Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes.

@article{Roskoski2016ClassificationOS,
  title={Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes.},
  author={Robert Roskoski},
  journal={Pharmacological research},
  year={2016},
  volume={103},
  pages={26-48}
}
Because dysregulation and mutations of protein kinases play causal roles in human disease, this family of enzymes has become one of the most important drug targets over the past two decades. The X-ray crystal structures of 21 of the 27 FDA-approved small molecule inhibitors bound to their target protein kinases are depicted in this paper. The structure of the enzyme-bound antagonist complex is used in the classification of these inhibitors. Type I inhibitors bind to the active protein kinase… CONTINUE READING

Citations

Publications citing this paper.
Showing 1-10 of 43 extracted citations

References

Publications referenced by this paper.
Showing 1-10 of 128 references

N

  • H. S. Meharena, P. Chang, M. M. Keshwani, K. Oruganty, A. K. Nene
  • Kannan, et al., Deciphering the structural basis…
  • 2013
Highly Influential
6 Excerpts

Similar Papers

Loading similar papers…