Heptares: Stabilizing GPCR discovery

Structure-based drug design is increasingly used to discover therapeutics against soluble protein targets such as kinases and proteases, but has not traditionally been used for GPCRs, the most common family of drug targets, because they quickly fall apart when removed from their natural membrane environment. Heptares Therapeutics Ltd. is developing a technology for stabilizing GPCRs in a soluble, functional conformation, allowing the targets to be screened against both small molecules and antibodies.

The company is pursuing a "platform plus product" strategy, developing its own pipeline of small molecules for neurology and endocrine indications while pursuing a partnering strategy on a target-by-target basis, co-founder and CEO Malcolm Weir told BioCentury...