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A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein (phosphorylation), a step that TKIs inhibit. TKIs are typically used as ...
Targeted covalent inhibitors (TCIs) or Targeted covalent drugs are rationally designed inhibitors that bind and then bond to their target proteins.These inhibitors possess a bond-forming functional group of low chemical reactivity that, following binding to the target protein, is positioned to react rapidly with a proximate nucleophilic residue at the target site to form a bond.
Nilotinib is a selective Bcr-Abl kinase inhibitor. [13] [18] Nilotinib is 10-30 fold more potent than imatinib in inhibiting activity of the Bcr-Abl tyrosine kinase and proliferation of Bcr-Abl expressing cells. [12] [18] [20] [21] The drug effectively inhibits the auto phosphorylation of Bcr-Abl on Tyr-177 that is involved in CML pathogenesis ...
Tyrosine kinase activity in the nucleus involves cell-cycle control and properties of transcription factors. [3] In this way, in fact, tyrosine kinase activity is involved in mitogenesis, or the induction of mitosis in a cell; proteins in the cytosol and proteins in the nucleus are phosphorylated at tyrosine residues during this process. [3]
Inhibitors of tyrosine kinase are mainly used against some specific forms of cancer. Subcategories. This category has the following 2 subcategories, out of 2 total. ...
Afatinib, sold under the brand name Gilotrif among others, is a medication which is used to treat non-small cell lung carcinoma (NSCLC). [2] [3] [4] It belongs to the tyrosine kinase inhibitor family of medications. [5]
Gefitinib is the first selective inhibitor of epidermal growth factor receptor's (EGFR) tyrosine kinase domain. Thus gefitinib is an EGFR inhibitor.The target protein (EGFR) is a member of a family of receptors which includes Her1(EGFR), Her2(erb-B2), Her3(erb-B3) and Her4 (Erb-B4).
Dasatinib is an ATP-competitive protein tyrosine kinase inhibitor. The main targets of dasatinib are BCR/Abl (the "Philadelphia chromosome"), Src, c-Kit, ephrin receptors, and several other tyrosine kinases. [12] Strong inhibition of the activated BCR-ABL kinase distinguishes dasatinib from other CML treatments, such as imatinib and nilotinib.