GPCR Drug Discovery | StaR® Technology
A StaR® is a stabilised GPCR containing a small number of point mutations that greatly improve its thermostability without disrupting its pharmacology. StaR® technology is transferrable across GPCR families and allows the selection of stable, functionally relevant, purified conformations of target GPCRs that retain their expected drug-binding characteristics. The StaR® technology is based on world-class science from the MRC Laboratory of Molecular Biology (Cambridge, UK), with which Heptares maintains exclusive consultancies and active collaboration. In addition, Heptares has access to all IP generated from LMB relating to the application of the StaR® technology to GPCRs and other transmembrane proteins.
Turkey beta1 adrenergic receptor with stabilising mutations bound to the partial agonist salbutamol. (pdb code: 2Y04). Chainbow coloration (i.e. Blue= N-terminus / Red= C-terminus). Acknowledgements. Warne et al, Nature. 2011. |
