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KIN59 is a purine riboside derivative that allosterically inhibits thymidine phosphorylase (TPase; IC₅₀s = 44 and 67 μM for purified E. coli and human enzymes, respectively). Through this action, KIN59 blocks the conversion of thymidine to thymine. KIN59 inhibits TPase-induced angiogenesis in a chicken chorioallantoic membrane assay and reduces endothelial cell migration without impacting proliferation. KIN59 also inhibits the binding of fibroblast growth factor 2 (FGF2) to FGF receptor 1, preventing the growth and neovascularization of subcutaneous tumors induced by FGF2-transformed endothelial cells injected in immunodeficient nude mice.

5’-O-Tritylinosine acts as an allosteric inhibitor of angiogenic enzyme thymidine phosphorylase.

5’O-Tritylinosine acts as an allosteric inhibitor of angiogenic enzyme thymidine phosphorylase.

[1] SANDRA LIEKENS. The nucleoside derivative 5’-O-trityl-inosine (KIN59) suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action.[J]. The Journal of Biological Chemistry, 2004, 279 28: 29598-29605. DOI: 10.1074/jbc.m402602200
[2] SANDRA LIEKENS. 5’-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesis.[J]. Molecular Pharmacology, 2006, 70 2: 501-509. DOI: 10.1124/mol.105.021188
[3] SANDRA LIEKENS. The thymidine phosphorylase inhibitor 5’-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonist.[J]. Molecular Cancer Therapeutics, 2012, 11 4: 817-829. DOI: 10.1158/1535-7163.mct-11-0738