Výsledky vyhledávání - "Ng, Howard P."

Structure Function Differences in Nonpeptide CCR1 Antagonists for Human and Mouse CCR1

Autor: Richard Horuk, Guo-Ping Wei, Ng Howard P, Margaret A. McCarrick, Laura Dunning, James Onuffer, Meina Liang, Mary Rosser

Publikováno v: The Journal of Immunology. 170:1910-1916

A useful strategy for identifying ligand binding domains of G protein-coupled receptors has been the exploitation of species differences in antagonist potencies. We have used this approach for the CCR1 chemokine receptor with a novel series of antago

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9285216e9a797cd16a5d58ea0ddc3ad1
https://doi.org/10.4049/jimmunol.170.4.1910

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Design, Synthesis, and Activity of a Novel Series of Factor Xa Inhibitors: Optimization of Arylamidine Groups

Autor: Sunil K. Koovakkat, Brad O. Buckman, Keith Eagen, Shung Wu, Ng Howard P, Raju Mohan, Wei Xu, Elena Ho, Lan Trinh, Babu Subramanyam, Meg McCarrick, Gary Phillips, Morrissey Michael M, Michael Pinkerton, William J. Guilford, Marc Whitlow, Amy Liang, David D. Davey

Publikováno v: Journal of Medicinal Chemistry. 45:2484-2493

A novel series of diaryloxypyridines have been designed as selective nanomolar factor Xa (fXa) inhibitors for use as anticoagulants. In this paper, we describe our efforts to identify an additional interaction and a replacement for the distal amidine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d684bc55897a8351d1b9be1346519e43
https://doi.org/10.1021/jm0200660

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Design, Synthesis, and Biological Activity of Novel Factor Xa Inhibitors: 4-Aryloxy Substituents of 2,6-Diphenoxypyridines††See ref. 1

Publikováno v: Bioorganic & Medicinal Chemistry. 10:657-666

A novel series of triaryloxypyridines have been designed to inhibit factor Xa, a serine protease strategically located in the coagulation cascade. Inhibitor 5e has a K I against factor Xa of 0.12 nM and is greater than 8000- and 2000-fold selective o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::61b28124500c42b131140d9bea08868f
https://doi.org/10.1016/s0968-0896(01)00338-8

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A Non-peptide Functional Antagonist of the CCR1 Chemokine Receptor Is Effective in Rat Heart Transplant Rejection

Publikováno v: Journal of Biological Chemistry. 276:4199-4204

Chemokines like RANTES appear to play a role in organ transplant rejection. Because RANTES is a potent agonist for the chemokine receptor CCR1, we examined whether the CCR1 receptor antagonist BX471 is efficacious in a rat heterotopic heart transplan

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::878f551401bcfa7987af8c947333087a
https://doi.org/10.1074/jbc.m007457200

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Identification and Characterization of a Potent, Selective, and Orally Active Antagonist of the CC Chemokine Receptor-1

Publikováno v: Journal of Biological Chemistry. 275:19000-19008

The CC chemokine receptor-1 (CCR1) is a prime therapeutic target for treating autoimmune diseases. Through high capacity screening followed by chemical optimization, we identified a novel non-peptide CCR1 antagonist, R-N-[5-chloro-2-[2-[4-[(4-fluorop

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96836a4797891eb0ce582451db65d51a
https://doi.org/10.1074/jbc.m001222200

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Chemokine Receptor Antagonists

Autor: Richard Horuk, Ng Howard P

Publikováno v: Medicinal Research Reviews. 20:155-168

Chemokines belong to a large family of chemoattractant molecules involved in the directed migration of immune cells. They achieve their cellular effects by direct interaction with cell surface receptors. Chemokines appear to be involved in a variety

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fe07a597bb965311700ef1c445069fb0
https://doi.org/10.1002/(sici)1098-1128(200003)20:2<155::aid-med3>3.0.co

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Species selectivity of a small molecule antagonist for the CCR1 chemokine receptor

Autor: Joseph Hesselgesser, Mary Rosser, M. Liang, Richard Horuk, R. M. Snider, Ghannam Ameen F, John G. Bauman, P. J. Kretschmer, Ng Howard P, Michael M. Morrissey, H. D. Perez, Imadul Islam, Laura Dunning, Karen May, Haifeng Pu

Publikováno v: European Journal of Pharmacology. 389:41-49

The species specificity of a small molecule antagonist for the human CCR1 chemokine receptor, 2-2-diphenyl-5-(4-chlorophenyl)piperidin-1-yl)valeronitrile (CCR1 antagonist 1), has been examined using cloned CCR1 receptors from various species. The com

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d428713d410eca88d08e68565d0fb58e
https://doi.org/10.1016/s0014-2999(99)00863-8

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Discovery of Novel Non-Peptide CCR1 Receptor Antagonists

Autor: Karen May, John G. Bauman, Joseph Hesselgesser, Michael M. Morrissey, Ng Howard P, Richard Horuk, M. Liang, Imadul Islam, R. M. Snider, H. D. Perez, Ghannam Ameen F

Publikováno v: Journal of Medicinal Chemistry. 42:4680-4694

Ligands for the CCR1 receptor (MIP-1alpha and RANTES) have been implicated in a number of chronic inflammatory diseases, most notably multiple sclerosis and rheumatoid arthritis. Because these ligands share a common receptor, CCR1, we sought to disco

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b22aa4c7750092a1000f22c3df454c21
https://doi.org/10.1021/jm990316l

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