imidazoles

Summary

Summary: Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).

Top Publications

  1. ncbi In vivo activation of the p53 pathway by small-molecule antagonists of MDM2
    Lyubomir T Vassilev
    Department of Discovery Oncology, Roche Research Center, Hoffmann La Roche, Inc, Nutley, NJ 07110, USA
    Science 303:844-8. 2004
  2. doi Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
    Sauveur Michel Maira
    Oncology Disease Area, Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH4002 Basel, Switzerland
    Mol Cancer Ther 7:1851-63. 2008
  3. doi NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations
    Violeta Serra
    Laboratory of Oncology Research, Medical Oncology Service, Vall d Hebron University Hospital, Barcelona, Spain
    Cancer Res 68:8022-30. 2008
  4. ncbi Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury
    Alexei Degterev
    Department of Cell Biology, Harvard Medical School, 240 Longwood Avenue, Boston, Massachusetts 02115, USA
    Nat Chem Biol 1:112-9. 2005
  5. doi Applied aspects of neonicotinoid uses in crop protection
    Alfred Elbert
    Bayer CropScience, Development, Agronomic Development, Alfred Nobel Strasse 50, D 40789 Monheim, Germany
    Pest Manag Sci 64:1099-105. 2008
  6. doi Olmesartan for the delay or prevention of microalbuminuria in type 2 diabetes
    Hermann Haller
    Department of Nephrology and Hypertension, Hannover Medical School, Hannover, Germany
    N Engl J Med 364:907-17. 2011
  7. doi Denosumab compared with zoledronic acid for the treatment of bone metastases in patients with advanced breast cancer: a randomized, double-blind study
    Alison T Stopeck
    University of Arizona, Arizona Cancer Center, Tucson, AZ, USA
    J Clin Oncol 28:5132-9. 2010
  8. doi Neonicotinoid pesticide reduces bumble bee colony growth and queen production
    Penelope R Whitehorn
    School of Natural Sciences, University of Stirling, Stirling FK9 4LA, UK
    Science 336:351-2. 2012
  9. pmc Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy
    Sanjeev Shangary
    Comprehensive Cancer Center and Departments of University of Michigan, Ann Arbor, Michigan 48109, USA
    Annu Rev Pharmacol Toxicol 49:223-41. 2009
  10. pmc An amino-bisphosphonate targets MMP-9-expressing macrophages and angiogenesis to impair cervical carcinogenesis
    Enrico Giraudo
    Department of Biochemistry and Biophysics, Diabetes Center, and Comprehensive Cancer Center, University of California, San Francisco, San Francisco, California, USA
    J Clin Invest 114:623-33. 2004

Research Grants

Detail Information

Publications326 found, 100 shown here

  1. ncbi In vivo activation of the p53 pathway by small-molecule antagonists of MDM2
    Lyubomir T Vassilev
    Department of Discovery Oncology, Roche Research Center, Hoffmann La Roche, Inc, Nutley, NJ 07110, USA
    Science 303:844-8. 2004
    ..These compounds bind MDM2 in the p53-binding pocket and activate the p53 pathway in cancer cells, leading to cell cycle arrest, apoptosis, and growth inhibition of human tumor xenografts in nude mice...
  2. doi Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
    Sauveur Michel Maira
    Oncology Disease Area, Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH4002 Basel, Switzerland
    Mol Cancer Ther 7:1851-63. 2008
    ..Collectively, the preclinical data show that NVP-BEZ235 is a potent dual PI3K/mTOR modulator with favorable pharmaceutical properties. NVP-BEZ235 is currently in phase I clinical trials...
  3. doi NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations
    Violeta Serra
    Laboratory of Oncology Research, Medical Oncology Service, Vall d Hebron University Hospital, Barcelona, Spain
    Cancer Res 68:8022-30. 2008
    ..In summary, NVP-BEZ235 inhibits the PI3K/mTOR axis and results in antiproliferative and antitumoral activity in cancer cells with both wild-type and mutated p110-alpha...
  4. ncbi Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury
    Alexei Degterev
    Department of Cell Biology, Harvard Medical School, 240 Longwood Avenue, Boston, Massachusetts 02115, USA
    Nat Chem Biol 1:112-9. 2005
    ..Our study identifies a previously undescribed basic cell-death pathway with potentially broad relevance to human pathologies...
  5. doi Applied aspects of neonicotinoid uses in crop protection
    Alfred Elbert
    Bayer CropScience, Development, Agronomic Development, Alfred Nobel Strasse 50, D 40789 Monheim, Germany
    Pest Manag Sci 64:1099-105. 2008
    ..These innovative developments for life-cycle management, jointly with the introduction of generic products, will, within the next few years, turn neonicotinoids into the most important chemical class in crop protection...
  6. doi Olmesartan for the delay or prevention of microalbuminuria in type 2 diabetes
    Hermann Haller
    Department of Nephrology and Hypertension, Hannover Medical School, Hannover, Germany
    N Engl J Med 364:907-17. 2011
    ..We investigated whether treatment with an angiotensin-receptor blocker (ARB) would delay or prevent the occurrence of microalbuminuria in patients with type 2 diabetes and normoalbuminuria...
  7. doi Denosumab compared with zoledronic acid for the treatment of bone metastases in patients with advanced breast cancer: a randomized, double-blind study
    Alison T Stopeck
    University of Arizona, Arizona Cancer Center, Tucson, AZ, USA
    J Clin Oncol 28:5132-9. 2010
    ....
  8. doi Neonicotinoid pesticide reduces bumble bee colony growth and queen production
    Penelope R Whitehorn
    School of Natural Sciences, University of Stirling, Stirling FK9 4LA, UK
    Science 336:351-2. 2012
    ..Given the scale of use of neonicotinoids, we suggest that they may be having a considerable negative impact on wild bumble bee populations across the developed world...
