thymidine phosphorylase การใช้

• Recent research has found that thymidine phosphorylase is also involved in angiogenesis.
• Tipiracil causes area under the curve 37-fold, by inhibiting thymidine phosphorylase.
• Thymidine phosphorylase has also been found to play a dual role in both cancer development and therapy.
• Tipiracil helps maintain the blood concentration of trifluridine by inhibiting the enzyme thymidine phosphorylase which metabolizes trifluridine.
• The reaction is catalysed by, pyrimidine-nucleoside phosphorylase,, uridine phosphorylase, and, thymidine phosphorylase.
• Tipiracil prevents the degradation of trifluridine via thymidine phosphorylase ( TP ) when taken orally and also has antiangiogenic properties.
• However, thymidine phosphorylase has also been found to play an essential role in the activation of the anti-cancer drug capecitabine.
• It is a combination of two active pharmaceutical ingredients : trifluridine, a nucleoside analog, and tipiracil, a thymidine phosphorylase inhibitor.
• It was then hypothesized that orally administered FTD concentrations could be increased and maintained if the drug was given with a thymidine phosphorylase inhibitor.
• Thymidine phosphorylase or pyrimidine-nucleoside phosphorylase adds 2-deoxy-alpha-D-ribose 1-phosphate to thymine, forming thymidine.
• Unlike typical mitochondrial diseases caused by mitochondrial DNA ( mtDNA ) mutations, MNGIE is caused by mutations in the TYMP gene, which encodes the enzyme thymidine phosphorylase.
• Thymidine phosphorylase catalyzes the reversible phosphorylation of thymidine, deoxyuridine, and their analogs ( except deoxycytidine ) to their respective bases ( thymine / uracil ) and 2-deoxyribose 1-phosphate.
• Experiments show inhibition of angiogenic effect by thymidine phosphorylase in the presence of 6-amino-5-chlorouracil, an transforming growth factor-?1 and varies over the course of the menstrual cycle.
• Not only has thymidine phosphorylase been shown to be identical to platelet-derived endothelial cell growth factor ( PD-ECGF ), which is an endogenous factor involved in the formation of new vasculature, but also the products of the enzyme may contribute to the stimulation of endothelial cell chemotaxis.
• Researchers later found out that trifluridine, when taken orally, was broken down into the inactive metabolites 5-trifluoromethyluracil and 5-trifluoromethyl-2, 4 ( 1 " H ", 3, " H " )-pyrimidinedione ( FTY ) during its extensive first pass metabolism in the liver via the enzyme thymidine phosphorylase.