Inhibition of human UDP-glucuronosyltransferase (UGT) enzymes by kinase inhibitors: Effects of dabrafenib, ibrutinib, nintedanib, trametinib and BIBF 1202.

Adenine / analogs & derivatives Glucuronosyltransferase / antagonists & inhibitors Humans Imidazoles / pharmacology Indoles / pharmacology Microsomes, Liver / enzymology Oximes / pharmacology Piperidines Protein Kinase Inhibitors / pharmacology Pyrazoles / pharmacology Pyridones / pharmacology Pyrimidines / pharmacology Pyrimidinones / pharmacology
BIBF 1202 (PubChem CID, 11606145) Dabrafenib (PubChem CID, 44462760) Drug-drug interaction Drug-endobiotic interaction Enzyme inhibition Ibrutinib (PubChem CID, 24821094) In vitro-in vivo extrapolation Kinase inhibitor Nintedanib (PubChem CID, 135423438) Propofol (PubChem CID, 4943) Trametinib (PubChem CID, 11707110) Trifluoperazine (PubChem CID, 5566) UDP-Glucuronosyltransferase β-Estradiol (PubChem CID, 5757)

Journal

Biochemical pharmacology
ISSN: 1873-2968
Titre abrégé: Biochem Pharmacol
Pays: England
ID NLM: 0101032

Informations de publication

Date de publication:
11 2019
Historique:
received: 11 07 2019
accepted: 19 08 2019
pubmed: 25 8 2019
medline: 14 7 2020
entrez: 25 8 2019
Statut: ppublish

Résumé

We have demonstrated previously that the kinase inhibitors (KIs) lapatinib, pazopanib, regorafenib and sorafenib are potent inhibitors of UGT1A1 and UGTs 1A7-1A10. The present study characterised the effects of four additional drugs in this class, dabrafenib, ibrutinib, nintedanib and trametinib, on human UGT enzyme activities in vitro. Dabrafenib, ibrutinib, nintedanib and trametinib were potent inhibitors of human liver microsomal UGT1A1; K

Identifiants

DOI: 10.1016/j.bcp.2019.08.018 PMID: 31445021
pubmed: 31445021
pii: S0006-2952(19)30306-5
doi: 10.1016/j.bcp.2019.08.018
pii:
doi:

Substances chimiques

Imidazoles 0
Indoles 0
Oximes 0
Piperidines 0
Protein Kinase Inhibitors 0
Pyrazoles 0
Pyridones 0
Pyrimidines 0
Pyrimidinones 0
ibrutinib 1X70OSD4VX
trametinib 33E86K87QN
Glucuronosyltransferase EC 2.4.1.17
nintedanib G6HRD2P839
Adenine JAC85A2161
dabrafenib QGP4HA4G1B

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

113616

Informations de copyright

Crown Copyright © 2019. Published by Elsevier Inc. All rights reserved.

Auteurs

Porntipa Korprasertthaworn (P)

Department of Clinical Pharmacology, College of Medicine and Public Health, Flinders University, Adelaide, Australia; Department of Pharmacology, Faculty of Science, Mahidol University, Bangkok, Thailand. Electronic address: Porntipa.kor@mahidol.ac.th.

Nuy Chau (N)

Department of Clinical Pharmacology, College of Medicine and Public Health, Flinders University, Adelaide, Australia. Electronic address: Nuy.chau@flinders.edu.au.

Pramod C Nair (PC)

Department of Clinical Pharmacology, College of Medicine and Public Health, Flinders University, Adelaide, Australia; Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia. Electronic address: Pramod.nair@flinders.edu.au.

Andrew Rowland (A)

Department of Clinical Pharmacology, College of Medicine and Public Health, Flinders University, Adelaide, Australia; Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia. Electronic address: Andrew.rowland@flinders.edu.au.

John O Miners (JO)

Department of Clinical Pharmacology, College of Medicine and Public Health, Flinders University, Adelaide, Australia; Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia. Electronic address: John.miners@flinders.edu.au.

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Classifications MeSH

questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Purines › Adénine › Inhibition of human...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Glycosyltransferase › Hexosyltransferases › Glucuronosyltransferase › Inhibition of human...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Inhibition of human...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Imidazoles › Inhibition of human...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Indoles › Inhibition of human...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Microsomes › Microsomes du foie › Inhibition of human...
questionsmedicales.fr › Composés chimiques organiques › Amines › Hydroxylamines › Oximes › Inhibition of human...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pipéridines › Inhibition of human...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Inhibition of human...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Pyrazoles › Inhibition of human...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyridines › Pyridones › Inhibition of human...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrimidines › Inhibition of human...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrimidines › Pyrimidinones › Inhibition of human...