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.
Article
in Chinese
| 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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Piperazines
/
Classification
/
Protein Serine-Threonine Kinases
/
Hematologic Neoplasms
/
Therapeutic Uses
/
Protein Kinase Inhibitors
/
Drug Therapy
/
Aurora Kinases
Limits:
Humans
Language:
Chinese
Journal:
Journal of Experimental Hematology
Year:
2009
Type:
Article
Similar
MEDLINE
...
LILACS
LIS