申请人:THE GENERAL HOSPITAL CORPORATION
公开号:US20160138077A1
公开(公告)日:2016-05-19
Disclosed herein are compounds and methods for detecting enzyme activity. In some embodiments, the enzyme is a deacetylase enzyme such as HDAC. The compound of the invention comprises a detectable label, a linker, and an enamide group. The compound can be enzymatically cleaved by the enzyme of interest to produce a nucleophilic fragment that includes the detectable label. Measurement of a signal generated by the detectable label can indicate enzyme activity. The compounds can be used as either in vivo or in vitro enzyme probes.
本文披露了一种检测酶活性的化合物和方法。在某些实施例中,该酶是去乙酰化酶,如HDAC。该发明的化合物包括可检测的标记、连接剂和烯酰胺基团。该化合物可以被感兴趣的酶酶切割,产生包含可检测标记的亲核片段。通过测量可检测标记产生的信号可以指示酶活性。这些化合物可以用作体内或体外酶探针。