cyclohexanes

Summary

Summary: A group of alicyclic hydrocarbons with the general formula R-C6H11.

Top Publications

  1. pmc Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity
    Patrick Dorr
    Discovery Biology, Pfizer Global Research and Development Sandwich Laboratories, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 49:4721-32. 2005
  2. ncbi Maraviroc versus efavirenz, both in combination with zidovudine-lamivudine, for the treatment of antiretroviral-naive subjects with CCR5-tropic HIV-1 infection
    David A Cooper
    University of New South Wales, Sydney, Australia
    J Infect Dis 201:803-13. 2010
  3. pmc HIV-1 escape from the CCR5 antagonist maraviroc associated with an altered and less-efficient mechanism of gp120-CCR5 engagement that attenuates macrophage tropism
    Michael Roche
    Centers for Virology, Monash University, Australia
    J Virol 85:4330-42. 2011
  4. pmc V3 determinants of HIV-1 escape from the CCR5 inhibitors Maraviroc and Vicriviroc
    Reem Berro
    Department of Microbiology and Immunology, Weill Medical College of Cornell University, New York, NY 10065, USA
    Virology 427:158-65. 2012
  5. pmc A maraviroc-resistant HIV-1 with narrow cross-resistance to other CCR5 antagonists depends on both N-terminal and extracellular loop domains of drug-bound CCR5
    John C Tilton
    Department of Microbiology, University of Pennsylvania, 301C Johnson Pavilion, 3610 Hamilton Walk, Philadelphia, PA 19104, USA
    J Virol 84:10863-76. 2010
  6. ncbi Efficacy of short-term monotherapy with maraviroc, a new CCR5 antagonist, in patients infected with HIV-1
    Gerd Fatkenheuer
    Department of Internal Medicine, Division of Infectious Diseases, Haus 11, University of Cologne, Joseph Stelzmann Strasse 9, D 50924 Cologne, Germany
    Nat Med 11:1170-2. 2005
  7. ncbi Population-based V3 genotypic tropism assay: a retrospective analysis using screening samples from the A4001029 and MOTIVATE studies
    Rachel A McGovern
    BC Centre for Excellence in HIV AIDS, St Paul s Hospital, Vancouver, British Columbia, Canada
    AIDS 24:2517-25. 2010
  8. pmc Evaluation of the genotypic prediction of HIV-1 coreceptor use versus a phenotypic assay and correlation with the virological response to maraviroc: the ANRS GenoTropism study
    Patricia Recordon-Pinson
    Laboratoire de Virologie, CHU de Bordeaux, Bordeaux Cedex, France
    Antimicrob Agents Chemother 54:3335-40. 2010
  9. pmc Emergence of CXCR4-using human immunodeficiency virus type 1 (HIV-1) variants in a minority of HIV-1-infected patients following treatment with the CCR5 antagonist maraviroc is from a pretreatment CXCR4-using virus reservoir
    Mike Westby
    Pfizer Global Research and Development, Sandwich, United Kingdom
    J Virol 80:4909-20. 2006
  10. pmc In vitro effect of anti-human immunodeficiency virus CCR5 antagonist maraviroc on chemotactic activity of monocytes, macrophages and dendritic cells
    R Rossi
    Department of Public Health and Infectious Diseases, Istituto Pasteur Fondazione Cenci Bolognetti, Sapienza University, Rome
    Clin Exp Immunol 166:184-90. 2011

Research Grants

Detail Information

Publications316 found, 100 shown here

  1. pmc Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity
    Patrick Dorr
    Discovery Biology, Pfizer Global Research and Development Sandwich Laboratories, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 49:4721-32. 2005
    ..Clinical trials are ongoing to further investigate the potential of using maraviroc for the treatment of HIV-1 infection and AIDS...
  2. ncbi Maraviroc versus efavirenz, both in combination with zidovudine-lamivudine, for the treatment of antiretroviral-naive subjects with CCR5-tropic HIV-1 infection
    David A Cooper
    University of New South Wales, Sydney, Australia
    J Infect Dis 201:803-13. 2010
    ..The MERIT (Maraviroc versus Efavirenz in Treatment-Naive Patients) study compared maraviroc and efavirenz, both with zidovudine-lamivudine, in antiretroviral-naive patients with R5 human immunodeficiency virus type 1 (HIV-1) infection...
  3. pmc HIV-1 escape from the CCR5 antagonist maraviroc associated with an altered and less-efficient mechanism of gp120-CCR5 engagement that attenuates macrophage tropism
    Michael Roche
    Centers for Virology, Monash University, Australia
    J Virol 85:4330-42. 2011
    ....
  4. pmc V3 determinants of HIV-1 escape from the CCR5 inhibitors Maraviroc and Vicriviroc
    Reem Berro
    Department of Microbiology and Immunology, Weill Medical College of Cornell University, New York, NY 10065, USA
    Virology 427:158-65. 2012
    ..In summary, VVC and MVC trigger the evolution of distinct HIV-1 resistance patterns in V3...
  5. pmc A maraviroc-resistant HIV-1 with narrow cross-resistance to other CCR5 antagonists depends on both N-terminal and extracellular loop domains of drug-bound CCR5
    John C Tilton
    Department of Microbiology, University of Pennsylvania, 301C Johnson Pavilion, 3610 Hamilton Walk, Philadelphia, PA 19104, USA
    J Virol 84:10863-76. 2010
    ....
  6. ncbi Efficacy of short-term monotherapy with maraviroc, a new CCR5 antagonist, in patients infected with HIV-1
    Gerd Fatkenheuer
    Department of Internal Medicine, Division of Infectious Diseases, Haus 11, University of Cologne, Joseph Stelzmann Strasse 9, D 50924 Cologne, Germany
    Nat Med 11:1170-2. 2005
    ..6 log(10) copies/ml at all twice daily doses >or=100 mg. These results provide proof of concept that CCR5 antagonism is a viable antiretroviral therapeutic approach...
  7. ncbi Population-based V3 genotypic tropism assay: a retrospective analysis using screening samples from the A4001029 and MOTIVATE studies
    Rachel A McGovern
    BC Centre for Excellence in HIV AIDS, St Paul s Hospital, Vancouver, British Columbia, Canada
    AIDS 24:2517-25. 2010
    ..This analysis retrospectively examined the performance of population-based sequence analysis of HIV-1 env V3-loop to predict coreceptor tropism...
  8. pmc Evaluation of the genotypic prediction of HIV-1 coreceptor use versus a phenotypic assay and correlation with the virological response to maraviroc: the ANRS GenoTropism study
    Patricia Recordon-Pinson
    Laboratoire de Virologie, CHU de Bordeaux, Bordeaux Cedex, France
    Antimicrob Agents Chemother 54:3335-40. 2010
    ..The baseline weighted genotypic sensitivity score was associated with VR at month 6. There were strong arguments in favor of using genotypic coreceptor use assays for determining which patients would respond to CCR5 antagonist...
  9. pmc Emergence of CXCR4-using human immunodeficiency virus type 1 (HIV-1) variants in a minority of HIV-1-infected patients following treatment with the CCR5 antagonist maraviroc is from a pretreatment CXCR4-using virus reservoir
    Mike Westby
    Pfizer Global Research and Development, Sandwich, United Kingdom
    J Virol 80:4909-20. 2006
    ..Importantly, in all three patients, circulating virus reverted to predominantly CCR5 tropic following cessation of maraviroc...
  10. pmc In vitro effect of anti-human immunodeficiency virus CCR5 antagonist maraviroc on chemotactic activity of monocytes, macrophages and dendritic cells
    R Rossi
    Department of Public Health and Infectious Diseases, Istituto Pasteur Fondazione Cenci Bolognetti, Sapienza University, Rome
    Clin Exp Immunol 166:184-90. 2011
    ..The drug might have a potential role in the down-regulation of HIV-associated chronic inflammation by blocking the recirculation and trafficking of MO and MDC...