  9. pmc Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy
    Sanjeev Shangary
    Comprehensive Cancer Center and Departments of University of Michigan, Ann Arbor, Michigan 48109, USA
    Annu Rev Pharmacol Toxicol 49:223-41. 2009
    ..A number of these small-molecule inhibitors, such as analogs of MI-219 and Nutlin-3, have progressed to advanced preclinical development or early phase clinical trials...
  10. pmc An amino-bisphosphonate targets MMP-9-expressing macrophages and angiogenesis to impair cervical carcinogenesis
    Enrico Giraudo
    Department of Biochemistry and Biophysics, Diabetes Center, and Comprehensive Cancer Center, University of California, San Francisco, San Francisco, California, USA
    J Clin Invest 114:623-33. 2004
    ....
  11. doi A meta-analysis of experiments testing the effects of a neonicotinoid insecticide (imidacloprid) on honey bees
    James E Cresswell
    School of Biosciences, University of Exeter, Hatherly Laboratories, Prince of Wales Road, Exeter, EX4 4PS, UK
    Ecotoxicology 20:149-57. 2011
    ....
  12. doi Adjuvant endocrine therapy plus zoledronic acid in premenopausal women with early-stage breast cancer: 62-month follow-up from the ABCSG-12 randomised trial
    Michael Gnant
    Department of Surgery, Comprehensive Cancer Centre Vienna, Medical University of Vienna, A 1090 Vienna, Austria
    Lancet Oncol 12:631-41. 2011
    ..We have now assessed long-term clinical efficacy including disease-free survival and disease outcomes in patients receiving anastrozole or tamoxifen with or without zoledronic acid...
  13. pmc Interactions between Nosema microspores and a neonicotinoid weaken honeybees (Apis mellifera)
    Cedric Alaux
    INRA, UMR 406 Abeilles et Environnement, Laboratoire Biologie et Protection de l abeille, Site Agroparc, 84914 Avignon, France
    Environ Microbiol 12:774-82. 2010
    ..This provides the first evidences that interaction between an infectious organism and a chemical can also threaten pollinators, interactions that are widely used to eliminate insect pests in integrative pest management...
  14. pmc Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells
    Saskia M Brachmann
    Novartis Institutes for BioMedical Research, Oncology Disease Area, CH 4002 Basel, Switzerland
    Proc Natl Acad Sci U S A 106:22299-304. 2009
    ..Overall, this study will provide guidance for patient stratification for forthcoming breast cancer phase II trials for NVP-BEZ235...
  15. doi Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study
    Ezra E W Cohen
    Section of Hematology Oncology, Department of Medicine, University of Chicago Division of Biological Sciences, 5801 S Ellis, Chicago, IL 60637, USA
    J Clin Oncol 26:4708-13. 2008
    ..This multi-institutional study assessed the activity and safety of axitinib, an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3 in patients with advanced thyroid cancer...
  16. ncbi Activation of p38 mitogen-activated protein kinase in spinal microglia is a critical link in inflammation-induced spinal pain processing
    Camilla I Svensson
    Department of Anesthesiology, University of California, San Diego, La Jolla, California, USA
    J Neurochem 86:1534-44. 2003
    ..Taken together, these results indicate that spinal p38 MAPK is involved in inflammation-induced pain and that activated spinal microglia play a direct role in spinal nociceptive processing...
  17. pmc NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomas
    Ta Jen Liu
    Department of Neuro Oncology, The University of Texas M D Anderson Cancer Center, Unit 431, 1515 Holcombe Boulevard, Houston, TX 77030
    Mol Cancer Ther 8:2204-10. 2009
    ..These results warrant further development of NVP-BEZ235 for clinical trials for human gliomas or other advanced cancers with altered PI3K/Akt/mTOR signaling...
  18. ncbi MDM2 inhibitors for cancer therapy
    Lyubomir T Vassilev
    Discovery Oncology, Roche Research Center, Hoffmann La Roche Inc, Nutley, NJ 07110, USA
    Trends Mol Med 13:23-31. 2007
    ..Here, the new developments in the quest for pharmacological p53 activators are reviewed with an emphasis on small-molecule inhibitors of the p53-MDM2 interaction...
  19. pmc The efficacy of the novel dual PI3-kinase/mTOR inhibitor NVP-BEZ235 compared with rapamycin in renal cell carcinoma
    Daniel C Cho
    Division of Hematology and Oncology, Beth Israel Deaconess Medical Center, Boston, Massachusetts 02215, USA
    Clin Cancer Res 16:3628-38. 2010
    ....
  20. doi Phase II study of axitinib in sorafenib-refractory metastatic renal cell carcinoma
    Brian I Rini
    Department of Solid Tumor Oncology and Urology, Cleveland Clinic Taussig Cancer Institute, 9500 Euclid Ave, Desk R35, Cleveland, OH 44195, USA
    J Clin Oncol 27:4462-8. 2009
    ....
  21. ncbi Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results
    Hope S Rugo
    University of California, San Francisco Comprehensive Cancer Center, USA
    J Clin Oncol 23:5474-83. 2005
    ....
  22. pmc Pesticide exposure in honey bees results in increased levels of the gut pathogen Nosema
    Jeffery S Pettis
    USDA ARS Bee Research Laboratory, Beltsville, MD, USA
    Naturwissenschaften 99:153-8. 2012
    ..Interactions between pesticides and pathogens could be a major contributor to increased mortality of honey bee colonies, including colony collapse disorder, and other pollinator declines worldwide...
  23. ncbi YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Cancer Res 67:8014-21. 2007
    ..Further extensive investigation of YM155 in many types of cancer, including HRPC, seems to be worthwhile to develop this novel therapeutic approach...
  24. pmc Paradoxical suppression of cellular senescence by p53
    Zoya N Demidenko
    Department of Cell Stress Biology, Roswell Park Cancer Institute, Buffalo, NY 14263, USA
    Proc Natl Acad Sci U S A 107:9660-4. 2010
    ..Thus, in spite of its ability to induce cell cycle arrest, p53 can act as a suppressor of cellular senescence...
