Discovery of 4-Amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin- 3-yl)pyrido[2,3-d]pyrimidine, an Orally Active, Non-Nucleoside Adenosine Kinase Inhibitor

2001 ◽  
Vol 44 (13) ◽  
pp. 2133-2138 ◽  
Author(s):  
Chih-Hung Lee ◽  
Meiqun Jiang ◽  
Marlon Cowart ◽  
Greg Gfesser ◽  
Richard Perner ◽  
...  
Keyword(s):  
Kinase Inhibitor ◽  
Adenosine Kinase ◽  
Orally Active

Analgesic and anti-inflammatory effects of A-286501, a novel orally active adenosine kinase inhibitor

Pain ◽  
2002 ◽  
Vol 96 (1) ◽  
pp. 107-118 ◽  
Author(s):  
Michael F. Jarvis ◽  
Haixia Yu ◽  
Steve McGaraughty ◽  
Carol T. Wismer ◽  
Joe Mikusa ◽  
...  
Keyword(s):  
Kinase Inhibitor ◽  
Adenosine Kinase ◽  
Anti Inflammatory ◽  
Orally Active

Protective effect of an adenosine kinase inhibitor in septic shock

Resuscitation ◽  
1995 ◽  
Vol 29 (2) ◽  
pp. 180 ◽  
Author(s):  
GS Firestein ◽  
D Boyle ◽  
DA Bullough ◽  
HE Gruber ◽  
FG Sajjadi ◽  
...  
Keyword(s):  
Septic Shock ◽  
Protective Effect ◽  
Kinase Inhibitor ◽  
Adenosine Kinase

The Effect of GP683, an Adenosine Kinase Inhibitor, on the Desflurane Anesthetic Requirement in Dogs

1997 ◽  
Vol 85 (3) ◽  
pp. 675-680 ◽  
Author(s):  
Baoguo Wang ◽  
Jun Tang ◽  
Paul F. White ◽  
Alan C. Foster ◽  
Heather M. Grettenberger ◽  
...  
Keyword(s):  
Kinase Inhibitor ◽  
Adenosine Kinase ◽  
Anesthetic Requirement

scholarly journals Homocysteine enhances the inhibitory effect of extracellular adenosine on the synthesis of proteins in isolated rat hepatocytes

1995 ◽  
Vol 310 (3) ◽  
pp. 893-896 ◽  
Author(s):  
S Tinton ◽  
P Buc-Calderon
Keyword(s):  
Protein Synthesis ◽  
Kinase Inhibitor ◽  
Adenine Nucleotides ◽  
Rat Hepatocytes ◽  
Isolated Hepatocytes ◽  
Adenosine Kinase ◽  
Isolated Rat Hepatocytes ◽  
Extracellular Adenosine ◽  
Inhibition Of Protein Synthesis ◽  
Isolated Rat

Previous work has shown that extracellular adenosine inhibits the incorporation of radiolabelled leucine into proteins in isolated rat hepatocytes [Tinton, Lefebvre, Cousin and Buc Calderon (1993) Biochim. Biophys. Acta 1176, 1-6]. In this study, we investigated whether its metabolism into adenine nucleotides, inosine or S-adenosylhomocysteine (AdoHcy) is required to induce such an impairment. Incubation of isolated hepatocytes in the presence of adenosine at 0.5 or 1 mM reduces the synthesis of proteins by about 45% after 120 min of incubation. Such an inhibition occurred without cell lysis and was not modified by adding the adenosine kinase inhibitor 5-iodotubercidin (15 microM) or the adenosine deaminase inhibitor coformycin (0.1 microM). It is therefore unlikely that the anabolic and catabolic pathways of adenosine are involved in the inhibition of protein synthesis. Adenosine (1 mM) increased the level of AdoHcy and S-adenosylmethionine by 20- and 5-fold respectively after 60 min of incubation and reduced the methylation index. These events as well as the inhibition of protein synthesis were strongly enhanced in the presence of L-homocysteine (2 mM). It is therefore concluded that the metabolism of adenosine into AdoHcy, which is known to be a potent inhibitor of cellular methylation reactions, may play an important role in the control of translation.

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