Identification of aspartic acid-203 in human thymidine phosphorylase as an important residue for both catalysis and non-competitive inhibition by the small molecule "crystallization chaperone" 5'-O-tritylinosine (KIN59).

@article{Bronckaers2009IdentificationOA,
  title={Identification of aspartic acid-203 in human thymidine phosphorylase as an important residue for both catalysis and non-competitive inhibition by the small molecule "crystallization chaperone" 5'-O-tritylinosine (KIN59).},
  author={Annelies Bronckaers and L. Enrique Aguado and Ana Negri and M-J Camarasa and Jan Balzarini and M-J P{\'e}rez-P{\'e}rez and Federico Gago and Sandra Liekens},
  journal={Biochemical pharmacology},
  year={2009},
  volume={78 3},
  pages={231-40}
}
Thymidine phosphorylase (TP) is a catabolic enzyme in thymidine metabolism that is frequently upregulated in many solid tumors. Elevated TP levels are associated with tumor angiogenesis, metastasis and poor prognosis. Therefore, the use of TP inhibitors might offer a promising strategy for cancer treatment. The tritylated inosine derivative 5'-O-tritylinosine (previously designated KIN59) is a non-competitive inhibitor of TP which was previously found to be instrumental for the crystallization… CONTINUE READING
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