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A protein kinase inhibitor (PKI) is a type of enzyme inhibitor that blocks the action of one or more protein kinases. [1] Protein kinases are enzymes that phosphorylate (add a phosphate, or PO 4, group) to a protein and can modulate its function. [2] The phosphate groups are usually added to serine, threonine, or tyrosine amino acids on the ...
BRAF kinase inhibitor. BRAF kinase mutation V600E-positive Metastatic melanoma. Skin reactions, secondary malignancies (mostly squamous cell carcinoma), anaphylaxis (rare) and hypotension (rare). Abbreviations/Acronyms: IM – Intramuscular. IV – Intravenous. IA – Intra-arterial. SC – Subcutaneous. PO – Per os, oral. IP – Intrapleural.
Adavosertib is a Wee1 kinase inhibitor that is undergoing numerous clinical trials in the treatment of refractory solid tumors. [9] However, toxicities such as myelosuppression , diarrhea , and supraventricular tachyarrhythmia have arisen while attempting to determine the toxicity and effectiveness of the drug.
Paracrine signalling mediates the response to epidermal growth factor receptor kinase inhibitors. Paracrine activates epidermal growth factor receptor in endothelial cells of the tumor to do this. [23] Dasatinib is a Src tyrosine kinase inhibitor that is effective both as a senolytic and as therapy for chronic myelogenous leukemia. [24]
Above is a ball-and-stick model of the inorganic phosphate molecule (H PO 4 2−).Colour coding: P (orange); O (red); H (white). The chemical activity of a protein kinase involves removing a phosphate group from ATP and covalently attaching it to one of three amino acids that have a free hydroxyl group.
Pages in category "Protein kinase inhibitors" The following 62 pages are in this category, out of 62 total. This list may not reflect recent changes. ...
A number of Rho kinase inhibitors are known. [15] [16] [17]Chemical structure of fasudil. AT-13148 [18]; BA-210; β-ElemeneBelumosudil; Chroman 1 [19] [20]; DJ4, which is a selective multi-specific ATP competitive inhibitor of activity of ROCK1 (IC50 of 5 nM), ROCK2 (IC50 of 50 nM), MRCKα (IC50 of 10 nM) and MRCKβ (IC50 of 100 nM) kinases without affecting activity of PAK1 and DMPK at 5 μM ...
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. ...