aminoquinolines

Summary

Summary: Quinolines substituted in any position by one or more amino groups.

Top Publications

  1. ncbi Imiquimod-induced psoriasis-like skin inflammation in mice is mediated via the IL-23/IL-17 axis
    Leslie van der Fits
    Department of Dermatology, Erasmus Medical Center, Rotterdam, The Netherlands
    J Immunol 182:5836-45. 2009
  2. pmc Rational design and characterization of a Rac GTPase-specific small molecule inhibitor
    Yuan Gao
    Division of Experimental Hematology, Children s Hospital Research Foundation, Cincinnati, OH 45229, USA
    Proc Natl Acad Sci U S A 101:7618-23. 2004
  3. 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
  4. pmc Pyridostatin analogues promote telomere dysfunction and long-term growth inhibition in human cancer cells
    Sebastian Müller
    Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK
    Org Biomol Chem 10:6537-46. 2012
  5. pmc A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands
    Deepak Koirala
    Department of Chemistry and Biochemistry and School of Biomedical Sciences, Kent State University, Kent, Ohio 44242, USA
    Nat Chem 3:782-7. 2011
  6. ncbi The small antitumoral immune response modifier imiquimod interacts with adenosine receptor signaling in a TLR7- and TLR8-independent fashion
    Michael P Schön
    Rudolf Virchow Center, DFG Research Center for Experimental Biomedicine and Department of Dermatology, Bayerische Julius Maximilians University, Wurzburg, Germany
    J Invest Dermatol 126:1338-47. 2006
  7. ncbi Imiquimod: mode of action
    M P Schön
    Rudolf Virchow Center, DFG Research Center for Experimental Biomedicine and Department of Dermatology, Julius Maximilians University, Wurzburg, Germany
    Br J Dermatol 157:8-13. 2007
  8. pmc Tumoricidal activity of TLR7/8-activated inflammatory dendritic cells
    Georg Stary
    Department of Dermatology, Division of Immunology, Allergy and Infectious Diseases, Medical University of Vienna, 1090 Vienna, Austria
    J Exp Med 204:1441-51. 2007
  9. pmc Langerin(neg) conventional dendritic cells produce IL-23 to drive psoriatic plaque formation in mice
    Christian Wohn
    Department of Immunology, Erasmus MC, University Medical Center, 3015 GE, Rotterdam, The Netherlands
    Proc Natl Acad Sci U S A 110:10723-8. 2013
  10. pmc Discordant temporal evolution of Pfcrt and Pfmdr1 genotypes and Plasmodium falciparum in vitro drug susceptibility to 4-aminoquinolines after drug policy change in French Guiana
    Eric Legrand
    Institut Pasteur de la Guyane, Centre National de Référence sur la Chimiorésistance du Paludisme dans la région Antilles Guyane, Cayenne, French Guiana
    Antimicrob Agents Chemother 56:1382-9. 2012

Research Grants

Detail Information

Publications265 found, 100 shown here

  1. ncbi Imiquimod-induced psoriasis-like skin inflammation in mice is mediated via the IL-23/IL-17 axis
    Leslie van der Fits
    Department of Dermatology, Erasmus Medical Center, Rotterdam, The Netherlands
    J Immunol 182:5836-45. 2009
    ..This rapid and convenient model allows further elucidation of pathogenic mechanisms and evaluation of new therapies in psoriasis...
  2. pmc Rational design and characterization of a Rac GTPase-specific small molecule inhibitor
    Yuan Gao
    Division of Experimental Hematology, Children s Hospital Research Foundation, Cincinnati, OH 45229, USA
    Proc Natl Acad Sci U S A 101:7618-23. 2004
    ..Thus, NSC23766 constitutes a Rac-specific small-molecule inhibitor that could be useful to study the role of Rac in various cellular functions and to reverse tumor cell phenotypes associated with Rac deregulation...
  3. 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...
  4. pmc Pyridostatin analogues promote telomere dysfunction and long-term growth inhibition in human cancer cells
    Sebastian Müller
    Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK
    Org Biomol Chem 10:6537-46. 2012
    ..Our data emphasize the potential of a senescence-mediated anticancer therapy through the use of G-quadruplex targeting small molecules based on the molecular framework of pyridostatin...
  5. pmc A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands
    Deepak Koirala
    Department of Chemistry and Biochemistry and School of Biomedical Sciences, Kent State University, Kent, Ohio 44242, USA
    Nat Chem 3:782-7. 2011
    ..We anticipate that this single-molecule platform can provide detailed insights into the mechanical, kinetic and thermodynamic properties of liganded bio-macromolecules, which have biological relevance...
  6. ncbi The small antitumoral immune response modifier imiquimod interacts with adenosine receptor signaling in a TLR7- and TLR8-independent fashion
    Michael P Schön
    Rudolf Virchow Center, DFG Research Center for Experimental Biomedicine and Department of Dermatology, Bayerische Julius Maximilians University, Wurzburg, Germany
    J Invest Dermatol 126:1338-47. 2006
    ..These novel mechanisms presumably act synergistic with the positive induction of proinflammatory cytokines and can, at least in part, explain the profound inflammation observed in some patients in vivo...
  7. ncbi Imiquimod: mode of action
    M P Schön
    Rudolf Virchow Center, DFG Research Center for Experimental Biomedicine and Department of Dermatology, Julius Maximilians University, Wurzburg, Germany
    Br J Dermatol 157:8-13. 2007
    ..Since imiquimod, a nucleoside analogue of the imidazoquinoline family, has shown efficacy against many tumour entities, its mode of action has become a focus of scientific interest...
  8. pmc Tumoricidal activity of TLR7/8-activated inflammatory dendritic cells
    Georg Stary
    Department of Dermatology, Division of Immunology, Allergy and Infectious Diseases, Medical University of Vienna, 1090 Vienna, Austria
    J Exp Med 204:1441-51. 2007
    ....
  9. pmc Langerin(neg) conventional dendritic cells produce IL-23 to drive psoriatic plaque formation in mice
    Christian Wohn
    Department of Immunology, Erasmus MC, University Medical Center, 3015 GE, Rotterdam, The Netherlands
    Proc Natl Acad Sci U S A 110:10723-8. 2013
    ..These results suggest therapeutic targeting of IL-23 production by cDCs to refine current treatment strategies for psoriasis. ..
  10. pmc Discordant temporal evolution of Pfcrt and Pfmdr1 genotypes and Plasmodium falciparum in vitro drug susceptibility to 4-aminoquinolines after drug policy change in French Guiana
    Eric Legrand
    Institut Pasteur de la Guyane, Centre National de Référence sur la Chimiorésistance du Paludisme dans la région Antilles Guyane, Cayenne, French Guiana
    Antimicrob Agents Chemother 56:1382-9. 2012
    ..Identification of novel markers of resistance to these antimalarials is needed in this South American area...
