Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Adam J. Cotterell"'
Autor:
David P. Fairlie, Junxian Lim, Weijun Xu, Adam J. Cotterell, Yaowu He, John D. Hooper, Mei-Kwan Yau, Mark N. Adams, Jacky Y. Suen, Praveen K. Madala
Publikováno v:
Pharmacological Research. 117:328-342
Proteinase-activated receptor 2 (PAR(2)) is a G protein -coupled receptor involved in metabolism, inflammation, and cancers. It is activated by proteolysis, which exposes a nascent N -terminal sequence that becomes a tethered agonist. Short synthetic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8e6e39d23198242f59e67d8fe66c0c6c
https://doi.org/10.1016/j.phrs.2016.12.020
https://doi.org/10.1016/j.phrs.2016.12.020
Autor:
Paula M. Loria, Aline Dantas de Araujo, David Price, Adam J. Cotterell, David A. Griffith, Spiros Liras, Timothy A. Hill, David P. Fairlie, Weijun Xu, David R. Derksen, Robert V. Stanton, Fabien Plisson, Huy N. Hoang, Justin M. Mitchell, David J. Edmonds
Publikováno v:
European Journal of Medicinal Chemistry. 127:703-714
Glucagon-like peptide (GLP-1) is an endogenous hormone that induces insulin secretion from pancreatic islets and modified forms are used to treat diabetes mellitus type 2. Understanding how GLP-1 interacts with its receptor (GLP-1R) can potentially l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a1066e3cc401d5d060001151234d3a5
https://doi.org/10.1016/j.ejmech.2016.10.044
https://doi.org/10.1016/j.ejmech.2016.10.044
Autor:
Mei-Kwan Yau, Jacky Y. Suen, David P. Fairlie, Ligong Liu, Rink-Jan Lohman, David A. Vesey, Robert Reid, Junxian Lim, Adam J. Cotterell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:986-991
Activation of protease activated receptor 2 (PAR2) has been implicated in inflammatory and metabolic disorders and its inhibition may yield novel therapeutics. Here, we report a series of PAR2 antagonists based on C-terminal capping of 5-isoxazolyl-L
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69f71fcb85c45b4eab3c8ba10f9499c5
https://doi.org/10.1016/j.bmcl.2015.12.048
https://doi.org/10.1016/j.bmcl.2015.12.048
Autor:
Praveer Gupta, David P. Fairlie, Robert Reid, Thomas J Fairlie, David A. Vesey, Adam J. Cotterell, Rink-Jan Lohman, Abishek Iyer, Matthew J. Sweet
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 356:387-396
Vorinostat and other inhibitors of different histone deacetylase (HDAC) enzymes are currently being sought to modulate a variety of human conditions, including chronic inflammatory diseases. Some HDAC inhibitors are anti-inflammatory in rodent models
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21c9f4a1a16cfffcae659fd562843da3
https://doi.org/10.1124/jpet.115.229328
https://doi.org/10.1124/jpet.115.229328
Autor:
Adam J. Cotterell, Mark E. Cooper, Alan Han, Mei-Kwan Yau, Rink-Jan Lohman, Jacky Y. Suen, David P. Fairlie, Junxian Lim, Ligong Liu, David A. Vesey
Publikováno v:
British Journal of Pharmacology. 171:4112-4124
andincreased ERK1/2 phosphorylation. In human kidney tubule cells, GB88 inhibited cytokine secretion (IL6, IL8, GM-CSF, TNF-α)mediated by PAR2. A rat paw oedema induced by PAR2 agonists was also inhibited by orally administered GB88 andcompared with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0e2799ea94379c0e95cf62dd8c5d18fb
https://doi.org/10.1111/bph.12757
https://doi.org/10.1111/bph.12757
Autor:
Robert Reid, Ligong Liu, Rink-Jan Lohman, David A. Vesey, Grant D. Barry, Jeffrey Y. W. Mak, Mei-Kwan Yau, Jacky Y. Suen, Junxian Lim, Adam J. Cotterell, Yuhong Jiang, David P. Fairlie
Publikováno v:
ACS medicinal chemistry letters. 7(12)
PAR2 antagonists have potential for treating inflammatory, respiratory, gastrointestinal, neurological, and metabolic disorders, but few antagonists are known. Derivatives of GB88 (3) suggest that all four of its components bind at distinct PAR2 site
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3622729220d54ca866992899f1acdf3
https://pubmed.ncbi.nlm.nih.gov/27994760
https://pubmed.ncbi.nlm.nih.gov/27994760
Autor:
Vernon Seow, Adam J. Cotterell, Junxian Lim, Weijun Xu, Jacky Y. Suen, David P. Fairlie, Martin J. Stoermer, W. Mei Kok, Rink-Jan Lohman, Mei-Kwan Yau, Matthew J. Sweet, Robert Reid
Publikováno v:
Scientific Reports
Drug discovery and translation are normally based on optimizing efficacy by increasing receptor affinity, functional potency, drug-likeness (rule-of-five compliance) and oral bioavailability. Here we demonstrate that residence time of a compound on i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::576f09ed534eec95e0408e518dc69c39
http://europepmc.org/articles/PMC4837355
http://europepmc.org/articles/PMC4837355
Autor:
Grant D. Barry, David P. Fairlie, Rink-Jan Lohman, Ligong Liu, David A. Vesey, Adam J. Cotterell, Jacky Y. Suen
Publikováno v:
The FASEB Journal. 26:2877-2887
Multiple serine proteases exert proinflammatory actions by signaling through protease-activated receptor-2 (PAR2) on the cell surface. Although inhibitors of individual proteases are anti-inflammatory, we sought to discover whether the first potent a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7f5dc941b92153ac2923574fc8a73a4
https://doi.org/10.1096/fj.11-201004
https://doi.org/10.1096/fj.11-201004
Autor:
Adam J. Cotterell, Rink-Jan Lohman, Jacky Y. Suen, David P. Fairlie, Giang Thanh Le, Maria A. Halili, Guy Barry
Publikováno v:
British Journal of Pharmacology. 165:1413-1423
BACKGROUND AND PURPOSE Many cells express proteinase activated receptor 2 (PAR2) on their plasma membrane. PAR2 is activated by proteolytic enzymes, such as trypsin and tryptase that cleave the receptor N-terminus, inititating signalling to intracell
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d16d18cda84a444306c4b3f297642e14
https://doi.org/10.1111/j.1476-5381.2011.01610.x
https://doi.org/10.1111/j.1476-5381.2011.01610.x
Autor:
Jacky Y. Suen, Grant D. Barry, Adam J. Cotterell, Robert Reid, Giang Thanh Le, David P. Fairlie
Publikováno v:
Journal of Medicinal Chemistry. 53:7428-7440
Human protease activated receptor 2 (PAR2) is a G protein-coupled receptor that is associated with inflammatory diseases and cancers. PAR2 is activated by serine proteases that cleave its N-terminus and by synthetic peptides corresponding to the new
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57d62419b29b95d36cab5fc3e3c720a9
https://doi.org/10.1021/jm100984y
https://doi.org/10.1021/jm100984y