Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394

[Image: see text] Glucokinase (GK) catalyzes the phosphorylation of glucose to glucose-6-phosphate. We present the structure–activity relationships leading to the discovery of AM-2394, a structurally distinct GKA. AM-2394 activates GK with an EC(50) of 60 nM, increases the affinity of GK for glucose...

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Vydáno v:ACS Med Chem Lett
Hlavní autoři: Dransfield, Paul J., Pattaropong, Vatee, Lai, Sujen, Fu, Zice, Kohn, Todd J., Du, Xiaohui, Cheng, Alan, Xiong, Yumei, Komorowski, Renee, Jin, Lixia, Conn, Marion, Tien, Eric, DeWolf, Walter E., Hinklin, Ronald J., Aicher, Thomas D., Kraser, Christopher F., Boyd, Steven A., Voegtli, Walter C., Condroski, Kevin R., Veniant-Ellison, Murielle, Medina, Julio C., Houze, Jonathan, Coward, Peter
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2016
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4948016/
https://ncbi.nlm.nih.gov/pubmed/27437083
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00140
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