HPLC/ESI-MS对DNA拓扑异构酶靶向化合物的亲和超滤测定用于候选药物筛选。

Hong Zhang, Yuan-Jiang Pan
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引用次数: 0

摘要

介绍了一种筛选试验方法。该方法是基于抗肿瘤候选物对拓扑异构酶的亲和力。在这种方法中,以拓扑异构酶为靶点,筛选出抗肿瘤候选物。传统的复杂化合物分析通常会由于相对较低的浓度而遇到信号抑制,但活性化合物的酶亲和筛选可以有效地将所需的分析人员集中到小体积的高浓度中。活性化合物通过超滤从非亲和化合物中分离出来。保留在过滤器上的分子-酶复合物随后通过酸化分离得到拓扑异构酶-亲和化合物,用于高效液相色谱联用电喷雾电离质谱检测(ESI-MS)分析。这种基于酶亲和力的筛选试验提供了一种高度特异性和高效的方法,可以直接筛选、鉴定和获得候选药物,从而提高了高通量筛选活动的准确性和速度。
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Affinity ultrafiltration of DNA topoisomerases-targeted compounds determined with HPLC/ESI-MS for drug candidate screening.
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