Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.

  title={Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.},
  author={Shaoyong Lu and Xin-heng He and Duan Ni and J. Zhang},
  journal={Journal of medicinal chemistry},
  • Shaoyong Lu, Xin-heng He, +1 author J. Zhang
  • Published 2019
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • Allosteric modulators bound to structurally diverse allosteric sites can achieve better pharmacological advantages than orthosteric ligands. The discovery of allosteric modulators, however, has been traditionally serendipitous, owing to the complex nature of allosteric modulation. Recent advances in the understanding of allosteric regulatory mechanisms and remarkable availability of structural data of allosteric proteins and modulators, as well as their complexes, have greatly contributed to… CONTINUE READING
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