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    • 2. 发明申请
    • Self-immolative probes for enzyme activity detection
    • 用于酶活性检测的自发性探针
    • US20120122136A1
    • 2012-05-17
    • US12927497
    • 2010-11-16
    • Maciej SzczepanikIrina V. LebedevaYuejun XiangPraveen PandeWayne Forrest Patton
    • Maciej SzczepanikIrina V. LebedevaYuejun XiangPraveen PandeWayne Forrest Patton
    • C12Q1/26C07D491/22G01N21/75C07D493/10C07D413/14C07D237/32C07D311/08
    • C12Q1/26C07D311/08C07D491/052C07D491/20C07D493/10C09K11/06C09K2211/1022C09K2211/1088C12Q1/37C12Q1/44C12Q1/485G01N2333/902G01N2500/00Y10T436/18
    • Provided is a compound comprising the structure: (SIG)-(SI-MOD)m. In this compound, SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. With this compound, when MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided is a method of determining whether a sample comprises an activator, using the above-described compound. Additionally provided is a method of determining whether a cell comprises a nitroreductase using the above-described compound where nitroreductase is the activator. Further provided is a method of determining whether a mammalian cell is hypoxic using the above-described compound where nitroreductase is the activator. A method of detecting a microorganism that comprises a nitroreductase, using the above-described compound where nitroreductase is the activator, is also provided. Also provided is a method of identifying nitroreductase in a sample, using the above-described compound where nitroreductase is the activator.
    • 提供了包含以下结构的化合物:(SIG) - (SI-MOD)m。 在该化合物中,SIG是信号分子,SI是与SIG结合的自消除结构,使得SIG相对于没有SI的SIG的信号具有降低的信号,MOD是与SI结合的部分,其经受 活化剂,m为1至约10的整数。用该化合物,当MOD被活化剂修饰时,SI是不稳定的并且从SIG自分离,使得SIG产生增加的信号。 还提供了使用上述化合物来确定样品是否包含活化剂的方法。 另外提供了使用上述硝基还原酶是活化剂的化合物来确定细胞是否包含硝基还原酶的方法。 还提供了使用上述硝基还原酶是活化剂的化合物来确定哺乳动物细胞是否缺氧的方法。 还提供了使用上述硝基还原酶为活化剂的化合物检测包含硝基还原酶的微生物的方法。 还提供了使用上述硝酸还原酶是活化剂的化合物来鉴定样品中的硝基还原酶的方法。