The potentiation of menadione on imatinib by downregulation of ABCB1 expression.
Clin Exp Pharmacol Physiol
; 47(6): 997-1004, 2020 06.
Article
em En
| MEDLINE
| ID: mdl-32112424
ABSTRACT
Imatinib was the first BCR-ABL inhibitor used in clinical practice to treat chronic myeloid leukaemia (CML) and significantly improve the life expectancy of CML patients in the chronic phase. However, a portion of CML patients are resistant to imatinib. This study aimed to determine whether menadione (Vitamin K3) can improve imatinib efficacy in CML and to thoroughly explore the combination regimen mechanism between imatinib and menadione. Menadione improved imatinib efficacy in K562 cells by downregulating ABCB1 expression and increased the intracellular concentration of imatinib, which confirmed that this combination regimen is more effective than imatinib monotherapy. The results demonstrate that menadione and imatinib combination therapy may be a promising approach to refractory CML.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Leucemia Mielogênica Crônica BCR-ABL Positiva
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Protocolos de Quimioterapia Combinada Antineoplásica
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Vitamina K 3
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Inibidores de Proteínas Quinases
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Mesilato de Imatinib
Limite:
Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article