-ME) affect the survival and differentiative potential of cholinergic precursors from the embryonic septal nuclei and basal forebrain: involvement of ras signaling
    L Ni
    Department of Biological Sciences, Rutgers University/Newark, 101 Warren St, Newark, NJ 07102, USA
    Brain Res Dev Brain Res 130:207-16. 2001
    ..Treatment of the cultures with PD98059 to inhibit MEK returned cultures to a 'low-dose' phenotype. These data suggest that redox status of basal forebrain precursors affect both their survival and differentiative potential...
  94. ncbi Stimulation of extracellular signal-regulated kinases and proliferation in rat osteoblastic cells by parathyroid hormone is protein kinase C-dependent
    J T Swarthout
    Cell and Molecular Biology Program and the Departments of Pharmacological and Physiological Science and Orthopedic Surgery, Saint Louis University School of Medicine, St. Louis, Missouri, USA
    J Biol Chem 276:7586-92. 2001
    ..Thus, activation of ERKs and proliferation by PTH is protein kinase C-dependent, but stimulation occurs independently of the EGF receptor and Ras activation...
  95. ncbi nitric oxide triggers the phosphatidylinositol 3-kinase/Akt survival pathway in insulin-producing RINm5F cells by arousing Src to activate insulin receptor substrate-1
    Juan R Tejedo
    Laboratory of Biochemistry of the Immune System, Department of Medical Biochemistry and Molecular Biology, University of Sevilla, 41009 Sevilla, Spain
    Endocrinology 145:2319-27. 2004
    ..These data strengthen the notion that NO production at physiological levels plays a role in protection from apoptosis in pancreatic beta-cells...
  96. ncbi A constituent of green tea, epigallocatechin-3-gallate, activates endothelial nitric oxide synthase by a phosphatidylinositol-3-OH-kinase-, cAMP-dependent protein kinase-, and Akt-dependent pathway and leads to endothelial-dependent vasorelaxation
    Mario Lorenz
    Medizinische Klinik mit Schwerpunkt Kardiologie, Angiologie, Pneumologie, Charit, Campus Mitte, , Berlin D-10117, Germany
    J Biol Chem 279:6190-5. 2004
    ....
  97. ncbi Akt down-regulation of p38 signaling provides a novel mechanism of vascular endothelial growth factor-mediated cytoprotection in endothelial cells
    J P Gratton
    Department of Pharmacology and Molecular Cardiobiology Program, Boyer Center for Molecular Medicine, Yale University School of Medicine, New Haven, Connecticut 06536, USA
    J Biol Chem 276:30359-65. 2001
    ..Thus, cross-talk between the Akt and p38 MAPK pathways may regulate the level of cytoprotection versus apoptosis and is a new mechanism to explain the cytoprotective actions of Akt...
  98. ncbi Inhibition of the c-Jun N-terminal kinase signaling pathway by the mixed lineage kinase inhibitor CEP-1347 (KT7515) preserves metabolism and growth of trophic factor-deprived neurons
    Charles A Harris
    Department of Molecular Biology and Pharmacology, Washington University, St. Louis, Missouri 63110, USA
    J Neurosci 22:103-13. 2002
    ....
  99. ncbi Nitric oxide regulates cGMP-dependent cAMP-responsive element binding protein phosphorylation and Bcl-2 expression in cerebellar neurons: implication for a survival role of nitric oxide
    Elisabetta Ciani
    Department of Biology, University of Bologna, Italy
    J Neurochem 82:1282-9. 2002
    ..These results not only confirm the role of CREB in neuronal survival but also provide circumstantial evidence for a novel link among NO, CREB activation and survival...
  100. ncbi Sodium nitroprusside-induced mitochondrial apoptotic events in insulin-secreting RINm5F cells are associated with MAP kinases activation
    J C Bernabé
    Laboratory of Biochemistry of the Immune System, University of Sevilla, Spain
    Exp Cell Res 269:222-9. 2001
    ..Thus, we propose that exposure to apoptotic concentrations of NO triggers ERK- and p38-dependent cytochrome c release, caspase 3 activation, and PI3K-dependent Bcl-2 phosphorylation...
  101. ncbi Phosphorylation of extracellular signal-regulated kinase in primary afferent neurons by noxious stimuli and its involvement in peripheral sensitization
    Yi Dai
    Department of Anatomy and Neuroscience, Hyogo College of Medicine, Hyogo 663-8501, Japan
    J Neurosci 22:7737-45. 2002
    ..Thus, pERK in primary afferents by noxious stimulation in vivo showed distinct characteristics of expression and may be correlated with the functional activity of primary afferent neurons...

Research Grants75

  1. An Aldosterone-Endothelin Feedback Mechanism on Sodium Homeostasis
    CHARLES S contact WINGO; Fiscal Year: 2010
    ..This study will examine whether endothelin acts as a local inhibitory mechanism and feedback control system on the action of aldosterone. ..