  11. pmc Maraviroc for previously treated patients with R5 HIV-1 infection
    Roy M Gulick
    Weill Cornell Medical College, New York, NY 10065, USA
    N Engl J Med 359:1429-41. 2008
    ..CC chemokine receptor 5 antagonists are a new class of antiretroviral agents...
  12. ncbi Maraviroc, a CCR5 coreceptor antagonist that blocks entry of human immunodeficiency virus type 1
    Joshua S Hunt
    University of Kentucky College of Pharmacy, University of Kentucky Medical Center, Lexington, Kentucky 40536, USA
    Pharmacotherapy 29:295-304. 2009
    ..Long-term studies with both targets are required to explore the critical issues of efficacy and immunologic safety, as the function of these coreceptors is linked to host chemokine pathways...
  13. ncbi A combination of polymorphic mutations in V3 loop of HIV-1 gp120 can confer noncompetitive resistance to maraviroc
    Yuzhe Yuan
    Department of Medical Virology, Graduate School of Medical Sciences, Kumamoto University, Honjo 1 1 1, Kumamoto 860 8665, Japan
    Virology 413:293-9. 2011
    ..This type of library virus is useful for isolation of escape viruses from effective entry inhibitors...
  14. pmc An altered and more efficient mechanism of CCR5 engagement contributes to macrophage tropism of CCR5-using HIV-1 envelopes
    Jasminka Sterjovski
    Center for Virology, Burnet Institute, Melbourne, Victoria, Australia
    Virology 404:269-78. 2010
    ..Thus, enhanced gp120-CCR5 interactions may contribute to M-tropism of R5 HIV-1 strains through different structural mechanisms...
  15. ncbi Lack of short-term increase in serum mediators of fibrogenesis and in non-invasive markers of liver fibrosis in HIV/hepatitis C virus-coinfected patients starting maraviroc-based antiretroviral therapy
    J Macias
    Unidad de Enfermedades Infecciosas y Microbiología, Hospital Universitario de Valme, Avda Bellavista s n, 41014, Seville, Spain
    Eur J Clin Microbiol Infect Dis 31:2083-8. 2012
    ..As TGF-beta1 levels have been shown to increase over time in HCV infection and liver fibrosis worsens rapidly in HIV/HCV coinfection, these parameters seem to evolve in a different way in MVC-treated patients...
  16. ncbi The Aspergillus fumigatus toxin fumagillin suppresses the immune response of Galleria mellonella larvae by inhibiting the action of haemocytes
    John P Fallon
    Medical Mycology Unit, Department of Biology, National Institute for Cellular Biotechnology, National University of Ireland Maynooth, Co Kildare, Ireland
    Microbiology 157:1481-8. 2011
    ..During growth of the fungus in the larvae, this toxin, along with others, may facilitate growth by suppressing the cellular immune response...
  17. ncbi Molecular interactions of CCR5 with major classes of small-molecule anti-HIV CCR5 antagonists
    Rama Kondru
    Department of Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304, USA
    Mol Pharmacol 73:789-800. 2008
    ..The fully mapped binding pocket of CCR5 is being used for structure-based design and lead optimization of novel anti-HIV CCR5 inhibitors with improved potency and better resistance profile...
  18. ncbi Clinical outcome in resistant HIV-2 infection treated with raltegravir and maraviroc
    Darius Armstrong-James
    Imperial College, St Stephens AIDS Trust, Chelsea and Westminster Hospital, London, UK
    Antiviral Res 86:224-6. 2010
    ..Further studies are required to assess the clinical efficacy of maraviroc in HIV-2 infection...
  19. pmc Fungal metabolite gliotoxin inhibits assembly of the human respiratory burst NADPH oxidase
    Shohko Tsunawaki
    Department of Infectious Diseases, National Research Institute for Child Health and Development, Setagaya, Tokyo 154 8567, Japan
    Infect Immun 72:3373-82. 2004
    ..These results suggest that A. fumigatus may confront PMN by inhibiting the assembly of the NADPH oxidase with its hyphal product, GT...
  20. pmc Involvement of outer membrane protein TolC, a possible member of the mar-sox regulon, in maintenance and improvement of organic solvent tolerance of Escherichia coli K-12
    R Aono
    Department of Bioengineering, Faculty of Bioscience and Biotechnology, Tokyo Institute of Technology, Yokohama, Japan
    J Bacteriol 180:938-44. 1998
    ..The tolerance level was restored by transformation of the transductants with a wild-type tolC gene. Therefore, it is evident that TolC is essential for E. coli to maintain organic solvent tolerance...
  21. ncbi Does fumagillin control the recently detected invasive parasite Nosema ceranae in western honey bees (Apis mellifera)?
    Geoffrey R Williams
    Department of Biology, Acadia University, Wolfville, NS, Canada B4P 2R6
    J Invertebr Pathol 99:342-4. 2008
    ..Molecular sequencing of 15 infected colonies identified N. ceranae in 93.3% of cases, suggesting that fumagillin is successful at temporarily reducing this recent invasive parasite in western honey bees...
  22. ncbi Fumagillin: an anti-infective as a parent molecule for novel angiogenesis inhibitors
    Benjamin Lefkove
    Department of Dermatology, Emory University School of Medicine, Atlanta, GA 30322, USA
    Expert Rev Anti Infect Ther 5:573-9. 2007
    ....
  23. ncbi Heat shock transcription factor 1 protects heart after pressure overload through promoting myocardial angiogenesis in male mice
    Yunzeng Zou
    Shanghai Institute of Cardiovascular Diseases, Zhongshan Hospital, Fudan University, Shanghai 200032, China
    J Mol Cell Cardiol 51:821-9. 2011
    ..We conclude that HSF1 promotes cardiac angiogenesis through suppression of p53 and subsequent upregulation of HIF-1 in endothelial cells during chronic pressure overload, leading to the maintenance of cardiac adaptation...
  24. ncbi Concentration-dependent effects of anticonvulsant enaminone methyl 4-(4'-bromophenyl)aminocyclohex-3-en-6-methyl-2-oxo-1-oate on neuronal excitability in vitro
    K V V Ananthalakshmi
    Department of Applied Therapeutics, Faculty of Pharmacy, Kuwait University, P O Box 24923, Safat 13110, Kuwait
    Neuroscience 141:345-56. 2006
    ..These two actions of methyl 4-(4'-bromophenyl)aminocyclohex-3-en-6-methyl-2-oxo-1-oate on neuronal excitability would have therapeutic implications in future clinical use of enaminones as anticonvulsants in seizure disorders...
  25. pmc Intensification of antiretroviral therapy with a CCR5 antagonist in patients with chronic HIV-1 infection: effect on T cells latently infected
    Carolina Gutierrez
    Infectious Diseases Department, Hospital Universitario Ramon y Cajal, and IRYCIS, Madrid, Spain
    PLoS ONE 6:e27864. 2011
    ..The primary objective was to assess the effect of MVC intensification on latently infected CD4(+) T cells in chronically HIV-1-infected patients receiving antiretroviral therapy...
  26. ncbi Immune recovery and T cell subset analysis during effective treatment with maraviroc
    Francesca Cossarini
    Department of Infectious Diseases, San Raffaele Scientific Institute, Milan, Italy
    J Antimicrob Chemother 67:2474-8. 2012
    ..Patients treated with maraviroc frequently show high CD4+ T cell increases. The aim of this study was to detail the characteristics of maraviroc-induced immune recovery...
