Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Paul J, Dunford"'
Autor:
Carl L Manthey, Beverley A Moore, Yanqing Chen, Matthew J Loza, Xiang Yao, Hao Liu, Stanley M Belkowski, Holly Raymond-Parks, Paul J Dunford, Francisco Leon, Jennifer E Towne, Scott E Plevy
Publikováno v:
PLoS ONE, Vol 14, Iss 11, p e0223918 (2019)
BACKGROUND & AIMS:Originally believed to be primarily a disorder of T-cell signaling, evidence shows that macrophage-lineage cells also contribute to the pathogenesis of Crohn's disease (CD). Colony stimulating factor-1 (CSF-1) is a key regulator of
Externí odkaz:
https://doaj.org/article/accefd4db87e43df909fc191a4931e30
Autor:
Gary S. Firestein, David L. Boyle, Dion Chen, Cesar Calderon, Samuel E. DePrimo, Paul J. Dunford, Robin L. Thurmond, William Barchuk
Publikováno v:
Inflammation Research. 68:261-274
In a double-blind, placebo-controlled, multiple-dose study, we assessed the molecular mechanism of action of the selective histamine-4-receptor antagonist toreforant. Patients with active rheumatoid arthritis (RA) despite methotrexate were randomized
Autor:
Jennifer E. Towne, Beverley A. Moore, Stanley M. Belkowski, Paul J. Dunford, S Plevy, Francisco Leon, Yanqing Chen, Xiang Yao, Matthew J. Loza, Hao Liu, Holly Raymond-Parks, Carl L. Manthey
Publikováno v:
PLoS ONE, Vol 14, Iss 11, p e0223918 (2019)
PLoS ONE
PLoS ONE
Background & aims Originally believed to be primarily a disorder of T-cell signaling, evidence shows that macrophage-lineage cells also contribute to the pathogenesis of Crohn's disease (CD). Colony stimulating factor-1 (CSF-1) is a key regulator of
Autor:
David L, Boyle, Samuel E, DePrimo, Cesar, Calderon, Dion, Chen, Paul J, Dunford, William, Barchuk, Gary S, Firestein, Robin L, Thurmond
Publikováno v:
Inflammation research : official journal of the European Histamine Research Society ... [et al.]. 68(4)
In a double-blind, placebo-controlled, multiple-dose study, we assessed the molecular mechanism of action of the selective histamine-4-receptor antagonist toreforant.Patients with active rheumatoid arthritis (RA) despite methotrexate were randomized
Autor:
Robin L, Thurmond, Jennifer, Venable, Brad, Savall, David, La, Sandra, Snook, Paul J, Dunford, James P, Edwards
Publikováno v:
Handbook of experimental pharmacology. 241
The discovery of the histamine H
Autor:
Brad M. Savall, Paul J. Dunford, James P. Edwards, David La, Sandra Snook, Jennifer Venable, Robin L. Thurmond
Publikováno v:
Handbook of Experimental Pharmacology ISBN: 9783319581927
The discovery of the histamine H4 receptor (H4R) provided a new avenue for the exploration of the physiological role of histamine, as well as providing a new drug target for the development of novel antihistamines. The first step in this process was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::67a2481327f1dd586f254551076f6775
https://doi.org/10.1007/164_2016_130
https://doi.org/10.1007/164_2016_130
Autor:
Alexa Kollmeier, Andrew J. Greenspan, Paul J. Dunford, Yichuan Xia, Xie L. Xu, Bei Zhou, Robin L. Thurmond, Bin Chen, Klaus Francke
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 350:181-187
The histamine H4 receptor (H4R) is a promising target for the treatment of pruritus. A clinical study was conducted to evaluate the safety and efficacy of the H4R antagonist, JNJ 39758979 [(R)-4-(3-amino-pyrrolidin-1-yl)-6-isopropyl-pyrimidin-2-ylami
Autor:
Michael D. Hack, Brad M. Savall, Kevin Tays, Paul J. Dunford, Jeffery M. Cowden, Ronald L. Wolin, James P. Edwards, Frank Chavez, Robin L. Thurmond
Publikováno v:
Journal of Medicinal Chemistry. 57:2429-2439
This report discloses the discovery and SAR of a series of 6-alkyl-2-aminopyrimidine derived histamine H4 antagonists that led to the development of JNJ 39758979, which has been studied in phase II clinical trials in asthma and atopic dermatitis. Bui
Autor:
David La, Karlsson Lars, Peter Ward, Paul J. Dunford, Robin L. Thurmond, Xie L. Xu, Andrew Greenspan, Bin Chen
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 349:176-184
The histamine H4 receptor (H(4)R) has been shown to have preclinical involvement in both inflammatory and pruritic responses. JNJ-39758979 [(R)-4-(3-amino-pyrrolidin-1-yl)-6-isopropyl-pyrimidin-2-ylamine] is a potent and selective H(4)R antagonist wi
Autor:
James P. Edwards, Laurent Gomez, Paul J. Dunford, Michael P. Curtis, Aaron M. Kearney, Savall Brad M, Steven P. Meduna, Jeffery M. Cowden, Frank Chavez, Robin L. Thurmond, Cheryl A. Grice
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6577-6581
This report discloses the development of a series of tricyclic histamine H(4) receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and