6YD7

X-ray structure of furin in complex with the canavanine-based inhibitor 4-guanidinomethyl-phenylacetyl-Arg-Tle-Canavanine-Amba

6YD7 の概要

• エントリーDOI: 10.2210/pdb6yd7/pdb
• 分子名称: Furin, 4-guanidinomethyl-phenylacetyl-Arg-Tle-Canavanine-Amba, CALCIUM ION, ... (8 entities in total)
• 機能のキーワード: protease, inhibitor, complex, canavanine, hydrolase
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 53371.96

構造登録者

Dahms, S.O. (登録日: 2020-03-20, 公開日: 2021-02-17, 最終更新日: 2024-01-31)

主引用文献

Lam van, T.V.,Heindl, M.R.,Schlutt, C.,Bottcher-Friebertshauser, E.,Bartenschlager, R.,Klebe, G.,Brandstetter, H.,Dahms, S.O.,Steinmetzer, T.
The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin.
Acs Med.Chem.Lett., 12:426-432, 2021

PubMed Abstract: Furin activates numerous viral glycoproteins, and its inhibition prevents virus replication and spread. Through the replacement of arginine by the less basic canavanine, new inhibitors targeting furin in the trans-Golgi network were developed. These inhibitors exert potent antiviral activity in cell culture with much lower toxicity than arginine-derived analogues, most likely due to their reduced protonation in the blood circulation. Thus, despite its important physiological functions, furin might be a suitable antiviral drug target.

PubMed: 33732412
DOI: 10.1021/acsmedchemlett.0c00651

実験手法

X-RAY DIFFRACTION (1.8 Å)