Discovery of new allosteric drugs

The RCaH crystallisation lab is a pillar of Diamond’s XChem facility. The approach has proved particularly powerful for discovering new allosteric drugging opportunities.

In PTO1B, long abandoned as undruggable, fragments revealed how to exploit dramatic movements. In α7 nicotinic acetylcholine receptor, where normal fluctuations of neurotransmitter release must be retained, a vestibular site was shown to modulate activity.