  27. ncbi TNP-470, an angiogenesis inhibitor, suppresses the progression of peritoneal fibrosis in mouse experimental model
    Yoko Yoshio
    Second Department of Internal Medicine, Division of Renal Care Unit, Nagasaki University School of Medicine, Nagasaki, Japan
    Kidney Int 66:1677-85. 2004
    ..The aim of the present study was to evaluate the effect of TNP-470, an anti-angiogenic compound, on the development of peritoneal fibrosis induced by chlorhexidine gluconate (CG)...
  28. pmc Maraviroc, a CCR5 antagonist, prevents development of hepatocellular carcinoma in a mouse model
    Laura Ochoa-Callejero
    Oncology Area, Center for Biomedical Research of La Rioja CIBIR, Logrono, Spain
    PLoS ONE 8:e53992. 2013
    ..Clinical studies are needed to demonstrate the efficacy of this drug, or other CCR5 inhibitors, in patients with high risk of developing HCC...
  29. ncbi Hepatic safety and tolerability in the maraviroc clinical development program
    Ayman Ayoub
    Pfizer Global Research and Development, Sandwich, UK
    AIDS 24:2743-50. 2010
    ..This analysis suggests that maraviroc does not present significant risks to hepatic safety when taken at the recommended doses in the populations studied...
  30. ncbi Modulatory effects of the CCR5 antagonist maraviroc on microglial pro-inflammatory activation elicited by gp120
    Lucia Lisi
    Institute of Pharmacology, Catholic University Medical School, Rome, Italy
    J Neurochem 120:106-14. 2012
    ..In this experimental paradigm, maraviroc significantly increased microglial activation, thus suggesting that its chronic use can exacerbate neuronal pathology, especially in HIV-experienced patients with higher cerebral IFNγ levels...
  31. ncbi Anticonvulsant enaminone E139 suppresses epileptiform activity in rat hippocampal slices
    Kethireddy V V Ananthalakshmi
    Department of Applied Therapeutics, Faculty of Pharmacy, Kuwait University, PO Box 24923, Safat 13110, Kuwait
    Epilepsy Res 76:85-92. 2007
    ..We conclude that E139 suppresses in vitro seizures in the hippocampus by synaptic and non-synaptic mechanisms. These actions on network activity may underlie their reported in vivo anticonvulsant effects...
  32. ncbi Maraviroc intensification of stable antiviral therapy in HIV-1-infected patients with poor immune restoration: MARIMUNO-ANRS 145 study
    Lise Cuzin
    Infectious Diseases Department, University Hospital, Toulouse, France
    J Acquir Immune Defic Syndr 61:557-64. 2012
    ..To address the ability of a 24-week Maraviroc (MVC) intensification of a stable antiretroviral therapy (cART) to significantly increase the CD4 cell count slope...
  33. ncbi Entry inhibitors in the treatment of HIV-1 infection
    John C Tilton
    Department of Microbiology, University of Pennsylvania, 301C Johnson Pavilion, 3610 Hamilton Walk, Philadelphia, PA 19104, United States
    Antiviral Res 85:91-100. 2010
    ..This article forms part of a special issue of Antiviral Research marking the 25th anniversary of antiretroviral drug discovery and development, Vol 85, issue 1, 2010...
  34. pmc Anticonvulsant enaminones depress excitatory synaptic transmission in the rat brain by enhancing extracellular GABA levels
    Samuel B Kombian
    Department of Applied Therapeutics, Faculty of Pharmacy, Kuwait University, PO Box 24923, Safat 13110, Kuwait
    Br J Pharmacol 145:945-53. 2005
    ..Our data suggest that anticonvulsant enaminones cause EPSC depression by enhancing extracellular GABA levels possibly through the inhibition of either GABA reuptake or GABA-T enzyme, or both...
  35. ncbi Calculation of the free energy of solvation for neutral analogs of amino acid side chains
    Alessandra Villa
    Groningen Biomolecular Sciences and Biotechnology Institute GBB, Department of Biophysical Chemistry, University of Groningen, Nijenborgh 4, 9747 AG Groningen, The Netherlands
    J Comput Chem 23:548-53. 2002
    ..The dependence of the calculated free energies on the atomic partial charges was also studied...
  36. ncbi Angiogenesis inhibitor, TNP-470, prevents diet-induced and genetic obesity in mice
    Ebba Brakenhielm
    Microbiology and Tumor Biology Center, Karolinska Institutet, Stockholm, Sweden
    Circ Res 94:1579-88. 2004
    ..Our findings suggest that similarly to growth and organogenesis in other tissues, adipose tissue growth is dependent on angiogenesis. Our observations may have conceptual implications for the prevention of obesity and related disorders...
  37. ncbi HIV-1 dual/mixed tropic isolates show different genetic and phenotypic characteristics and response to maraviroc in vitro
    Valentina Svicher
    Department of Experimental Medicine, University of Rome Tor Vergata, Via Montpellier 1, 00133 Rome, Italy
    Antiviral Res 90:42-53. 2011
    ....
  38. doi Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists
    Robert J Cherney
    J Med Chem 51:721-4. 2008
    We describe the design, synthesis, and evaluation of novel disubstituted cyclohexanes as potent CCR2 antagonists...
  39. ncbi TNP-470, an angiogenesis inhibitor, attenuates the development of allograft vasculopathy
    Mark D Denton
    Division of Nephrology, Department of Medicine, Children s Hospital, 300 Longwood Avenue, Boston, MA 02115, USA
    Transplantation 78:1218-21. 2004
    ..08+/-0.11). Therefore, TNP-470 interrupts the progression of CAV when given late but does not prevent its development when given immediately posttransplantation...
  40. ncbi Preclinical assessment of the distribution of maraviroc to potential human immunodeficiency virus (HIV) sanctuary sites in the central nervous system (CNS) and gut-associated lymphoid tissue (GALT)
    D K Walker
    Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Sandwich, UK
    Xenobiotica 38:1330-9. 2008
    ....
  41. pmc Protection of rhesus macaques from vaginal infection by vaginally delivered maraviroc, an inhibitor of HIV-1 entry via the CCR5 co-receptor
    Ronald S Veazey
    Tulane National Primate Research Center, Covington, LA, USA
    J Infect Dis 202:739-44. 2010
    ..These findings validate MVC development as a vaginal microbicide for women and should guide clinical programs...
  42. pmc Effects of CYP3A4 inhibitors on the pharmacokinetics of maraviroc in healthy volunteers
    Samantha Abel
    Pfizer Global R and D, Sandwich, UK
    Br J Clin Pharmacol 65:27-37. 2008
    ..To evaluate the influence of cytochrome P450 (CYP) 3A4 inhibitors on the clinical pharmacokinetics of maraviroc, a novel CCR5 antagonist...
  43. ncbi PRESERVE-beta: two-year efficacy and safety of initial combination therapy with nateglinide or glyburide plus metformin
    John Gerich
    General Clinical Research Center, University of Rochester, New York, USA
    Diabetes Care 28:2093-9. 2005
    ..To compare long-term efficacy and safety of initial combination therapy with nateglinide/metformin versus glyburide/metformin...
  44. pmc Reduced maximal inhibition in phenotypic susceptibility assays indicates that viral strains resistant to the CCR5 antagonist maraviroc utilize inhibitor-bound receptor for entry
    Mike Westby
    Globel Research and Development, Pfizer Ltd, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom
    J Virol 81:2359-71. 2007
    ..This hypothesis was further corroborated by the observation that a high concentration of maraviroc blocks the activity of aplaviroc against maraviroc-resistant virus...
  45. ncbi Amino-alkyl-cyclohexanes are novel uncompetitive NMDA receptor antagonists with strong voltage-dependency and fast blocking kinetics: in vitro and in vivo characterization
    C G Parsons
    Department of Pharmacology, Merz Co, Frankfurt am Main, Germany
    Neuropharmacology 38:85-108. 1999
    ..The 36 amino-alkyl-cyclohexanes tested displaced [3H]-(+)-MK-801 binding to rat cortical membranes with K(i)s between 1.5 and 143 microM...
