Small-molecule kinase inhibitors: an analysis of FDA-approved drugs. Drug Discov Today 2016;21:5-10.Wu, P.; Nielsen, T. E.; Clausen, M. H. Small-Molecule Kinase Inhibitors: An Analysis of FDA-Approved Drugs. Drug Discovery Today 2016, 21, 5-10....
Couto M, Mastandrea I, Cabrera M, Cabral P, Teixidor F, Cerecetto H, Vinas C. Small- molecule kinase-inhibitors-loaded boron cluster as hybrid agents for glioma-cell-target- ing therapy. Chemistry. 2017;23:9233-9238. DOI: 10.1002/chem.201701965...
(2003) The selective tyrosine kinase inhibitor, STI571, inhibits growth of anaplastic thyroid cancer cells. J Clin Endocrinol Metab 88: 1889–1896 Article CAS Google Scholar Dziba JM and Ain KB (2004) Imatinib mesylate (Gleevec; STI571) monotherapy is ineffective in suppressing human anaplastic...
We screened a small-molecule library of diverse compounds for selective inhibitors of KIF18A MT-ATPase motor activity. Two compound hits were discovered that phenocopied the effects of KIF18A KD in cells; these hits are structurally distinct from the KIF18A inhibitor BTB-1 (refs. 27,28). Next...
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Small-molecule kinase inhibitors: an analysis of FDA-approved drugs Small-molecule kinase inhibitors (SMKIs), 28 of which are approved by the US Food and Drug Administration (FDA), have been actively pursued as promising ta... Peng,Wu,Thomas,... - 《Drug Discovery Today》 被引量: 115发表...
molecule that binds to the active conformation of a kinase in the ATP pocket,” the type II inhibitor as “a small molecule that binds to an inactive (usually DFG-OUT) conformation of a kinase,” and the type III inhibitor as “a non-ATP competitive inhibitor” or allosteric inhibitor. Al...
Regorafenib was the first small-molecule kinase inhibitor approved for the third-line treatment of metastatic CRC. It improves patient survival by inhibiting multiple growth-promoting protein kinases involved in tumor cell production, tumor angiogenesis, and maintenance of the tumor microenvironment. Fru...
small molecule kinase inhibitorc-Met kinase is the receptor for hepatocyte growth factor. Primarily expressed on epithelial and mesenchymal cells its normal function is associated with wound healing, liver regeneration and embryo development. However, dysregulation of c-Met through overexpression, gene ...
Researchers have identified two small-molecule inhibitors that effectively targeted the focal adhesion kinase (FAK), an enzyme present in certain cancers that helps tumors thrive and survive. If the drugs are developed into oral therapeutic agents in the future, they could open up the potential for...