  25. pmc Dual targeting of phosphoinositide 3-kinase and mammalian target of rapamycin using NVP-BEZ235 as a novel therapeutic approach in human ovarian carcinoma
    Chintda Santiskulvong
    Division of Gynecologic Oncology, Departments of Obstetrics and Gynecology, UCLA David Geffen School of Medicine, Los Angeles, CA 90095 1740, USA
    Clin Cancer Res 17:2373-84. 2011
    ..This study evaluates the effect of dual PI3K and mTOR inhibition using NVP-BEZ235 in preclinical models of ovarian cancer as a potential novel therapeutic strategy...
  26. doi Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3
    Dana D Hu-Lowe
    Department of Cancer Biology, PGRD La Jolla, Pfizer, Inc, San Diego, California 92121, USA
    Clin Cancer Res 14:7272-83. 2008
    ..We provide a comprehensive description of its in vitro characteristics and activities, in vivo antiangiogenesis, and antitumor efficacy and translational pharmacology data...
  27. ncbi Translocation of neonicotinoid insecticides from coated seeds to seedling guttation drops: a novel way of intoxication for bees
    V Girolami
    Dipartimento di Agronomia Ambientale e Produzioni Vegetali, Entomologia, Universita di Padova, Viale dell Universita 16, 35020 Legnaro, Padova, Italy
    J Econ Entomol 102:1808-15. 2009
    ..When bees consume guttation drops, collected from plants grown from neonicotinoid-coated seeds, they encounter death within few minutes...
  28. doi Activity of the novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 against T-cell acute lymphoblastic leukemia
    Francesca Chiarini
    Department of Human Anatomy, University of Bologna, Bologna, Italy
    Cancer Res 70:8097-107. 2010
    ....
  29. doi Efficacy and safety of axitinib in patients with advanced non-small-cell lung cancer: results from a phase II study
    Joan H Schiller
    University of Texas Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 8852, USA
    J Clin Oncol 27:3836-41. 2009
    ....
  30. doi Combination of nutlin-3 and VX-680 selectively targets p53 mutant cells with reversible effects on cells expressing wild-type p53
    C F Cheok
    A STAR, Immunos, Singapore
    Cell Death Differ 17:1486-500. 2010
    ..We highlight the distinct roles of p53 and p73 in mediating the cellular responses to VX-680 and suggest that dual protection by p53 and p73 are needed to guard against endoreduplication and polyploidy...
  31. doi NVP-BEZ235 as a new therapeutic option for sarcomas
    Maria C Manara
    Laboratorio di Ricerca Oncologica, Istituto Ortopedico Rizzoli, Bologna, Italy
    Clin Cancer Res 16:530-40. 2010
    ..To evaluate the in vitro and in vivo effects of NVP-BEZ235, a dual pan-phosphoinositide 3-kinase-mammalian target of rapamycin inhibitor in the three most common musculoskeletal tumors (osteosarcoma, Ewing's sarcoma, and rhabdomyosarcoma)...
  32. doi Effect of axitinib (AG-013736) on fatigue, thyroid-stimulating hormone, and biomarkers: a phase I study in Japanese patients
    Toru Mukohara
    National Cancer Center Hospital East, Oncology Hematology, Kashiwa, Japan
    Cancer Sci 101:963-8. 2010
    ..Axitinib 5 mg twice-daily is the recommended starting dose for Japanese patients. This trial is registered with ClinicalTrials.gov, identifier NCT00447005...
  33. ncbi Selective impairment of TLR-mediated innate immunity in human newborns: neonatal blood plasma reduces monocyte TNF-alpha induction by bacterial lipopeptides, lipopolysaccharide, and imiquimod, but preserves the response to R-848
    Ofer Levy
    Channing Laboratory, Brigham and Women s Hospital, Boston, MA 02115, USA
    J Immunol 173:4627-34. 2004
    ..Conversely, relative preservation of responses to R-848 may present unique opportunities for augmenting innate and acquired immunity in the human newborn...
  34. doi Dual inhibition of PI3K and mTORC1/2 signaling by NVP-BEZ235 as a new therapeutic strategy for acute myeloid leukemia
    Nicolas Chapuis
    Institut Cochin, Universite Paris Descartes, CNRS UMR8104 INSERM U1016 Service d Hématologie Biologique, Hopital Cochin, AP HP, Paris, France
    Clin Cancer Res 16:5424-35. 2010
    ..We therefore tested, in this study, the antileukemic activity of the dual PI3K/mTOR ATP-competitive inhibitor NVP-BEZ235 compound (Novartis)...
  35. pmc Neonicotinoids in bees: a review on concentrations, side-effects and risk assessment
    Tjeerd Blacquière
    Plant Research International, Wageningen University and Research, Wageningen, The Netherlands
    Ecotoxicology 21:973-92. 2012
    ..Molecular markers may be used to improve risk assessment by a better understanding of the mode of action (interaction with receptors) of neonicotinoids in bees leading to the identification of environmentally safer compounds...
  36. ncbi Human TLR7 or TLR8 independently confer responsiveness to the antiviral compound R-848
    Marion Jurk
    Nat Immunol 3:499. 2002
  37. doi Synergistic action of a RAF inhibitor and a dual PI3K/mTOR inhibitor in thyroid cancer
    Ning Jin
    Cancer Biology Division, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland, USA
    Clin Cancer Res 17:6482-9. 2011
    ..We tested a novel drug combination targeting RAF, phosphoinositide 3-kinase (PI3K), and mTOR, plus VEGFR2 and RET, in thyroid cancer preclinical models with defined genetic backgrounds...
  38. pmc Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition
    Anthony C Faber
    Massachusetts General Hospital Cancer Center, Harvard Medical School, Charlestown, MA 02129, USA
    Proc Natl Acad Sci U S A 106:19503-8. 2009
    ..These data indicate simultaneous inhibition of PI3K-mTOR and MEK signaling is an effective strategy for treating EGFR mutant lung cancers, including those with acquired resistance to EGFR TKIs...
