Research progress on aurora kinase inhibitor MK-0457 in therapy for some hematological malignancies -- review / 中国实验血液学杂志
Journal of Experimental Hematology
;
(6): 810-815, 2009.
Artigo
em Chinês
| WPRIM
| ID: wpr-334019
ABSTRACT
Recent work indicates that an Aurora kinase inhibitor MK-0457 (VX-680), a small-molecule inhibitor of Aurora kinases A, B, C and BCR-ABL, FLT-3, JAK-2, can block the progression of cell growth cycle, causing apoptosis in a range of human tumors. MK-0457 has the activity against expressions of wild-type and mutated bcr-abl gene, including the T315I mutant, and can inhibit the activity of FLT-3, JAK-2 and their mutated types as well. Clinical applications suggest that the MK-0457 has therapeutic effect on the highly refractory CML and CML with poor prognosis, Ph(+) ALL with T315I mutant, relapse refractory AML and JAK-2 positive myeloproliferative diseases (MPD). The intensive preclinical studies and the on-going phase II clinical trials will open up a new vista of therapy for some hematological malignancies. This review focuses on the pharmacologic action of MK-0457 and its clinical trial as well as combined application.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Piperazinas
/
Classificação
/
Proteínas Serina-Treonina Quinases
/
Neoplasias Hematológicas
/
Usos Terapêuticos
/
Inibidores de Proteínas Quinases
/
Tratamento Farmacológico
/
Aurora Quinases
Limite:
Humanos
Idioma:
Chinês
Revista:
Journal of Experimental Hematology
Ano de publicação:
2009
Tipo de documento:
Artigo
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