Journal
INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 74, Issue 3, Pages 217-222Publisher
INDIAN PHARMACEUTICAL ASSOC
DOI: 10.4103/0250-474X.106063
Keywords
Ciprofloxacin; HtrA2; moxifloxacin Mycobacterium tuberculosis; ofloxacin
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Funding
- Biotechnology Information System (BTIS), Department of Biotechnology (DBT), Ministry of Science and Technology, Government of India, India
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Daisy, et al.: Targeting HtrA2 with Fluoroquinolones and their Analogues Tuberculosis is a highly communicable and chronic respiratory disease caused by pathogenic bacterium Mycobacterium tuberculosis. The drug - resistant species of Mycobacterium tuberculosis are tough to cure due to its resistant activity toward potential drugs. Available inhibitors of tuberculosis include few antimicrobial fluoroquinolone agents like ciprofloxacin, ofloxacin, and moxifloxacin to treat resistant Mycobacterium strains. Literature study elucidates that macromolecular target namely, HtrA2 of Mycobacterium tuberculosis play a dual role of protease and chaperone. These two activities are dependent on temperature, with low temperatures promoting the chaperone function and high temperatures promoting serine protease activity. Under normal physiological conditions HtrA2 acts as a quality control factor and promotes cell survival. In the present investigation, we screened fluoroquinolone such as ciprofloxacin, moxifloxacin and ofloxacin and their analogues based on better Docking score, absorption, distribution, metabolism and excretion screening and Lipinski's rule of 5, to find out their efficiency on resistant strain through in silico study. From the results observed, the analogues are suggested to be potent inhibitors of HtrA2 with sufficient scope for further exploration.
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