Zobrazeno 1 - 10 of 19 pro vyhledávání: '"Daniel E. Croker"'
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Akademický článek
A Comparative Study of Impedance versus Optical Label-Free Systems Relative to Labelled Assays in a Predominantly Gi Coupled GPCR (C5aR) Signalling
Autor: Reena Halai, Daniel E. Croker, Jacky Y. Suen, David P. Fairlie, Matthew A. Cooper
Publikováno v: Biosensors, Vol 2, Iss 3, Pp 273-290 (2012)
Profiling ligand function on G-protein coupled receptors (GPCRs) typically involves using transfected cells over-expressing a target of interest, a labelled ligand, and intracellular secondary messenger reporters. In contrast, label-free assays are s
Externí odkaz: https://doaj.org/article/eb1a431e04c74c30aab0bf8d598b640b
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2
Characterisation of small molecule ligands 4CMTB and 2CTAP as modulators of human FFA2 receptor signalling
Autor: Nicholas L. Massey, Reena Halai, Mark E. Cooper, Philip M. Hansbro, Zoe Schofield, Chantal Donovan, Avril A. B. Robertson, Daniel E. Croker, Ernest H. L. Tee, David Edwards, Trent M. Woodruff
Publikováno v: Scientific Reports, Vol 8, Iss 1, Pp 1-12 (2018)
Scientific Reports
Short chain fatty acids (SCFAs) are protective against inflammatory diseases. Free fatty acid receptor 2 (FFA2), is a target of SCFAs however, their selectivity for FFA2 over other FFA receptors is limited. This study aimed to functionally characteri
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c837f4eaa5dcc1d7a73799deb68e520
http://link.springer.com/article/10.1038/s41598-018-36242-1
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3
Identification, Synthesis, and Biological Evaluation of the Major Human Metabolite of NLRP3 Inflammasome Inhibitor MCC950
Autor: Geraldine Kaeslin, Manohar Salla, Janet C. Reid, Paul V. Bernhardt, Avril A. B. Robertson, Ruby Pelingon, Daniel E. Croker, Elizabeth M. J. Gillam, Mark S. Butler, Mark E. Cooper, Jong Min Baek
Publikováno v: ACS Medicinal Chemistry Letters. 7:1034-1038
MCC950 is an orally bioavailable small molecule inhibitor of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome that exhibits remarkable activity in multiple models of inflammatory disease. Incubation of MCC950 with human li
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3fbb01788df5c9fe4de18ac60e0dcb3
https://doi.org/10.1021/acsmedchemlett.6b00198
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4
Discovery of functionally selective C5aR2 ligands: novel modulators of C5a signalling
Autor: Mark E. Cooper, Reena Halai, Trent M. Woodruff, Peter N. Monk, Daniel E. Croker, Christodoulos A. Floudas, Zoe Schofield, Geraldine Kaeslin, Mike Cl Wu, Richard J. Clark, Mark At Blaskovich, Dimitrios Morikis
Publikováno v: Immunology & Cell Biology. 94:787-795
The complement cascade is comprised of a highly sophisticated network of innate immune proteins that are activated in response to invading pathogens or tissue injury. The complement activation peptide, C5a, binds two seven transmembrane receptors, na
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37b8e227f6b17b83d148a607e9a967c6
https://doi.org/10.1038/icb.2016.43
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6
C5a2 can modulate ERK1/2 signaling in macrophages via heteromer formation with C5a1 and β‐arrestin recruitment
Autor: Reena Halai, Andreas Klos, Elisabeth Wende, Peter N. Monk, Mark E. Cooper, Beate Fehlhaber, Daniel E. Croker, Geraldine Kaeslin
Publikováno v: Immunology & Cell Biology. 92:631-639
The complement system is a major component of our innate immune system, in which the complement proteins C5a and C5a-des Arg bind to two G-protein-coupled receptors: namely, the C5a receptor (C5a1) and C5a receptor like-2 receptor (C5a2, formerly cal
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c2805f7180ee4d8b06859a9cc2dd90c
https://doi.org/10.1038/icb.2014.32
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C5a, but not C5a‐des Arg, induces upregulation of heteromer formation between complement C5a receptors C5aR and C5L2
Autor: Reena Halai, David P. Fairlie, Daniel E. Croker, Mark E. Cooper
Publikováno v: Immunology & Cell Biology. 91:625-633
Receptors for C5a have an important role in innate immunity and inflammation where their expression and activation is tightly regulated. There are two known receptors for C5a: the C5a receptor (C5aR) and the C5a receptor like-2 (C5L2) receptor. Here
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::896dbbb47a5fce39bb831067e7e308d6
https://doi.org/10.1038/icb.2013.48
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Conopeptide-Derived κ-Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive Properties
Autor: Paul F. Alewood, Andreas Brust, Stuart M. Brierley, Lotten Ragnarsson, Richard J. Lewis, Sonia Garcia-Caraballo, Åsa Andersson, Daniel E. Croker, Kapil Jain, Joel Castro, Barbara Colless
Publikováno v: Journal of medicinal chemistry. 59(6)
Opioid receptor screening of a conopeptide library led to a novel selective κ-opioid agonist peptide (conorphin T). Intensive medicinal chemistry, guided by potency, selectivity, and stability assays generated a pharmacophore model supporting ration
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::71be34f2a9ec798552963d866ee88c31
https://pubmed.ncbi.nlm.nih.gov/26859603
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9
χ-Conopeptide Pharmacophore Development: Toward a Novel Class of Norepinephrine Transporter Inhibitor (Xen2174) for Pain
Autor: Daniel E. Croker, Richard J. Lewis, Roger Drinkwater, Barbara Colless, Christina I. Schroeder, Maree T. Smith, Elka Palant, Dianne Alewood, Carsten K. Nielsen, Paul F. Alewood, Brad Patterson, Andreas Brust, David Wilson
Publikováno v: Journal of Medicinal Chemistry. 52:6991-7002
Norepinephrine (NE) amplifies the strength of descending pain inhibition, giving inhibitors of spinal NET clinical utility in the management of pain. chi-MrIA isolated from the venom of a predatory marine snail noncompetitively inhibits NET and rever
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03ab71c72a55e63daacd16ae7b4e3b86
https://doi.org/10.1021/jm9003413
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10
Conopressin-T from Conus tulipa Reveals an Antagonist Switch in Vasopressin-like Peptides
Autor: Gilles Guillon, Åsa Andersson, Richard J. Lewis, Sébastien Dutertre, Natalie G. Lumsden, Markus Muttenthaler, Daniel E. Croker, Norelle L. Daly, Paul F. Alewood, David J. Craik
Publikováno v: Journal of Biological Chemistry
Journal of Biological Chemistry, American Society for Biochemistry and Molecular Biology, 2008, 283 (11), pp.7100-7108. ⟨10.1074/jbc.M706477200⟩
Journal of Biological Chemistry, 2008, 283 (11), pp.7100-7108. ⟨10.1074/jbc.M706477200⟩
International audience; We report the discovery of conopressin-T, a novel bioactive peptide isolated from Conus tulipa venom. Conopressin-T belongs to the vasopressin-like peptide family and displays high sequence homology to the mammalian hormone ox
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f894c908bb9f6245e16f2ff046a26cf2
https://doi.org/10.1074/jbc.m706477200
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