Drug-target residence time: critical information for lead optimization.

@article{Lu2010DrugtargetRT,
  title={Drug-target residence time: critical information for lead optimization.},
  author={Hao Lu and Peter J. Tonge},
  journal={Current opinion in chemical biology},
  year={2010},
  volume={14 4},
  pages={467-74}
}
Failure due to poor in vivo efficacy is a primary contributor to attrition during the development of new chemotherapeutics. Lead optimization programs that in their quest for efficacy focus solely on improving the affinity of drug-target binding are flawed, since this approach ignores the fluctuations in drug concentration that occur in vivo. Instead the lifetime of the drug-target complex must also be considered, since drugs only act when they are bound to their targets. Consequently, to… CONTINUE READING

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