1.
ACS Chem Biol
; 12(5): 1183-1187, 2017 05 19.
Artigo
em Inglês
| MEDLINE
| ID: mdl-28318222
RESUMO
PF-956980 has been used previously as a JAK3-selective chemical probe in numerous cell-based experiments. Here, we report that not only is PF-956980 a pan-JAK ATP-competitive inhibitor but it also causes selective reduction of endogenous JAK2 and JAK3 protein levels in human primary immune cells (in a time-dependent manner), leaving the other JAK family members (JAK1 and TYK2) unchanged. We found that PF-956980 selectively downregulated JAK2 and JAK3 mRNA, corresponding to changes observed at the protein level. This work highlights therapeutic opportunities for the development of pharmacological inhibitors that also modulate the expression of their cognate binding proteins.
Assuntos
Regulação para Baixo , Janus Quinase 2/genética , Janus Quinase 3/genética , Pirimidinas/farmacologia , Pirróis/farmacologia , Trifosfato de Adenosina/metabolismo , Ligação Competitiva , Células Cultivadas , Humanos , Sistema Imunitário/citologia , Janus Quinase 2/análise , Janus Quinase 3/análise , Inibidores de Proteínas Quinases/farmacologia , RNA Mensageiro/análise , RNA Mensageiro/efeitos dos fármacos
2.
J. investig. allergol. clin. immunol
; 27(3): 187-189, 2017.
Artigo
em Inglês
| IBECS
| ID: ibc-163170
RESUMO
No disponible