Crystal Structure of Avian Aminoimidazole-4-carboxamide Ribonucleotide Transformylase in Complex with a Novel Non-folate Inhibitor Identified by Virtual Ligand Screening*

  title={Crystal Structure of Avian Aminoimidazole-4-carboxamide Ribonucleotide Transformylase in Complex with a Novel Non-folate Inhibitor Identified by Virtual Ligand Screening*},
  author={Lan Xu and Chenglong Li and Arthur J. Olson and Ian A. Wilson},
  journal={Journal of Biological Chemistry},
  pages={50555 - 50565}
Aminoimidazole-4-carboxamide ribonucleotide transformylase (AICAR Tfase), one of the two folate-dependent enzymes in the de novo purine biosynthesis pathway, is a promising target for anti-neoplastic chemotherapy. Although classic antifolates, such as methotrexate, have been developed as anticancer agents, their general toxicity and drug resistance are major issues associated with their clinical use and future development. Identification of inhibitors with novel scaffolds could be an attractive… 

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