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. doi 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 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
  4. 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
  5. doi 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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

Research Grants

Detail Information

Publications296 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. doi 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 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...
  4. 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
    ....
  5. doi 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...
  6. 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...
  7. 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...
  8. 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
    ....
  9. 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...
  10. 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...
  11. 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...
  12. 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
    ....
  13. 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...
  14. 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...
  15. doi 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...
  16. doi 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
    ....
  17. 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...
  18. 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...
  19. 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...
  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. 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...
  22. 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...
  23. 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...
  24. 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...
  25. 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
    ....
  26. 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...
  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. 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...
  29. doi 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
    ....
  30. 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...
  31. 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...
  32. doi 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...
  33. 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...
  34. 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...
  35. doi 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...
  36. 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...
  37. doi 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...
  38. 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...
  39. 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...
  40. 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...
  41. 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...
  42. 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...
  43. 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...
  44. 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
    ....
  45. 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...
  46. doi 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...
  47. 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...
  48. doi 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...
  49. 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...
  50. 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...
  51. 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...
  52. 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...
  53. 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...
  54. 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
    ....
  55. 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...
  56. 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...
  57. doi 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...
  58. 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
    ....
  59. 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
    ....
  60. 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...
  61. 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...
  62. 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...
  63. 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...
  64. doi 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...
  65. doi 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...
  66. 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...
  67. 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 ..
  68. 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...
  69. 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...
  70. 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...
  71. 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...
  72. 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
    ....
  73. 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
    ....
  74. 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...
  75. 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
    ....
  76. pmc C-C chemokine receptor type 5 (CCR5) utilization of transmitted and early founder human immunodeficiency virus type 1 envelopes and sensitivity to small-molecule CCR5 inhibitors
    Qinxue Hu
    Centre for Infection and Immunity, St George s University of London, London, UK
    J Gen Virol 91:2965-73. 2010
    ..Taken together, these findings demonstrate that T/F R5 Envs are heterogeneous with respect to the mechanisms of CCR5 utilization. These data may have implications for therapeutic and prophylactic use of CCR5-based antiretrovirals...
  77. ncbi Induction of intrauterine growth restriction by reducing placental vascular growth with the angioinhibin TNP-470
    Catrin S Rutland
    School of Biomedical Sciences, University of Nottingham, Nottingham, NG7 2UH United Kingdom
    Biol Reprod 73:1164-73. 2005
    ..5. This study provides conclusive evidence that administration of TNP-470 interferes with placental vascular proliferation and vessel caliber and results in a reproducible model of IUGR...
  78. doi 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)...
  79. doi Primary genotypic resistance of HIV-1 to CCR5 antagonists in CCR5 antagonist treatment-naive patients
    Cathia Soulie
    UMPC Université Paris 06, Paris, France
    AIDS 22:2212-4. 2008
    ..The V3 loop region was rather polymorphic, and 7.3% of patients showed viruses with combinations of mutations in V3 loop previously described to be involved in maraviroc resistance, a licensed CCR5 antagonist...
  80. pmc Assessment of the absorption, metabolism and absolute bioavailability of maraviroc in healthy male subjects
    Samantha Abel
    Pfizer Global R and D, Sandwich, UK
    Br J Clin Pharmacol 65:60-7. 2008
    ..v.) maraviroc and determine the absolute bioavailability of oral maraviroc. Metabolite profiling was also conducted. Data from both of these studies were used to construct a mass-balance model for maraviroc...
  81. 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...
  82. ncbi TNP-470 blockage of VEGF synthesis is dependent on MAPK/COX-2 signaling pathway in PDGF-BB-activated hepatic stellate cells
    Yan Qing Wang
    Center for the Study of Liver Disease, Department of Surgery, The University of Hong Kong, Pokfulam, Hong Kong
    Biochem Biophys Res Commun 341:239-44. 2006
    ..In summary, our findings suggest that TNP-470 exhibits the observed anti-angiogenic properties in activated HSCs by targeting the COX-2/phospho-p44/42 MAPK pathway to inhibit VEGF production...