  46. pmc Adipose tissue mass can be regulated through the vasculature
    Maria A Rupnick
    Division of Cardiovascular Medicine, Brigham and Women s Hospital, Boston, MA 02115, USA
    Proc Natl Acad Sci U S A 99:10730-5. 2002
    ..We conclude that adipose tissue mass is sensitive to angiogenesis inhibitors and can be regulated by its vasculature...
  47. pmc Effects of maraviroc and efavirenz on markers of immune activation and inflammation and associations with CD4+ cell rises in HIV-infected patients
    Nicholas Funderburg
    Case Western Reserve University, Cleveland, Ohio, United States of America
    PLoS ONE 5:e13188. 2010
    ..Maraviroc treatment for HIV-1 infected patients results in larger CD4(+) T cell rises than are attributable to its antiviral activity alone. We investigated whether this is due to modulation of T cell activation and inflammation...
  48. ncbi CCR5 antagonists: comparison of efficacy, side effects, pharmacokinetics and interactions--review of the literature
    J M Emmelkamp
    Department of Medicine I, University Clinic Bonn, Sigmund Freud Str 25, 53105 Bonn, Germany
    Eur J Med Res 12:409-17. 2007
    ..Extended follow-up of the vicriviroc trials showed no further case of malignancy, reassuring the overall good tolerability profile of the drug so far...
  49. ncbi Maraviroc: a review of its use in the management of CCR5-tropic HIV-1 infection
    Caroline M Perry
    Adis, a Wolters Kluwer Business, Auckland, New Zealand
    Drugs 70:1189-213. 2010
    ..Available data indicate that maraviroc may also have a role in treatment-naive adults with CCR5-tropic HIV-1 infection, a population in whom CCR5-tropic HIV-1 is often the major quasispecies...
  50. ncbi The angiogenesis inhibitor tnp-470 effectively inhibits human neuroblastoma xenograft growth, especially in the setting of subclinical disease
    S Shusterman
    Division of Oncology, The Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, USA
    Clin Cancer Res 7:977-84. 2001
    ..We speculate that TNP-470 may be a useful adjuvant therapy for high-risk neuroblastoma patients, particularly when used in settings of minimal disease status...
  51. ncbi Assessing theoretical risk and benefit suggested by genetic association studies of CCR5: experience in a drug development programme for maraviroc
    Jeremy Wheeler
    Pfizer Research and Development, Sandwich, Kent, UK
    Antivir Ther 12:233-45. 2007
    ..There was, however, evidence to suggest rheumatoid arthritis as a potential therapeutic target for a CCR5 antagonist. Clinical evidence would be required to confirm these findings...
  52. ncbi Subgroup analyses of maraviroc in previously treated R5 HIV-1 infection
    Gerd Fatkenheuer
    Universitätsklinik Köln, Cologne, Germany
    N Engl J Med 359:1442-55. 2008
    ....
  53. ncbi Maraviroc-containing regimen suppresses HIV replication in the cerebrospinal fluid of patients with neurological symptoms
    Giovanna Melica
    Department of Clinical Immunology, Henri Mondor Hospital, Université Paris XII Creteil, Creteil, France
    AIDS 24:2130-3. 2010
    ..The median (range) maraviroc concentration in plasma was 347 ng/ml (123-2678). Four patients had CSF concentrations above the protein-adjusted inhibitory concentration (IC90) of 0.57 ng/ml (0.06-10.7) with a median of 102 ng/ml (35-173)...
  54. pmc Detection of low-frequency pretherapy chemokine (CXC motif) receptor 4 (CXCR4)-using HIV-1 with ultra-deep pyrosequencing
    John Archer
    University of Manchester, UK
    AIDS 23:1209-18. 2009
    ....
  55. pmc Evolution of CCR5 antagonist resistance in an HIV-1 subtype C clinical isolate
    Timothy J Henrich
    Division of Infectious Diseases, Brigham and Women s Hospital, Boston, MA, USA
    J Acquir Immune Defic Syndr 55:420-7. 2010
    ..Here, we test the contribution of gp120 mutations to CCR5 antagonist resistance and investigate why certain minority V3 variants emerged as the dominant species under drug pressure...
  56. ncbi Treatment of HIV infection with the CCR5 antagonist maraviroc
    Wiete Kromdijk
    Slotervaart Hospital, Department of Pharmacy and Pharmacology, Louwesweg 6, 1066 EC Amsterdam, The Netherlands
    Expert Opin Pharmacother 11:1215-23. 2010
    ..New drug classes are thus required. Maraviroc is the first chemokine receptor 5 antagonist approved for use in treatment experienced HIV patients with a R5-tropic virus...
  57. ncbi Inhibition of inflammatory corneal angiogenesis by TNP-470
    A M Joussen
    Department of Vitreoretinal Surgery, Center for Ophthalmology, University of Cologne, Koln, Germany
    Invest Ophthalmol Vis Sci 42:2510-6. 2001
    ..Topical and systemic delivery of the drug were investigated in a murine model as well as inhibition of endothelial cell proliferation in vitro and in vivo...
  58. ncbi Improved prandial glucose control with lower risk of hypoglycemia with nateglinide than with glibenclamide in patients with maturity-onset diabetes of the young type 3
    Tiinamaija Tuomi
    Department of Medicine Diabetology, Helsinki University Central Hospital, P O Box 340, FIN 00029 HUS, Helsinki, Finland
    Diabetes Care 29:189-94. 2006
    ....
  59. ncbi Developing clinical role of a CCR5 co-receptor antagonist in HIV-1 infection
    David J Caldwell
    Assistant Professor of Clinical and Administrative Sciences ULM College of Pharmacy, 1800 Bienville Drive, Monroe, LA 71201, USA
    Expert Opin Pharmacother 9:3231-42. 2008
    ..Maraviroc is the only approved CCR5 coreceptor antagonist on the market for treatment of HIV-1 infection. It uses a previously untargeted step in the HIV-1 replication cycle necessary for viral entry into the host cell...
  60. ncbi Decreased blood glucose excursion by nateglinide ameliorated neuropathic changes in Goto-Kakizaki rats, an animal model of non-obese type 2 diabetes
    Yoshiro Kitahara
    Pharmaceutical Research Laboratories, Ajinomoto, Kawasaki, Japan
    Metabolism 51:1452-7. 2002
    ..These results suggest that meticulous control of postprandial hyperglycemia is essential to inhibit the development of neuropathy in type 2 diabetes...
  61. ncbi Effects of Nosema bombi and its treatment fumagillin on bumble bee (Bombus occidentalis) colonies
    Robin Whittington
    Department of Biological Sciences, Simon Fraser University, 8888 University Drive, Burnaby, BC, Canada V5A 1S6
    J Invertebr Pathol 84:54-8. 2003
    ..Therefore, whole bee and frass sampling is useful for determining if N. bombi is present or absent, but not for obtaining accurate estimates of the intensity of N. bombi infections...
  62. ncbi Maraviroc
    Hind Fadel
    Department of Internal Medicine, Mayo Clinic, Rochester, Minnesota, USA
    Drugs Today (Barc) 43:749-58. 2007
    ..In these studies, maraviroc also demonstrated acceptable safety and tolerability profiles with adverse events and discontinuation rates in general comparable to those noted in the placebo arms...
  63. ncbi Reduction of vascular and permeable regions in solid tumors detected by macromolecular contrast magnetic resonance imaging after treatment with antiangiogenic agent TNP-470
    Zaver M Bhujwalla
    Department of Radiology, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
    Clin Cancer Res 9:355-62. 2003
    ..Magnetic resonance imaging (MRI) is one such noninvasive technique that is routinely used clinically...
