Zobrazeno 1 - 10
of 16
pro vyhledávání: '"James Jakway"'
Autor:
Neil Wishart, Viswanath Devanarayan, Lori A. Dowding, Christopher M. Harris, David C. Jordan, Robert V. Talanian, Eric R. Goedken, James Jakway, Jeffrey W. Voss
Publikováno v:
SLAS Discovery. 17:857-867
Development of inhibitor compounds selective against undesirable targets is critical in drug discovery. Selectivity ratios for candidate compounds are evaluated by dividing potencies from two assays assessing the off-target and target. Because all po
Autor:
Jay S. Fine, James Fossetta, Minglang Wu, Waldemar Gonsiorek, Carol Terminelli, Richard W. Bond, Daniel Lundell, J. Robert Merritt, Aki Cynthia J, Jianhua Chao, Zhenmin He, R. William Hipkin, James Jakway, Younong Yu, Taveras Arthur G, Diane Rindgen, Gaifa Lai, Rosemary Mayer-Ezel, Xuedong Fan, Michael P. Dwyer, Chao Jianping, Hongchen Qiu, Biju J. Purakkattle, Hong Bian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1318-1322
Comprehensive SAR studies were undertaken in the 3,4-diaminocyclobut-3-ene-1,2-dione class of CXCR2/CXCR1 receptor antagonists to explore the role of the heterocycle on chemokine receptor binding affinities, functional activity, as well as oral expos
Autor:
Art Taveras, Daniel Lundell, Xuedong Fan, James Fossetta, Michael P. Dwyer, Jianhua Chao, Hongchen Qiu, M. Motasim Billah, R. William Hipkin, Waldemar Gonsiorek, James Jakway, David Hesk, Gregory Deno
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 322:477-485
In neutrophils, growth-related protein-alpha (CXCL1) and interleukin-8 (CXCL8), are potent chemoattractants (Cytokine 14:27-36, 2001; Biochemistry 42:2874-2886, 2003) and can stimulate myeloperoxidase release via activation of the G protein-coupled r
Autor:
Kaiser Bernd, Aki Cynthia J, Rosemary Mayer-Ezel, Chao Jianping, R. William Hipkin, Richard W. Bond, Taveras Arthur G, Daniel Lundell, Jianhua Chao, Laura L. Rokosz, Purakkattle J. Biju, James Jakway, Viyyoor M. Girijavallabhan, Jay S. Fine, Tara M. Stauffer, James Fossetta, Wei Wang, Ge Li, Hong Bian, J. Robert Merritt, Waldemar Gonsiorek, Xuedong Fan, Baldwin John J, Michael P. Dwyer, Carol Terminelli, Younong Yu, Diane Rindgen, Lynne E. Ozgur
Publikováno v:
Journal of Medicinal Chemistry. 49:7603-7606
Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and
Autor:
Jianhua Cao, Pauline C. Ting, Neng-Yang Shih, Shelby P. Umland, Robert G. Aslanian, Fang Tian, Zhidan Liu, Charles G. Garlisi, Yuntao Wan, Himanshu Shah, Ying Huang, James Jakway
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3020-3023
Structure-activity relationship study of bipiperidine amide 1 has identified the reverse bipiperidine amide 4a as a CC chemokine-3 (CCR3) receptor antagonist. Optimization of the structure-activity relationship of compound 4a has resulted in the iden
Autor:
M. Berlin, Hongchen Qiu, Maria A. Rivelli, Shelby P. Umland, James Jakway, Charles A. Rizzo, L. M. Varty, Yuntao Wan, Mccormick Kevin D, John A. Hey, Jennifer C. Mutter, Michel R. Corboz
Publikováno v:
Autonomic and Autacoid Pharmacology. 23:208-219
1. Pig nasal mucosal strips were incubated with alpha-adrenoceptor antagonists followed by alpha2-adrenoceptor agonist concentration-response curves. 2. Contractions elicited by the alpha2-adrenoceptor agonists BHT-920 (pD2 = 6.16 +/- 0.07), UK 14,30
Autor:
Shelby P. Umland, M. Motasim Billah, Yuntao Wan, Charles G. Garlisi, Fang Tian, Pauline C. Ting, Robert W. Egan, Hongchen Qiu, James Jakway, David Hesk, Himanshu Shah
Publikováno v:
European Journal of Pharmacology. 456:1-10
Study of the CC chemokine receptor 3 (CCR3) has been limited to using radiolabeled agonist chemokines. A small molecule CCR3 antagonist, 2-[(6-amino-2-benzothiazolyl)thio]-N-[1-[(3,4-dichlorylphenyl)methyl]-4-piperidinyl]acetamide, Banyu (I), was tri
Autor:
M. Motasim Billah, Yuntao Wan, Fang Tian, Jennifer Shortall, James Jakway, Himanshu Shah, Robert W. Egan, Charles G. Garlisi, Shelby P. Umland
Publikováno v:
Journal of Leukocyte Biology. 67:441-447
A novel pharmacological study of CCR3 receptor reserve in a CCR3-transfected cell (CREM3) and human eosinophils was done; functional responses measured were increases in intracellular calcium and chemotaxis. Eotaxin, eotaxin-2, monocyte chemoattracta
Autor:
Manish N. Patel, Himanshu Shah, James Jakway, Charles G. Garlisi, M. Motasim Billah, Robert W. Egan, Shelby P. Umland, Jennifer Shortall, Vinod Hegde, Shad Razac, D. Stelts, Ted T. Kung, Angela Falcone
Publikováno v:
American Journal of Respiratory Cell and Molecular Biology. 20:481-492
We compared the effects of cyclosporin A (CSA) and a macrotetrolide antibiotic, dinactin, on human T-cell proliferation and cytokine production induced by stimulation of the T-cell receptor alone (monoclonal antibody [mAb] directed against CD3) or in
Autor:
Daniel M. Solomon, Pauline C. Ting, Sidney R. Smith, Demetris N. Zambas, James Jakway, Carol Terminelli, Joe F. Lee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2749-2754
2-[10,11-Dihydro-5-ethoxy-5 H -dibenzo[a,d]cyclohepten-5-yl]-N,N-dimethyl-ethanamine (1) has been found to possess anticytokine activity. The synthesis and structure-activity relationship study of a series of analogues are reported.