  83. doi CD4+ T-cell restoration after 48 weeks in the maraviroc treatment-experienced trials MOTIVATE 1 and 2
    David M Asmuth
    University of California Davis, Sacramento, CA, USA
    J Acquir Immune Defic Syndr 54:394-7. 2010
    ..To determine factors associated with CD4 responses to maraviroc (MVC)-containing regimens in treatment-experienced patients...
  84. doi A double-blind, placebo-controlled trial of maraviroc in treatment-experienced patients infected with non-R5 HIV-1
    Michael Saag
    School of Medicine, University of Alabama, Birmingham, AL 35294 2050, USA
    J Infect Dis 199:1638-47. 2009
    ..A phase 2b study was conducted to determine the safety and efficacy of maraviroc in combination with optimized background therapy in treatment-experienced patients infected with dual- or mixed-tropic HIV-1...
  85. ncbi Complete remission of Bomirski Ab amelanotic melanoma in hamsters treated with the angiogenesis inhibitor TNP-470
    A Mysliwski
    Department of Histology and Immunology University of Gdansk, Gdansk, 80 210 Poland
    Neoplasma 49:319-22. 2002
    ..Thus, Ab melanoma can be effectively cured with TNP-470 angiogenesis inhibitor when the substance is applied locally...
  86. 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...
  87. ncbi Nateglinide alone or with metformin safely improves glycaemia to target in patients up to an age of 84
    J U Weaver
    Queen Elizabeth Hospital, University of Newcastle upon Tyne, Tyne and Wear, UK
    Diabetes Obes Metab 6:344-52. 2004
    ....
  88. ncbi Restoration of early insulin secretion after a meal in type 2 diabetes: effects on lipid and glucose metabolism
    G Dimitriadis
    2nd Department of Internal Medicine, Research Institute and Diabetes Center, Athens University Medical School, Athens, Greece
    Eur J Clin Invest 34:490-7. 2004
    ..In type 2 diabetes (T2D) insulin secretion after a meal is delayed; this may have an impact on the development of hyperglycaemia and hyperlipidaemia...
  89. doi Insulin exocytosis in Goto-Kakizaki rat beta-cells subjected to long-term glinide or sulfonylurea treatment
    Junko Kawai
    Department of Biochemistry, Kyorin University School of Medicine, Mitaka, Tokyo 181 8611, Japan
    Biochem J 412:93-101. 2008
    ..We conclude that treatment of GK rats with nateglinide and glibenclamide varies in long-term effects on beta-cell functions; nateglinide treatment appears overall to be more beneficial...
  90. ncbi A Phase I and pharmacokinetic study of TNP-470 administered weekly to patients with advanced cancer
    P Bhargava
    Lombardi Cancer Center, Georgetown University Medical Center, Washington, DC 20007, USA
    Clin Cancer Res 5:1989-95. 1999
    ..v over 4 h. The principal DLT was neurotoxicity, which appeared to be dose-related and was completely reversible. On the basis of the short plasma t(1/2) of TNP-470, exploration of a prolonged i.v. infusion schedule is warranted...
  91. ncbi Sulfonylurea induced beta-cell apoptosis in cultured human islets
    Kathrin Maedler
    Division of Endocrinology and Diabetes, University Hospital, CH 8091 Zurich, Switzerland
    J Clin Endocrinol Metab 90:501-6. 2005
    ....
  92. 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...
  93. ncbi Nateglinide improves postprandial hyperglycemia and insulin secretion in renal transplant recipients
    Monica Hagen Voytovich
    Section of Nephrology, Department of Medicine, Rikshospitalet Radiumhospitalet HF, University of Oslo, Oslo, Norway
    Clin Transplant 21:246-51. 2007
    ..Our main objective was to investigate the safety and effect of nateglinide treatment on postprandial plasma glucose excursions and insulin secretion in RTR with PPHG...
  94. ncbi Insulin glargine in combination with nateglinide in people with Type 2 diabetes: a randomized placebo-controlled trial
    U K Dashora
    School of Clinical Medical Sciences Diabetes, University of Newcastle upon Tyne, UK
    Diabet Med 24:344-9. 2007
    ..To determine the effect of adding nateglinide to therapy with insulin glargine in adults with Type 2 diabetes previously treated with insulin and with poor blood glucose control...
