Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 2. Leveraging Structure-Based Drug Design to Identify Analogues with Improved Pharmacokinetic Profiles

In the previous report, we described the discovery and optimization of novel small molecule disruptors of the GK-GKRP interaction culminating in the identification of 1 (AMG-1694). Although this analogue possessed excellent in vitro potency and was a useful tool compound in initial proof-of-concept...

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Veröffentlicht in:Journal of medicinal chemistry 2014-01, Vol.57 (2), p.325-338
Hauptverfasser: St. Jean, David J., Ashton, Kate S., Bartberger, Michael D., Chen, Jie, Chmait, Samer, Cupples, Rod, Galbreath, Elizabeth, Helmering, Joan, Hong, Fang-Tsao, Jordan, Steven R., Liu, Longbin, Kunz, Roxanne K., Michelsen, Klaus, Nishimura, Nobuko, Pennington, Lewis D., Poon, Steve F., Reid, Darren, Sivits, Glenn, Stec, Markian M., Tadesse, Seifu, Tamayo, Nuria, Van, Gwyneth, Yang, Kevin C., Zhang, Jiandong, Norman, Mark H., Fotsch, Christopher, Lloyd, David J., Hale, Clarence
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Sprache:eng
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