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Improvement and Validation of the Fluorescence-Based Histone Deacetylase Assay Using an Internal Standard
Archiv der Pharmazie ( IF 5.1 ) Pub Date : 2001-07-01 , DOI: 10.1002/1521-4184(200107)334:7<248::aid-ardp248>3.0.co;2-k
K Hoffmann 1 , B Heltweg , M Jung
Affiliation  

The determination of the activity of histone deacetylase (HDAC) and the potency of its inhibitors has become an important goal in medicinal chemistry. This is due both to the involvement of HDAC in gene regulation and the ability of its inhibitors to modulate transcription and induce differentation and/or apoptosis in cancer cells. We have previously reported the development of a non‐isotopic assay for HDAC using a fluorescent derivative of ε‐acetyl lysine. It can replace existing methods that rely on radioactively labeled histones or oligopeptides as substrates. Here we report validation and improvement of the procedure using an internal standard for the quantitation of the fluorescent substrate by HPLC.

中文翻译:

使用内标改进和验证基于荧光的组蛋白脱乙酰酶检测

组蛋白去乙酰化酶 (HDAC) 活性及其抑制剂效力的测定已成为药物化学中的一个重要目标。这是由于 HDAC 参与基因调控及其抑制剂在癌细胞中调节转录和诱导分化和/或凋亡的能力。我们之前曾报道过使用 ε-乙酰赖氨酸的荧光衍生物对 HDAC 进行非同位素测定的发展。它可以取代依赖放射性标记的组蛋白或寡肽作为底物的现有方法。在这里,我们报告了使用 HPLC 定量荧光底物的内标对程序的验证和改进。
更新日期:2001-07-01
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