  95. ncbi TNP-470 inhibits growth and the production of vascular endothelial growth factor of uterine carcinosarcoma cells in vitro
    M Emoto
    Department of Obstetrics and Gynecology, School of Medicine, Fukuoka University, Japan
    Anticancer Res 20:601-4. 2000
    ..This is the first study to examine the inhibitory and anti-angiogenic effects of angiogenesis inhibitor TNP-470, a synthetic analogue of fumagillin, for human uterine carcinosarcoma in vitro...
  96. ncbi Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist
    Anders Larsson
    Orebro Life Science Center, Department of Natural Sciences, Orebro University, SE 701 82 Orebro, Sweden
    J Med Chem 49:7366-72. 2006
    ..The remaining BFRs did not successfully interact with the ligand pocket, were not able to replace a synthetic androgen from the receptor, and failed to activate the receptor...
  97. ncbi Effects of nateglinide and glibenclamide on prothrombotic factors in naïve type 2 diabetic patients treated with metformin: a 1-year, double-blind, randomized clinical trial
    Giuseppe Derosa
    Department of Internal Medicine and Therapeutics, University of Pavia, Italy
    Intern Med 46:1837-46. 2007
    ..To evaluate the effect on coagulation and fibrinolysis parameters and on non-conventional cardiovascular risk factors of metformin plus nateglinide or glibenclamide in naïve type 2 diabetes patients...
  98. ncbi Beta-cell function in mild type 2 diabetic patients: effects of 6-month glucose lowering with nateglinide
    Andrea Mari
    Institute of Biomedical Engineering, National Research Council, Corso Stati Uniti 4, 35127 Padua, Italy
    Diabetes Care 28:1132-8. 2005
    ....
  99. ncbi Pharmacokinetics and metabolism of nateglinide in humans
    M L Weaver
    Drug Metabolism and Pharmacokinetics, Preclinical Safety, Novartis Institute for Biomedical Research, East Hanover, New Jersey 07936, USA
    Drug Metab Dispos 29:415-21. 2001
    ..Glucuronic acid conjugates resulting from direct glucuronidation of the carboxylic acid were also present. The major metabolite in plasma and urine was the result of hydroxylation of the methine carbon of the isopropyl group...
  100. ncbi Repaglinide versus nateglinide monotherapy: a randomized, multicenter study
    Julio Rosenstock
    Dallas Diabetes and Endocrine Center, 7777 Forest Lane, Suite C618, Dallas, TX 75230, USA
    Diabetes Care 27:1265-70. 2004
    ..A randomized, parallel-group, open-label, multicenter 16-week clinical trial compared efficacy and safety of repaglinide monotherapy and nateglinide monotherapy in type 2 diabetic patients previously treated with diet and exercise...
  101. ncbi Targeting postprandial hyperglycemia: a comparative study of insulinotropic agents in type 2 diabetes
    Mary F Carroll
    Internal Medicine Endocrinology, University of New Mexico, Albuquerque, New Mexico 87131, USA
    J Clin Endocrinol Metab 88:5248-54. 2003
    ....

Research Grants85

  1. Nitrile-Containing Decalins in Medicine
    FRASER FLEMING; Fiscal Year: 2005
    ..abstract_text> ..
  2. SECOND RECEPTORS FOR PRIMATE IMMUNODEFICIENCY VIRUSES
    John Moore; Fiscal Year: 2005
    ..We will identify what coreceptor(s) mediate CCR5-inhibitor insensitive SIV entry in vitro. ..
  3. HOSTILE ENVIRONMENTS PROMOTE INVASION AND METATASIS
    Zaver Bhujwalla; Fiscal Year: 2007
    ..The studies proposed in this application will lead to the potential identification of targets and pathways for the prevention of metastatic disease. ..
  4. MANGANESE (III) BASED OXIDATIVE FREE RADICAL CYCLIZATION
    BARRY SNIDER; Fiscal Year: 2000
    ....