  64. ncbi CCR5 blockade in combination with cyclosporine increased cardiac graft survival and generated alternatively activated macrophages in primates
    Jun Li
    Department of Cardiovascular Surgery, Union Hospital, Huazhong University of Science and Technology, Wuhan 430022, China
    J Immunol 186:3753-61. 2011
    ..In conclusion, MVC/CsA protects cardiac allograft in primates and this effect is associated with generating AAMs through activation of the PPARγ nuclear receptor...
  65. pmc Maraviroc in treatment-experienced patients with HIV-1 infection - experience from routine clinical practice
    S Reuter
    Clinic for Gastroenterology, Hepatology and Infectious, University Hospital, Dusseldorf, Germany
    Eur J Med Res 15:231-7. 2010
    ..Few data are available about the efficacy of maraviroc (MVC) during routine use. We characterized indications for MVC use and the efficacy of MVC in clinical practice...
  66. pmc RNase H mediated cleavage of RNA by cyclohexene nucleic acid (CeNA)
    B Verbeure
    Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium
    Nucleic Acids Res 29:4941-7. 2001
    ..The CeNA:RNA duplex is cleaved by RNase H. The Vmax and Km of the cleavage reaction for CeNA:RNA and DNA:RNA is in the same range, although the kcat value is about 600 times lower in the case of CeNA:RNA...
  67. ncbi Anti-inflammatory effect of maraviroc in an HIV-infected patient with concomitant myositis: a case report
    Amedeo F Capetti
    1st Division of Infectious Diseases, Luigi Sacco Hospital, Milan, Italy
    J Int Assoc Physicians AIDS Care (Chic) 9:201-2. 2010
    ..After only 3 months the patient's CK levels had normalized and with the help of rehabilitation he recovered the ability to walk, which he still maintains at the one year of observation...
  68. ncbi Maraviroc is a substrate for OATP1B1 in vitro and maraviroc plasma concentrations are influenced by SLCO1B1 521 T>C polymorphism
    Marco Siccardi
    Department of Infectious Diseases, University of Torino, Amedeo di Savoia Hospital, Torino, Italy
    Pharmacogenet Genomics 20:759-65. 2010
    ..The 521 T>C polymorphism has been correlated earlier with higher plasma concentrations of several drugs and the aim of this study was to determine whether this polymorphism influences trough concentrations of maraviroc...
  69. ncbi Insulinotropic meglitinide analogues
    A Dornhorst
    Department of Metabolic Medicine, Faculty of Medicine, Imperial College, Hammersmith Hospital Campus, Du Cane Road, W12 0NN, London, UK
    Lancet 358:1709-16. 2001
    ..However, one hope for newer combinations of diabetic drugs is that the functional life of the beta cell can be extended, thereby delaying the need for insulin injections...
  70. ncbi Occurrence of Cystosporogenes sp. (Protozoa, Microsporidia) in a multi-species insect production facility and its elimination from a colony of the eastern spruce budworm, Choristoneura fumiferana (Clem.) (Lepidoptera: Tortricidae)
    Kees van Frankenhuyzen
    Great Lakes Forestry Centre, Canadian Forest Service, Natural Resources Canada, 1219 Queen Street East, Sault Ste Marie, Ont, P6A 2E5, Canada
    J Invertebr Pathol 87:16-28. 2004
    ..A clean colony was established by conducting individual matings and selecting disease-free offspring...
  71. ncbi Assessment of the anti-obesity effects of the TNP-470 analog, CKD-732
    Yoo Mee Kim
    Division of Endocrinology, Department of Internal Medicine, NHIC Ilsan Hospital, Goyang, Republic of Korea
    J Mol Endocrinol 38:455-65. 2007
    ..These results should be carefully verified to assess the utility of CKD-732 as an anti-obesity drug...
  72. ncbi Effect of four antimicrobials against an Encephalitozoon sp. (Microsporidia) in a grasshopper host
    Shajahan Johny
    Department of Biological Sciences, Illinois State University, Normal, Illinois 61790 4120, USA
    Parasitol Int 57:362-7. 2008
    ..Our study suggests that quinine and related alkaloids should be further examined for antimicrosporidial activity, and streptomycin should be examined as a possible enhancer of microsporidiosis...
  73. pmc Differential use of CCR5 by HIV-1 clinical isolates resistant to small-molecule CCR5 antagonists
    Timothy J Henrich
    Brigham and Women s Hospital, Boston, Massachusetts, USA
    Antimicrob Agents Chemother 56:1931-5. 2012
    ..This heterogeneity makes it difficult to draw general conclusions about the relationship between patterns of CCR5 antagonist resistance and the use of specific CCR5 domains for entry...
  74. ncbi Calculation of the water-cyclohexane transfer free energies of neutral amino acid side-chain analogs using the OPLS all-atom force field
    Justin L MacCallum
    Department of Biological Sciences, University of Calgary, 2500 University Drive NW, Calgary, Alberta T2N 1N4, Canada
    J Comput Chem 24:1930-5. 2003
    ..0 and 4.1 kJ/mol, respectively. The largest errors, of more than 7.5 kJ/mol, are found for histidine, glutamine, and glutamatic acid...
  75. ncbi Protein adducts of 1,4-benzoquinone and benzene oxide among smokers and nonsmokers exposed to benzene in China
    N Rothman
    Department of Environmental Sciences and Engineering, School of Public Health, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599-7400, USA
    Cancer Epidemiol Biomarkers Prev 10:831-8. 2001
    ..Interestingly, cigarette smoking increased Alb adducts of 1,4-BQ but not of BO, suggesting that benzene from cigarette smoke was not the primary contributor to the 1,4-BQ adducts...
  76. ncbi Maraviroc is able to inhibit dual-R5 viruses in a dual/mixed HIV-1-infected patient
    Jori Symons
    Department of Virology, Medical Microbiology, University Medical Center Utrecht, Heidelberglaan 100, 3584 CX Utrecht, The Netherlands
    J Antimicrob Chemother 66:890-5. 2011
    ..The objective of the study was to investigate the impact of maraviroc on viruses with different co-receptor preferences in a patient with a dual/mixed (D/M) infection...
  77. ncbi Small molecule inhibitors of methionine aminopeptidase type 2 (MetAP-2)
    Thomas Garrabrant
    Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, Spring House, Pennsylvania 19477, USA
    Angiogenesis 7:91-6. 2004
    ....
  78. pmc Assessment of the pharmacokinetics, safety and tolerability of maraviroc, a novel CCR5 antagonist, in healthy volunteers
    Samantha Abel
    Pfizer Global Research and Development, Sandwich, UK
    Br J Clin Pharmacol 65:5-18. 2008
    ..To evaluate the pharmacokinetics, safety and tolerability of single and multiple oral doses of maraviroc in healthy volunteers...
  79. ncbi The effects of nateglinide following oral glucose load in impaired glucose tolerance subjects: rapid insulin stimulation by nateglinide in IGT subjects
    Takahisa Hirose
    Department of Internal Medicine, Nishinomiya Municipal Central Hospital, Nishinomiya, Hyogo 663 8014, Japan
    Endocr J 49:649-52. 2002
    ..A single dose of nateglinide was shown to almost normalize the glycemic response curve after a 75 g OGTT and to restore impairment in early insulin response in IGT subjects...
  80. pmc Inhibition of lymph node metastasis by an anti-angiogenic agent, TNP-470
    Y Ohta
    Department of Surgery I, School of Medicine, Kanazawa University, Japan
    Br J Cancer 75:512-5. 1997
    ..The inhibition ratios of lymph node metastasis were 82.3% at 10 mg kg-1, 97.2% at 30 mg kg-1 and 97.5% at 100 mg kg-1 respectively. This agent may be useful to inhibit lymph node metastasis...
