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O-GlcNAcトランスファーゼ阻害剤の発見

Benjamin J Gross¹, Brian C Kraybill, Suzanne Walker

¹Department of Microbiology and Molecular Genetics, Harvard Medical School, Boston, Massachusetts 02115, USA.

Journal of the American Chemical Society

|October 20, 2005

まとめ

研究者は,大量のO-GlcNAc移転酵素 (OGT) とスクリーニングアッセイを生産するための新しいシステムを開発しました. これは,O-GlcNAcylationの研究を支援する,OGTのための新しい小分子阻害剤の発見につながった.

科学分野:

バイオケミストリーバイオケミストリー
分子生物学は分子生物学である.
化学生物学化学生物学とは

背景:

O-GlcNAcylationは,真核細胞の信号伝達経路を調節する重要な翻訳後の修正である.
O-GlcNAc移転酶 (OGT) の小分子阻害剤の開発は,O-GlcNAcylationを研究するために不可欠です.
以前の課題には,OGTの表現が低いことと,効果的な高通量スクリーニング方法の欠如が含まれていました.

研究の目的:

OGT触媒領域の大規模生産のための発現システムを開発する.
OGT阻害剤を特定するための光ベースの測定法を作成する.
OGT.の新種の小分子阻害剤を発見すること.

主な方法:

大量のOGT触媒ドメインを生成する表現システムを設計しました.
光ベースの基板アナログ位移測定法を実装しました.
OGT阻害剤を特定するために,化合物ライブラリをスクリーニングしました.

主要な成果:

大量のOGT触媒ドメインを成功裏に生産しました.
OGT活動のための高通量スクリーニングアッセイを開発し,検証しました.
新しい小分子OGT阻害剤のセットを特定しました.

結論:

開発された発現システムとアッセイは,OGT阻害剤の発見を容易にする.
これらの発見は,OGT.の構造的および機能的研究のための基礎を提供します.
特定された阻害剤は,O-GlcNAcylationを調査するための貴重なツールです.

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