Currently, more than 20 different tyrosine kinase targets are under evaluation in drug discovery projects for cancer treatment. A number of tyrosine kinase inhibitors have been tested in various phases of clinical trials. This chapter provides an overview of identification, characterization, and ...
Sorafenib: Targeting Multiple Tyrosine Kinases in Cancer Sorafenib (BAY 43-9006, Nexavar) is an oral multiple tyrosine kinase inhibitor. Main targets are receptor tyrosine kinase pathways frequently deregulated i... J Hasskarl - 《Recent Results Cancer Res》 被引量: 53发表: 2014年 Eph receptor ...
In general, there are four modes of RTK dimerization which lead to activation of the tyrosine kinase domain. In the first mode, receptor dimerization is completely ligand mediated without any direct contact between the extracellular regions of the two receptors, such as in the case of TrkA (NGF...
Since their invention in the early 2000s, tyrosine kinase inhibitors (TKIs) have gained prominence as the most effective pathway-directed anti-cancer agents. TKIs have shown significant utility in the treatment of multiple hematological malignancies and solid tumors, including chronic myelogenous leukemia...
Several specific tyrosine kinase inhibitors, like Gleevec, Iressa and Tarceva, have been successfully used in cancer treatment. However, there are subsets of tumors that do not respond to TKI treatment. This resistance may be due to the drug extrusion activity of multidrug resistance ABC ...
Palmer, Mechanistic insight into ALK receptor tyrosine kinase in human cancer biology, Nat. Rev. Cancer 13 (2013) 685.Hallberg, B.; Palmer, R. H. Mechanistic insight into ALK receptor tyrosine kinase in human cancer biology. Nat. Rev. Cancer 13:685-700; 2013....
The role of receptor tyrosine kinases (RTKs) in cancer began only about three decades ago; however, the amount of research and progress dedicated to the study of RTKs has been explosive, considering the vast quantity of kno...
Abstract 1531: BCR-Abl tyrosine kinase inhibitor Nilotinib (Tasigna®) reverses ABCB1/Pgp- and ABCG2/BCRP-mediated multidrug resistance Over-expression of ABC transporters are involved in the extrusion of therapeutic drugs, leading to MDR, which can eventually produce cancer chemotherapy failure. Pr...
The role of EFGR TKI in NSCLC will be discussed in detail and data from these studies will be used to illustrate the challenges in designing clinical trials and interpreting outcomes. 展开 关键词: Tyrosine kinase inhibitors, non-small cell lung cancer, gefitinib, erlotinib, biomarkers DOI: ...
et al. Anaplastic lymphoma kinase (ALK) in human cancer. J. Mol. Endocrinol. 47, R11–R23 (2011). Article CAS PubMed Google Scholar Chiarle, R., Voena, C., Ambrogio, C., Piva, R. & Inghirami, G. The anaplastic lymphoma kinase in the pathogenesis of cancer. Nature Rev. Cancer ...