  81. ncbi Maraviroc: a coreceptor CCR5 antagonist for management of HIV infection
    Raymond Yost
    Summa Health System, Akron, Ohio, USA
    Am J Health Syst Pharm 66:715-26. 2009
    ..The mechanism of action, pharmacology, pharmacokinetics, clinical efficacy, drug interactions, adverse effects, dosage and administration, cost, and role in therapy of maraviroc are reviewed...
  82. ncbi Methionine aminopeptidase-2 as a selective target of myofibroblasts in pulmonary fibrosis
    Daniel Kass
    Division of Pulmonary, Allergy, and Critical Care, Department of Medicine, Columbia University College of Physicians and Surgeons, 630 West 168th Street, New York, NY 10032, USA
    Am J Respir Cell Mol Biol 37:193-201. 2007
    ..We propose that MetAP2 plays a role in the proliferation of fibroblasts and myofibroblasts in fibrotic lung diseases and may serve as a novel pharmacologic target in IPF...
  83. ncbi Depletion of methionine aminopeptidase 2 does not alter cell response to fumagillin or bengamides
    Sunkyu Kim
    Novartis Pharmaceuticals, East Hanover, New Jersey 07936, USA
    Cancer Res 64:2984-7. 2004
    ..Moreover, MetAp2-depleted endothelial cells remain responsive to inhibition by either fumagillin or a newly identified MetAp2 enzyme inhibitor. These data suggest that MetAp2 function is not required for endothelial cell proliferation...
  84. pmc A pièce de resistance: how HIV-1 escapes small molecule CCR5 inhibitors
    John P Moore
    Weill Medical College of Cornell University, New York, NY 10065, USA
    Curr Opin HIV AIDS 4:118-24. 2009
    ..We review what has been learned from in-vitro resistance studies, and how this relates to what is being seen, or can be anticipated, in clinical studies...
  85. pmc Population pharmacokinetic/pharmacodynamic analysis of CCR5 receptor occupancy by maraviroc in healthy subjects and HIV-positive patients
    Maria C Rosario
    Department of Clinical Pharmacology, Pfizer Global R and D, Groton, CT, USA
    Br J Clin Pharmacol 65:86-94. 2008
    ....
  86. pmc HIV-1 resistance to maraviroc conferred by a CD4 binding site mutation in the envelope glycoprotein gp120
    Annette N Ratcliff
    Department of Molecular Biology and Microbiology, Case Western Reserve University, Cleveland, OH, USA
    J Virol 87:923-34. 2013
    ..In contrast, our structural models on K425 gp120 suggest that this resistant mutation impacts CD4 interactions and highlights a novel pathway for MVC resistance...
  87. ncbi Trace analysis of fumagillin in honey by liquid chromatography-diode array-electrospray ionization mass spectrometry
    M A J Nozal
    IU CINQUIMA, Analytical Chemistry, Faculty of Sciences, University of Valladolid, 47005 Valladolid, Spain
    J Chromatogr A 1190:224-31. 2008
    ..The developed method has been applied to the analysis of fumagillin residues in honey samples collected from veterinary treated beehives, infected by Nosema ceranae and fed with the technical product at different doses...
  88. ncbi Effects of TNP-470 on proliferation and apoptosis in human colon cancer xenografts in nude mice
    Zong Hai Huang
    Department of Surgery, Zhujiang Hospital, First Military Medical University, Guangzhou 510282, Guangdong Province, China
    World J Gastroenterol 9:281-3. 2003
    ..To study the effect of TNP-470 on cell growth, proliferation and apoptosis in human colon cancer xenografts in nude mice...
  89. ncbi [CCR5-antagonists: contribution of a new antiretroviral class to the management of HIV infection]
    I Poizot-Martin
    Service d immunohématologie clinique, centre d informations et de soins de l immunodéficience humaine et des hépatites virales, CIC Antenne Sud, pôle oncologie spécialités médicales et chirurgicales, Hopital Sainte Marguerite, 270, boulevard Sainte Marguerite, 13009 Marseille, France
    Med Mal Infect 40:245-55. 2010
    ....
  90. ncbi Tumor cytotoxicity and endothelial Rac inhibition induced by TNP-470 in anaplastic thyroid cancer
    Dorit Nahari
    Department of Surgery, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75390 9156, USA
    Mol Cancer Ther 6:1329-37. 2007
    ..In endothelial cells, TNP-470 prevented vascular endothelial growth factor-induced endothelial permeability, intercellular gap formation, and ruffle formation by preventing Rac1 activation...
  91. ncbi Amino-alkyl-cyclohexanes as a novel class of uncompetitive NMDA receptor antagonists
    W Danysz
    Merz Co, Eckenheimer Landstrasse 100 104, Frankfurt, 60318, Germany
    Curr Pharm Des 8:835-43. 2002
    ..The present review describes the rational for developing amino-alkyl-cyclohexanes, as new uncompetitive NMDA receptor antagonists based on our positive experience with memantine which has been ..
  92. ncbi Post-exposure prophylaxis with a maraviroc-containing regimen after occupational exposure to a multi-resistant HIV-infected source person
    Frédéric Méchaï
    1 AP HP, Internal Medicine and Infectious Diseases Department, Bicetre University Hospital, Paris XI University, Le Kremin Bicêtre, France
    J Med Virol 80:9-10. 2008
    ..Post-exposure prophylaxis was well tolerated, with no increase in liver function tests. The health care worker remained HIV-negative after a 6-month follow-up...
  93. ncbi Treatment with CCR5 antagonists: which patient may have a benefit?
    M C Mueller
    Department of Infectious Diseases, Med Poliklinik, University Hospital of Munich, Campus Innenstadt, Pettenkoferstr 8a, 80336 Munich, Germany
    Eur J Med Res 12:441-52. 2007
    ..Clinical efficacy in patients from regions with A and D predominance should be studied in future trials. In conclusion, MVR will be of benefit for patients in various treatment situations and regions...
  94. ncbi Cerebrospinal fluid maraviroc concentrations in HIV-1 infected patients
    Aylin Yilmaz
    Department of Infectious Diseases, The Sahlgrenska Academy, University of Gothenburg, Gothenburg, Sweden
    AIDS 23:2537-40. 2009
    ..63 ng/ml (range 1.83-12.2). CSF samples exceeded the median EC90 for maraviroc (0.57 ng/ml) by at least three-fold. The CSF levels of maraviroc found in this study likely contribute to viral suppression in the CSF...
  95. ncbi Raltegravir, maraviroc, etravirine: an effective protease inhibitor and nucleoside reverse transcriptase inhibitor-sparing regimen for salvage therapy in HIV-infected patients with triple-class experience
    Silvia Nozza
    Department of Infectious Diseases, San Raffaele Scientific Institute, Italy
    AIDS 24:924-8. 2010
    ..Although long-term safety needs further study, this protease inhibitor and nucleoside analogue-sparing regimen showed sustained efficacy...
  96. pmc Maraviroc concentrates in the cervicovaginal fluid and vaginal tissue of HIV-negative women
    Julie B Dumond
    Division of Pharmacotherapy and Experimental Therapeutics, University of North Carolina at Chapel Hill Eshelman School of Pharmacy, Chapel Hill, NC 27599 7360, USA
    J Acquir Immune Defic Syndr 51:546-53. 2009
    ..To compare single- and multiple-dose maraviroc exposures in cervicovaginal fluid (CVF) and vaginal tissue (VT) with blood plasma (BP) and quantify maraviroc protein binding in CVF...
