Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents

@article{Khan2006MolecularBF,
  title={Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents},
  author={Javed A. Khan and Xiao Tao and Liang Tong},
  journal={Nature Structural \&Molecular Biology},
  year={2006},
  volume={13},
  pages={582-588}
}
Nicotinamide phosphoribosyltransferase (NMPRTase) has a crucial role in the salvage pathway of NAD+ biosynthesis, and a potent inhibitor of NMPRTase, FK866, can reduce cellular NAD+ levels and induce apoptosis in tumors. We have determined the crystal structures at up to 2.1-Å resolution of human and murine NMPRTase, alone and in complex with the reaction product nicotinamide mononucleotide or the inhibitor FK866. The structures suggest that Asp219 is a determinant of substrate specificity of… Expand
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