  11. pmc Imiquimod clears tumors in mice independent of adaptive immunity by converting pDCs into tumor-killing effector cells
    Barbara Drobits
    Institute for Cancer Research, Department of Medicine I, Comprehensive Cancer Center, Medical University of Vienna, Vienna, Austria
    J Clin Invest 122:575-85. 2012
    ..Our results demonstrate that imiquimod treatment leads to CCL2-dependent recruitment of pDCs and their transformation into a subset of killer DCs able to directly eliminate tumor cells...
  12. pmc Toll-like receptor 7 mediates pruritus
    Tong Liu
    Sensory Plasticity Laboratory, Pain Research Center, Department of Anesthesiology, Perioperative and Pain Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, Massachusetts, USA
    Nat Neurosci 13:1460-2. 2010
    ..Our results indicate that TLR7 mediates itching and is a potential therapeutic target for anti-itch treatment in skin disease conditions...
  13. pmc Small-molecule-mediated G-quadruplex isolation from human cells
    Sebastian Müller
    Department of Chemistry, The University of Cambridge, Cambridge CB2 1EW, UK
    Nat Chem 2:1095-8. 2010
    ..We show that telomeres are targets for the probe, providing further evidence of the formation of G-quadruplexes in human cells...
  14. ncbi Bacterial RNA and small antiviral compounds activate caspase-1 through cryopyrin/Nalp3
    Thirumala Devi Kanneganti
    University of Michigan Medical School, Department of Pathology and Comprehensive Cancer Center, Ann Arbor, Michigan 48109, USA
    Nature 440:233-6. 2006
    ..These results reveal a critical role for cryopyrin in host defence through bacterial RNA-mediated activation of caspase-1, and provide insights regarding the pathogenesis of autoinflammatory syndromes...
  15. ncbi A new primaquine analogue, tafenoquine (WR 238605), for prophylaxis against Plasmodium falciparum malaria
    G D Shanks
    US Army Medical Research Unit, Nairobi, Kenya
    Clin Infect Dis 33:1968-74. 2001
    ..Prophylactic regimens of 200 mg or 400 mg of tafenoquine, taken weekly for < or =13 weeks, are highly efficacious in preventing falciparum malaria and are well tolerated...
  16. ncbi Imiquimod 5% cream for the treatment of actinic keratosis: results from a phase III, randomized, double-blind, vehicle-controlled, clinical trial with histology
    Rolf Markus Szeimies
    Klinikum der Universitat Regensburg, Klinik und Poliklinik fur Dermatologie, Regensburg, Germany
    J Am Acad Dermatol 51:547-55. 2004
    ..Increasing evidence suggests imiquimod may be a safe therapeutic option for the treatment of actinic keratosis (AK). The diagnosis and assessment of most AK lesions is made clinically, without histologic confirmation...
  17. pmc In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon
    Leonardo K Basco
    Unité de Recherche Paludologie Afro Tropicale, Institut de recherche pour le developpement IRD, Organisation de Coordination pour la lutte contre les Endémies en Afrique Centrale OCEAC, Yaounde, Cameroon
    Antimicrob Agents Chemother 47:1391-4. 2003
    ..257, P < 0.05). These results suggest that further development of piperaquine, in combination with dihydroartemisinin, holds promise for use in chloroquine-resistant regions of endemicity...
  18. pmc Immunization of malignant melanoma patients with full-length NY-ESO-1 protein using TLR7 agonist imiquimod as vaccine adjuvant
    Sylvia Adams
    Department of Medicine, Division of Medical Oncology, New York University Cancer Institute, School of Medicine, New York, NY 10016, USA
    J Immunol 181:776-84. 2008
    ..Imiquimod's adjuvant effects require further evaluation and likely need optimization of parameters such as formulation, dose, and timing relative to Ag exposure for maximal immunogenicity...
  19. ncbi Imiquimod 5% cream for the treatment of superficial basal cell carcinoma: results from two phase III, randomized, vehicle-controlled studies
    John Geisse
    Solano Dermatology Associates, Vallejo, CA 94589, USA
    J Am Acad Dermatol 50:722-33. 2004
    ..Imiquimod has been shown to be efficacious as a topical treatment for basal cell carcinoma (BCC)...
  20. ncbi Inhibition of Rac1 decreases the severity of pancreatitis and pancreatitis-associated lung injury in mice
    Marcelo G Binker
    CBRHC Research Center, Arribenos 1697, P 1, Buenos Aires, 1426, Argentina
    Exp Physiol 93:1091-103. 2008
    ....
  21. ncbi Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities
    Peter B Madrid
    Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94143 2280, USA
    Bioorg Med Chem Lett 15:1015-8. 2005
    ..Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2...
  22. ncbi Imiquimod 5% cream for the treatment of superficial basal cell carcinoma: a double-blind, randomized, vehicle-controlled study
    John K Geisse
    Solano Dermatology Associates, Vallejo, California 94589, USA
    J Am Acad Dermatol 47:390-8. 2002
    ..Imiquimod 5% cream may provide an effective nonsurgical treatment for superficial basal cell carcinoma (sBCC) based on results of previous studies...
  23. ncbi Tumor-selective induction of apoptosis and the small-molecule immune response modifier imiquimod
    Margarete Schön
    Department of Dermatology, Otto von Guericke University, Magdeburg, Germany
    J Natl Cancer Inst 95:1138-49. 2003
    ..Imiquimod acts both indirectly, via cytokine-mediated stimulation of cellular immune responses, and directly, through unknown mechanisms against tumor cells. We examined the mechanism by which imiquimod induces apoptosis in cancer cells...
  24. pmc The effect of the PQ1 anti-breast cancer agent on normal tissues
    Ying Ding
    Department of Biochemistry, Kansas State University, Manhattan, Kansas 66506, USA
    Anticancer Drugs 23:897-905. 2012
    ..Our studies indicate that the administration of PQ1 by an oral gavage can be achieved with low toxicity to normal vital organs...
  25. pmc Sensitive and rapid method for amino acid quantitation in malaria biological samples using AccQ.Tag ultra performance liquid chromatography-electrospray ionization-MS/MS with multiple reaction monitoring
    Jenny M Armenta
    Virginia Bioinformatics Institute, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, USA
    Anal Chem 82:548-58. 2010
    ..falciparum and human red blood cells samples. This study should provide a valuable insight into the performance of UPLC-ESI-MS/MS for amino acid quantitation using AccQ*Tag derivatization...
  26. ncbi Dosing with 5% imiquimod cream 3 times per week for the treatment of actinic keratosis: results of two phase 3, randomized, double-blind, parallel-group, vehicle-controlled trials
    Neil Korman
    Department of Dermatology, University Hospitals of Cleveland, Case Western Reserve University, Cleveland, Ohio, USA
    Arch Dermatol 141:467-73. 2005
    ..To evaluate the efficacy and safety of 5% imiquimod cream compared with vehicle in the treatment of actinic keratosis (AK)...
