6YQA

Taka-amylase in complex with alpha-glucosyl epi-cyclophellitol aziridine inhibitor

これはPDB形式変換不可エントリーです。

6YQA の概要

• エントリーDOI: 10.2210/pdb6yqa/pdb
• 分子名称: Alpha-amylase, 2-acetamido-2-deoxy-beta-D-glucopyranose, 1,2-ETHANEDIOL, ... (7 entities in total)
• 機能のキーワード: inhibitor, complex, amylase, hydrolase
• 由来する生物種: Aspergillus oryzae
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 111495.60

構造登録者

Armstrong, Z.,Chen, Y.,Artola, M.,Overkleeft, H.,Davies, G. (登録日: 2020-04-16, 公開日: 2021-02-24, 最終更新日: 2024-01-24)

主引用文献

Chen, Y.,Armstrong, Z.,Artola, M.,Florea, B.I.,Kuo, C.L.,de Boer, C.,Rasmussen, M.S.,Abou Hachem, M.,van der Marel, G.A.,Codee, J.D.C.,Aerts, J.M.F.G.,Davies, G.J.,Overkleeft, H.S.
Activity-Based Protein Profiling of Retaining alpha-Amylases in Complex Biological Samples.
J.Am.Chem.Soc., 143:2423-2432, 2021

PubMed Abstract: Amylases are key enzymes in the processing of starch in many kingdoms of life. They are important catalysts in industrial biotechnology where they are applied in, among others, food processing and the production of detergents. In man amylases are the first enzymes in the digestion of starch to glucose and arguably also the preferred target in therapeutic strategies aimed at the treatment of type 2 diabetes patients through down-tuning glucose assimilation. Efficient and sensitive assays that report selectively on retaining amylase activities irrespective of the nature and complexity of the biomaterial studied are of great value both in finding new and effective human amylase inhibitors and in the discovery of new microbial amylases with potentially advantageous features for biotechnological application. Activity-based protein profiling (ABPP) of retaining glycosidases is inherently suited for the development of such an assay format. We here report on the design and synthesis of 1,6--cyclophellitol-based pseudodisaccharides equipped with a suite of reporter entities and their use in ABPP of retaining amylases from human saliva, murine tissue as well as secretomes from fungi grown on starch. The activity and efficiency of the inhibitors and probes are substantiated by extensive biochemical analysis, and the selectivity for amylases over related retaining endoglycosidases is validated by structural studies.

PubMed: 33497208
DOI: 10.1021/jacs.0c13059

実験手法

X-RAY DIFFRACTION (1.67 Å)