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デング熱ウイルスのポリメラーゼの結晶学的断片スクリーニングは,非核酸抗菌剤の開発のための複数の結合部位を明らかにする

Manisha Saini^1,2, Jasmin C Aschenbrenner^3,4, Francesc Xavier Ruiz^1,2

¹Center for Advanced Biotechnology and Medicine, Rutgers, the State University of New Jersey, Piscataway, New Jersey 08854, United States.

Journal of medicinal chemistry

|September 2, 2025

まとめ

研究者たちは,デング熱ウイルス (DENV) の抗ウイルス薬の可能性を探すため,1108 個の断片を検出しました. 彼らは60の化合物を特定し,DENV非構造タンパク質5 (NS5) のRNA依存RNAポリメラーゼ (RdRp) に新しい結合部位を発見した.

科学分野:

ウイルス学
構造生物学
薬物の発見

背景:

デング熱ウイルス (DENV) は,年間約4億人を感染させ,世界的な健康負担を大きく引き起こす.
現在,DENV感染に対して有効な抗ウイルス薬は入手できません.

研究の目的:

DENVに対する抗ウイルス薬の開発の潜在的な出発点を特定する.
非構造タンパク質5 (NS5) のDENVセロタイプ2RNA依存RNAポリメラーゼ (RdRp) ドメインの結合部位を断片ベースのスクリーニングで探求する.

主な方法:

大規模な結晶学的断片スクリーンが実施された.
1108個の断片をDENV-2 NS5 RdRpドメインに対してスクリーニングした.
ヒット化合物とその結合部位は構造分析を用いて特定された.

主要な成果:

活性部位,Nポケット,RNAトンネルを含む既知の結合部位で60のヒット化合物が特定されました.
新しい結合部位と断片結合ホットスポットは,親指部位IIで発見されました.
構造データはDENV RdRp抑制に関する洞察を提供します.

結論:

特定された断片と新しい結合部位は,非核酸抑制剤の開発に有望な経路を提供します.
これらの発見は,DENVや他のフラビウイルスRdRpsを標的とした構造ベースの薬剤設計に価値があります.

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