  5. USE OF DNA ADDUCTS IN THE STUDY OF PAH CARCINOGENESIS
    Eleanor Rogan; Fiscal Year: 1992
    ..If so, this will open a new era of research in elucidating mechanisms of carcinogenesis of PAH...
  6. CARBOHYDRATE ARTIFICIAL RECEPTORS AND MECHANISTIC PROBES
    Eric Anslyn; Fiscal Year: 1993
    ..The electrode development will be performed with currently used deposition methods and voltametric and amperometric techniques...
  7. AVERMECTIN, TETRODOTOXIN, & RADICAL-ALDEHYDE CYCLIZATION
    Bert Fraser Reid; Fiscal Year: 1990
    ..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...
  8. FUSED POLYCYCLIC AMINES VIA DOUBLE ANNULATION
    Robert Grossman; Fiscal Year: 2003
    ..The yohimbine and corynanthine analogs will be tested for alpha-adrenoceptor antagonist activity. ..
  9. FUSED POLYCYCLIC AMINES VIA DOUBLE ANNULATION
    Robert Grossman; Fiscal Year: 2004
    ..The yohimbine and corynanthine analogs will be tested for alpha-adrenoceptor antagonist activity. ..
  10. FUSED POLYCYCLIC AMINES VIA DOUBLE ANNULATION
    Robert Grossman; Fiscal Year: 2002
    ..The yohimbine and corynanthine analogs will be tested for alpha-adrenoceptor antagonist activity. ..
  11. FUSED POLYCYCLIC AMINES VIA DOUBLE ANNULATION
    Robert Grossman; Fiscal Year: 2001
    ..The yohimbine and corynanthine analogs will be tested for alpha-adrenoceptor antagonist activity. ..
  12. SYNTHESIS OF EUNICELLIN DITERPENES AND RELATED COMPOUNDS
    MATTHIAS MCINTOSH; Fiscal Year: 2000
    ....
  13. SYNTHESIS OF EUNICELLIN DITERPENES AND RELATED COMPOUNDS
    MATTHIAS MCINTOSH; Fiscal Year: 1999
    ....
  14. SYNTHESIS OF EUNICELLIN DITERPENES AND RELATED COMPOUNDS
    MATTHIAS MCINTOSH; Fiscal Year: 2001
    ....
  15. SYNTHESIS OF EUNICELLIN DITERPENES AND RELATED COMPOUNDS
    MATTHIAS MCINTOSH; Fiscal Year: 2003
    ....
  16. SYNTHESIS OF EUNICELLIN DITERPENES AND RELATED COMPOUNDS
    MATTHIAS MCINTOSH; Fiscal Year: 2001
    ....
  17. SYNTHESIS OF EUNICELLIN DITERPENES AND RELATED COMPOUNDS
    MATTHIAS MCINTOSH; Fiscal Year: 2002
    ....
  18. High-Spin Iron(IV)-oxo Complexes-True Mimics of Enzymatic Non-Heme Iron
    AIDAN MCDONALD; Fiscal Year: 2009
    ..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. ..
  19. 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. ..
  20. STUDY OF BIOLOGICALLY ACTIVE MICROBIAL METABOLITES
    HEINZ FLOSS; Fiscal Year: 1993
    ....
  21. BIOLOGICALLY ACTIVE MICROBIAL METABOLITES
    HEINZ FLOSS; Fiscal Year: 1992
    ....
  22. STUDY OF BIOLOGICALLY ACTIVE MICROBIAL METABOLITES
    HEINZ FLOSS; Fiscal Year: 1990
    ....
  23. STUDY OF BIOLOGICALLY ACTIVE MICROBIAL METABOLITES
    HEINZ FLOSS; Fiscal Year: 1991
    ....
  24. LARGE-RING AND HELICAL COMPLEXING AGENTS FOR METAL IONS
    Thomas Bell; Fiscal Year: 1990
    ..Selective ionophores may be used to construct ion-selective electrodes for clinical analysis of metal ions in blood serum and urine...
  25. EXOGENOUS/ENDOGENOUS CANNABINOIDS--CHEMISTRY & BEHAVIOR
    TORBJORN JARBE; Fiscal Year: 1999
    ..Approval of this proposal would create financial stability and ensure that the above goals can be met. ..
