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可快速偵測碳酸酐酶及篩選磺胺類藥物之開關型螢光探針

Fluorescent On/Off Switcher with Tunable Affinity for the Rapid Detection of Carbonic Anhydrase and Sulfonamide Drugs

摘要


本研究發展一種對環境敏感螢光分子以快速且具專一性的偵測活體細胞中的碳酸酐酶(humanCarbonic Anhydrase II, hCA II)。此新穎螢光分析方法也可以應用於快速篩選許多可抑制碳酸酐酶的磺胺類藥物。此探針之螢光增益原理是利用hCA II磺胺類結合域之疏水性環境和外部環境之差異,使環境敏感螢光分子產生顯著之螢光變化,而藉由加入和探針競爭蛋白結合域之配體可使螢光訊號減弱。

並列摘要


We have developed a new analytical tool for the rapid and specific detection of hCAII protein in cellular lysates and various sulfonamide drugs. In this paper, three sulfonamide probes were designed and synthesized by coupling of environment-sensitive fluorophore, 4-sulfamonyl- 7-aminobenzoxadiazole (SBD) to sulfonamide ligands. One of the fluorescent probes was further applied to visualize the expression of hCAII on the cell surface of living cells. Our fluorescence turn-on strategy is based on the environment-sensitive fluorophore SBD and can be exhibit fluorescence enhancement upon the binding of the environment-sensitive fluorescent probes to hydrophobic binding domain of hCA protein. The fluorescence can be switched-off again by the addition of a ligand competing with the fluorescent probe for the protein ligand binding domain.

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