Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Autor: Amanda J. Kennedy, Linda Sundström, Stefan Geschwindner, Eunice K. Y. Poon, Yuhong Jiang, Rongfeng Chen, Rob Cooke, Shawn Johnstone, Andrew Madin, Junxian Lim, Qingqi Liu, Rink-Jan Lohman, Anneli Nordqvist, Maria Fridén-Saxin, Wenzhen Yang, Dean G. Brown, David P. Fairlie, Niek Dekker

Publikováno v: Communications Biology, Vol 3, Iss 1, Pp 1-13 (2020)

Kennedy et al. report the pharmacological and in vivo profiling of two small molecule PAR2 inhibitors and an agonist. They conclude that while the small molecule agonist and one of the inhibitors bind to the orthosteric PAR2 binding site, the other i

Externí odkaz: https://doaj.org/article/e6a39fb1480d47f3b76e5e7e14d4b26c

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Autor: Dean G. Brown, Wenzhen Yang, Rongfeng Chen, Shawn Donald Johnstone, Maria Fridén-Saxin, Stefan Geschwindner, Anneli Nordqvist, Junxian Lim, Linda Sundström, Yuhong Jiang, Qingqi Liu, David P. Fairlie, Rob Cooke, Andrew Madin, Rink-Jan Lohman, Amanda J. Kennedy, Eunice K. Y. Poon, Niek Dekker

Publikováno v: Communications Biology, Vol 3, Iss 1, Pp 1-13 (2020)
Communications Biology

Protease-activated receptor-2 (PAR2) has been implicated in multiple pathophysiologies but drug discovery is challenging due to low small molecule tractability and a complex activation mechanism. Here we report the pharmacological profiling of a pote

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29bc78f0bf12d02422571e4e9bc27be1
https://doaj.org/article/e6a39fb1480d47f3b76e5e7e14d4b26c

International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin1) and GPR1 (Chemerin2) Nomenclature, Pharmacology, and Function

Autor: Anthony P. Davenport, Amanda J. Kennedy

Publikováno v: Pharmacological Reviews. 70:174-196

Chemerin, a chemoattractant protein and adipokine, has been identified as the endogenous ligand for a G protein-coupled receptor encoded by the gene CMKLR1 (also known as ChemR23), and as a consequence the receptor protein was renamed the chemerin re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7d41560019732199c6d2ddb6ceffb505
https://doi.org/10.1124/pr.116.013177

Characterization of homologous sphingosine-1-phosphate lyase isoforms in the bacterial pathogen Burkholderia pseudomallei

Autor: Christopher J. McLean, Jon Marles-Wright, Rafael Custodio, Jonathan Lowther, Amanda J. Kennedy, Jacob Pollock, David J. Clarke, Alan R. Brown, Dominic J. Campopiano

Publikováno v: Mclean, C J, Marles-wright, J, Custodio, R, Lowther, J, Kennedy, A J, Pollock, J, Clarke, D, Brown, A R & Campopiano, D J 2016, ' Characterization of homologous sphingosine-1-phosphate lyase isoforms in the bacterial pathogen Burkholderia pseudomallei ', Journal of lipid research, vol. 58, no. 1, pp. 137-150 . https://doi.org/10.1194/jlr.M071258
Journal of Lipid Research, Vol 58, Iss 1, Pp 137-150 (2017)

Sphingolipids (SLs) are ubiquitous elements in eukaryotic membranes and are also found in some bacterial and viral species. As well as playing an integral structural role, SLs also act as potent signalling molecules involved in numerous cellular path

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::79f853f54448271ecf8bf7e47b28af3a
https://www.pure.ed.ac.uk/ws/files/30257988/20161026_Campopiano_McLean_et_al_Text_and_Figs_Resubmission.pdf

Abstract P183: Chemokine-like Receptor 1 Mediates the Vasoconstrictor Actions of Chemerin in vitro and in vivo

Autor: Amanda J. Kennedy, Cai Read, Rhoda E. Kuc, Peiran Yang, Janet J. Maguire, Anthony P. Davenport

Publikováno v: Hypertension. 68

Hypertensive patients have significantly higher plasma concentrations of the adipokine chemerin compared with healthy controls, and levels of chemerin positively correlate with systolic and diastolic blood pressure. Chemerin activates chemokine-like

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::68af986b678c54edb07671d4e275ec14
https://doi.org/10.1161/hyp.68.suppl_1.p183