Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic α-amylase

Autor:	Christina R. Tysoe, Sami Caner, Matthew B. Calvert, Anna Win-Mason, Gary D. Brayer, Stephen G. Withers
Rok vydání:	2019
Předmět:	0303 health sciences 03 medical and health sciences Chemistry 0302 clinical medicine 030220 oncology & carcinogenesis General Chemistry 3. Good health 030304 developmental biology
Zdroj:	Chemical Science
ISSN:	2041-6520
Popis:	Simplified analogues of montbretin A bind similarly to human alpha amylase and with nanomolar affinity. Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, KI = 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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18982f3cc8fb86724cbae779804f55d2 https://pubmed.ncbi.nlm.nih.gov/32206255 Zobrazit plný text záznamu