Protein structure enables rational drug design
© KATERYNA KON/SCIENCE PHOTO LIBRARY
A detailed structural analysis of a protein receptor found on immune cells offers a molecular roadmap for drug developers to design new therapeutics for inflammatory diseases and cancers.
The chemokine receptor 2 (CXCR2) is a key mediator of immune cell trafficking and recruitment. The receptor’s involvement in autoimmune disorders such as colitis and some cancers has made it an attractive drug target, but so far no CXCR2-directed therapeutic candidates have demonstrated efficacy in a clinical setting.
To enable better informed drug-discovery efforts, a ShanghaiTech University–led team has determined the atomic structure of CXCR2 in both its active and inactive states.
The results revealed unique modes of binding and activation — structural insights that can now be exploited by scientists hoping to create more potent and selective inhibitors of the receptor.
- Nature 585, 135–140 (2020). doi: 10.1038/s41586-020-2492-5