Prothiwa, Michaela; Bottcher, Thomas published an article in 2020, the title of the article was Competitive profiling for enzyme inhibitors using chemical probes.Name: 2-Chloroacetamide And the article contains the following content:
Enzyme inhibitors are central tools for chem. biol. In this chapter we will discuss the application of chem. probes for competitive profiling of inhibitors of the quinolone biosynthesis enzyme PqsD of Pseudomonas aeruginosa. The human pathogen P. aeruginosa produces a large diversity of 2-alkyl-4(JH)-quinolones and their derivatives as metabolites with major roles in quorum sensing, virulence, and interspecies competition. PqsD is a central enzyme in the biosynthesis of all ofthese quinolones and hence an interesting target for inhibitor discovery. Aaivity-based probes with an elearophilic warhead bind covalently to aaive site nucleophiles like cysteine or serine. An α-chloroacetamide probe with terminal alkyne tag allowed to selectively label the aaive site cysteine of PqsD and was demonstrated to be a useful tool for inhibitor discovery using competition experiments Potent inhibitors bind to the aaive site and thereby prevent labeling ofthe enzyme by the probe. Labeling intensity is quantified. on polyacrylamide gels by the fluorescence of a reporter tag appended by bioorthogonal click chem. The competitive inhibitor profiling strategy has many advantages over traditional screening approaches and is applicable in vitro as well as in live cells. Here we describe the synthesis of an activity-based probe and provide our detailed protocols for target enzyme labeling as well as its application for the screening for potent enzyme inhibitors of PqsD by a competitive profiling strategy. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Name: 2-Chloroacetamide
The Article related to acetamides: chemistry, bacterial proteins: antagonists & inhibitors, bacterial proteins: biosynthesis, bacterial proteins: genetics, binding, competitive, catalytic domain, click chemistry: methods, electrophoresis, polyacrylamide gel: methods, enzyme inhibitors: chemistry, enzyme inhibitors: pharmacology and other aspects.Name: 2-Chloroacetamide
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