Inhibition of interleukin-1β and prostaglandin E2 thermogenesis by glycyl-glutamine, a pro-opiomelanocortin-derived peptide

2001 ◽  
Vol 894 (2) ◽  
pp. 316-320 ◽  
Author(s):  
Garth E. Resch ◽  
William R. Millington
Biomolecules ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 275
Author(s):  
Anastasia Psarra ◽  
Maria A. Theodoropoulou ◽  
Martin Erhardt ◽  
Marina Mertiri ◽  
Christiana Mantzourani ◽  
...  

Prostaglandin E2 (PGE2) is a key mediator of inflammation, and consequently huge efforts have been devoted to the development of novel agents able to regulate its formation. In this work, we present the synthesis of various α-ketoheterocycles and a study of their ability to inhibit the formation of PGE2 at a cellular level. A series of α-ketobenzothiazoles, α-ketobenzoxazoles, α-ketobenzimidazoles, and α-keto-1,2,4-oxadiazoles were synthesized and chemically characterized. Evaluation of their ability to suppress the generation of PGE2 in interleukin-1β plus forskolin-stimulated mesangial cells led to the identification of one α-ketobenzothiazole (GK181) and one α-ketobenzoxazole (GK491), which are able to suppress the PGE2 generation at a nanomolar level.


2017 ◽  
Vol 60 ◽  
pp. 27-31 ◽  
Author(s):  
Anna Nilsson ◽  
Louise Elander ◽  
Martin Hallbeck ◽  
Unn Örtegren Kugelberg ◽  
David Engblom ◽  
...  

1995 ◽  
Vol 57 (4) ◽  
pp. 619-629 ◽  
Author(s):  
John A. Dibattista ◽  
Jean-Pierre Pelletier ◽  
Muhammad Zafarullah ◽  
Kazushi Iwata ◽  
Johanne Martel-Pelletier

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