  39. doi A multi-center phase II evaluation of the small molecule survivin suppressor YM155 in patients with unresectable stage III or IV melanoma
    Karl D Lewis
    University of Colorado Health Sciences Center, Aurora, CO, USA
    Invest New Drugs 29:161-6. 2011
    ..YM155 is a small molecule suppressant of survivin that has been shown in preclinical cell lines, xenograft models and phase I studies to have anti-tumor activity...
  40. pmc RFID tracking of sublethal effects of two neonicotinoid insecticides on the foraging behavior of Apis mellifera
    Christof W Schneider
    Institut für Bienenkunde, Department of Biological Science, Goethe University, Frankfurt am Main, Germany
    PLoS ONE 7:e30023. 2012
    ..We contribute further information on the understanding of how honeybees are affected by sublethal doses of insecticides...
  41. ncbi Axitinib treatment in patients with cytokine-refractory metastatic renal-cell cancer: a phase II study
    Olivier Rixe
    Pitie Salpetriere Hospital, University of Paris, Paris, France
    Lancet Oncol 8:975-84. 2007
    ..We aimed to assess the activity and safety of axitinib in patients with metastatic renal-cell cancer who had failed on previous cytokine-based treatment...
  42. ncbi Activation of p53 by MDM2 antagonists can protect proliferating cells from mitotic inhibitors
    Daisy Carvajal
    Discovery Oncology, Roche Research Center, Hoffmann La Roche Inc, Nutley, New Jersey 07110, USA
    Cancer Res 65:1918-24. 2005
    ..Second, pretreatment with MDM2 antagonists before chemotherapy of tumors with mutant p53 may offer a partial protection to proliferating normal tissues...
  43. ncbi p38 mitogen-activated protein kinase is activated after a spinal nerve ligation in spinal cord microglia and dorsal root ganglion neurons and contributes to the generation of neuropathic pain
    Shan Xue Jin
    Neural Plasticity Research Group, Department of Anesthesia and Critical Care, Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts 02129, USA
    J Neurosci 23:4017-22. 2003
    ..Coactivation of p38 in DRG neurons and spinal microglia may contribute to later phases of neuropathic pain...
  44. pmc Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235
    Pieter J A Eichhorn
    Medical Oncology Program, Vall d Hebron Institut de Oncologia, Barcelona, Spain
    Cancer Res 68:9221-30. 2008
    ..Our data show that deregulation of the PI3K pathway, either through loss-of-function mutations in PTEN or dominant activating mutations in PIK3CA, leads to lapatinib resistance, which can be effectively reversed by NVP-BEZ235...
  45. ncbi Toxicity and nicotinic acetylcholine receptor interaction of imidacloprid and its metabolites in Apis mellifera (Hymenoptera: Apidae)
    R Nauen
    Bayer AG, Agrochemicals Division, Research Insecticides, Building 6220, D 51368 Leverkusen, Germany
    Pest Manag Sci 57:577-86. 2001
    ..The electrophysiological data revealed Hill coefficients of approximately 1, indicating a single binding site responsible for an activation of the receptor and no direct cooperativity or allosteric interaction with a second binding site...
  46. ncbi A protein kinase involved in the regulation of inflammatory cytokine biosynthesis
    J C Lee
    Department of Cellular Biochemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406
    Nature 372:739-46. 1994
    ..Binding of the pyridinyl-imidazole compounds inhibited CSBP kinase activity and could be directly correlated with their ability to inhibit cytokine production, suggesting that the CSBPs are critical for cytokine production...
  47. ncbi Morbidity and Mortality After Stroke, Eprosartan Compared with Nitrendipine for Secondary Prevention: principal results of a prospective randomized controlled study (MOSES)
    Joachim Schrader
    Department of Internal Medicine, St Josefs Hospital, Cloppenburg, Germany
    Stroke 36:1218-26. 2005
    ..In hypertensive stroke patients, for the same level of blood pressure control, eprosartan will be more effective than nitrendipine in reducing cerebrovascular and cardiovascular morbidity and mortality...
  48. ncbi Zoledronic acid and clinical fractures and mortality after hip fracture
    Kenneth W Lyles
    Duke University Medical Center, Durham, NC, USA
    N Engl J Med 357:1799-809. 2007
    ..Mortality is increased after a hip fracture, and strategies that improve outcomes are needed...
  49. doi E2F-1 transcriptional activity is a critical determinant of Mdm2 antagonist-induced apoptosis in human tumor cell lines
    M Kitagawa
    Helen Diller Family Comprehensive Cancer Center and Cancer Research Institute, University of California, San Francisco, CA 94115, USA
    Oncogene 27:5303-14. 2008
    ..Furthermore, our results suggest that tumor cells, including Rb mutated cells, which harbor wild-type p53 and high E2F transcriptional activity, could be a good target for Mdm2 antagonist therapy...
  50. ncbi HDM2 antagonist Nutlin-3 disrupts p73-HDM2 binding and enhances p73 function
    L M S Lau
    Division of Hematology Oncology, Department of Paediatrics, Hospital for Sick Children, University of Toronto, Ontario, Canada
    Oncogene 27:997-1003. 2008
    ....
  51. doi Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor
    Mark J Mulvihill
    OSI Oncology, OSI Pharmaceuticals, Inc, 41 Pinelawn, Melville, NY 11747, USA
    Future Med Chem 1:1153-71. 2009
    ..The IGF-1 receptor (IGF-1R) has been implicated in the promotion of tumorigenesis, metastasis and resistance to cancer therapies. Therefore, this receptor has become a major focus for the development of anticancer agents...
  52. ncbi Abnormal foraging behavior induced by sublethal dosage of imidacloprid in the honey bee (Hymenoptera: Apidae)
    E C Yang
    Department of Entomology, National Chung Hsing University, Taichung, Taiwan
    J Econ Entomol 101:1743-8. 2008
    ..Returning bees also showed delay in their return trips. Our results demonstrated that sublethal dosages of imidacloprid were able to affect foraging behavior of honey bees...
