Zobrazeno 1 - 10
of 154
pro vyhledávání: '"James E. Krause"'
Autor:
Harry Brielmann, David J. Matson, Bertrand L. Chenard, Mark T. Kershaw, W. Rycroft, Nicola Burnaby-Davies, Marci Crandall, Stéphane De Lombaert, Kevin J. Hodgetts, William J. Martin, Rajagopal Bakthavatchalam, Beth Ann Murphy, Timothy M. Caldwell, G Mason, A. Brian Jones, Xiaozhang Zheng, Helen Perrett, Susan Boyce, James E. Krause, Daniel N. Cortright, Charles A. Blum, Rachael Conley, Scott M. Capitosti
Publikováno v:
Journal of Medicinal Chemistry. 53:3330-3348
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a nonselective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective a
Publikováno v:
Current Eye Research. 34:57-61
Purpose: We examined the potential for the pro-inflammatory complement proteins C5a and C3a to increase VEGF expression in ARPE-19 cells. Materials and Methods: Expression of complement receptors in ARPE-19 cells was evaluated by RT-PCR. VEGF secreti
Autor:
Jayaraman Chandrasekhar, Raymond F. Horvath, Ping Ge, Stéphane De Lombaert, Hutchison Alan J, Kevin J. Hodgetts, Dario Doller, Robbin Brodbeck, James E. Krause, Diane Hoffman, Michael Gulianello, Yoon Taeyoung, John H. Kehne
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4486-4490
The design, synthesis and structure-activity relationship studies of a novel series of CRF-1 receptor antagonists, the 2-arylpyrimidines, are described. The effects of substitution on the aromatic ring and the pyrimidine core on CRF-1 receptor bindin
Autor:
Rajagopal Bakthavatchalam, Lawrence K. Fung, Bertrand L. Chenard, David J. Matson, Chu K. Ngo, Marci Crandall, Stéphane De Lombaert, Daniel N. Cortright, Harry Brielmann, Charles A. Blum, Mark T. Kershaw, Jayaraman Chandrasekhar, Marta Day, Xiaozhang Zheng, James E. Krause, Kevin J. Hodgetts
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4573-4577
A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates excellent in vivo potency and efficacy in an acute inflam
Autor:
Diane Hoffman, Ping Ge, Raymond F. Horvath, Kevin J. Hodgetts, Yoon Taeyoung, John H. Kehne, Stéphane De Lombaert, James E. Krause, Michael Gulianello, Mark T. Kershaw, Jayaraman Chandrasekhar, Robbin Brodbeck, Dario Doller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:891-896
The design, synthesis and structure-activity relationships of a novel series of CRF-1 receptor antagonist, the 1-aryl-4-alkylaminoisoquinolines, is described. The effects of substitution on the aromatic ring, the amino group and the isoquinoline core
Autor:
Katrin Stemberger, M. Kralinger, Eduard Schmid, James E. Krause, Josef Troger, Johannes Leierer, Barbara Teuchner, Gertrud Haas, G. F. Kieselbach, Quynh Anh Nguyen, Reiner Fischer-Colbrie
Publikováno v:
Peptides. 27:3370-3376
Very recently, the authors found levels of neurokinin (NK) A-like immunoreactivities in the human retina which were more than five times higher than those of substance P (SP). The present study aimed to find out how many of these immunoreactivities c
Autor:
S P Sivam, James E. Krause
Publikováno v:
Journal of Neurochemistry. 59:2278-2284
The aim of the study was to test whether the synthesis of substance P (SP) and that of its receptor (also known as NK1 receptor) are coordinately regulated after chronic pharmacologic intervention in two neural systems, the spinal cord and basal gang
Autor:
Olivier Morteau, James E. Krause, Dubhfeasa M. Slattery, Norma P. Gerard, Alison A. Humbles, Shoji Okinaga, Michele Bennett Kinrade, Robbin Brodbeck, Hyeryun Choe, Zsusanna Zsengeller, Craig Gerard
Publikováno v:
Biochemistry. 42:9406-9415
C5a anaphylatoxin, a potent inflammatory mediator, is known to act through a specific G protein coupled receptor. However, some of the complex effects of C5a in vivo may not be explained solely by the deletion of the known receptor. Here, we show tha
Autor:
R. Yamamoto, Leah Conroy, J. Lyons, S. Munemitsu, Yasuo Takeda, R. Clark, J. Schreurs, James E. Krause, M. Innis
Publikováno v:
Journal of Neurochemistry. 64:1622-1631
The rat substance P (SP) receptor (SPR) was expressed in insect Sf9 cells by infection with recombinant baculovirus. The receptor bound SP with high affinity (KD = 360 pM) and had a rank order of affinity of SP > neurokinin A > neurokinin B. Ligand a
Publikováno v:
Journal of Neurochemistry. 64:1183-1191
The substance P (neurokinin-1) receptor belongs to the family of seven putative transmembrane domain receptors that are coupled via G proteins to phospholipase C activation. Homologous desensitization of substance P-stimulated responses has been desc