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Novel lead compound identified via virtual screening validated as a selective kappa-opioid receptor agonist

Summary

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.

Technology Benefits

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

Technology Application

Pain treatment without side effects such as addiction and dysphoriaChemical tool to study the endogenous opioid system

Detailed Technology Description

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*Abstract

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*Inquiry

Jerry KokoshkaColumbia Technology VenturesTel: (212) 854-8444Email: TechTransfer@columbia.edu

*IR

CU13090

*Principal Investigator

*Publications

Ana Negri, Marie-Laurie Rives, Michael J. Caspers, Thomas E. Prisinzano, Jonathan A. Javitch, and Marta Filizola. Discovery of a Novel Selective Kapp-Opiod Receptro Agonist Using Crystal Structure-Based Virtual Screening. J Chem Inf Model, Vol. 53, Issue 3, March 2013, pp. 521-526.Marie-Laurie Rives, Mary Rossillo, Lee-Yuan Liu-Chen, and Jonathan A. Javitch. 6'-Guanidinonaltrindole (6'-GNTI) Is a G Protein-biased k-Opioid Receptor Agonist That Inhibits Arrestin Recruitment. J Biolog Chem, Vol. 287, Issue 32, Aug 2012, pp. 27050-27054.

Country/Region

USA