Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic alpha-amylase.
Tysoe, C.R., Caner, S., Calvert, M.B., Win-Mason, A., Brayer, G.D., Withers, S.G.(2019) Chem Sci 10: 11073-11077
- PubMed: 32206255 
- DOI: https://doi.org/10.1039/c9sc02610j
- Primary Citation of Related Structures:  
6OBX, 6OCN - PubMed Abstract: 
Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, K I = 60 and 70 nM, with improved specificity over medically relevant glycosidases, making them promising candidates for controlling blood glucose. Crystallographic analysis confirmed similar binding modes and identified new active site interactions.
- Department of Chemistry , University of British Columbia , 2036 Main Mall , Vancouver BC , Canada V6T 1Z1 . Email: withers@chem.ubc.ca.
Organizational Affiliation: