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Synthesis and evaluation of a selective fluorogenic Pup derived assay reagent for Dop, a potential drug target in Mycobacterium tuberculosis.
- Source :
-
Chembiochem : a European journal of chemical biology [Chembiochem] 2012 Sep 24; Vol. 13 (14), pp. 2056-60. Date of Electronic Publication: 2012 Aug 24. - Publication Year :
- 2012
-
Abstract
- 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.<br /> (Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Subjects :
- Amidohydrolases antagonists & inhibitors
Amino Acid Sequence
Bacterial Proteins antagonists & inhibitors
Biocatalysis
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
High-Throughput Screening Assays
Hydrolysis
Kinetics
Molecular Sequence Data
Peptides chemical synthesis
Peptides chemistry
Peptides metabolism
Substrate Specificity
Ubiquitins antagonists & inhibitors
Virulence Factors antagonists & inhibitors
Amidohydrolases metabolism
Bacterial Proteins metabolism
Fluorescent Dyes chemistry
Mycobacterium tuberculosis drug effects
Ubiquitins metabolism
Virulence Factors metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1439-7633
- Volume :
- 13
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Chembiochem : a European journal of chemical biology
- Publication Type :
- Academic Journal
- Accession number :
- 22927162
- Full Text :
- https://doi.org/10.1002/cbic.201200460