Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 1. Discovery of a Novel Tool Compound for in Vivo Proof-of-Concept

Small molecule activators of glucokinase have shown robust efficacy in both preclinical models and humans. However, overactivation of glucokinase (GK) can cause excessive glucose turnover, leading to hypoglycemia. To circumvent this adverse side effect, we chose to modulate GK activity by targeting...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 57; no. 2; pp. 309 - 324
Main Authors:	Ashton, Kate S., Andrews, Kristin L., Bryan, Marion C., Chen, Jie, Chen, Kui, Chen, Michelle, Chmait, Samer, Croghan, Michael, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Jordan, Steve R., Kurzeja, Robert J. M., Michelsen, Klaus, Pennington, Lewis D., Poon, Steve F., Sivits, Glenn, Van, Gwyneth, Vonderfecht, Steve L., Wahl, Robert C., Zhang, Jiandong, Lloyd, David J., Hale, Clarence, St. Jean, David J.
Format:	Journal Article
Language:	English
Published:	United States American Chemical Society 23-01-2014
Subjects:	Animals Binding Sites Carrier Proteins - chemistry Carrier Proteins - metabolism Crystallography, X-Ray Glucokinase - chemistry Glucokinase - metabolism Hepatocytes - drug effects Hepatocytes - metabolism High-Throughput Screening Assays Humans Hypoglycemia - chemically induced Hypoglycemic Agents - adverse effects Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Piperazines - adverse effects Piperazines - chemistry Piperazines - pharmacology Protein Conformation Protein Transport Rats Rats, Zucker Stereoisomerism Structure-Activity Relationship Sulfonamides - adverse effects Sulfonamides - chemistry Sulfonamides - pharmacology
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