  27. pmc Synthesis, antiprotozoal, antimicrobial, β-hematin inhibition, cytotoxicity and methemoglobin (MetHb) formation activities of bis(8-aminoquinolines)
    Kirandeep Kaur
    Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S A S Nagar, Punjab 160 062, India
    Bioorg Med Chem 19:197-210. 2011
    ..search of potent antimalarials based on 8-aminoquinoline structural framework, three series of novel bis(8-aminoquinolines) using convenient one to four steps synthetic procedures were synthesized...
  28. pmc Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway
    Yuji Kan
    Department of Dermatology, Sapporo Medical University School of Medicine, Sapporo, Japan
    J Virol 86:10338-46. 2012
    ..These results indicated that imiquimod acted as an antagonist for adenosine receptor A(1) and induced a host antiviral protein, cystatin A. The process occurred independently of TLR7 and type I IFNs...
  29. pmc Antimalarial activity and mechanisms of action of two novel 4-aminoquinolines against chloroquine-resistant parasites
    Anna Caroline Campos Aguiar
    Centro de Pesquisas Rene Rachou, Fundacao Oswaldo Cruz, Belo Horizonte, Minas Gerais, Brazil
    PLoS ONE 7:e37259. 2012
    ..Taken together, the two CQ analogues represent promising molecules which seem to act in a crucial point for the parasite, inhibiting hemozoin formation...
  30. pmc Review: Improving the therapeutic index of 8-aminoquinolines by the use of drug combinations: review of the literature and proposal for future investigations
    Hla Y Myint
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland, USA
    Am J Trop Med Hyg 85:1010-4. 2011
    Because 8-aminoquinolines affect critical survival stages of Plasmodium parasites, treatment and control of malaria could be markedly improved by more widespread use of these drugs; however, hemolytic toxicity, which is widely prevalent ..
  31. ncbi Inhibition of Rac activity alleviates lipopolysaccharide-induced acute pulmonary injury in mice
    Hong yi Yao
    The Second Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou 310009, PR China
    Biochim Biophys Acta 1810:666-74. 2011
    ..Here, we investigated the roles of Rac including Rac1 and Rac2 in lipopolysaccharide (LPS)-induced pulmonary injury...
  32. ncbi Evaluation of imiquimod for the therapy of external genital and anal warts in comparison with destructive therapies
    H Schöfer
    Department of Dermatology and Venerology, University Hospital, J W Goethe University, Theodor Stern Kai 7, 60590 Frankfurt M, Germany
    Br J Dermatol 157:52-5. 2007
    ....
  33. ncbi Blockade of Rac1 activity induces G1 cell cycle arrest or apoptosis in breast cancer cells through downregulation of cyclin D1, survivin, and X-linked inhibitor of apoptosis protein
    Tatsushi Yoshida
    Division of Therapeutic Proteins, Office of Biotechnology Products, Center for Drug, Evaluation and Research, Food and Drug Administration, Bethesda, Maryland 20892, USA
    Mol Cancer Ther 9:1657-68. 2010
    ..Overall, our results indicate that Rac1 plays a central role in breast cancer cell survival through regulation of NF-kappaB-dependent gene products...
  34. ncbi Enhanced type I interferon signaling and recruitment of chemokine receptor CXCR3-expressing lymphocytes into the skin following treatment with the TLR7-agonist imiquimod
    Joerg Wenzel
    Department of Dermatology, University of Bonn, Bonn, Germany
    J Cutan Pathol 32:257-62. 2005
    ..We hypothesize that TLR7-signaling strongly induces the production of interferon (IFN) alpha, which is able to enhance Th1-mediated cellular antiviral and antitumor immunity...
  35. ncbi Treatment options in melanoma in situ: topical and radiation therapy, excision and Mohs surgery
    Corinne Erickson
    University of Maryland School of Medicine, Baltimore, MD 21201, USA
    Int J Dermatol 49:482-91. 2010
    ..Radiation is much less frequently used. Topical imiquimod has also been more recently proposed, in small case reports in the literature, as a therapy for MIS. However, controversies exist with all approaches...
  36. ncbi The treatment of actinic keratoses with a combination of 5-fluorouracil and imiquimod creams
    Norman M Price
    Department of Dermatology at USCF, San Francisco, CA, USA
    J Drugs Dermatol 6:778-81. 2007
    ..5-fluorouracil (5-FU) and imiquimod creams are accepted topical therapies for actinic keratosis (AK). Both are associated with a prolonged course of treatment with an inflammatory response that may preclude the treatment process...
  37. ncbi Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model
    Hidemichi Suyama
    Department of Anesthesiology and Critical Care, Graduate School of Biomedical Sciences, Hiroshima University, Kasumi 1 2 3, Minami Ku, Hiroshima 734 8551, Japan
    Neurosci Lett 351:133-6. 2003
    ..JTC-801, given orally in food, alleviated heat-evoked hyperalgesia in CCI rats, suggesting that it is useful for the treatment of neuropathic pain...
  38. pmc In vitro activities of trioxaquines against Schistosoma mansoni
    Jérôme Boissier
    UMR 5244 CNRS UPVD EPHE, Laboratoire de Biologie et d Ecologie Tropicale et Méditerranéenne, Universite de Perpignan, 52 Avenue Paul Alduy, 66860 Perpignan, France
    Antimicrob Agents Chemother 53:4903-6. 2009
    ..In this range of concentrations, artemisinin derivatives (artesunate and artemether) have no activity...
  39. ncbi Topical imiquimod and intralesional interleukin-2 increase activated lymphocytes and restore the Th1/Th2 balance in patients with metastatic melanoma
    D S Green
    Department of Oncology, St George s University of London, London SW17 0RE, UK
    Br J Dermatol 159:606-14. 2008
    ..Here we report the results of immunological analysis with the aim of highlighting correlations with our clinical findings...
  40. pmc Immunization with a Toll-like receptor 7 and/or 8 agonist vaccine adjuvant increases protective immunity against Leishmania major in BALB/c mice
    Wen Wei Zhang
    Department of Microbiology and Immunology, 3775 University Street, McGill University, Montreal, Quebec H2A 2B4, Canada
    Infect Immun 76:3777-83. 2008
    ..These observations suggest that topically administered imiquimod or subcutaneously injected R848 represent potential vaccine adjuvants to enhance the TH1 response, which can be used with existing or new vaccine formulations...
  41. ncbi Imiquimod in the treatment of lentigo maligna
    S F Rajpar
    Skin Oncology Service, University Hospital Birmingham NHS Trust, Birmingham B29 6JD, UK
    Br J Dermatol 155:653-6. 2006
    ..Lentigo maligna (LM) is treated to prevent progression to lentigo maligna melanoma (LMM). Surgery remains the treatment of choice, although topical immunotherapy with imiquimod has recently become a popular alternative...
  42. pmc The TLR7 agonists imiquimod and gardiquimod improve DC-based immunotherapy for melanoma in mice
    Fang Ma
    Institute of Immunopharmacology and Immunotherapy, School of Pharmaceutical Sciences, Shandong University, Jinan, China
    Cell Mol Immunol 7:381-8. 2010
    ..More importantly, they can be used as vaccine adjuvants to potentiate the efficiency of DC-based tumor immunotherapy...