  53. doi Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors
    Romina Marone
    Department of Biomedicine, University of Basel, Mattenstrasse 28, CH 4058 Basel, Switzerland
    Mol Cancer Res 7:601-13. 2009
    ..Based on the above results, NVP-BEZ235, which has entered phase I/II clinical trials in patients with advanced solid tumors, has a potential in metastatic melanoma therapy...
  54. ncbi Differential binding of p53 and nutlin to MDM2 and MDMX: computational studies
    Thomas Leonard Joseph
    Bioinformatics Institute A STAR, Matrix, Singapore
    Cell Cycle 9:1167-81. 2010
    ..These conclusions provide insight into future drug design for dual inhibitors of MDM2 and MDMX, both of which are oncoproteins found overexpressed in many cancers...
  55. ncbi Small anti-viral compounds activate immune cells via the TLR7 MyD88-dependent signaling pathway
    Hiroaki Hemmi
    Department of Host Defense, Research Institute for Microbial Diseases, Osaka University, 3 1 Yamada oka, Suita, Osaka 565 0871, Japan
    Nat Immunol 3:196-200. 2002
    ..Imidazoquinoline-induced signaling events were also abolished in both MyD88- and TLR7-deficient mice...
  56. ncbi Effects of imidacloprid and deltamethrin on associative learning in honeybees under semi-field and laboratory conditions
    Axel Decourtye
    Laboratoire de Neurobiologie Comparée des Invertébrés, INRA, BP 23, 91440 Bures sur Yvette, France
    Ecotoxicol Environ Saf 57:410-9. 2004
    ....
  57. doi The novel orally bioavailable inhibitor of phosphoinositol-3-kinase and mammalian target of rapamycin, NVP-BEZ235, inhibits growth and proliferation in multiple myeloma
    Philipp Baumann
    Department of Hematology and Oncology Medizinische Klinik Innenstadt, Klinikum der Universitat Munchen, Germany
    Exp Cell Res 315:485-97. 2009
    ..Taken together, inhibition of PI3 kinase/mTOR by NVP-BEZ235 is highly effective and NVP-BEZ235 represents a potential new candidate for targeted therapy in multiple myeloma...
  58. doi Antitumor activity of the selective MDM2 antagonist nutlin-3 against chemoresistant neuroblastoma with wild-type p53
    Tom Van Maerken
    Center for Medical Genetics, Ghent University Hospital, Ghent, Belgium
    J Natl Cancer Inst 101:1562-74. 2009
    ..Mutational inactivation of p53 is rare in neuroblastoma tumors at diagnosis and occurs in only a subset of multidrug-resistant neuroblastomas...
  59. pmc MDM2 antagonists induce p53-dependent apoptosis in AML: implications for leukemia therapy
    Kensuke Kojima
    Section of Molecular Hematology and Therapy, Department of Blood and Marrow Transplantation, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Blvd, Unit 448, Houston, TX 77030, USA
    Blood 106:3150-9. 2005
    ..p53 activation by targeting the p53-MDM2 interaction might offer a novel therapeutic strategy for AML that retain wild-type p53...
  60. doi Antitumor effects of YM155, a novel survivin suppressant, against human aggressive non-Hodgkin lymphoma
    Aya Kita
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Leuk Res 35:787-92. 2011
    ..YM155 increased survival significantly versus rituximab in disseminated Ramos models. This study suggests that YM155 may represent an effective treatment for aggressive lymphomas...
  61. pmc The synergistic action of imidacloprid and flumethrin and their release kinetics from collars applied for ectoparasite control in dogs and cats
    Dorothee Stanneck
    Bayer Animal Health GmbH, Leverkusen, Germany
    Parasit Vectors 5:73. 2012
    ..A new polymer matrix collar has recently been developed which is registered for 8 months use in cats and dogs. The basic properties of this collar have been investigated in several in vitro and in vivo studies...
  62. ncbi New risk assessment approach for systemic insecticides: the case of honey bees and imidacloprid (Gaucho)
    Marie Pierre Halm
    Centre d Etude et de Recherche du Médicament de Normandie, 5 rue Vaubenard, 14032 Caen, France
    Environ Sci Technol 40:2448-54. 2006
    ..These data are discussed in the light of field observations made on honey bee mortalities and disappearances. New perspectives are given to better determine the risk posed by systemic insecticides to honey bees...
  63. doi YM155, a novel survivin suppressant, enhances taxane-induced apoptosis and tumor regression in a human Calu 6 lung cancer xenograft model
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Anticancer Drugs 22:454-62. 2011
    ....
  64. doi Broad spectrum and potent antitumor activities of YM155, a novel small-molecule survivin suppressant, in a wide variety of human cancer cell lines and xenograft models
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma, Inc, Tsukuba, Ibaraki, Japan
    Cancer Sci 102:614-21. 2011
    ..The broad and potent antitumor activity presented in the present study is indicative of the therapeutic potential of YM155 in the clinical setting...
  65. pmc Vertical targeting of the phosphatidylinositol-3 kinase pathway as a strategy for treating melanoma
    Saadia A Aziz
    Department of Pathology, Yale University School of Medicine, Yale Cancer Center, New Haven, Connecticut 06510, USA
    Clin Cancer Res 16:6029-39. 2010
    ..We studied in vitro activity of a novel dual PI3K/mTOR inhibitor NVP-BEZ235 and activity of the combination of NVP-BEZ235 and the MAP/ERK kinase (MEK) inhibitor AZD6244...
  66. ncbi Mechanism-specific signatures for small-molecule p53 activators
    Ingeborg M M van Leeuwen
    Karolinska Institutet, Stockholm, Sweden
    Cell Cycle 10:1590-8. 2011
    ....
  67. doi Efficacy of zoledronic acid in postmenopausal women with early breast cancer receiving adjuvant letrozole: 36-month results of the ZO-FAST Study
    H Eidtmann
    Klinik fur Gynakologie und Geburtshilfe, Universitäts Frauenklinik Kiel, Kiel, Germany
    Ann Oncol 21:2188-94. 2010
    ..Aromatase inhibitors (AIs) are accepted as adjuvant therapy for postmenopausal women (PMW) with hormone-responsive early breast cancer (EBC) with superior efficacy to tamoxifen. However, increased bone loss is associated with AIs...
