Pan Zhengying, Jeffery Douglas A, Chehade Kareem, Beltman Jerlyn, Clark James M, Grothaus Paul, Bogyo Matthew, Baruch Amos
Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett. 2006 Jun 1;16(11):2882-5. doi: 10.1016/j.bmcl.2006.03.012. Epub 2006 Mar 22.
A series of diphenylphosphonate-based probes were developed for the trypsin-like serine proteases. These probes selectively target serine proteases rather than general serine hydrolases that are targets for fluorophosphonate-based probes. This increased selectivity allows detection of low abundance serine proteases in complex proteomes using simple SDS-PAGE methods. We present here the application of multiple probes in enzyme activity profiling of intact mast cells, a type of inflammatory cell implicated in allergy and autoimmune diseases.
开发了一系列基于二苯基膦酸酯的用于类胰蛋白酶丝氨酸蛋白酶的探针。这些探针选择性地靶向丝氨酸蛋白酶，而不是基于氟膦酸酯的探针所针对的一般丝氨酸水解酶。这种更高的选择性使得能够使用简单的SDS-PAGE方法在复杂蛋白质组中检测低丰度丝氨酸蛋白酶。我们在此展示了多种探针在完整肥大细胞（一种与过敏和自身免疫性疾病有关的炎症细胞类型）的酶活性分析中的应用。
