X-ray Structural and Biological Evaluation of a Series of Potent and Highly Selective Inhibitors of Human Coronavirus Papain-like Proteases

@inproceedings{BezSantos2014XraySA,
  title={X-ray Structural and
Biological Evaluation
of a Series of Potent and Highly Selective Inhibitors of Human Coronavirus
Papain-like Proteases},
  author={Yahira M. B{\'a}ez-Santos and Scott J. Barraza and Michael D. Wilson and Michael P. Agius and Anna Maria Mielech and Nicole M. Davis and Susan C Baker and Scott D Larsen and Andrew D. Mesecar},
  booktitle={Journal of medicinal chemistry},
  year={2014}
}
Structure-guided design was used to generate a series of noncovalent inhibitors with nanomolar potency against the papain-like protease (PLpro) from the SARS coronavirus (CoV). A number of inhibitors exhibit antiviral activity against SARS-CoV infected Vero E6 cells and broadened specificity toward the homologous PLP2 enzyme from the human coronavirus NL63. Selectivity and cytotoxicity studies established a more than 100-fold preference for the coronaviral enzyme over homologous human… CONTINUE READING
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papain-like protease of human SARS coronavirus: mechanistic and inhibitor design implications

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