A method for direct assessment of tissue-nonspecific alkaline phosphatase (TNAP) inhibitors in blood samples.
A method for direct assessment of tissue-nonspecific alkaline phosphatase (TNAP) inhibitors in blood samples.
复制标题
一种直接评估血液样本中组织非特异性碱性磷酸酶 (TNAP) 抑制剂的方法。
DOI：
10.1007/978-1-62703-562-0_6
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发表时间：
2013
期刊：
影响因子：
--
通讯作者：
Ma,Chen-Ting
中科院分区：
文献类型：
--
作者：
Sergienko,EduardA;Sun,Qing;Ma,Chen-Ting
Tissue nonspecific alkaline phosphatase (TNAP) is one of four human alkaline phosphatases (AP), a family of exocytic enzymes that catalyze hydrolysis of phospho-monoesters in bone, liver, kidney, and various other tissues. Overexpression of TNAP gives rise to excessive bone and soft tissue mineralization, including blood vessel calcification. Our prior screening campaigns have found several leads against this attractive therapeutic target using in vitro assay with a recombinant enzyme; these compounds were further optimized using medicinal chemistry approaches. To prioritize compounds for their use in animal models, we have designed and developed a biomarker assay for in situ detection of TNAP activity within human and mouse blood samples at physiological pH. This assay is suitable for screening compounds in 1,536-well plates using blood plasma from different mammalian species. The user may choose from two different substrates based on the need for greater assay simplicity or sensitivity.