  68. pmc The combination of RAD001 and NVP-BEZ235 exerts synergistic anticancer activity against non-small cell lung cancer in vitro and in vivo
    Cheng Xiong Xu
    Department of Hematology and Medical Oncology, Emory University School of Medicine and Winship Cancer Institute, Atlanta, Georgia, United States of America
    PLoS ONE 6:e20899. 2011
    ..Taken together, our results suggest that the combination of RAD001 and BEZ235 is a novel strategy for cancer therapy...
  69. pmc Enhancing the cellular uptake of Py-Im polyamides through next-generation aryl turns
    Jordan L Meier
    Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA
    Nucleic Acids Res 40:2345-56. 2012
    ..Overall this provides a step forward for controlling the intracellular concentration of Py-Im polyamides that will prove valuable for future applications in which biological potency is essential...
  70. pmc DNA damage response to the Mdm2 inhibitor nutlin-3
    Rajeev Verma
    Department of Molecular and Cell Biology U3125, University of Connecticut, Storrs, CT 06269, USA
    Biochem Pharmacol 79:565-74. 2010
    ..Although this effect may suppress illegitimate homologous recombination repair, it may also increase the risk of clastogenic events...
  71. ncbi Mouse double minute antagonist Nutlin-3a enhances chemotherapy-induced apoptosis in cancer cells with mutant p53 by activating E2F1
    G Ambrosini
    Laboratory of New Drug Development, Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA
    Oncogene 26:3473-81. 2007
    ..Nutlin-3a therefore may provide a therapeutic benefit in tumors with mutant p53 provided it is combined with chemotherapy...
  72. doi Restoration of p53 pathway by nutlin-3 induces cell cycle arrest and apoptosis in human rhabdomyosarcoma cells
    Mitsuru Miyachi
    Department of Pediatrics, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kyoto, Japan
    Clin Cancer Res 15:4077-84. 2009
    ..In this study, we evaluated whether nutlin-3, a recently developed small-molecule antagonist of MDM2, has an effect on p53-dependent cell cycle arrest and apoptosis in cultured human RMS cell lines...
  73. pmc First-line treatment with zoledronic acid as compared with clodronic acid in multiple myeloma (MRC Myeloma IX): a randomised controlled trial
    Gareth J Morgan
    Institute of Cancer Research, Royal Marsden NHS Foundation Trust, London, UK
    Lancet 376:1989-99. 2010
    ..We aimed to establish whether bisphosphonates can affect clinical outcomes in patients with multiple myeloma...
  74. ncbi Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885
    Alastair J King
    Department of Oncology, MMPD CEDD, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Cancer Res 66:11100-5. 2006
    ....
  75. ncbi Cellular quiescence caused by the Mdm2 inhibitor nutlin-3A
    Lioubov G Korotchkina
    Department of Cell Stress Biology, Roswell Park Cancer Institute, BLSC, Buffalo, NY, USA
    Cell Cycle 8:3777-81. 2009
    ..We discuss that Mdm antagonists could be used in combination with chemotherapy to reversibly arrest normal cells, thus protecting them during chemotherapy of cancer (cyclotherapy)...
  76. pmc Dual phosphoinositide 3-kinase/mammalian target of rapamycin blockade is an effective radiosensitizing strategy for the treatment of non-small cell lung cancer harboring K-RAS mutations
    Georgia Konstantinidou
    Division of Hematology and Oncology, Simmons Comprehensive Cancer Center, and Hamon Center for Therapeutic Oncology Research, Department of Pathology, University of Texas Southwestern Medical Center, Dallas, Texas TX 75390, USA
    Cancer Res 69:7644-52. 2009
    ..These findings may have general applicability in cancer therapy, because aberrant activation of PI3K occurs frequently in human cancer...
  77. ncbi Metabolism of imidacloprid in Apis mellifera
    Séverine Suchail
    INRA, UMR 406 INRA UAPV Ecologie des invertébrés, Site Agroparc, 84914 Avignon Cedex 9, France
    Pest Manag Sci 60:291-6. 2004
    ..Thus, 5-hydroxyimidacloprid and olefin could not be the major metabolites in the worker bees...
  78. doi A double-blinded head-to-head trial of minodronate and alendronate in women with postmenopausal osteoporosis
    Hiroshi Hagino
    Rehabilitation Division and School of Health Science, Tottori University, Yonago, Tottori 683 8504, Japan
    Bone 44:1078-84. 2009
    ..In a randomized, active-controlled, double-blinded, multicenter study, the efficacy and safety of minodronate were examined and compared to that of alendronate...
  79. ncbi Once-yearly zoledronic acid for treatment of postmenopausal osteoporosis
    Dennis M Black
    University of California, San Francisco, San Francisco, CA 94107, USA
    N Engl J Med 356:1809-22. 2007
    ..We assessed the effects of annual infusions of zoledronic acid on fracture risk during a 3-year period...
  80. pmc Cyclic pyrrole-imidazole polyamides targeted to the androgen response element
    David M Chenoweth
    Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, California 91125, USA
    J Am Chem Soc 131:7182-8. 2009
    ..We find that cyclic Py-Im polyamides 1-3 bind DNA with exceptionally high affinities and regulate the expression of AR target genes in cell culture studies, from which we infer that the cycle is cell permeable...
  81. doi Phase I study of YM155, a novel survivin suppressant, in patients with advanced solid tumors
    Taroh Satoh
    Department of Medical Oncology, Kinki University School of Medicine, Osaka, Japan
    Clin Cancer Res 15:3872-80. 2009
    ..The aim of this study was to determine the maximum tolerated dose (MTD) and to assess the safety, pharmacokinetics, and antitumor activity of YM155 in patients with advanced refractory solid tumors...