  43. ncbi The TLR7 agonist imiquimod enhances the anti-melanoma effects of a recombinant Listeria monocytogenes vaccine
    Noah Craft
    Division of Dermatology, Department of Medicine and Specialty Training and Advanced Research Program, David Geffen School of Medicine, University of California, Los Angeles, CA 90095 1747, USA
    J Immunol 175:1983-90. 2005
    ..The results of these studies have broad implications for future designs of immunotherapeutic vaccines against tumors and the treatment of metastatic melanoma...
  44. pmc The impact of phenotypic and genotypic G6PD deficiency on risk of plasmodium vivax infection: a case-control study amongst Afghan refugees in Pakistan
    Toby Leslie
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, United Kingdom
    PLoS Med 7:e1000283. 2010
    ..The deficiency has a potentially serious interaction with antirelapse therapies (8-aminoquinolines such as primaquine)...
  45. ncbi Generalized psoriasis induced by topical treatment of actinic keratosis with imiquimod
    P A Fanti
    Int J Dermatol 45:1464-5. 2006
  46. ncbi Antimalarial activities of ferroquine conjugates with either glutathione reductase inhibitors or glutathione depletors via a hydrolyzable amide linker
    Natascha Chavain
    Universite de Lille 1, Unite de Catalyse et Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, B P 90108, 59652 Villeneuve d Ascq cedex, France
    Bioorg Med Chem 17:8048-59. 2009
    ....
  47. pmc Role of Rac1 GTPase in JNK signaling and delayed neuronal cell death following global cerebral ischemia
    Quan Guang Zhang
    Developmental Neurobiology Program, Institute of Molecular Medicine and Genetics, Medical College of Georgia, Augusta, GA 30912, USA
    Brain Res 1265:138-47. 2009
    ..As a whole, these studies demonstrate an important role for Rac1 in activation of the prodeath MLK3-JNK kinase signaling pathway and delayed neuronal cell death following cerebral ischemia...
  48. ncbi Hybrid molecules with a dual mode of action: dream or reality?
    Bernard Meunier
    Palumed, rue Pierre et Marie Curie, BP 28262, 31262 Labège Cedex, France
    Acc Chem Res 41:69-77. 2008
    ..More than 100 trioxaquines have been prepared by Palumed over a period of 4 years, and in collaboration with Sanofi-Aventis, the trioxaquine PA1103-SAR116242 has been selected in January 2007 as candidate for preclinical development...
  49. ncbi Cutting edge: priming of CTL by transcutaneous peptide immunization with imiquimod
    Gerd Rechtsteiner
    Institute for Immunology, Johannes Gutenberg University, Mainz, Germany
    J Immunol 174:2476-80. 2005
    ..Our results obtained by simple e.c. application of an ointment, without further skin irritating procedures, provide the basis for the development of new, easy to use vaccines against cancer or virus-associated diseases...
  50. ncbi Identification and characterization of pDC-like cells in normal mouse skin and melanomas treated with imiquimod
    Francesca Palamara
    Department of Dermatology, Division of Immunology, Allergy and Infectious Diseases, Medical University of Vienna, Austria
    J Immunol 173:3051-61. 2004
    ..Therefore, strategies aimed at activating and directing these cells into neoplastic tissues may be a promising and novel approach for the immunotherapy of various types of cancer...
  51. ncbi Treatment of experimental leishmaniasis with the immunomodulators imiquimod and S-28463: efficacy and mode of action
    S Buates
    Institute of Parasitology, McGill University, Ste Anne de Bellevue, Quebec, Canada H9X 3V9
    J Infect Dis 179:1485-94. 1999
    ..Imiquimod and a related compound, S-28463, effectively stimulated leishmanicidal activity in macrophages; moreover, imiquimod stimulated signal transduction associated with inducing nitric oxide synthesis in macrophages...
  52. ncbi Isoquine and related amodiaquine analogues: a new generation of improved 4-aminoquinoline antimalarials
    Paul M O'Neill
    Department of Chemistry, The Robert Robinson Laboratories, University of Liverpool, Liverpool L69 7ZD, UK
    J Med Chem 46:4933-45. 2003
    ..On the basis of these promising initial studies, isoquine (ISQ1 (3a)) represents a new second generation lead worthy of further investigation as a cost-effective and potentially safer alternative to amodiaquine...
  53. ncbi Superoxide constricts rat pulmonary arteries via Rho-kinase-mediated Ca(2+) sensitization
    Greg A Knock
    King s College London, UK
    Free Radic Biol Med 46:633-42. 2009
    ..Hydrogen peroxide did not activate Rho-kinase. We conclude that in rat small pulmonary artery, superoxide triggers Rho-kinase-mediated Ca(2+) sensitization and vasoconstriction independent of hydrogen peroxide...
  54. pmc Selection of a trioxaquine as an antimalarial drug candidate
    Frédéric Coslédan
    Palumed, rue Pierre et Marie Curie, BP 28262, F 31682 Labège Cedex, France
    Proc Natl Acad Sci U S A 105:17579-84. 2008
    ....
  55. pmc Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes
    Françoise Benoit-Vical
    Laboratoire de Chimie de Coordination du CNRS, 205 route de Narbonne, 31077 Toulouse Cedex 4, France
    Antimicrob Agents Chemother 51:1463-72. 2007
    ..The ease of chemical synthesis of this trioxaquine prototype should be considered an additional advantage and would make these drugs affordable without perturbations of the drug supply...
  56. ncbi Generalized exacerbation of psoriasis associated with imiquimod cream treatment of superficial basal cell carcinomas
    N Rajan
    Clin Exp Dermatol 31:140-1. 2006
  57. ncbi Synthetic TLR agonists reveal functional differences between human TLR7 and TLR8
    Keith B Gorden
    3M Pharmaceuticals, St Paul, MN 55144, USA
    J Immunol 174:1259-68. 2005
    ..Thus, this study demonstrated that TLR7 and TLR8 agonists differ in their target cell selectivity and cytokine induction profile...
  58. ncbi Psoriasis induced by topical imiquimod
    Jason K Wu
    Department of Dermatology, Princess Alexandra Hospital, Brisbane, Queensland, Australia
    Australas J Dermatol 45:47-50. 2004
    ..Nine-and-a-half weeks after completing treatment the patient developed disseminated small psoriatic lesions. Other recognized triggers of psoriasis were not identified. The psoriasis resolved slowly with conventional treatment...
  59. ncbi Randomized dose-ranging study of the safety and efficacy of WR 238605 (Tafenoquine) in the prevention of relapse of Plasmodium vivax malaria in Thailand
    D S Walsh
    Department of Immunology, US Army Medical Component, Armed Forces Research Institute of Medical Sciences, Bangkok, Thailand
    J Infect Dis 180:1282-7. 1999
    ..Among patients treated with chloroquine only, there were 4 relapses (days 40, 43, 49, and 84). WR 238605 was safe, well tolerated, and effective in preventing P. vivax relapse...
