A structural characterization of the isoniazid Mycobacterium tuberculosis drug target, Rv2971, in its unliganded form.
Acta Crystallogr F Struct Biol Commun
; 70(Pt 5): 572-7, 2014 May.
Article
em En
| MEDLINE
| ID: mdl-24817712
ABSTRACT
Aldo-keto reductases (AKR) are a large superfamily of NADPH-dependent oxidoreductases and play a role in detoxification of toxic metabolites. Rv2971, an AKR in Mycobacterium tuberculosis, has recently been identified as a target of isoniazid, a key first-line drug against tuberculosis. Here, the cloning, expression, purification, crystallization and structural characterization of Rv2971 are described. To gain insight into its function, the crystal structure of Rv2971 was successfully determined to 1.60 Å resolution in its unliganded form. The structure exhibits a TIM-barrel fold typical of AKRs, revealing structural characteristics essential for function and substrate specificities, allowing a structural comparison between Rv2971 and other mycobacterial AKRs.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sistemas de Liberação de Medicamentos
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Aldeído Redutase
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Isoniazida
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Mycobacterium tuberculosis
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Antituberculosos
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
Acta Crystallogr F Struct Biol Commun
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Austrália