A Two-Tiered In Vitro Approach to De-Risk Drug Candidates for Potential Bile Salt Export Pump Inhibition Liabilities in Drug Discovery.

ATP Binding Cassette Transporter, Subfamily B, Member 11 / antagonists & inhibitors Chemical and Drug Induced Liver Injury / prevention & control Coculture Techniques Drug Discovery / methods Drug Evaluation, Preclinical / methods Hepatocytes Humans Inhibitory Concentration 50 Multidrug Resistance-Associated Protein 2 Multidrug Resistance-Associated Proteins / antagonists & inhibitors Taurocholic Acid / metabolism

Journal

Drug metabolism and disposition: the biological fate of chemicals
ISSN: 1521-009X
Titre abrégé: Drug Metab Dispos
Pays: United States
ID NLM: 9421550

Informations de publication

Date de publication:
11 2020
Historique:
received: 17 04 2020
accepted: 03 08 2020
pubmed: 19 9 2020
medline: 14 9 2021
entrez: 18 9 2020
Statut: ppublish

Résumé

Hepatocellular accumulation of bile salts by inhibition of bile salt export pump (BSEP/

Identifiants

DOI: 10.1124/dmd.120.000086 PMID: 32943412
pubmed: 32943412
pii: dmd.120.000086
doi: 10.1124/dmd.120.000086
doi:

Substances chimiques

ABCB11 protein, human 0
ABCC2 protein, human 0
ATP Binding Cassette Transporter, Subfamily B, Member 11 0
Multidrug Resistance-Associated Protein 2 0
Multidrug Resistance-Associated Proteins 0
Taurocholic Acid 5E090O0G3Z

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1147-1160

Informations de copyright

Copyright © 2020 by The American Society for Pharmacology and Experimental Therapeutics.

Auteurs

Michael J Hafey (MJ)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey michael_hafey@merck.com.

Robert Houle (R)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

Keith Q Tanis (KQ)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

Ian Knemeyer (I)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

Jackie Shang (J)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

Qing Chen (Q)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

Andreas Baudy (A)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

James Monroe (J)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

Frank D Sistare (FD)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

Raymond Evers (R)

Departments of Pharmacokinetics, Pharmacodynamics & Drug Metabolism (PPDM) (M.J.H., R.H., I.K., J.S., Q.C., R.E.), Genetics and Pharmacogenomics (K.Q.T.), and Safety Assessment and Laboratory Animal Resources (SALAR) (A.B., J.M., F.D.S.), Merck & Co., Inc., Kenilworth, New Jersey.

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Classifications MeSH

questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Protéines de transport membranaire › Pompes ioniques › Transporteurs d'anions › Transporteurs d'anions organiques › Transporteurs d'anions organiques ATP-dépendants › Sous-famille B de transporteurs à cassette liant l'ATP › Membre-11 de la sous-famille B à cassette liant l'ATP › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Troubles dus à des produits chimiques › Intoxication › Lésions hépatiques dues aux substances › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Techniques d'investigation › Techniques in vitro › Techniques de culture › Techniques de coculture › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Cellules › Cellules épithéliales › Hépatocytes › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Concentration inhibitrice 50 › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Protéines de transport membranaire › Pompes ioniques › Transporteurs d'anions › Transporteurs d'anions organiques › Transporteurs d'anions organiques ATP-dépendants › Protéines associées à la multirésistance aux médicaments › Protéine-2 associée à la multirésistance aux médicaments › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Protéines de transport membranaire › Pompes ioniques › Transporteurs d'anions › Transporteurs d'anions organiques › Transporteurs d'anions organiques ATP-dépendants › Protéines associées à la multirésistance aux médicaments › A Two-Tiered In Vitro Approach to De-Risk Drug...
questionsmedicales.fr › Composés polycycliques › Composés à cycles fusionnés › Stéroïdes › Cholanes › Acides choliques › Acide taurocholique › A Two-Tiered In Vitro Approach to De-Risk Drug...