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Br J Cancer ; 106(6): 1148-52, 2012 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-22343623

RESUMO

BACKGROUND: It is becoming increasingly recognised that opioids are responsible for tumour growth. However, the effects of opioids on tumour growth have been controversial. METHODS: The effects of κ-opioid receptor (KOR) agonist on the growth of non-small cell lung cancer (NSCLC) cells were assessed by a cell proliferation assay. Western blotting was performed to ascertain the mechanism by which treatment with KOR agonist suppresses tumour growth. RESULTS: Addition of the selective KOR agonist U50,488H to gefitinib-sensitive (HCC827) and gefitinib-resistant (H1975) NSCLC cells produced a concentration-dependent decrease in their growth. These effects were abolished by co-treatment with the selective KOR antagonist nor-BNI. Furthermore, the growth-inhibitory effect of gefitinib in HCC827 cells was further enhanced by co-treatment with U50,488H. With regard to the inhibition of tumour growth, the addition of U50, 488H to H1975 cells produced a concentration-dependent decrease in phosphorylated-glycogen synthase kinase 3ß (p-GSK3ß). CONCLUSION: The present results showed that stimulation of KOR reduces the growth of gefitinib-resistant NSCLC cells through the activation of GSK3ß.


Assuntos
(trans)-Isômero de 3,4-dicloro-N-metil-N-(2-(1-pirrolidinil)-ciclo-hexil)-benzenoacetamida/farmacologia , Proliferação de Células/efeitos dos fármacos , Receptores Opioides kappa/agonistas , Antineoplásicos/farmacologia , Carcinoma Pulmonar de Células não Pequenas , Linhagem Celular Tumoral , Sobrevivência Celular , Resistencia a Medicamentos Antineoplásicos , Receptores ErbB/genética , Gefitinibe , Expressão Gênica , Quinase 3 da Glicogênio Sintase/metabolismo , Glicogênio Sintase Quinase 3 beta , Humanos , Mutação de Sentido Incorreto , Naltrexona/análogos & derivados , Naltrexona/farmacologia , Fosforilação , Proteínas Proto-Oncogênicas c-akt/metabolismo , Quinazolinas/farmacologia , Receptores Opioides kappa/antagonistas & inibidores , Receptores Opioides kappa/genética , Receptores Opioides kappa/metabolismo , Fator de Transcrição STAT3/metabolismo , Transdução de Sinais
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