Rational use of plasma protein and tissue binding data in drug design.

@article{Liu2014RationalUO,
  title={Rational use of plasma protein and tissue binding data in drug design.},
  author={Xingrong Liu and Matthew E Wright and Cornelis E. C. A. Hop},
  journal={Journal of medicinal chemistry},
  year={2014},
  volume={57 20},
  pages={8238-48}
}
It is a commonly accepted assumption that only unbound drug molecules are available to interact with their targets. Therefore, one of the objectives in drug design is to optimize the compound structure to increase in vivo unbound drug concentration. In this review, theoretical analyses and experimental observations are presented to illustrate that low plasma protein binding does not necessarily lead to high in vivo unbound plasma concentration. Similarly, low brain tissue binding does not lead… CONTINUE READING

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