[Research progress of JAK-3 kinase and its inhibitors].
Yao Xue Xue Bao
; 51(10): 1520-9, 2016 10.
Article
em Zh
| MEDLINE
| ID: mdl-29932316
ABSTRACT
JAK-3, a member of the Janus kinase family, is a protein tyrosine kinase, which plays an important role in the JAK-STAT signaling pathway. Previous studies showed that regulation of JAK-3's activity plays a crucial role in the treatment of diseases such as rheumatoid arthritis. Many reports have been published with a focus on selective JAK-3 inhibitors, some of which showed excellent JAK-3 selectivity and inhibitory activities. Among the JAK-3 inhibitors reported, tofacitinib has satisfactory therapeutic benefits in the clinical trials, and has been approved for treatment of patients with rheumatoid arthritis. However, some JAK-3 inhibitors exhibited moderate to severe side effects, which need to be controlled by drug improvement. In order to pave the way for improvement of current JAK-3 inhibitors and development of new JAK-3 inhibitors, we provide an outline of the structure of JAK-3 and strategies in development of its inhibitors.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Artrite Reumatoide
/
Pirimidinas
/
Pirróis
/
Inibidores de Proteínas Quinases
/
Janus Quinase 3
Limite:
Humans
Idioma:
Zh
Ano de publicação:
2016
Tipo de documento:
Article