Research progress on aurora kinase inhibitor MK-0457 in therapy for some hematological malignancies -- review.
- Author:
Yi-Qiong LIANG
1
;
Bao-An CHEN
;
Ya-Li CHEN
Author Information
1. Department of Hematology, Zhongda Hospital, Southeast University Clinical Medical College, Nanjing, Jiangsu Province, China.
- Publication Type:Journal Article
- MeSH:
Aurora Kinases;
Hematologic Neoplasms;
classification;
drug therapy;
Humans;
Piperazines;
therapeutic use;
Protein Kinase Inhibitors;
therapeutic use;
Protein-Serine-Threonine Kinases;
antagonists & inhibitors
- From:
Journal of Experimental Hematology
2009;17(3):810-815
- CountryChina
- Language:Chinese
-
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.
