Novel lead compound identified via virtual screening validated as a selective kappa-opioid receptor agonist
Pain relief and management can be achieved via targeted binding of opioid receptors by agonists. While currently available opioid receptor agonists effectively reduce pain, they can also cause addiction. Kappa-opioid receptors are a subtype that can be targeted to reduce pain without this side effect. Columbia scientists identified a selective kappa-opioid receptor agonist via high throughput in silico screening and validated it via BRET-based assays.
Effective pain treatment with minimal side effectsSelective at kappa-opioid receptorProvides scaffold for development of new molecules with G protein bias, resulting in better analgesics with less adverse effects Patent Information:Patent Pending (WO/2014/127256)Tech Ventures Reference: IR CU13090, CU12282
Pain treatment without side effects such as addiction and dysphoriaChemical tool to study the endogenous opioid system
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