Application of tyrosine kinase inhibitors as a promising targeting treatment for myeloproliferative neoplasms --- review.

Abstract

As well as playing vital roles in main cellular processes, such as abnormal proliferation, differentiation, survival, apoptosis, and a lot of tyrosine kinases (TK) are involved in oncogenesis. TK or components of their signal pathways have been found abnormal in many hematological malignancies. Therefore, tyrosine kinase inhibitors (TKI) have been provided a great deal of enthusiasm for development of therapy in myeloproliferative neoplasms (MPN). Representativity, the treatment of chronic myelogenous leukemia (CML) was revolutionary for the design of imatinib mesylate (IM), which is a BCR/ABL TKI. Subsequently, because of need for the resistance or intolerance, novel agents are being explored and imatinib has now been extended to eosinophilia-associated myeloid neoplasms with PDGFRA, PDGFRB or FGFR1 gene mutations. Recently, JAK2 inhibitor drugs are currently being tested in clinical trials. Here, the current review mainly focuses on the role of TK in classic MPN including CML, polycythemia vera (PV), primary myelofibrosis (PMF), essential thrombocythemia (ET), and advances of targeting these abnormalities with small molecule inhibitors.

• Authors: Min Wei, Chun-Ji Gao
• Journal: Zhongguo shi yan xue ye xue za zhi (Zhongguo Shi Yan Xue Ye Xue Za Zhi) Vol. 19 Issue 4 Pg. 1064-70 (Aug 2011) ISSN: 1009-2137 [Print] China
• PMID: 21867645 (Publication Type: Journal Article, Review)

Chemical References

• Protein-Tyrosine Kinases

Topics

• Drug Delivery Systems
• Humans
• Myeloproliferative Disorders (drug therapy)
• Protein-Tyrosine Kinases (antagonists & inhibitors, metabolism)