通过光基质库发现适用于体内向的受组织限制的生物反应
Kentaro Yoshioka, Toru Komatsu1, Akihiro Nakada
1PRESTO, Japan Science and Technology Agency (JST) , Kawaguchi, Saitama 332-0012, Japan.
Journal of the American Chemical Society
|September 12, 2015
概括
研究人员确定了二氧化碳酶2 (CES2) 是激活基化物的酶. 这种酶对可以在体内向肝脏和脏提供光染料,从而有助于开发新药.
科学领域:
- 生物化学
- 酵素学
- 化学生物学
背景情况:
- 组织特异性生物反应是开发向化学生物工具和前期药物的关键.
- 酶的发现对于确定特定的生物反应途径至关重要.
研究的目的:
- 开发一种用于发现组织特异性酶活性的新查方法.
- 为了确定光基质和前期药物的向输送的酶掩盖组对.
主要方法:
- 使用光基板库选方法分析组织提取物.
- 用式电泳凝测定和质指纹测定来识别候选蛋白质.
- 使用特定基质验证了已识别的蛋白质的酶活性.
主要成果:
- 皮鲁维尔化物被确定为由碳氧化酶2 (CES2) 特别化的基质.
- 炭酸乙酶2 (CES2) 主要局部存在于肝脏和脏组织中.
- 在体内,pyruvyl向组/CES2酶对促进了7 - 氨基-4 - 甲基胺向肝脏和脏的输送.
结论:
- 开发的查方法对于发现组织特异性酶活性是有效的.
- 皮鲁维尔向组/CES2酶对显示了向药物输送和成像的潜力.
- 这种方法可以扩展到识别其他掩盖组/酶对,用于先进的前药物和光基质开发.
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