  97. ncbi Pharmacokinetics, safety and tolerability of a single oral dose of maraviroc in HIV-negative subjects with mild and moderate hepatic impairment
    Samantha Abel
    Pfizer Global Research and Development, Sandwich, UK
    Antivir Ther 14:831-7. 2009
    ..The objective of this study was to evaluate the pharmacokinetics of maraviroc in subjects with mild or moderate hepatic impairment compared with subjects with normal hepatic function. Safety and tolerability were also assessed...
  98. ncbi Nateglinide alone and in combination with metformin improves glycemic control by reducing mealtime glucose levels in type 2 diabetes
    E S Horton
    Joslin Diabetes Center, Boston, Massachusetts 02215, USA
    Diabetes Care 23:1660-5. 2000
    ....
  99. ncbi Reviews of anti-infective agents: maraviroc: the first of a new class of antiretroviral agents
    Rodger D MacArthur
    Wayne State University, Detroit, Michigan, USA
    Clin Infect Dis 47:236-41. 2008
    ..HIV-1 mechanisms of resistance to maraviroc, assays to determine viral coreceptor use (tropism), drug safety, and clinical use of maraviroc are discussed at length...
  100. ncbi A pharmacokinetic-pharmacodynamic model to optimize the phase IIa development program of maraviroc
    Maria C Rosario
    Department of Clinical Pharmacology, Pfizer Clinical R and D, Groton, CT 06340, USA
    J Acquir Immune Defic Syndr 42:183-91. 2006
    ....
  101. ncbi Angiostatic agents prevent the development of endometriosis-like lesions in the chicken chorioallantoic membrane
    Annemiek W Nap
    Department of Obstetrics and Gynaecology, Research Institute Growth and Development GROW, Maastricht University and University Hospital, Maastricht, The Netherlands
    Fertil Steril 83:793-5. 2005
    ....

Research Grants62

  1. High-Spin Iron(IV)-oxo Complexes-True Mimics of Enzymatic Non-Heme Iron
    AIDAN RICHARD MCDONALD; Fiscal Year: 2010
    ..Ultimately this will allow us to more efficiently develop medicines to treat certain illnesses, and for the 'clean'natural removal of toxins from the environment. ..
  2. MANGANESE (III) BASED OXIDATIVE FREE RADICAL CYCLIZATION
    BARRY SNIDER; Fiscal Year: 2000
    ....
  3. Visible Light Photocatalyzed Cycloaddition Reactions with Cyclopropyl Sulfides
    Danielle M Schultz; Fiscal Year: 2013
    ..In addition, the findings from this research will lend insight into the development of other useful ring opening transformations that proceed through visible light photoredox catalysis. ..
  4. AVERMECTIN, TETRODOTOXIN, & RADICAL-ALDEHYDE CYCLIZATION
    Bert Fraser Reid; Fiscal Year: 1991
    ..The early stages of our synthesis uses some novel chemistry of 1,6-anhydro sugars in order to lay the structural framework for assembling the condensed skeleton of tetrodotoxin...
  5. FUSED POLYCYCLIC AMINES VIA DOUBLE ANNULATION
    Robert Grossman; Fiscal Year: 2004
    ..The yohimbine and corynanthine analogs will be tested for alpha-adrenoceptor antagonist activity. ..
  6. SYNTHESIS OF EUNICELLIN DITERPENES AND RELATED COMPOUNDS
    MATTHIAS MCINTOSH; Fiscal Year: 2003
    ....
  7. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2009
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. ..
  8. Enantioselective Synthesis of Leustroducsin B
    THOMAS HUNTER; Fiscal Year: 2005
    ....
  9. Synthesis of Glycomimetics and Related Structures
    DAVID MOOTOO; Fiscal Year: 2006
    DESCRIPTION (provided by applicant): Highly oxygenated tetrahydropyrans and cyclohexanes are of interest as biochemical probes for disease related mechanisms, and, or drug leads for new therapeutic agents...
  10. NON-PEPTIDE PEPTIDOMIMETICS
    Ralph Hirschmann; Fiscal Year: 2004
    ..Finally, we will explore (K) the pharmacokinetic profiles of our lead mimics through our collaborations with expert biologists. ..
  11. INTRAMOLECULAR CYCLIZATIONS OF CYCLODECENES
    James White; Fiscal Year: 1990
    ..Several other strategies, including one that involves transannular radical cyclization of an oxygen-stabilized radical center and another that makes use of a variant of an anion accelerated Cope rearrangement, will also be investigated...
  12. Chrolactomycin and Okilactomycin: Novel Antitumor Agents
    Todd Bosanac; Fiscal Year: 2004
    ..An extension of the Petasis-Ferrier rearrangement will be employed to construct the tetrahydropyranone core. ..
  13. CONFORMATIONAL STABILITY OF GLOBULAR PROTEINS
    CARLOS PACE; Fiscal Year: 2006
    ..To gain a better understanding of protein solubility, we will study the effect of single changes in the amino acid sequence of RNase Sa on the solubility of the folded and unfolded states of the protein. ..
  14. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2007
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  15. 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. ..
  16. TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
    LEO PAQUETTE; Fiscal Year: 2003
    ..These include, but are not limited to, the 1-deoxy, D-homo-, 2-desmethyl, and 12-methylene derivatives, in addition to the D-ring invertomer and the C-nor isomer. ..
  17. Anal Dysplasia in HIV+ and HIV- men
    Timothy Wilkin; Fiscal Year: 2006
    ..This study will help provide important new information on which groups of HIV+ men may benefit from screening and how HAART may modify this risk. ..
  18. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2003
    ....
  19. PROTEIN SYNTHESIS INITIATION IN ANIMAL CELLS
    Bansidhar Datta; Fiscal Year: 2002
    ..This research is expected to provide valuable information regarding the mechanism of protein synthesis initiation in normal, cancerous, and virus- infected animal cells. ..
  20. ADULT AIDS CLINICAL TRIALS GROUP
    Michael Saag; Fiscal Year: 2007
    ..abstract_text> ..
  21. Augmentation of DNA Vaccine-Elicited Immunity to HIV/SIV
    DAN BAROUCH; Fiscal Year: 2008
    ..The long-term objectives of these studies are to develop novel vaccine regimens that recruit APCs to the site of inoculation in animal models and to consider advancing the most promising strategies into clinical trials. ..
  22. MECHANISMS OF CANNABINOIDS ANTIEMETIC ACTIONS
    NISSAR DARMANI; Fiscal Year: 2001
    ..The results will define an important role for the cannabinoid receptors in the vomiting circuits and may implicate an antiemetic role for the endogenous cannabinoids. ..
  23. MAb-based targeted chemotherapy of lung cancer
    Serengulam Govindan; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  24. MECHANISMS OF CANNABINOID'S ANTIEMETIC ACTIONS
    NISSAR DARMANI; Fiscal Year: 2007
    ..The results will have important implications for the therapeutic utility of these "agonist antiemetics". [unreadable] [unreadable]..
  25. Metal-Mediated Routes to Biaryls
    Bruce Lipshutz; Fiscal Year: 2007
    ..A particular, albeit representative, application of a novel substituted cyclo-NOBIN will be studied for selected asymmetric aldol reactions. ..
  26. ENVIRONMENTAL EPOXIDES--MECHANISMS OF OVOTOXICITY
    Patricia Hoyer; Fiscal Year: 2002
    ..The results of these studies will provide greater insight as to the impact of exposure to ovotoxic environmental chemicals on reproductive health in women. ..
  27. Ovary Intact Murine Model for Menopause
    Patricia Hoyer; Fiscal Year: 2007
    ..Characterization of the VCD-treated mouse will, therefore, make a profound contribution to the study of menopause-related pathologies and, therefore, to women's health. ..
  28. Image-Guided Pro-Drug/Enzyme Therapy
    Zaver Bhujwalla; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  29. Inhibition of Interspecies Bacterial Quorum Sensing
    MARTIN SEMMELHACK; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  30. SIGNALING PATHWAYS IN CHEMICAL INDUCED OVOTOXICITY
    Patricia B Hoyer; Fiscal Year: 2010
    ..This will lead to an appreciation of the global impact of the environment on the reproductive life span in women. ..
