Selective PKCδ Inhibitor B106 Elicits Uveal Melanoma Growth Inhibitory Effects Independent of Activated PKC Isoforms.
ACS Chem Biol
; 14(1): 132-136, 2019 01 18.
Article
em En
| MEDLINE
| ID: mdl-30525429
ABSTRACT
In uveal melanoma (UM) cells, the protein kinase C (pathway) is almost generally constitutively activated as a result of an activating mutation in either the GNAQ or the GNA11 G-protein. A pan-PKC inhibitor, sotrastaurin (also named AEB071), is in clinical trials for treatment of UM patients with limited success and eliciting adverse effects. Interestingly, genetic interference with expression of just one PKC isoform, e.g., PKCδ, is sufficient to reduce UM cell proliferation. Therefore, we tested the effect of a recently described specific PKCδ inhibitor, B106, on growth and survival of UM cell lines. Surprisingly, we found that B106 efficiently induced apoptosis in several cell lines, but apparently independent of activated PKCδ.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Neoplasias Uveais
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Carbazóis
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Cromanos
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Inibidores de Proteínas Quinases
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Proteína Quinase C-delta
Limite:
Humans
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article