BioWorld International Correspondent

LONDON - Heptares Therapeutics Ltd., the latest spinout from the UK's Medical Research Council (MRC), secured further seed capital after validating its novel G-protein coupled receptor (GPCR) stabilization technology.

The founding scientists at the MRC Laboratory of Molecular Biology (LMB), Cambridge, have used the platform technology to solve the structure of the beta-1 adrenergic receptor.

"It's a major achievement and a landmark for UK science and research, and for the people involved," Malcolm Weir, CEO, told BioWorld International. "Its significance is not only in getting the structure, but also showing the utility of the method."

London-based Heptares did not disclose how much money it raised, but Weir said it will fund the company for the next 12-18 months, as the basic research progresses. The technology will now be applied to a list of GPCRs that are involved in central nervous system and metabolic disorders.

While GPCRs are the targets of more than 50 percent of marketed drugs and the single most important family of drug targets in humans, their inherent instability makes them intractable to structural studies and in vitro screening. By stabilizing them, Heptares' StaR (for stabilized receptors) technology makes GPCRs amenable to these conventional drug discovery approaches.

Weir said that the company has selected GPCRs that are well characterized, with supporting biology, as the initial subjects of further stabilization work. "This successful application of the technology greatly increases the probability that we can get structures for other GPCRs, and now we can systematize the process."

With the beta-1 adrenergic receptor solved, Heptares will kick off its drug discovery activities also. "With the structure in hand, we can start to do quite a lot from the drug design point of view. The company will be searching for both small molecule and antibodies against its targets.

The company has revealed few details of its platform technology, developed by scientific founders Richard Henderson, director of the LMB, and Chris Tate, also of LMB, but claims the StaR technology is capable of produce large quantities of purified, functional GPCRs.