Research progresses of Mycobacterium tuberculosis cytochrome P450s as a potential drug target / 药学学报
Yao Xue Xue Bao
; (12): 427-434, 2014.
Article
en Zh
| WPRIM
| ID: wpr-245066
Biblioteca responsable:
WPRO
ABSTRACT
Identification and validation of a new target is one of the most important steps for new antituberculosis (TB) drug discovery. Researches have shown that Mycobacterium tuberculosis (Mtb) encodes 20 CYP450 enzymes which play important roles in the synthesis and metabolism of lipid, cholesterol utilization, and the electron transport of respiratory chain in Mtb. With the critical roles within the organism as well as the protein structures of six Mtb CYP450 enzymes being clarified, some of them have been highlighted as potential anti-tuberculosis targets. In this paper, the phylogenetic analysis, the structural features, and the enzymatic functions of Mtb CYPs, as well as the mechanism of interactions with selective inhibitors such as azole antifungal agents for the CYPs have been reviewed and summarized. The druggability of the CYPs has also been analyzed for their further utility as targets in high throughput screening and rational design of more selective inhibitors.
Texto completo:
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Índice:
WPRIM
Asunto principal:
Farmacología
/
Filogenia
/
Azoles
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Tuberculosis
/
Química
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Sistemas de Liberación de Medicamentos
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Sistema Enzimático del Citocromo P-450
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Quimioterapia
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Descubrimiento de Drogas
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Inhibidores Enzimáticos del Citocromo P-450
Límite:
Humans
Idioma:
Zh
Revista:
Yao Xue Xue Bao
Año:
2014
Tipo del documento:
Article