Differential scanning fluorimetry as secondary screening platform for small molecule inhibitors of Bcl-XL.

@article{Wan2009DifferentialSF,
  title={Differential scanning fluorimetry as secondary screening platform for small molecule inhibitors of Bcl-XL.},
  author={Kah Fei Wan and Sifang Wang and Christopher John Brown and Victor C-K Yu and Michael Entzeroth and David Philip Lane and May Ann Lee},
  journal={Cell cycle},
  year={2009},
  volume={8 23},
  pages={3943-52}
}
Since apoptosis is impaired in malignant cells overexpressing prosurvival Bcl-2 proteins, drugs mimicking their natural antagonists, BH3-only proteins, might overcome chemoresistance. Small molecule inhibitors of Bcl-X(L) function have been discovered from diverse structure classes using rational drug design as well as high-throughput screening (HTS) approaches. However, most of the BH3 mimetics that have been identified via screening based on fluorescence polarization displayed an affinity for… CONTINUE READING
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