  31. Comparative In Vivo Biodistribution of Characterized Manufactured Nanomaterials
    Nancy A Monteiro Riviere; Fiscal Year: 2010
    ..These coordinated studies will provide data to link physical chemical characterizations to in vivo MNM disposition. ..
  32. Nucleus Accumbens-Mediated Feeding: Output Pathways
    Thomas R Stratford; Fiscal Year: 2010
    ....
  33. CELL SUBPOPULATIONS IN THE PRIMATE CORPUS LUTEUM
    Richard Stouffer; Fiscal Year: 2001
    ..Overall, the proposed research may have relevance to an understanding of certain ovarian disorders such as ovarian hyperstimulation syndrome and luteal phase defects where microvasculature growth may be disrupted. ..
  34. Efficacy and toxicity of TRAIL against gliomas
    Vinay K Puduvalli; Fiscal Year: 2010
    ..The results of this study could also potentially provide a basis for clinical trials using TRAIL or analogues against gliomas and allow rational selection of agents to modulate the tumor resistance to TRAIL. ..
  35. Novel Adenovirus Vaccine Vectors for HIV/SIV
    Dan H Barouch; Fiscal Year: 2010
    ..abstract_text> ..
  36. FINE TUNING BINOLS AND BINAPS FOR ASYMMETRIC SYNTHESIS
    Bruce Lipshutz; Fiscal Year: 2001
    ..From ligands of this type come further options, such as opportunities for polymer mounting, and potentially of greatest attention, conversion to substituted cyclo BINAPs. ..
  37. FUNCTIONAL ANALOGS OF THE ENEDIYNE TOXINS
    MARTIN SEMMELHACK; Fiscal Year: 2001
    ..The potency of the enediyne in DNA cleavage is very sensitive to positioning on the DNA and proper design of the delivery agents is a critical component. ..
  38. Molecular Imaging of Angiogenesis by MRI
    Gregory Lanza; Fiscal Year: 2007
    ..Apply mathematical models of tissue compartmentalization to determine the contributions of target binding and vascular permeability to MRI signal enhancement. ..
  39. VOLATILE MARKERS OF ORAL MALODOR IN THE BREATH
    Michael Phillips; Fiscal Year: 2004
    ....
  40. UMKC School of Dentistry Oral and Craniofacial Biology
    J Eick; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable]..
  41. Chimeric Adenovirus Vaccine Vectors for HIV/SIV
    DAN BAROUCH; Fiscal Year: 2005
    ..Within the two-year time frame of this award, sufficient data will be generated with candidate chimeric rAd vaccines to justify further vaccine/challenge studies in rhesus monkeys. ..
  42. ISLET FUNCTION IN TYPE 2 DIABETES
    Steven Kahn; Fiscal Year: 2003
    ..The applicant has successfully trained a number of young investigators in the areas of patient-oriented and basic research and a plan to continue doing so is presented. ..
  43. HIV NEUTRALIZATION IN VITRO & IN SHIV-INFECTED MACAQUES
    John Moore; Fiscal Year: 2001
    ....
  44. Free-Living Physical Activity and Energy Expenditure
    Carol Boozer; Fiscal Year: 2003
    ..Finally, data from these studies will provide the basis for a future application to conduct a longitudinal, PA intervention study in this population. ..
  45. ENTRY INHIBITORS AS TOPICAL MICROBICIDES AGAINST HIV-1
    John Moore; Fiscal Year: 2004
    ..Moore, Ph.D., Fusion-Inhibitor Acquisition, Evaluation and Formulation; Administrative Core: John P. Moore, Ph.D. ..
  46. Correlative trial of fenretinide against Glioblastomas
    VINAY PUDUVALLI; Fiscal Year: 2003
    ..Such data could be relevant not only to future trials of retinoids in gliomas but also for ongoing trials of fenretinide in other malignancies. ..
  47. CHRYSTALLIZING DISULFIDE-STABILIZED HIV-1 ENV PROTEINS
    John Moore; Fiscal Year: 2004
    ..Any information accruing from the structure of a native Env trimer could facilitate the rational design of Env-based vaccines. ..
  48. Minimal-disease radioimmunotherapy of colorectal cancer
    Serengulam Govindan; Fiscal Year: 2003
    ..Successful feasibility study will lead to extended preclinical therapy studies and the initiation of a clinical Phase I RAIT trial in a SBIR Phase II program. ..
  49. NEW DEVELOPMENTS IN ORGANOCOPPER CHEMISTRY
    R Dieter; Fiscal Year: 2004
    ..The proposed synthetic routes to pyrrolidine aza sugars will develop the potential synthetic power of alpha-aminoalkylcuprate chemistry. ..
  50. Cytokine-Augmented DNA Vaccine-Elicited Immunity to HIV
    DAN BAROUCH; Fiscal Year: 2005
    ..Raphael Dolin, Dean for Clinical Programs, Harvard Medical School, will guide Dr. Barouch's development as an independent investigator. In addition, a committee of distinguished scientists will oversee his progress toward independence. ..
  51. Irreversible inhibitors of cholesterol esterase
    LORRAINE DECK; Fiscal Year: 2005
    ....
  52. VOLATILE MARKERS OF PULMONARY TUBERCULOSIS IN THE BREATH
    Michael Phillips; Fiscal Year: 2006
    ..Also, it could potentially reduce the mortality and morbidity caused by pulmonary TB. [unreadable] [unreadable] [unreadable]..
  53. MULTIDICIPLINARY FUNCTIONAL IMAGING OF CANCER
    Zaver Bhujwalla; Fiscal Year: 2002
    ..abstract_text> ..
  54. Optimizing Foamy Virus Vectors for Gene Therapy & Vaccine Applications
    WILLAM HARDY; Fiscal Year: 2006
    ..I am seeking a KO8 grant to allow me to expand my HIV clinical research career with basic science training to enable me to undertake translational studies directed at HIV therapeutics. ..
  55. Validation of rat models for resistant epilepsy therapy
    Wolfgang Loscher; Fiscal Year: 2005
    ..Our goal is to establish standard assays that can be employed by researchers to continue the search for treatments of drug resistant epilepsy. ..
  56. Imaging Lymphatic Clearance in Tumor Metastasis
    Zaver Bhujwalla; Fiscal Year: 2003
    ..abstract_text> ..
  57. Chronic Cannabinoids, Tumor Growth and Hyperalgesia
    DARRYL HAMAMOTO; Fiscal Year: 2005
    ..Positive results from these studies would suggest that cannabinoids could be useful for the treatment of cancer pain. ..
  58. Microporidiosis in AIDS
    ELIZABETH DIDIER; Fiscal Year: 2004
    ..This model will provide a better understanding of how the immune response functions to control microsporidia that replicate in different sites within a host cell. ..
  59. Modified Envelope Glycoproteins for HIV-1 Vaccine
    John P Moore; Fiscal Year: 2010
    ..11/07) Page 2 Form Page 2 ..
  60. Skin Manifestations of Tuberous Sclerosis
    Jack Arbiser; Fiscal Year: 2009
    ..Specific Aim 3. To determine whether dysregulation of p16ink4a and PTCH (patched) acts as a modifier of theTS phenotype in transgenic mice expressing dominant negative tuberin. ..
  61. CYTOMIMETIC ORGANIC CHEMISTRY
    FREDRIC MENGER; Fiscal Year: 2007
    ....
  62. RECENT ADVANCES IN AIDS AND HIV RESEARCH
    Michael Saag; Fiscal Year: 2007
    ..CME credit for attending physicians will be provided. ..