  82. doi Antimyeloma activity of the orally bioavailable dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235
    Douglas W McMillin
    Jerome Lipper Multiple Myeloma Center, Department of Medical Oncology, Dana Farber Cancer Institute, Boston, Massachusetts 02115, USA
    Cancer Res 69:5835-42. 2009
    ..g., dexamethasone and doxorubicin) or novel (e.g., bortezomib) anti-MM agents showed lack of antagonism. These results indicate that BEZ235 merits clinical testing, alone and in combination with other agents, in MM...
  83. doi HIPK2 regulation by MDM2 determines tumor cell response to the p53-reactivating drugs nutlin-3 and RITA
    Cinzia Rinaldo
    Department of Experimental Oncology, Molecular Oncogenesis Laboratory, Regina Elena Cancer Institute, Rome, Italy
    Cancer Res 69:6241-8. 2009
    ..These data indicate that strategies of p53 reactivation by MDM2 inhibition should also take into consideration MDM2 targets other than p53, such as the apoptosis activator HIPK2...
  84. ncbi Distribution of [(14)C]imidacloprid in sunflowers (Helianthus annuus L.) following seed treatment
    François M Laurent
    INRA, UMR Xenobiotiques, B P 3, 180 chemin de Tournefeuille, 31931 Toulouse Cedex 9, France
    J Agric Food Chem 51:8005-10. 2003
    ..In pollen, concentrations of imidacloprid were 13 ng x g(-1). Thus, imidacloprid residues from Gaucho seed treatment contaminated sunflower pollen, involving the translocation of imidacloprid within the plant...
  85. doi MDM2 antagonist nutlin-3 displays antiproliferative and proapoptotic activity in mantle cell lymphoma
    Yoko Tabe
    Hematopathology Section, Laboratory of Pathology, National Cancer Institute, NIH, Bethesda, Maryland 20892, USA
    Clin Cancer Res 15:933-42. 2009
    ..We wished to determine whether Nutlin-3, a novel small-molecule murine double minute 2 (MDM2) antagonist that efficiently activates TP53, might be effective in inducing cell death in MCL...
  86. ncbi Long-term efficacy of zoledronic acid for the prevention of skeletal complications in patients with metastatic hormone-refractory prostate cancer
    Fred Saad
    Centre Hospitalier de l Universite de Montreal, Hopital Notre Dame, Montreal, Quebec, Canada
    J Natl Cancer Inst 96:879-82. 2004
    ..Long-term treatment with 4 mg of zoledronic acid is safe and provides sustained clinical benefits for men with metastatic hormone-refractory prostate cancer...
  87. pmc Nutlin-3a activates p53 to both down-regulate inhibitor of growth 2 and up-regulate mir-34a, mir-34b, and mir-34c expression, and induce senescence
    Kensuke Kumamoto
    Laboratory of Human Carcinogenesis, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, Maryland 20892 4258, USA
    Cancer Res 68:3193-203. 2008
    ....
  88. doi Multicenter phase II trial of YM155, a small-molecule suppressor of survivin, in patients with advanced, refractory, non-small-cell lung cancer
    Giuseppe Giaccone
    Vrije Universiteit Medical Center, Amsterdam, The Netherlands
    J Clin Oncol 27:4481-6. 2009
    ..To evaluate the antitumor activity and safety of YM155, a novel, small-molecule suppressor of survivin, as single-agent therapy in patients with previously treated, advanced non-small-cell lung cancer (NSCLC)...
  89. ncbi Antiinflammatory effects of angiotensin II subtype 1 receptor blockade in hypertensive patients with microinflammation
    Danilo Fliser
    Division of Nephrology, Department of Internal Medicine, Medical School Hannover, Carl Neuberg Strasse 1, 30625 Hannover, Germany
    Circulation 110:1103-7. 2004
    ....
  90. pmc Acquisition of p53 mutations in response to the non-genotoxic p53 activator Nutlin-3
    M H Aziz
    Department of Anatomy and Cell Biology, Rush University Medical Center, Chicago, IL 60612, USA
    Oncogene 30:4678-86. 2011
    ..These findings have implications for the potential clinical use of Nutlin and other small molecule MDM2 antagonists...
  91. doi Pharmacological activation of the p53 pathway in haematological malignancies
    Manujendra N Saha
    Division of Cellular and Molecular Biology, Toronto General Hospital Research Institute, University of Toronto, Canada
    J Clin Pathol 63:204-9. 2010
    ..This review will highlight recent findings in the research into molecules capable of modulating p53 protein activities and mechanisms that activate the p53 pathway, restoring response to therapy in haematological malignancies...
  92. pmc The effect of soaking allograft in bisphosphonate: a pilot dose-response study
    Thomas Jakobsen
    Orthopaedic Research Laboratory, Aarhus University Hospital, Norrebrogade 44, Building 1A, DK 8000 Aarhus C, Denmark
    Clin Orthop Relat Res 468:867-74. 2010
    ..Long-term survival of uncemented total joint replacements relies on osseointegration. With reduced bone stock impacted morselized allograft enhances early implant fixation but is subject to resorption...
  93. doi Rapid analysis of neonicotinoid insecticides in guttation drops of corn seedlings obtained from coated seeds
    Andrea Tapparo
    Universita degli Studi di Padova, Dipartimento di Scienze Chimiche, Via Marzolo 1, 35131 Padova, Italy
    J Environ Monit 13:1564-8. 2011
    ....
  94. doi Comparative vascular and renal tubular effects of angiotensin II receptor blockers combined with a thiazide diuretic in humans
    Lionel Coltamai
    Service of Nephrology and Hypertension Consultation, Department of Medicine, CHUV, Lausanne, Switzerland
    J Hypertens 28:520-6. 2010
    ....
  95. doi Transcriptomic and proteomic effects of a neonicotinoid insecticide mixture in the marine mussel (Mytilus galloprovincialis, Lam.)
    Francesco Dondero
    Department of Environmental and Life Sciences, Universita del Piemonte Orientale Amedeo Avogadro, Alessandria, Italy
    Sci Total Environ 408:3775-86. 2010
    ..Notwithstanding the growing attention to the ecotoxicological effects of neonicotinoids, there is a lack of information on their toxicodynamics and their mixture effects, in particular, in aquatic organisms...
