6OBX

Montbretin A analogue M10-MbA in complex with Human pancreatic alpha-amylase

6OBX の概要

• エントリーDOI: 10.2210/pdb6obx/pdb
• 分子名称: Pancreatic alpha-amylase, CHLORIDE ION, CALCIUM ION, ... (7 entities in total)
• 機能のキーワード: amylase, diabetes, obesity, glucosyl hydrolase, hydrolase
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 57030.86

構造登録者

Caner, S.,Brayer, G.D. (登録日: 2019-03-21, 公開日: 2020-02-12, 最終更新日: 2024-10-23)

主引用文献

Tysoe, C.R.,Caner, S.,Calvert, M.B.,Win-Mason, A.,Brayer, G.D.,Withers, S.G.
Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic alpha-amylase.
Chem Sci, 10:11073-11077, 2019

PubMed Abstract: Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, = 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.

PubMed: 32206255
DOI: 10.1039/c9sc02610j

実験手法

X-RAY DIFFRACTION (1.3 Å)