Sygnature Chemical Services will help Heptares Therapeutics progress one of its internal GPCR programs. Sygnature will use its synthetic chemistry expertise to produce a novel library for Heptares to evaluate against its purified, stabilized, and functional GPCR targets, StaRs™ (stabilised receptors).
This technology involves introducing a small number of point mutations into the structure of a GPCR to improve the molecule’s thermostability while preserving its functional and drug-binding conformation and characteristics in detergent-solubilized form. Heptares claims that the StaR technology overcomes problems traditionally associated with inherent instability of GPCRs and for the first time allows drug discovery methods such as crystallization, structure-based design, fragment screening, and ligand interaction analysis to be applied to traditionally intractable GPCRs.
The company’s most advanced project results from its discovery of highly novel antagonists of the A2a receptor. It says it plans to look for a development partner in the field of Parkinson’s disease early next year.