High-throughput Screening: Establishing Mathematical and Physical Models for Bio-target Immobilization

摘要

In high-throughput screening, the immobilization of bio-target shows a significant effect on the target performance, especially the conformation. This, ultimately, has an influence on the screening quality. In present article, a series of mathematical and physical models for target immobilization were established. As shown, in the immobilization process, if the plot of C */Q versus C * is a straight-line, the drugs obtained from in vitro screening are probably applicable to in vivo environment. Otherwise, when the linearity exists between ln Q or Q and ln C *, particularly between Q and ln C *, additional competition-experiments of known ligands are necessary. In addition, the immobilization in multilayer form, as well as its impact on screening quality, was also discussed in this article (C *, the equilibrium concentration of bio-target; Q, the adsorbance).