Nelfinavir and Its Active Metabolite M8 Are Partial Agonists and Competitive Antagonists of the Human Pregnane X Receptor.

Burk, Oliver; Kronenberger, Thales; Keminer, Oliver; Lee, Serene M L; Schiergens, Tobias S; Schwab, Matthias; Windshügel, Björn

Burk, Oliver; Kronenberger, Thales; Keminer, Oliver; Lee, Serene M L; Schiergens, Tobias S; Schwab, Matthias; Windshügel, Björn.

Afiliação

Burk O; Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Viscera
Kronenberger T; Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Viscera
Keminer O; Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Viscera
Lee SML; Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Viscera
Schiergens TS; Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Viscera
Schwab M; Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Viscera
Windshügel B; Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Viscera

Mol Pharmacol ; 99(3): 184-196, 2021 03.

Article em En | MEDLINE | ID: mdl-33483427

Assuntos

Hepatócitos/metabolismo; Nelfinavir/análogos & derivados; Nelfinavir/farmacologia; Receptor de Pregnano X/metabolismo; Subfamília B de Transportador de Cassetes de Ligação de ATP/genética; Sítios de Ligação; Citocromo P-450 CYP3A/genética; Relação Dose-Resposta a Droga; Regulação da Expressão Gênica/efeitos dos fármacos; Células Hep G2; Hepatócitos/citologia; Hepatócitos/efeitos dos fármacos; Humanos; Modelos Moleculares; Conformação Molecular; Simulação de Acoplamento Molecular; Nelfinavir/química; Receptor de Pregnano X/agonistas; Receptor de Pregnano X/antagonistas & inibidores; Receptor de Pregnano X/química; Cultura Primária de Células

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Nelfinavir / Hepatócitos / Receptor de Pregnano X Idioma: En Ano de publicação: 2021 Tipo de documento: Article

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Nelfinavir / Hepatócitos / Receptor de Pregnano X Idioma: En Ano de publicação: 2021 Tipo de documento: Article