  96. doi Breast-cancer adjuvant therapy with zoledronic acid
    Robert E Coleman
    Academic Unit of Clinical Oncology, Weston Park Hospital, University of Sheffield, United Kingdom
    N Engl J Med 365:1396-405. 2011
    ..We conducted a study to determine whether treatment with zoledronic acid, in addition to standard adjuvant therapy, would improve disease outcomes in such patients...
  97. doi Mdm2 inhibition induces apoptosis in p53 deficient human colon cancer cells by activating p73- and E2F1-mediated expression of PUMA and Siva-1
    Ramesh M Ray
    Department of Physiology, University of Tennessee Health Science Center, 894 Union Ave, Memphis, TN 38163, USA
    Apoptosis 16:35-44. 2011
    ..In summary, apoptosis in Caco2 cells lacking functional p53 occurred following the disruption of Mdm2 binding with p73 and Rb leading to the expression of pro-apoptotic proteins, PUMA, Noxa, and Siva-1...
  98. pmc Inhibition of the p38 kinase suppresses the proliferation of human ER-negative breast cancer cells
    Lu Chen
    Breast Center, Baylor College of Medicine, Houston, Texas 77030, USA
    Cancer Res 69:8853-61. 2009
    ..Because most ER-negative breast tumors express mutant p53, our results provide the foundation for future development of p38 inhibitors to target p38 for the treatment of p53 mutant and ER-negative breast cancers...
  99. pmc The transcription-independent mitochondrial p53 program is a major contributor to nutlin-induced apoptosis in tumor cells
    Angelina V Vaseva
    Department of Pathology, Stony Brook University, Stony Brook, NY 11794 8691, USA
    Cell Cycle 8:1711-9. 2009
    ..Moreover, at least in some tumors the transcriptional p53 activities in net balance not only are dispensable for the apoptotic Nutlin response, but appear to actively block its therapeutic effect...
  100. doi Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial
    Tony W Ho
    Merck Research Laboratories, North Wales, PA 19454 1099, USA
    Lancet 372:2115-23. 2008
    ..We aimed to assess the clinical profile of MK-0974 (telcagepant), an orally bioavailable antagonist of CGRP receptor...
  101. doi p21 does not protect cancer cells from apoptosis induced by nongenotoxic p53 activation
    M Xia
    Discovery Oncology, Roche Research Center, Hoffmann La Roche Inc, Nutley, NJ 07110, USA
    Oncogene 30:346-55. 2011
    ..Taken together our results suggest that p21 induction does not affect the apoptotic response to nongenotoxic p53 activation...

Research Grants79

  1. Approaches to Bioactive Aminoimidazole Natural Products
    CARL LOVELY; Fiscal Year: 2007
    ..research described in this submission are to provide a set of synthetic transformations for elaborating simple imidazoles into biologically relevant natural products and congeners...
  2. CYTOCHROMES B: MODELS & PROTEIN STUDIES
    Frances Walker; Fiscal Year: 1991
    ..investigation of 5-corrdiante Ni(II) porphyrins, and investigation of the effect of deportonation of coordinated imidazoles on the reactivity of the dioxygen complexes of Co(II) and Fe(II) porphyrins...
  3. Genetic Analysis of Echinocandin Sensitivity
    Santosh Katiyar; Fiscal Year: 2004
    ..Until recently, available antifungals were limited by systemic toxicity (polyenes and imidazoles), lack of fungicidal activity (triazoles and flucytosine), or narrow spectrum (allylamines)...
  4. Analogs: Unique Probes for Cannabinoid Receptors
    Brian Thomas; Fiscal Year: 2006
    ..modification of each substituent position of the pyrazole nucleus and also include alternative pyrazole, imidazoles and pyrazolo [l,5-f] phenanthridine ring systems where the substituents may or may not maintain the original ..
  5. Rational Development of Anti-Trypanosoma Cruzi Drugs
    Frederick Buckner; Fiscal Year: 2009
    ..2) Synthesize a series of disubstituted imidazoles as potential T. cruzi chemotherapeutics. Preliminary data shows that this series has potent anti-T...
  6. UV RESONANCE RAMAN STUDIES OF PROTEIN STRUCTURE
    Sanford Asher; Fiscal Year: 1992
    ..We will examine electronic communication between the heme molecular orbitals and those of imidazoles bound to the iron in model heme complexes...
  7. IDENTIFICATION OF RECEPTOR SPECIFIC OPIOID LIGANDS
    Richard Houghten; Fiscal Year: 2002
    ..peptidomimetics and over 4 million low molecular weight acyclic and heterocyclic compounds, including indole-imidazoles, quinazolinones, and bicyclic guanidines...
  8. Light activated bioactive substrate release
    RICHARD GIVENS; Fiscal Year: 2007
    ..4) that expand the repertoire of functional groups amenable to phototrigger release including the thiols, imidazoles, amines, phenols, hydroxyl, guanyl groups, (5) that are also chemically robust for applications in synthesis for ..
  9. CAUSES AND CONSEQUENCES OF ACID PH IN TUMORS
    Robert Gillies; Fiscal Year: 2002
    ..to improve measurements of pHe values in tumors using magnetic resonance spectral imaging (MRSI) of derivatized imidazoles. This approach has generated the first-every "pH maps" of living tissue...
  10. Therapeutic Modulation of COX-2-induced Immunosuppression in Metastatic RCC
    Brian Rini; Fiscal Year: 2007
    ..This project will have broad implications for the immunoregulation of cancer and how expression and modulation of COX-2 expression influences the immune response to cancer. ..
  11. Synthesis of Polyketides and Terpenes
    David A Evans; Fiscal Year: 2010
    ..As a consequence, organic synthesis is a critical discipline that continues to have an important impact on the fields of both medicine and biology. ..
  12. Gastrins and Receptors in Colon Carcinogenesis
    Pomila Singh; Fiscal Year: 2007
    ..These results are expected to impact diagnosis, prognosis and clinical management of patients with colon cancer. ..