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Structure of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) holoenzyme from an orthorhombic crystal form: an insight into the bifunctionality of the enzyme.
Dhagat, Urmi; Carbone, Vincenzo; Chung, Roland P-T; Schulze-Briese, Clemens; Endo, Satoshi; Hara, Akira; El-Kabbani, Ossama.
Afiliación
  • Dhagat U; Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, Parkville, Victoria 3052, Australia.
Acta Crystallogr Sect F Struct Biol Cryst Commun ; 63(Pt 10): 825-30, 2007 Oct 01.
Article en En | MEDLINE | ID: mdl-17909281
Mouse 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) is a bifunctional enzyme that catalyses the oxidoreduction of the 3- and 17-hydroxy/keto groups of steroid substrates such as oestrogens, androgens and neurosteroids. The structure of the AKR1C21-NADPH binary complex was determined from an orthorhombic crystal belonging to space group P2(1)2(1)2(1) at a resolution of 1.8 A. In order to identify the factors responsible for the bifunctionality of AKR1C21, three steroid substrates including a 17-keto steroid, a 3-keto steroid and a 3alpha-hydroxysteroid were docked into the substrate-binding cavity. Models of the enzyme-coenzyme-substrate complexes suggest that Lys31, Gly225 and Gly226 are important for ligand recognition and orientation in the active site.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Holoenzimas / Hidroxiesteroide Deshidrogenasas Tipo de estudio: Prognostic_studies Idioma: En Revista: Acta Crystallogr Sect F Struct Biol Cryst Commun Año: 2007 Tipo del documento: Article País de afiliación: Australia Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Holoenzimas / Hidroxiesteroide Deshidrogenasas Tipo de estudio: Prognostic_studies Idioma: En Revista: Acta Crystallogr Sect F Struct Biol Cryst Commun Año: 2007 Tipo del documento: Article País de afiliación: Australia Pais de publicación: Reino Unido