  26. 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. ..
  27. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2007
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. [unreadable] [unreadable]..
  28. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2006
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. [unreadable] [unreadable]..
  29. SMALL MOLECULE CATALYST OF PROTEIN FOLDING
    RONALD RAINES; Fiscal Year: 2000
    ..Moreover, BMC is a useful catalyst for the in vitro and in vivo folding of proteins that contain multiple disulfide bonds. ..
  30. ANTITUMOR AND ANTIVIRAL NUCLEOSIDE ANALOGUES
    Jiri Zemlicka; Fiscal Year: 2001
    ..In vivo activity and mechanism of action of active compounds will also be investigated. Selected analogues will also be studies as potential antitumor agents. ..
  31. ANTITUMOR AND ANTIVIRAL NUCLEOSIDE ANALOGUES
    Jiri Zemlicka; Fiscal Year: 1999
    ..In vivo activity and mechanism of action of active compounds will also be investigated. Selected analogues will also be studies as potential antitumor agents. ..
  32. ANTITUMOR AND ANTIVIRAL NUCLEOSIDE ANALOGUES
    Jiri Zemlicka; Fiscal Year: 2000
    ..In vivo activity and mechanism of action of active compounds will also be investigated. Selected analogues will also be studies as potential antitumor agents. ..
  33. Enantioselective Synthesis of Leustroducsin B
    THOMAS HUNTER; Fiscal Year: 2005
    ....
  34. Enantioselective Synthesis of Leustroducsin B
    THOMAS HUNTER; Fiscal Year: 2004
    ....
  35. INHIBITION OF COMPLEX CARBOHYDRATE BIOSYNTHESIS
    Bruce Ganem; Fiscal Year: 1991
    ..3)Enantioselective total syntheses are proposed for several unusual polyhydroxycyclopentanes and cyclohexanes which are potent glycosidase inhibitors...
  36. 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...
  37. Synthesis of Glycomimetics and Related Structures
    DAVID MOOTOO; Fiscal Year: 2004
    Highly oxygenated tetrahydropyrans and cyclohexanes are of interest as biochemical probes for disease related mechanisms, and, or drug leads for new therapeutic agents...
  38. Synthesis of Glycomimetics and Related Structures
    DAVID MOOTOO; Fiscal Year: 2005
    Highly oxygenated tetrahydropyrans and cyclohexanes are of interest as biochemical probes for disease related mechanisms, and, or drug leads for new therapeutic agents...
  39. Synthesis of Glycomimetics and Related Structures
    DAVID MOOTOO; Fiscal Year: 2003
    Highly oxygenated tetrahydropyrans and cyclohexanes are of interest as biochemical probes for disease related mechanisms, and, or drug leads for new therapeutic agents...
  40. NON-PEPTIDE PEPTIDOMIMETICS
    Ralph Hirschmann; Fiscal Year: 2001
    ..Finally, we will explore (K) the pharmacokinetic profiles of our lead mimics through our collaborations with expert biologists. ..
  41. 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. ..
  42. NON-PEPTIDE PEPTIDOMIMETICS
    Ralph Hirschmann; Fiscal Year: 2003
    ..Finally, we will explore (K) the pharmacokinetic profiles of our lead mimics through our collaborations with expert biologists. ..
  43. NON-PEPTIDE PEPTIDOMIMETICS
    Ralph Hirschmann; Fiscal Year: 2002
    ..Finally, we will explore (K) the pharmacokinetic profiles of our lead mimics through our collaborations with expert biologists. ..
  44. 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...
  45. FUNCTIONAL ANALOGS OF THE ENEDIYNE TOXINS
    MARTIN SEMMELHACK; Fiscal Year: 2000
    ..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. ..
  46. FUNCTIONAL ANALOGS OF THE ENEDIYNE TOXINS
    MARTIN SEMMELHACK; Fiscal Year: 1999
    ..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. ..
  47. 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. ..
  48. 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. ..
  49. Chrolactomycin and Okilactomycin: Novel Antitumor Agents
    Todd Bosanac; Fiscal Year: 2003
    ..An extension of the Petasis-Ferrier rearrangement will be employed to construct the tetrahydropyranone core. ..
