Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors.

@article{McTigue2012MolecularCI,
  title={Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors.},
  author={Michele A. McTigue and Brion William Murray and Jeffrey H Chen and Ya-li Deng and James E Solowiej and Robert S Kania},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2012},
  volume={109 45},
  pages={18281-9}
}
Analyses of compounds in clinical development have shown that ligand efficient-molecules with privileged physical properties and low dose are less likely to fail in the various stages of clinical testing, have fewer postapproval withdrawals, and are less likely to receive black box safety warnings. However, detailed side-by-side examination of molecular interactions and properties within single drug classes are lacking. As a class, VEGF receptor tyrosine kinase inhibitors (VEGFR TKIs) have… CONTINUE READING
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References

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Showing 1-10 of 43 references

Structure-Based Design and Characterization of Axitinib. Kinase Inhibitor Drugs, Drug Discovery and Development

  • RS Kania
  • New York),
  • 2009
Highly Influential
6 Excerpts

Crystal structure of the kinase domain of human vascular endothelial growth factor receptor 2: A key enzyme in angiogenesis

  • MA McTigue
  • Structure
  • 1999
Highly Influential
4 Excerpts

Comparative effectiveness of axitinib versus sorafenib in advanced renal cell carcinoma (AXIS): A randomised phase 3 trial

  • BI Rini
  • Lancet
  • 2011
2 Excerpts

Comprehensive analysis of kinase inhibitor selectivity

  • MI Davis
  • Nat Biotechnol
  • 2011
1 Excerpt

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