Peer-reviewed veterinary case report
Discovery of potent and bioavailable GSK-3beta inhibitors.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2010
- Authors:
- Gong, Leyi et al.
- Affiliation:
- Department of Medicinal Chemistry · United States
- Species:
- rodent
Abstract
Here we report on the discovery of a series of maleimides which have high potency and good selectivity for GSK-3beta. The incorporation of polar groups afforded compounds with good bioavailability. The most potent compound 34 has an IC(50) of 0.6nM for GSK-3beta, over 100-fold selectivity against a panel of other kinases, and shows efficacy in rat osteoporosis models. The X-ray structure of GSK-3beta protein with 34 bound revealed the binding mode of the template and provided insights for future optimization opportunities.
Find similar cases for your pet
PetCaseFinder finds other peer-reviewed reports of pets with the same symptoms, plus a plain-English summary of what was tried across them.
Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/20138512/