Synthesis and Evaluation of a Selective Fluorogenic Pup Derived Assay Reagent for Dop, a Potential Drug Target in Mycobacterium tuberculosis

A litter of pups: The synthesis and in vitro evaluation of new Pup‐based fluorogenic substrates for Dop, the mycobacterial depupylase, are described. A full‐length Pup–amidomethylcoumarin conjugate as well as an amino‐terminus‐truncated analogue exhibited high sensitivity and specificity towards hyd...

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Veröffentlicht in:	Chembiochem : a European journal of chemical biology 2012-09, Vol.13 (14), p.2056-2060
Hauptverfasser:	Merkx, Remco, Burns, Kristin E., Slobbe, Paul, El Oualid, Farid, El Atmioui, Dris, Darwin, K. Heran, Ovaa, Huib
Format:	Artikel
Sprache:	eng
Schlagworte:	Amidohydrolases - antagonists & inhibitors Amidohydrolases - metabolism Amino Acid Sequence Bacterial Proteins - antagonists & inhibitors Bacterial Proteins - metabolism Biocatalysis Communications deamidase of Pup (Dop) Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Fluorescent Dyes - chemistry fluorescent probes High-Throughput Screening Assays Hydrolysis Kinetics Molecular Sequence Data Mycobacterium tuberculosis Mycobacterium tuberculosis - drug effects Peptides - chemical synthesis Peptides - chemistry Peptides - metabolism protein-protein interactions Pup-proteasome system (PPS) Substrate Specificity tuberculosis Ubiquitins - antagonists & inhibitors Ubiquitins - metabolism Virulence Factors - antagonists & inhibitors Virulence Factors - metabolism
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Zusammenfassung:	A litter of pups: The synthesis and in vitro evaluation of new Pup‐based fluorogenic substrates for Dop, the mycobacterial depupylase, are described. A full‐length Pup–amidomethylcoumarin conjugate as well as an amino‐terminus‐truncated analogue exhibited high sensitivity and specificity towards hydrolysis by Dop. The substrates developed here might find application as high‐throughput screening assay reagents for the identification of Dop inhibitors.
ISSN:	1439-4227 1439-7633
DOI:	10.1002/cbic.201200460