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In vitro methods to assess 11ß-hydroxysteroid dehydrogenase type 1 activity.
Kley, Manuel; Moser, Seraina O; Winter, Denise V; Odermatt, Alex.
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  • Kley M; Division of Molecular and Systems Toxicology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland; Swiss Centre for Applied Human Toxicology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.
  • Moser SO; Division of Molecular and Systems Toxicology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland; Swiss Centre for Applied Human Toxicology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.
  • Winter DV; Division of Molecular and Systems Toxicology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.
  • Odermatt A; Division of Molecular and Systems Toxicology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland; Swiss Centre for Applied Human Toxicology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland. Electronic address: alex.odermatt@unibas.ch.
Methods Enzymol ; 689: 121-165, 2023.
Article en En | MEDLINE | ID: mdl-37802569
11ß-Hydroxysteroid dehydrogenase type 1 (11ß-HSD1) converts inactive 11-keto-glucocorticoids to their active 11ß-hydroxylated forms. It also catalyzes the oxoreduction of other endogenous and exogenous substrates. The ubiquitously expressed 11ß-HSD1 shows high levels in liver and other metabolically active tissues such as brain and adipose tissue. Pharmacological inhibition of 11ß-HSD1 was found to ameliorate adverse metabolic effects of elevated glucocorticoids in rodents and humans, improve wound healing and delay skin aging, and enhance memory and cognition in rodent Alzheimer's disease models. Thus, there is an interest to develop 11ß-HSD1 inhibitors for therapeutic purposes. This chapter describes in vitro methods to assess 11ß-HSD1 enzyme activity for different purposes, be it in disease models, for the assessment of the kinetics of novel substrates or for the screening and characterization of inhibitors. 11ß-HSD1 protein expression and preparations of the different biological samples are discussed first, followed by a description of a well-established and easily adaptable 11ß-HSD1 enzyme activity assay. Finally, different readout methods are shortly described. This chapter should provide the reader with a toolbox of methods to assess 11ß-HSD1 activity with instructions in the form of a decision tree for the choice and implementation of an appropriate enzyme activity assay.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: 11-beta-Hidroxiesteroide Deshidrogenasa de Tipo 1 / Glucocorticoides Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Methods Enzymol Año: 2023 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: 11-beta-Hidroxiesteroide Deshidrogenasa de Tipo 1 / Glucocorticoides Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Methods Enzymol Año: 2023 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Estados Unidos