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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Gepubliceerd in:ACS Med Chem Lett
Hoofdauteurs: 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
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: American Chemical Society 2016
Online toegang: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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