  60. pmc Analysis of cellular and behavioral responses to imiquimod reveals a unique itch pathway in transient receptor potential vanilloid 1 (TRPV1)-expressing neurons
    Se Jeong Kim
    Department of Pharmacology, University of California at San Diego, La Jolla, CA 92093, USA
    Proc Natl Acad Sci U S A 108:3371-6. 2011
    ..Our data provide evidence supporting the hypothesis that there is a specific subset of TRPV1-expressing neurons that is equipped with diverse intracellular mechanisms that respond to histamine, chloroquine, and IQ...
  61. ncbi Effect of huprine X on β-amyloid, synaptophysin and α7 neuronal nicotinic acetylcholine receptors in the brain of 3xTg-AD and APPswe transgenic mice
    Monika M Hedberg
    Karolinska Institutet, Department of Neurobiology, Care Sciences and Society, Division of Alzheimer Neurobiology, Karolinska University Hospital, Huddinge, Stockholm, Sweden
    Neurodegener Dis 7:379-88. 2010
    ..In this study, the aim was to investigate whether HX could affect the AD-related neuropathology in vivo in two mouse models...
  62. pmc Phase II trial of imiquimod and HPV therapeutic vaccination in patients with vulval intraepithelial neoplasia
    S Daayana
    Academic Unit of Obstetrics and Gynaecology, University of Manchester, St Mary s Hospital, Whitworth Park, Manchester M13 0JH, UK
    Br J Cancer 102:1129-36. 2010
    ..Vulval intraepithelial neoplasia (VIN) is a premalignant condition, which is frequently associated with type HPV16 infection, and multifocal disease has high rates of surgical treatment failure...
  63. ncbi Application of multicomponent reactions to antimalarial drug discovery. Part 2: New antiplasmodial and antitrypanosomal 4-aminoquinoline gamma- and delta-lactams via a 'catch and release' protocol
    Chitalu C Musonda
    Department of Chemistry, University of Cape Town, Rondebosch, South Africa
    Bioorg Med Chem 14:5605-15. 2006
    ..6 microM). Compound 17 inhibited the growth of Trypanosoma brucei with an ED(50) of 1.44 microM whilst exhibiting a favourable therapeutic index of 409 against a human KB cell line...
  64. ncbi Comparison of the potential multiple binding modes of bicyclam, monocylam, and noncyclam small-molecule CXC chemokine receptor 4 inhibitors
    Rebecca S Y Wong
    Genzyme Corporation, Cambridge, Massachusetts, USA
    Mol Pharmacol 74:1485-95. 2008
    ..These mechanistic studies might prove to be useful for the development of future generations of CXCR4 inhibitors with improved clinical pharmacology and safety profiles...
  65. ncbi Treatment of actinic keratoses with sequential use of photodynamic therapy; and imiquimod 5% cream
    Michael Shaffelburg
    Valley Professional Center, Kentville, Nova Scotia, Canada
    J Drugs Dermatol 8:35-9. 2009
    ..Field-directed therapies for actinic keratosis include photodynamic therapy and imiquimod...
  66. pmc Immune-mediated changes in actinic keratosis following topical treatment with imiquimod 5% cream
    Abel Torres
    Dermatology Office, Loma Linda University Medical Center, Loma Linda, California, USA
    J Transl Med 5:7. 2007
    ..The objective of this study was to identify the molecular processes responsible for the anti-lesional activity of imiquimod in subjects with actinic keratosis using global gene expression profiling...
  67. ncbi Imiquimod enhances the systemic immunity attained by local cryosurgery destruction of melanoma lesions
    Pedro Redondo
    Department of Dermatology, University Clinic of Navarra, Pamplona, Navarra, Spain
    J Invest Dermatol 127:1673-80. 2007
    ..These preclinical data and the simplicity of the procedures warrant the design of a pilot clinical trial...
  68. ncbi Genetic and pharmacologic evidence that Rac1 GTPase is involved in regulation of platelet secretion and aggregation
    H Akbar
    Division of Experimental Hematology, Cincinnati Children s Research Foundation, University of Cincinnati, Cincinnati, OH, USA
    J Thromb Haemost 5:1747-55. 2007
    ..Agonists that induce platelet secretion and aggregation also activate Rac1 GTPase, raising the possibility that Rac1 GTPase may be involved in regulation of platelet function...
  69. ncbi TLRs to cytokines: mechanistic insights from the imiquimod mouse model of psoriasis
    Barry Flutter
    St John s Institute of Dermatology, King s College London, London, UK
    Eur J Immunol 43:3138-46. 2013
    ..In this review, we will dissect the findings of the imiquimod model to date and ask how this model can inform us about the immunological aspects of human disease. ..
  70. ncbi Identification of multidrug resistant protein 1 of mouse leukemia P388 cells on a PVDF membrane using 6-aminoquinolyl-carbamyl (AQC)-amino acid analysis and World Wide Web (WWW)-accessible tools
    N Shindo
    Division of Biochemical Analysis, Juntendo University School of Medicine, Tokyo, Japan
    Anal Biochem 264:251-8. 1998
    ..A database search was carried out with bovine serum albumin as a calibration protein. MDR1 in P388/DOX was ranked first by both databases with high reliability (score 14 for ExPASy, distance 1.34 for EMBL)...
  71. ncbi 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode
    Trond Ulven
    7TM Pharma A S, Fremtidsvej 3, DK 2970 Hørsholm, Denmark
    J Med Chem 48:5684-97. 2005
    ..Docking studies suggested that the Asp123 interacts preferentially with the nitrogen of the central quinoline. Synthesis and testing of specific analogues supported our revised binding mode hypothesis...
  72. pmc 4-aminoquinolines active against chloroquine-resistant Plasmodium falciparum: basis of antiparasite activity and quantitative structure-activity relationship analyses
    Simon J Hocart
    Peptide Research, Department of Medicine, School of Medicine, Mail Stop SL 12, Tulane University Health Sciences Center, 1430 Tulane Ave, New Orleans, LA 70112 2699, USA
    Antimicrob Agents Chemother 55:2233-44. 2011
    ....
  73. ncbi Glucose-6-phosphate dehydrogenase deficiency and antimalarial drug development
    Ernest Beutler
    The Scripps Research Institute, La Jolla, California 92037, USA
    Am J Trop Med Hyg 77:779-89. 2007
    ..Additionally, the issues important for conducting larger clinical trials in populations in which G6PD deficiency is prevalent are examined, with a particular focus on antimalarial drug development...
  74. ncbi The TLR-7 agonist, imiquimod, enhances dendritic cell survival and promotes tumor antigen-specific T cell priming: relation to central nervous system antitumor immunity
    Robert M Prins
    Division of Neurosurgery, Department of Surgery, David Geffen School of Medicine, University of California, Los Angeles UCLA, CA 90095, USA
    J Immunol 176:157-64. 2006
    ..Nevertheless, immunotherapeutic targeting of malignant CNS tumors may be enhanced by the administration of the innate immune response modifier imiquimod...
