PERFORM Publications

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Title		Authors	PubMed ID
1	Strengthening community-based fisheries monitoring programs with Indigenous perspectives	Dewan K; Mulrennan ME; Georgekish E;	41332192 CONCORDIA
2	Identification of a Conserved Transcriptional Activator-Repressor Module Controlling the Expression of Genes Involved in Tannic Acid Degradation and Gallic Acid Utilization in Aspergillus niger	Arentshorst M; Falco MD; Moisan MC; Reid ID; Spaapen TOM; van Dam J; Demirci E; Powlowski J; Punt PJ; Tsang A; Ram AFJ;	37744122 CSFG
3	Characterization of a novel AA3_1 xylooligosaccharide dehydrogenase from Thermothelomyces myriococcoides CBS 398.93	Zhao H; Karppi J; Nguyen TTM; Bellemare A; Tsang A; Master E; Tenkanen M;	36476312 CSFG
4	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
5	Discovery and Expression of Thermostable LPMOs from Thermophilic Fungi for Producing Efficient Lignocellulolytic Enzyme Cocktails.	Agrawal D, Basotra N, Balan V, Tsang A, Chadha BS	31792786 CSFG
6	Four Aromatic Intradiol Ring Cleavage Dioxygenases from Aspergillus niger.	Semana P, Powlowski J	31540981 CHEMISTRY
7	Malbranchea cinnamomea: A thermophilic fungal source of catalytically efficient lignocellulolytic glycosyl hydrolases and metal dependent enzymes.	Mahajan C, Basotra N, Singh S, Di Falco M, Tsang A, Chadha BS	26476165 CSFG
8	A Combinatorial Approach To Study Cytochrome P450 Enzymes for De Novo Production of Steviol Glucosides in Baker's Yeast.	Gold ND, Fossati E, Hansen CC, DiFalco M, Douchin V, Martin VJJ	30474973 CSFG
9	In vivo α-hydroxylation of a 2-alkylindole antagonist of the OXE receptor for the eosinophil chemoattractant 5-oxo-6,8,11,14-eicosatetraenoic acid in monkeys.	Chourey S, Ye Q, Reddy CN, Cossette C, Gravel S, Zeller M, Slobodchikova I, Vuckovic D, Rokach J, Powell WS	28476332 PERFORM
10	Metabolism and pharmacokinetics of a potent N-acylindole antagonist of the OXE receptor for the eosinophil chemoattractant 5-oxo-6,8,11,14-eicosatetraenoic acid (5-oxo-ETE) in rats and monkeys.	Reddy CN, Alhamza H, Chourey S, Ye Q, Gore V, Cossette C, Gravel S, Slobodchikova I, Vuckovic D, Rokach J, Powell WS	29339225 PERFORM

Title:	Metabolism and pharmacokinetics of a potent N-acylindole antagonist of the OXE receptor for the eosinophil chemoattractant 5-oxo-6,8,11,14-eicosatetraenoic acid (5-oxo-ETE) in rats and monkeys.
Authors:	Reddy CN, Alhamza H, Chourey S, Ye Q, Gore V, Cossette C, Gravel S, Slobodchikova I, Vuckovic D, Rokach J, Powell WS
Link:	https://www.ncbi.nlm.nih.gov/pubmed/29339225?dopt=Abstract
DOI:	10.1016/j.ejps.2018.01.021
Publication:	European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
Keywords:	5-Lipoxygenase products; 5-Oxo-ETE; Drug metabolism; Eicosanoids; Eosinophils; OXE receptor antagonist;
PMID:	29339225	Category:	Eur J Pharm Sci	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, FL 32901-6982, USA. 2 Meakins-Christie Laboratories, Centre for Translational Biology, McGill University Health Centre, 1001 Decarie Blvd, Montreal, QC H4A 3J1, Canada. 3 Department of Chemistry and Biochemistry and PERFORM Centre, Concordia University, 7141 Sherbrooke St. W., Montréal, QC H4B 1R6, Canada. 4 Meakins-Christie Laboratories, Centre for Translational Biology, McGill University Health Centre, 1001 Decarie Blvd, Montreal, QC H4A 3J1, Canada. Electronic address: william.powell@mcgill.ca.

Description:

Metabolism and pharmacokinetics of a potent N-acylindole antagonist of the OXE receptor for the eosinophil chemoattractant 5-oxo-6,8,11,14-eicosatetraenoic acid (5-oxo-ETE) in rats and monkeys.

Eur J Pharm Sci. 2018 Mar 30;115:88-99

Authors: Reddy CN, Alhamza H, Chourey S, Ye Q, Gore V, Cossette C, Gravel S, Slobodchikova I, Vuckovic D, Rokach J, Powell WS

Abstract

We previously identified the indole 264 as a potent in vitro antagonist of the human OXE receptor that mediates the actions of the powerful eosinophil chemoattractant 5-oxo-ETE. No antagonists of this receptor are currently commercially available or are being tested in clinical studies. The lack of a rodent ortholog of the OXE receptor has hampered progress in this area because of the unavailability of commonly used mouse or rat animal models. In the present study, we examined the feasibility of using the cynomolgus monkey as an animal model to investigate the efficacy of orally administered 264 in future in vivo studies. We first confirmed that 264 is active in monkeys by showing that it is a potent inhibitor of 5-oxo-ETE-induced actin polymerization and chemotaxis in granulocytes. The major microsomal metabolites of 264 were identified by cochromatography with authentic chemically synthesized standards and LC-MS/MS as its ?2-hydroxy and ?2-oxo derivatives, formed by ?2-oxidation of its hexyl side chain. Small amounts of ?1-oxidation products were also identified. None of these metabolites have substantial antagonist potency. High levels of 264 appeared rapidly in the blood following oral administration to both rats and monkeys, and declined to low levels by 24?h. As with microsomes, its major plasma metabolites in monkeys were ?2-oxidation products. We conclude that the monkey is a suitable animal model to investigate potential therapeutic effects of 264. This, or a related compound with diminished susceptibility to ?2-oxidation, could be a useful therapeutic agent in eosinophilic disorders such as asthma.

PMID: 29339225 [PubMed - indexed for MEDLINE]

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