Novel lead compound identified via virtual screening validated as a selective kappa-opioid receptor agonist
- 總結
- 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.
- 技術優勢
- 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
- 技術應用
- Pain treatment without side effects such as addiction and dysphoriaChemical tool to study the endogenous opioid system
- 詳細技術說明
- None
- *Abstract
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None
- *Inquiry
- Jerry KokoshkaColumbia Technology VenturesTel: (212) 854-8444Email: TechTransfer@columbia.edu
- *IR
- CU13090
- *Principal Investigation
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- *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.
- 國家/地區
- 美國
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