  75. ncbi Administration of imiquimod, an interferon inducer, in asymptomatic human immunodeficiency virus-infected persons to determine safety and biologic response modification
    D Goldstein
    Department of Medical Oncology, Prince of Wales Hospital, National Centre in HIV Epidemiology and Clinical Research, University of New South Wales, Sydney, Australia
    J Infect Dis 178:858-61. 1998
    ..Imiquimod induced pronounced levels of circulating interferon in asymptomatic HIV-infected persons, with variable effect on virus load...
  76. pmc Synthesis and anti-breast cancer activities of substituted quinolines
    Aibin Shi
    Department of Chemistry, Kansas State University, Manhattan, KS 66506, USA
    Bioorg Med Chem Lett 18:3364-8. 2008
    ..IC(50) values of three other quinolines are in the nanomolar range, a desirable range for pharmacological testing...
  77. ncbi The mode of action of chloroquine. Non-weak base properties of 4-aminoquinolines and antimalarial effects on strains of Plasmodium
    E Veignie
    INSERM U 42, Biologie et Biochimie Parasitaires et Fongiques, Villeneuve d Ascq, France
    Ann Trop Med Parasitol 85:229-37. 1991
    ..The importance of the lysosomotropic properties of chloroquine has to be reconsidered in the light of this new information...
  78. pmc An in vivo drug screening model using glucose-6-phosphate dehydrogenase deficient mice to predict the hemolytic toxicity of 8-aminoquinolines
    Peng Zhang
    Division of Experimental Therapeutics and Division of Pathology, Walter Reed Army Institute of Research, Silver Spring, MD, USA
    Am J Trop Med Hyg 88:1138-45. 2013
    Anti-malarial 8-aminoquinolines drugs cause acute hemolytic anemia in individuals with glucose-6-phosphate dehydrogenase deficiency (G6PDD)...
  79. ncbi Psoriasis triggered by toll-like receptor 7 agonist imiquimod in the presence of dermal plasmacytoid dendritic cell precursors
    Michel Gilliet
    Department of Dermatology, University Hospital of Zurich, Zurich, Switzerland
    Arch Dermatol 140:1490-5. 2004
    ..It has been proposed that the innate immune system plays a central role in driving the autoimmune T-cell cascade leading to psoriasis; however, there is no direct evidence for this...
  80. ncbi Imiquimod, a topical immune response modifier, in the treatment of cutaneous metastases of malignant melanoma
    Anne B Bong
    Department of Dermatology and Venereology, Otto von Guericke University, Magdeburg, Germany
    Dermatology 205:135-8. 2002
    ..In addition, several studies have demonstrated antitumoral activity in solar keratoses, superficial basal cell carcinomas and Bowen's disease...
  81. pmc In vitro activity of ferroquine is independent of polymorphisms in transport protein genes implicated in quinoline resistance in Plasmodium falciparum
    Maud Henry
    Unité de Recherche en Biologie et Epidémiologie Parasitaires, Institut de Medecine Tropicale du Service de Sante des Armees, Boulevard Charles Livon, Parc le Pharo, 13998 Marseille Armees, France
    Antimicrob Agents Chemother 52:2755-9. 2008
    ..These data suggest the FQ may not interact with transport proteins in quinoline-resistant parasites. The present results justify further clinical trials of FQ in multidrug resistance areas...
  82. ncbi Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor
    Maria Rosaria Del Giudice
    Dipartimento del Farmaco, Istituto Superiore di Sanita, Viale Regina Elena 299, 00161 Roma, Italy
    Eur J Med Chem 46:1207-21. 2011
    ..In conclusion the present study set the basis for a systematic investigation on the structural modifications that can be introduced into novel ligands for NOPr and helped to feature the surrounds of the allosteric site of NOPr...
  83. ncbi 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity
    H Shinkai
    Central Pharmaceutical Research Institute, JT Inc, 1 1 Murasaki cho, Takatsuki, Osaka 569 1125, Japan
    J Med Chem 43:4667-77. 2000
    ..After a 4-aminoquinoline derivative was found to bind with the human ORL(1) receptor, a series of 4-aminoquinolines and related compounds were synthesized and their binding was evaluated...
  84. pmc Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines
    Kimberly Yearick
    Department of Chemistry, Department of Biochemistry and Cellular and Molecular Biology, and Center for Infectious Diseases, Georgetown University, 37th and O Streets, Washington, D C, USA
    J Med Chem 51:1995-8. 2008
    ..In particular 4b, 5a, 5b, 5d, 17a, and 17b were found to be significantly more potent than chloroquine against the resistant strains Dd2 and FCB...
  85. ncbi Treatment of lentigo maligna with imiquimod before staged excision
    Murray A Cotter
    Department of Dermatology, Huntsman Cancer Institute, University of Utah, Salt Lake City, Utah 84132 2409, USA
    Dermatol Surg 34:147-51. 2008
    ..Imiquimod 5% cream has demonstrated effectiveness in the treatment of lentigo maligna (LM) in several small studies. None of the studies to date have included posttreatment surgical removal to confirm negative histologic margins...
  86. ncbi Successful treatment of perianal Bowen's disease with imiquimod
    Sylvia van Egmond
    University of Melbourne Department of Medicine Dermatology, St Vincent s Hospital, Fitzroy, Australia
    Int J Dermatol 46:318-9. 2007
    ..To our knowledge only two cases of perianal BD, successfully treated with imiquimod, have been reported. We wish to present the third case, effectively treated with imiquimod...
  87. ncbi A new synthetic approach of N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide (JTC-801) and its analogues and their pharmacological evaluation as nociceptin receptor (NOP) antagonists
    Isabella Sestili
    Dipartimento del Farmaco, Istituto Superiore di Sanita, Viale Regina Elena 299, 00161 Rome, Italy
    Eur J Med Chem 39:1047-57. 2004
    ..Structural and conformational requirements for affinity were outlined by NOE NMR and computational methods and suggestions for a pharmacophore model design were provided...
  88. pmc Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801
    Hideki Yamada
    Central Pharmacological Research Institute, JT Inc, 1 1 Murasaki cho, Takatsuki, Osaka, 569 1125, Japan
    Br J Pharmacol 135:323-32. 2002
    ..These results suggest that JTC-801 may represent a new class of analgesics...
  89. ncbi Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation
    Hisayoshi Tamai
    Department of Anesthesiology, Faculty of Medicine, University of Tokyo, Tokyo, Japan
    Eur J Pharmacol 510:223-8. 2005
    ..In conclusion, N/OFQ receptor antagonist JTC-801 exerted anti-allodynic and anti-hyperalgesic effects in rats, suggesting that N/OFQ system might be involved in the modulation of neuropathic pain and inflammatory hyperalgesia...
