Adenosine A2A, discovered by Heptares, is a G-protein coupled receptor (GPCR) involved in the regulation of dopaminergic pathways in the brain.
Heptares said it has stabilised the A2A receptor using its proprietary StaR technology, determined the receptor’s binding characteristics through Biophysical Mapping, and resolved its 3D crystal structure using x-ray crystallography.
Shire has paid an upfront payment to Heptares and is also responsible to pay an option exercise payment, future milestone payments, plus royalties on product sales.
Heptares CEO Malcolm Weir said they are excited to sign this option agreement with Shire for the development of novel A2A antagonist, a new agent for treating patients suffering from debilitating CNS diseases.
"A2A is an important and clinically validated GPCR drug target, yet it has never been adequately addressed by the available older chemistries," Weir said.
"Heptares has discovered fundamentally novel chemotypes as the basis for a new and, we believe, superior approach to A2A receptor pharmacology."