Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis.
J Med Chem
; 61(19): 8563-8593, 2018 10 11.
Article
in En
| MEDLINE
| ID: mdl-29851474
ABSTRACT
Decaprenylphosphoryl-ß-d-ribose 2'-epimerase (DprE1), a vital enzyme for cell wall synthesis, plays a crucial role in the formation of lipoarabinomannan and arabinogalactan. It was first reported as a druggable target on the basis of inhibitors discovered in high throughput screening of a drug library. Since then, inhibitors with different types of chemical scaffolds have been reported for their activity against this enzyme. Formation of a covalent or noncovalent bond by the interacting ligand with the enzyme causes loss of its catalytic activity which ultimately leads to the death of the mycobacterium. This Perspective describes various DprE1 inhibitors as anti-TB agents reported to date.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Bacterial Proteins
/
Tuberculosis
/
Alcohol Oxidoreductases
/
Drug Development
/
Mycobacterium tuberculosis
/
Antitubercular Agents
Limits:
Humans
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
2018
Document type:
Article
Affiliation country:
India