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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izdano v:ACS Med Chem Lett
Main Authors: 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
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2016
Online dostop: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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