Keyword search (4,164 papers available)

"Wang R" Authored Publications:

Title Authors PubMed ID
1 Effect of a single dose of lorazepam on resting state functional connectivity in healthy adults Ferland MC; Wang R; Therrien-Blanchet JM; Remahi S; Côté S; Fréchette AJ; Dang-Vu TT; Liu H; Lepage JF; Théoret H; 40646404
PERFORM
2 Alternative Oxidase: From Molecule and Function to Future Inhibitors Li J; Yang S; Wu Y; Wang R; Liu Y; Liu J; Ye Z; Tang R; Whiteway M; Lv Q; Yan L; 38524433
BIOLOGY
3 Metabolism of anti-inflammatory OXE (oxoeicosanoid) receptor antagonists by nonhuman primates Cossette C; Chourey S; Ye Q; Reddy CN; Wang R; Poulet S; Slobodchikova I; Vuckovic D; Rokach J; Powell WS; 35158054
PERFORM
4 Novel highly potent OXE receptor antagonists with prolonged plasma lifetimes that are converted to active metabolites in vivo in monkeys. Ye Q, Chourey S, Reddy CN, Wang R, Cossette C, Gravel S, Slobodchikova I, Vuckovic D, Rokach J, Powell WS 31655025
PERFORM
5 Novel Highly Potent and Metabolically Resistant Oxoeicosanoid (OXE) Receptor Antagonists That Block the Actions of the Granulocyte Chemoattractant 5-Oxo-6,8,11,14-Eicosatetraenoic Acid (5-oxo-ETE). Chourey S, Ye Q, Reddy CN, Wang R, Cossette C, Gravel S, Slobodchikova I, Vuckovic D, Rokach J, Powell WS 29972644
PERFORM

 

Title:Novel Highly Potent and Metabolically Resistant Oxoeicosanoid (OXE) Receptor Antagonists That Block the Actions of the Granulocyte Chemoattractant 5-Oxo-6,8,11,14-Eicosatetraenoic Acid (5-oxo-ETE).
Authors:Chourey S,  Ye Q,  Reddy CN,  Wang R,  Cossette C,  Gravel S,  Slobodchikova I,  Vuckovic D,  Rokach J,  Powell WS
Link:https://www.ncbi.nlm.nih.gov/pubmed/29972644?dopt=Abstract
DOI:10.1021/acs.jmedchem.8b00154
Publication:Journal of medicinal chemistry
Keywords:
PMID:29972644 Category:J Med Chem Date Added:2019-05-31
Dept Affiliation: PERFORM
1 Claude Pepper Institute and Department of Chemistry, Florida Institute of Technology , 150 West University Boulevard , Melbourne , Florida 32901-6982 , United States.
2 Meakins-Christie Laboratories, Centre for Translational Biology , McGill University Health Centre , 1001 Decarie Boulevard , Montreal , Quebec H4A 3J1 , Canada.
3 Department of Chemistry and Biochemistry and PERFORM Centre , Concordia University , 7141 Sherbrooke Street West , Montréal , Quebec H4B 1R6 , Canada.

Description:

Novel Highly Potent and Metabolically Resistant Oxoeicosanoid (OXE) Receptor Antagonists That Block the Actions of the Granulocyte Chemoattractant 5-Oxo-6,8,11,14-Eicosatetraenoic Acid (5-oxo-ETE).

J Med Chem. 2018 Jul 26;61(14):5934-5948

Authors: Chourey S, Ye Q, Reddy CN, Wang R, Cossette C, Gravel S, Slobodchikova I, Vuckovic D, Rokach J, Powell WS

Abstract

5-Oxo-6,8,11,14-eicosatetraenoic acid (5-oxo-ETE) is a potent lipid mediator that induces tissue eosinophilia via the selective OXE receptor (OXE-R), which is an attractive therapeutic target in eosinophilic diseases. We previously identified indole OXE-R antagonists that block 5-oxo-ETE-induced primate eosinophil activation. Although these compounds possess good oral absorption, their plasma levels decline rapidly due to extensive oxidation of their hexyl side chain. We have now succeeded in dramatically increasing antagonist potency and resistance to metabolism by replacing the hexyl group with phenylpentyl or phenylhexyl side chains. Compared with our previous lead compound S-230, our most potent antagonist, S-C025, has an IC50 (120 pM) over 80 times lower and a substantially longer plasma half-life. A single major metabolite, which retains antagonist activity (IC50, 690 pM) and has a prolonged lifetime in plasma was observed. These new highly potent OXE-R antagonists may provide a novel strategy for the treatment of eosinophilic disorders like asthma.

PMID: 29972644 [PubMed - in process]




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