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Updated: Jul 15, 2026
09:57
System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
Structure, function and drug targeting in Mycobacterium tuberculosis cytochrome P450 systems
Kirsty J McLean1, Adrian J Dunford, Rajasekhar Neeli
1Manchester Interdisciplinary Biocentre, Faculty of Life Sciences, University of Manchester, 131 Princess Street, Manchester M1 7DN, UK.
Archives of Biochemistry and Biophysics
|May 8, 2007
Summary
Drug-resistant tuberculosis (Mtb) is rising, necessitating new antibiotics. Cytochrome P450 enzymes in Mtb are potential drug targets, as inhibiting them with azole drugs shows potent anti-mycobacterial activity.
Area of Science:
- Microbiology
- Biochemistry
- Drug Discovery
Background:
- Mycobacterium tuberculosis (Mtb) resurgence due to drug resistance.
- High number of cytochrome P450 (P450) enzymes in Mtb.
- Azole drugs show anti-mycobacterial activity by inhibiting P450s.
Purpose of the Study:
- Review current knowledge of Mtb P450s and redox partners.
- Highlight potential drug targets within Mtb P450s.
- Discuss P450 roles in host lipid and sterol/steroid transformations.
Main Methods:
- Literature review of Mtb P450 structure/function.
- Analysis of P450-azole drug interactions.
- Examination of P450 roles in host metabolism.
Main Results:
- Identified potential drug targets among Mtb P450s.
- Provided evidence for P450 involvement in host lipid metabolism.
- Detailed structural insights into heme binding and azole interactions.
- Characterized cytochrome P420 and azole resistance mechanisms.
Conclusions:
- Mtb P450s are promising targets for novel anti-tubercular therapies.
- Understanding P450-azole interactions is crucial for overcoming drug resistance.
- Further research into P450 function can guide new drug development strategies.
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