Bookcover of Design, Synthesis and Evaluation of Novel Inhibitors of CT and DosR
Booktitle:

Design, Synthesis and Evaluation of Novel Inhibitors of CT and DosR

Development of Bisubstrate Analog Inhibitors of Cholera Toxin and α-Helix Mimetics as Modulators of Dormancy Survival Regulator

VDM Verlag Dr. Müller (2011-02-03 )

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ISBN-13:

978-3-639-30969-0

ISBN-10:
3639309693
EAN:
9783639309690
Book language:
English
Blurb/Shorttext:
Infectious diseases cause millions of deaths each year. The top single disease killers include tuberculosis and diarrheal diseases. The diarrheal diseases caused by cholera toxin and E. coli heat-labile enterotoxin constitute a large part of the diarrhea-related deaths worldwide each year. While there are some efficacious drugs against Vibrio cholerae in the market, their resistance is developing quickly. We wish to develop synthetic molecules that could bind to CT with a high affinity to block the enzymatic reaction catalyzed by CT. We designed, synthesized and evaluated bisubstrate analogs targeting the active site of CT. The most potent inhibitor demonstrated an IC50 of around 40 μM. It could serve as a promising drug to treat cholera. The second project is to use α-helix mimetics for probing the protein-protein interactions of DosR. The main function of DosR is to mediate the transition of Mycobacteria tuberculosis into dormancy and may contribute to latency. Disruption of the dimerization of DosR could keep MTB in an active state, so that the existing drugs could treat them effectively. We employed small molecules and peptides as tools to achieve the goal.
Publishing house:
VDM Verlag Dr. Müller
Website:
http://www.vdm-verlag.de
By (author) :
Guangtao Zhang
Number of pages:
160
Published on:
2011-02-03
Stock:
Available
Category:
Organic chemistry
Price:
59.00 €
Keywords:
structure-based drug design, Cholera Toxin, inhibitor, CTA, bisubstrate analog, tuberculosis, dormancy survival regulator, peptide, Protein-Protein Interactions

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