  2. Nanoliter Lab-on-a-chip for Protein Crystallization
    Vamsee Pamula; Fiscal Year: 2007
    ..Recent antiviral drugs against AIDS are enzyme inhibitors, and their design was based on the detailed protein-drug interactions provided by crystal structures of the ..
  3. Pharmacogenetics and Cardiovascular Events
    Bruce Psaty; Fiscal Year: 2006
    ..products of these genes represent the sites of action for many cardiovascular drugs: angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, all classes of diuretics, alpha blockers, beta-blockers, central alpha ..
  4. Mechanism of Arsenic-Induced Diabetes
    Miroslav Styblo; Fiscal Year: 2002
    ..have shown that trivalent methylated metabolites (Mas-III and DMAs-III) are more potent cytotoxins and enzyme inhibitors than iAs-III...
  5. Improving Outcomes in Diabetic Nephropathy
    Robert Toto; Fiscal Year: 2003
    ..to ESRD despite inhibition of the renin-angiotensin-aldosterone system with angiotensin converting enzyme inhibitors (ACEIs) or angiotensin II type 1 receptor blockers (ARBs)...
  6. HE3 MR Diffusion & Low Dose CT Quantitation of Emphysema
    David Gierada; Fiscal Year: 2005
    ..proteinases in the pathogenesis of COPD is leading to searches for newer anti-inflammatory strategies and enzyme inhibitors. Though in the early stages of development, some of these new approaches may eventually provide therapy that ..
  7. Phase III Trial of Minocycline in ALS:I-Clinical Center
    Paul Gordon; Fiscal Year: 2006
    ..Caspase enzyme inhibitors and anti-inflammatory agents have been shown to slow progression in the ALS model (6,7,17,18)...
  8. Phase III Trial of Minocycline in ALS:I-Clinical Center
    Paul Gordon; Fiscal Year: 2007
    ..Caspase enzyme inhibitors and anti-inflammatory agents have been shown to slow progression in the ALS model (6,7,17,18)...
  9. REGULATION OF HEME OXYGENASE IN NEONATAL ANIMALS
    David Stevenson; Fiscal Year: 2001
    ..to address the regulation of HO transcription in culture and living animals in the presence and absence of enzyme inhibitors. This proposal contains three specific aims...
  10. Flavoenzymes in Pyrimidine Metabolism
    Bruce A Palfey; Fiscal Year: 2010
    ..The results of these studies will facilitate the design of enzyme inhibitors, which may be developed into useful drug candidates...
  11. Renin Angioensin Aldosterone System in Drub Abuse and HIV-associated Nephropathy
    Pravin C Singhal; Fiscal Year: 2010
    ..Our long term research goal is to develop strategies to slow down the progression as well as find a cure of this devastating kidney disease. ..
  12. Angiotensin II and diabetic retinopathy
    ALFONSO SCICLI; Fiscal Year: 2003
    Clinical trials suggest that Angiotensin Converting Enzyme inhibitors (ACEi) slow the progression of diabetic retinopathy...
  13. Angiotensin II and diabetic retinopathy
    ALFONSO SCICLI; Fiscal Year: 2006
    Clinical trials suggest that Angiotensin Converting Enzyme inhibitors (ACEi) slow the progression of diabetic retinopathy...
  14. A Family Partnership Intervention for Heart Failure
    Sandra Dunbar; Fiscal Year: 2009
    ..dietary sodium (24-hour urinary sodium), medication adherence to HF drugs including angiotensin converting enzyme inhibitors and diuretics (Medication Event Monitoring System), heart failure severity (brain natriuretic peptide levels)..
  15. Amidoglycosylation Reactions of Glycal Metallanitrenes
    Christian Rojas; Fiscal Year: 2007
    ..sugars, crucial molecular components and precursors in biological systems, including structural polymers, enzyme inhibitors, and cell-surface glycoproteins...
  16. Role and Relevance of Pept1 in Drug Absorption, Disposition, and Dynamics
    David E Smith; Fiscal Year: 2010
    ..g., ?-lactam antibiotics, angiotensin-converting enzyme inhibitors, antiviral nucleoside prodrugs) and potentially toxic peptidomimetics (e.g., 5-aminolevulinic acid)...
  17. Clinical Impact of Bradykinin Receptor Polymorphisms
    James Gainer; Fiscal Year: 2005
    ..a B2 receptor dependent-mechanism, is an integral contributor to the efficacy of angiotensin converting enzyme inhibitors. Animal studies suggest that genetic variation altering the regulation or function of the B2 receptor has ..
  18. ACE Inhibition and Novel Cardiovascular Risk Factors
    Marco Pahor; Fiscal Year: 2004
    Angiotensin converting enzyme inhibitors (ACE inhibitors) may prevent cardiovascular events in high risk persons and improve skeletal muscle function in heart failure patients by means of mechanisms that are independent of blood pressure ..