7OXF

Solution structure of bee apamin

7OXF の概要

• エントリーDOI: 10.2210/pdb7oxf/pdb
• NMR情報: BMRB: 34641
• 分子名称: Apamin (1 entity in total)
• 機能のキーワード: protein apamin toxin bee venom, toxin
• 由来する生物種: Apis mellifera (Honeybee)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 2034.39

構造登録者

Mineev, K.,Kuzmenkov, A.,Vassilevski, A. (登録日: 2021-06-22, 公開日: 2022-07-13, 最終更新日: 2023-06-14)

主引用文献

Kuzmenkov, A.I.,Peigneur, S.,Nasburg, J.A.,Mineev, K.S.,Nikolaev, M.V.,Pinheiro-Junior, E.L.,Arseniev, A.S.,Wulff, H.,Tytgat, J.,Vassilevski, A.A.
Apamin structure and pharmacology revisited.
Front Pharmacol, 13:977440-977440, 2022

PubMed Abstract: Apamin is often cited as one of the few substances selectively acting on small-conductance Ca-activated potassium channels (K2). However, published pharmacological and structural data remain controversial. Here, we investigated the molecular pharmacology of apamin by two-electrode voltage-clamp in oocytes and patch-clamp in HEK293, COS7, and CHO cells expressing the studied ion channels, as well as in isolated rat brain neurons. The microtitre broth dilution method was used for antimicrobial activity screening. The spatial structure of apamin in aqueous solution was determined by NMR spectroscopy. We tested apamin against 42 ion channels (K, K, Na, nAChR, ASIC, and others) and confirmed its unique selectivity to K2 channels. No antimicrobial activity was detected for apamin against Gram-positive or Gram-negative bacteria. The NMR solution structure of apamin was deposited in the Protein Data Bank. The results presented here demonstrate that apamin is a selective nanomolar or even subnanomolar-affinity K2 inhibitor with no significant effects on other molecular targets. The spatial structure as well as ample functional data provided here support the use of apamin as a K2-selective pharmacological tool and as a template for drug design.

PubMed: 36188602
DOI: 10.3389/fphar.2022.977440

実験手法

SOLUTION NMR