Zobrazeno 1 - 10
of 56
pro vyhledávání: '"Jay R. Luly"'
Autor:
Noah Tu, Kennan C. Marsh, Karl W. Mollison, Rolf Wagner, Gin C. Hsieh, Cynthia L. Henry, Merrill Nuss, Jay R. Luly, Denise Wilcox, Nwe Y. Bamaung, Benjamin C. Lane, Richard P. Carlson, Yung-Wu Chen, Thomas A. Fey, Luping Liu, Paul E. Wiedeman, Yat-Sun Or, James M. Trevillyan, George W. Carter, Peer B. Jacobson, Teresa A. Rosenberg, Stevan W. Djuric
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5340-5343
The synthesis and biological activities of rapamycin (I) analogs modified at the C-40 position are reported. Emphasis placed on compounds that potentially have an improved safety profile on account of their shorter in vivo half-life when compared wit
Autor:
Jay R. Luly, Kenneth G. Carson, David J Heilig, Wen Song Yue, Shixin Qin, Jie Jack Li, David T. Connor, Joseph Edwin Low, Roberta A Glynn, Bharat K. Trivedi, Qing Ye, Stephen W. Hunt, Steven R. Miller, Bruce D. Roth, Weixing Yang
Publikováno v:
Bioorganic & Medicinal Chemistry. 11:3777-3790
Interleukin-8 modulation is implicated in many inflammatory and cancer diseases. Starting from a mass-screening hit, the synthesis and structure-activity relationship of 2-amino-3-heteroarylquinoxalines as non-peptide, small molecule interleukine-8 r
Autor:
Marc Elgort, Jeffrey N. Miner, Jay R. Luly, Philip R. Kym, Steven W. Elmore, George W. Carter, Curtis M. Tyree, Ben Lane, Chun Wei Lin, Michael J. Coghlan, Junlian Hu, Jon Rosen, Peer B. Jacobson, Russell T. Turner, Masaki Nakane
Publikováno v:
Molecular Endocrinology. 17:860-869
Glucocorticoids (GCs) are commonly used to treat inflammatory disease; unfortunately, the long-term use of these steroids leads to a large number of debilitating side effects. The antiinflammatory effects of GCs are a result of GC receptor (GR)-media
Autor:
Paul E. Wiedeman, Jay R. Luly, Julie Wilkins, Yung-Wu Chen, Gerard D. Gagne, Michael P. Sheets, Morey L. Smith, Usha Warrior, James M. Trevillyan, Stephen J. Ballaron, Jane A. Fagerland, X. Grace Chiou, Karl W. Mollison, George W. Carter, Earl J. Gubbins, Stevan W. Djuric
Publikováno v:
Journal of Biological Chemistry. 276:48118-48126
NFAT (nuclear factor of activated T cell) proteins are expressed in most immune system cells and regulate the transcription of cytokine genes critical for the immune response. The activity of NFAT proteins is tightly regulated by the Ca(2+)/calmoduli
Publikováno v:
Tetrahedron Letters. 41:8853-8856
Several novel 4-substituted 4-arylpiperidines were synthesized. The chemistry leading to 4-(4-chlorophenyl)-4-fluoropiperidine ( 6 ), 4-azido-4-(4-chlorophenyl)piperidine ( 7 ) and 4-(4-chlorophenyl)-4-methylpiperidine ( 8 ) is described.
Autor:
David G. Nettesheim, Jay R. Luly, Andrew M. Petros, Karl W. Mollison, Yat Sun Or, Benjamin C. Lane, Paul E. Wiedeman, Stephen W. Fesik
Publikováno v:
Journal of Medicinal Chemistry. 42:4456-4461
C24-Deoxyascomycin was prepared in a two-step process from ascomycin and evaluated for its immunosuppressant activity relative to ascomycin and FK506. An intermediate in the synthetic pathway, Delta(23,24)-dehydroascomycin, was likewise evaluated. De
Autor:
Michael P. Sheets, Karl W. Mollison, Cannon John Burns, Robin M Kolano, Morey L. Smith, Jay R. Luly, Yung-Wu Chen, Melissa S. Pong, Thomas A. Fey, Donna M. Gauvin, George W. Carter, Nikolaos M. Nikolaidis, Yat-Sun Or, Benjamin C. Lane, Kennan C. Marsh, Gin C. Hsieh, James M. Trevillyan
Publikováno v:
Journal of Investigative Dermatology. 112:729-738
T lymphocytes play a critical part in inflammatory skin diseases but are targeted by available therapies that have only partial efficacy, significant side-effects, or both. Because psoriasis, atopic dermatitis, and allergic contact hypersensitivity a
Autor:
Melissa S. Pong, Michael P. Sheets, Thomas A. Fey, James M. Trevillyan, Morey L. Smith, Karl W. Mollison, Jay R. Luly, Joy Bauch, Stevan W. Djuric, Stephen J. Ballaron, Yung-Wu Chen, Kennan C. Marsh, Gin C. Hsieh, Robin M Kolano, Donna M. Gauvin, George W. Carter
Publikováno v:
Clinical Immunology. 90:133-140
To assess the duration of immunosuppression in FK506-dosed pigs, an undiluted whole blood assay was established to measure reactivities of T cells in their physiological milieu. PMA and ionomycin were shown to induce IL-2 production in swine blood. T
Autor:
Jay R. Luly, Michael J. Coghlan, Michael P. Sheets, Qinghua Xie, Karl W. Mollison, Alan X. Wang, Kennan C. Marsh, Gin C. Hsieh, Benjamin C. Lane
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2787-2792
A series of novel pyrazole carboxamides is disclosed that demonstrate strong immunosuppressant activity in rodent and human mixed leukocyte response (MLR) assays (IC501 microM). The synthesis, biological activity, mode of action, and pharmacokinetic
Autor:
Karl W. Mollison, Thomas A. Fey, Donna M. Gauvin, Michael P. Sheets, Morey L. Smith, Melissa Pong, Ruth Krause, Loan Miller, Yat Sun Or, Megumi Kawai, Rolf Wagner, Paul E. Wiedeman, Richard F. Clark, Indrani W. K. Gunawardana, Teresa A. Rhoades, Cynthia L. Henry, Noah P. Tu, Nwe Y. BaMaung, Hana Kopecka, Luping Liu, Qinghua Xie, Benjamin C. Lane, James M. Trevillyan, Kennan Marsh, George W. Carter, Yung-Wu Chen, Gin C. Hsieh, Jay R. Luly
Publikováno v:
Current Pharmaceutical Design. 4:367-379
Abstract: Drug therapy for the major inflammatory skin diseases, which include atopic dermatitis, psoriasis and allergic contact dermatitis, is often inadequate due to poor efficacy, toxicity, or both. Much research has focused on the macrolactam T c