  90. ncbi Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents
    Ashok Kumar
    Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow, India
    Bioorg Med Chem Lett 20:7059-63. 2010
    ..The promising antimalarial potency of compound 17 highlights the significance of exploring the privileged 4-aminoquinoline class for new antimalarials...
  91. pmc The SINS trial: a randomised controlled trial of excisional surgery versus imiquimod 5% cream for nodular and superficial basal cell carcinoma
    Mara Ozolins
    Centre of Evidence Based Dermatology, King s Meadow Campus, Lenton Lane, Nottingham, NG7 2NR, UK
    Trials 11:42. 2010
    ..2. To ascertain if certain phenotypic features and gene polymorphisms predict tumour responsiveness to treatment...
  92. ncbi Quinolinol and peptide inhibitors of zinc protease in botulinum neurotoxin A: effects of zinc ion and peptides on inhibition
    Huiguo Lai
    Department of Chemistry, Georgetown University, Washington, DC 20057, USA
    Arch Biochem Biophys 491:75-84. 2009
    ..67microM and to Peptide C-BoNT/A LC complex with a K(D) of 2.33microM. The insights of the interactions of quinolinols and peptides with the zinc protease of BoNT/A should aid in the development of inhibitors of metalloproteases...
  93. ncbi Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo
    Margaret A L Blackie
    Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa
    Bioorg Med Chem Lett 20:1078-80. 2010
    ..The in vivo efficacy of PQ, and salts thereof, have been determined in Plasmodium berghei ANKA and Plasmodium yoelii. Phenylequine hydrochloride has shown an ED(50) of 0.81 in P. yoelii (cf chloroquine ED(50)=1.31)...
  94. ncbi Susceptibility of Colombian Plasmodium falciparum isolates to 4-aminoquinolines and the definition of amodiaquine resistance in vitro
    Diego F Echeverry
    International Center for Medical Research and Training, CIDEIM, Cali, Colombia
    Mem Inst Oswaldo Cruz 101:341-4. 2006
    ....
  95. ncbi A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs
    Paul M O'Neill
    Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool L67 7ZD UK
    Curr Top Med Chem 6:479-507. 2006
    A broad overview is presented describing the current knowledge and the ongoing research concerning the 4-aminoquinolines (4AQ) as chemotherapeutic antimalarial agents...
  96. doi Imiquimod treatment of lentigo maligna: an open-label study of 34 primary lesions in 32 patients
    Urs V Buettiker
    Arch Dermatol 144:943-5. 2008
  97. ncbi Imiquimod and lentigo maligna: a search for prognostic features in a clinicopathological study with long-term follow-up
    A M Powell
    St John s Institute of Dermatology, Guy s and St Thomas NHS Trust, London SE1 7EH, UK
    Br J Dermatol 160:994-8. 2009
    ..Imiquimod is a topical immunomodulator which can generate a local cytotoxic response with potentially antiviral and antitumour effects...
  98. ncbi Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century
    Paul M O'Neill
    Department of Chemistry, University of Liverpool, Liverpool, United Kingdom
    J Med Chem 52:1408-15. 2009
    ..This has resulted in the availability of critical information to other drug development teams interested in developing antimalarials within this class...
  99. ncbi Towards the chemoinformatic-based identification of DNA methyltransferase inhibitors: 2D- and 3D-similarity profile of screening libraries
    Jakyung Yoo
    Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, FL 34987, USA
    Curr Comput Aided Drug Des 8:317-29. 2012
    ..This classification is valuable to select structure representations for similarity searching of any other screening library. This work represents a step forward to further advance epigenetic therapies using computational approaches...
  100. ncbi The opioid peptide nociceptin/orphanin FQ mediates prostaglandin E2-induced allodynia, tactile pain associated with nerve injury
    Emiko Okuda-Ashitaka
    Department of Medical Chemistry, Kansai Medical University, 10 15 Fumizono, Moriguchi 570 8506, Japan
    Eur J Neurosci 23:995-1004. 2006
    ..N/OFQ immunoreactive puncta were colocalized with EP4. Taken together, these results demonstrate that PGE(2) induced allodynia by stimulation of N/OFQ release in the spinal cord via EP4 receptor subtypes...
  101. ncbi A pilot study of treatment of lentigo maligna with 5% imiquimod cream
    C J Fleming
    Departments of Dermatology and Pathology, Ninewells Hospital and Medical School, Dundee DD1 9SY, UK
    Br J Dermatol 151:485-8. 2004
    ..Lentigo maligna (LM) is an in situ form of malignant melanoma, and surgical excision is often unsatisfactory. Imiquimod cream is an immune response modifier and induces a predominantly T-helper 1 type response...

Research Grants41

  1. Primaquine-binding proteins identified in Pneumocystis
    SHERRY QUEENER; Fiscal Year: 2006
    ..to standard therapy for patients with pneumonia caused by Pneumocystis, but the mechanism of action of 8-aminoquinolines against the organism and against others such as Plasmodium remains unknown...
  2. DEVELOPMENT OF AMINOQUINOLINE ANTIMALARIALS
    Jeffrey Conroy; Fiscal Year: 2000
    ..and chloroquine-, mefloquine- and multiply-resistant Plasmodium falciparum, and (3) Screen promising aminoquinolines for their resistance to metabolic inactivation by the P-450 system in vitro...
  3. Uveal Melanoma Micrometastasis
    Pierre L Triozzi; Fiscal Year: 2010
    ..Micrometastases, microscopic deposits of tumor that have spread via the bloodstream, are present in many patients with uveal melanoma at diagnosis. This project will test new methods of identifying and inhibiting these deposits. ..
  4. AAV-Based Plasmacytoid Dendritic Cell Cancer Vaccine
    Pierre L Triozzi; Fiscal Year: 2010
    ....
  5. Cannabinoid Regulation of Basal Ganglia Glutamate and GABA
    SCOTT RAWLS; Fiscal Year: 2007
    ..Our outcomes will be a first step in determining whether blocking endocannabinoid inactivation offers any therapeutic advantage over direct activation of cannabinoid receptors with marijuana. [unreadable] [unreadable] [unreadable]..
  6. Can beta-lactam antibiotics decrease morphine physical dependence?
    SCOTT RAWLS; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  7. Keratinocyte Costimulation and Th2-Cell Immune Deviation
    Anthony Gaspari; Fiscal Year: 2009
    ..Similar mechanistic studies of the molecular basis of other skin diseases such as psoriasis have led to the development of biological response modifiers that are now in clinical use. ..
  8. IRRITANTS EFFECTS ON EPIDERMAL ANTIGEN PRESENTATION
    Anthony Gaspari; Fiscal Year: 2002
    ....
  9. Dermatomyositis Skin Disease Severity Measure Validation
    JOSPEH JORIZZO; Fiscal Year: 2003
    ..abstract_text> ..
  10. Chemokine Potential in Cancer Immunotherapy
    Dean Johnston; Fiscal Year: 2002
    ..Chemokines that prove effective in these models could be directly translated to clinical trials under the direction of Dr. Jean-Claude Bystryn, the CoPI, at NYU Medical Center. ..
