Suicide substrate probes

Suicide substrate probes This type of ABP contains a masked electrophile that is activated after the probe fnnctions as snbstrate for the target enzyme. The activated electrophile then reacts with the nearby nncleophilic residne(s) in the active site such as 4-difluoromethylphenyl-fcEXcyclohexylammounium)phosphate to probe phosphatases (Bentley et al, 2002). 

Geurink PP, Florea BI, Van der Marel GA et al (2010) Probing the proteasome cavity in three steps bio-orthogonal photo-reactive suicide substrates. Chem Commun (Camb) 46 9052-9054... 

A mutant of the non-electroactive enzyme 3-lactamase where residue TyrlOS located close the active site was replaced by a cysteine by site-directed mutagenesis was successfully labeled with 24 and the redox potential of the probe was seen to shift by 20 mV in the presence of a suicide substrate in the enzyme active site... 

Prior, S.D., Dalton, H. 1985. Acetylene as a suicide substrate and active site probe for methane monooxygenase from Methylococcus capsulatus (Bath). FEMS Microbiol Lett 29 105-109. 

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