Development of a Novel Affinity Labeling Method for Target Identification of Bioactive Small Molecules

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  • 薬物標的タンパク質の同定を志向した新規アフィニティーラベル化法の開発
  • Review for award 薬物標的タンパク質の同定を志向した新規アフィニティーラベル化法の開発
  • Review for award ヤクブツ ヒョウテキ タンパクシツ ノ ドウテイ オ シコウ シタ シンキ アフィニティーラベルカホウ ノ カイハツ

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Abstract

<p>Target identification (target-ID) is an important step in elucidating the mechanisms of action of bioactive small molecules. In the past few decades, a number of target-ID methods have been developed. Among these, affinity labeling has been reliably used for specific modifications, as well as for the identification of weakly interacting protein targets, membrane-associated protein targets, and target-interacting proteins under native cellular conditions, which are generally difficult to achieve by conventional pull-down methods. In general, affinity labeling utilizes chemical probes composed of a bioactive small molecule, a reactive group, and a detection unit. However, the design and synthesis of highly functionalized chemical probes is often time-consuming. To address this issue, we have recently developed some simple affinity labeling methods using small fluorogenic tags, such as 4-alkoxy-7-nitro-2,1,3-benzoxadiazole (O-NBD), 2,3-dichloromaleimide (diCMI), and 4-azidophthalimide (AzPI), and successfully achieved the specific fluorescent labeling of target proteins, even in living cells. These methods should be useful for target-ID in phenotypic drug discovery.</p>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 139 (12), 1513-1521, 2019-12-01

    The Pharmaceutical Society of Japan

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