  11. Plasmodium Falciparum Metal Metabolism
    David Sullivan; Fiscal Year: 2009
    ..Plasmodium parasitism provides a comparison of "simple" erythrocyte cell to more complex infected cell. ..
  12. Host Factors in Susceptibility to Chlamydial Disease
    KYLE RAMSEY; Fiscal Year: 2006
    ....
  13. CNS Anti-tumor immunity induced by dendritic cell vaccination and TLR agonists
    Robert M Prins; Fiscal Year: 2010
    ..Thus, this is a mechanistic and translational project that is directly related to our long-term objectives stated above and to the mission of promoting public health. ..
  14. Control of Human Papillomavirus-16 Transcription
    Hans Ulrich Bernard; Fiscal Year: 2006
    ....
  15. Recombinant Interleukin-12 for Cutaneous T-Cell Lymphoma
    Alain Rook; Fiscal Year: 2006
    ..Moreover, the addition of low-dose IL-2 may yield a more efficacious combination of agents which may synergistically enhance anti-tumor immunity and clinical responses. ..
  16. Cd2+, Metallothionein and Transcriptional Control of Na+ Glucose Co-Transporter 1
    DAVID PETERING; Fiscal Year: 2009
    ..abstract_text> ..
  17. NEUROPHYSIOLOGICAL NMDA DYSFUNCTION IN SCHIZOPHRENIA
    Daniel Javitt; Fiscal Year: 2006
    ..The research will build upon studies currently supported by NIH research and career development awards to the candidate, and will permit the candidate to continue to devote >75 percent effort to research. ..
  18. Physiogical Control of Neuroblast Polarity in Drosophila
    Kenneth Robinson; Fiscal Year: 2005
    ..Endogenous electric fields are ubiquitous in development and arise whenever an epithelial layer is damaged, so these results will have implications for understanding development as well as wound healing. ..
  19. Determinants of Innate Immunity to Group B Streptococci
    Ofer Levy; Fiscal Year: 2005
    ..abstract_text> ..
  20. Middle School Life Science-Education Partnership-PhaseII
    DAVID PETERING; Fiscal Year: 2006
    ..7. To establish a robust program to sustain the module dissemination to teachers after the completion of the grant. ..
  21. MECHANISMS OF COGNITIVE DYSFUNCTION IN SCHIZOPHRENIA
    Daniel Javitt; Fiscal Year: 2005
    ..This study will evaluate neurophysiological and neurochemical hypotheses concerning potential etiology of early sensory processing dysfunction in schizophrenia. ..
  22. FISH CONSUMPTION RISK COMMUNICATION IN ETHNIC MILWAUKEE
    DAVID PETERING; Fiscal Year: 2004
    ....
  23. High-Density ERP mapping & FMRI
    Daniel Javitt; Fiscal Year: 2002
    ..The equipment will also permit monitoring of background EEG during both human and animal studies. Software is requested for state-of-the-art ERP dipole mapping and ERP/MRI co-registration. ..
  24. TREATMENT OF NEGATIVE SYMPTOMS AND COGNITIVE IMPAIRMENTS
    Daniel Javitt; Fiscal Year: 2003
    ..The study will provide new information on the efficacy of d-cycloserine and glycine for both persistent primary and secondary negative symptoms and its effect on cognitive functioning. ..
  25. CYTOKINE THERAPY OF CUTANEOUS T CELL LYMPHOMA
    Alain Rook; Fiscal Year: 2004
    ..abstract_text> ..
  26. Biochemical Effects of Disrupting HSP90
    Charles Erlichman; Fiscal Year: 2004
    ....
  27. Compositions for Prevention/Prophylactic Treatment of Poison Ivy Dermatitis
    Mahmoud Elsohly; Fiscal Year: 2006
    ..This proposal addresses a major public health problem, namely contact allergic dermatitis and promises the development of an effective agent to address this problem. [unreadable] [unreadable]..
  28. Phencyclidine Abuse & Psychosis: Biomedical Mechanisms
    Daniel C Javitt; Fiscal Year: 2010
    ....
  29. CYTOKINE DYSFUNCTION AND LUNG 5LO METABOLISM IN AIDS
    Michael Coffey; Fiscal Year: 2002
    ..This proposal will further enhance our ability to correct this defect and help boost AM, PBM, and PMN defenses against opportunistic infections in the lung in HIV disease. ..
  30. A Molecular Signature of Early Cervical Carcinoma
    Concepcion Diaz Arrastia; Fiscal Year: 2007
    ..I propose to identify a genomic and proteomic signature of cervical cancer that will predict the aggressive behavior of the tumor and function clinically to develop molecular-based treatment plans. ..
  31. OmpR and acid regulation of Escherichia coli fim genes
    WILLIAM SCHWAN; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  32. A Mouse Model of Gaucher Disease
    Ernest Beutler; Fiscal Year: 2005
    ..In particular, electron microscopy and light microscopy will be used to attempt to demonstrate the development of Gaucher cells in the chimeric mice. ..
  33. Dendritic cell defects in cutaneous T-cell lymphoma
    Alain Rook; Fiscal Year: 2007
    ..abstract_text> ..
  34. Adenosine Shapes Neonatal Toll-like Receptor Function
    Ofer Levy; Fiscal Year: 2010
    ..As a whole, these studies will deepen our understanding of how the unique physiology of the human newborn fundamentally alters innate immunity at birth. ..
  35. Transmucosal Intra-Oral Drug Delivery System for THC
    Mahmoud Elsohly; Fiscal Year: 2003
    ..abstract_text> ..
  36. Proline uptake in staphylococcus aureus pathogenesis
    WILLIAM SCHWAN; Fiscal Year: 2002
    ..The results of this study will help us understand the role of proline transport in S. aureus infections. ..
  37. Gene Gun Technology, Opioids, and Corneal Diseases
    IAN ZAGON; Fiscal Year: 2003
    ..Ultimately, such data can be employed to design molecular strategies to remedy visual dysfunction. ..
  38. Gene Modified Cell Lines as Vaccine for Pancreas Cancer
    Daniel Laheru; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable] ..
  39. FORMATION AND SURVIVAL OF RED BLOOD CELLS
    Ernest Beutler; Fiscal Year: 2001
    ..Should these point mutations fail to alter gene transcription, a search will be made for other potential mutations in linkage disequilibrium with the known -5,-8 and -24 polymorphisms, by sequencing upstream through the promotor. ..
  40. delta-Catenin and Cell-Cell Adhesion in Prostate Cancer
    Qun Lu; Fiscal Year: 2010
    ..Understanding the posttranslational modifications that control 8-catenin functions will unravel mechanisms by which S-catenin modulates gene expression and promotes CaP in vivo. ..
  41. Delta-Catenin Cleavage by Presenilin and Synaptic Remodeling
    Qun Lu; Fiscal Year: 2006
    ..It will also lay the foundation for future R01 investigation of the roles of delta-catenin proteolytic fragments in AD pathogenesis. ..