  50. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2003
    ....
  51. 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. ..
  52. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2001
    ....
  53. SYNTHESIS OF TEDANOLIDES CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 1999
    ....
  54. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2000
    ....
  55. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2002
    ....
  56. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2003
    ....
  57. PROTEIN SYNTHESIS INITIATION IN ANIMAL CELLS
    Bansidhar Datta; Fiscal Year: 2000
    ..This research is expected to provide valuable information regarding the mechanism of protein synthesis initiation in normal, cancerous, and virus- infected animal cells. ..
  58. PROTEIN SYNTHESIS INITIATION IN ANIMAL CELLS
    Bansidhar Datta; Fiscal Year: 2001
    ..This research is expected to provide valuable information regarding the mechanism of protein synthesis initiation in normal, cancerous, and virus- infected animal cells. ..
  59. Nitrile-Containing Decalins in Medicine
    FRASER FLEMING; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  60. 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. ..
  61. PROTEIN SYNTHESIS INITIATION IN ANIMAL CELLS
    Bansidhar Datta; Fiscal Year: 2001
    ..This research is expected to provide valuable information regarding the mechanism of protein synthesis initiation in normal, cancerous, and virus- infected animal cells. ..
  62. HIV: gp120, Chemokine Receptors & Macrophage Activation
    RONALD COLLMAN; Fiscal Year: 2008
    ..We anticipate that these studies will provide insight into the afferent mechanisms of M/M activation & neurotoxin production in HIVE and, ultimately, provide a rational basis for targeted strategies to interfere with this process. ..
  63. SIGNALING PATHWAYS IN CHEMICAL INDUCED OVOTOXICITY
    Patricia Hoyer; Fiscal Year: 2001
    ....
  64. CHEMICAL MECHANISMS OF BIOSYNTHESIS
    Richard Wolfenden; Fiscal Year: 2008
    ....
  65. CYTOMIMETIC ORGANIC CHEMISTRY
    FREDRIC MENGER; Fiscal Year: 2007
    ....
  66. Second Receptors For Primate Immunodeficeincy Viruses
    John Moore; Fiscal Year: 2009
    ..6P) viruses. Samples derived from these studies will be analyzed in vitro to gain insight into CCR5 and CXCR4 usage and resistance development in vivo. ..
  67. Metal-Mediated Routes to Biaryls
    Bruce Lipshutz; Fiscal Year: 2005
    ..A particular, albeit representative, application of a novel substituted cyclo-NOBIN will be studied for selected asymmetric aldol reactions. ..
  68. Nanostructured Dental Composite Restorative Materials
    J Eick; Fiscal Year: 2008
    ....
  69. New Technologies for Catalysis in Water
    Bruce Lipshutz; Fiscal Year: 2009
    ..This technology also is to be applied to other important cross-couplings, such as aminations and asymmetric additions of hydride to Michael acceptors, all in water at room temperature. ..
  70. RECENT ADVANCES IN AIDS AND HIV RESEARCH
    Michael Saag; Fiscal Year: 2007
    ..CME credit for attending physicians will be provided. ..
  71. FINE TUNING BINOLS AND BINAPS FOR ASYMMETRIC SYNTHESIS
    Bruce Lipshutz; Fiscal Year: 2000
    ..From ligands of this type come further options, such as opportunities for polymer mounting, and potentially of greatest attention, conversion to substituted cyclo BINAPs. ..
  72. Molecular Imaging of Angiogenesis by MRI
    Patrick Winter; Fiscal Year: 2006
    ..Apply mathematical models of tissue compartmentalization to determine the contributions of target binding and vascular permeability to MRI signal enhancement. ..
  73. SECOND RECEPTORS FOR PRIMATE IMMUNODEFICIENCY VIRUSES
    John Moore; Fiscal Year: 2004
    ..We will identify what coreceptor(s) mediate CCR5-inhibitor insensitive SIV entry in vitro. ..
  74. CHEMICAL MECHANISMS OF BIOSYNTHESIS
    Richard Wolfenden; Fiscal Year: 2009
    ....