Small molecule inhibitors of PSD95-nNOS protein-protein interactions as novel analgesics.

dc.contributor.authorLee, Wan-Hung
dc.contributor.authorXu, Zhili
dc.contributor.authorAshpole, Nicole M.
dc.contributor.authorHudmon, Andy
dc.contributor.authorKulkarni, Pushkar M.
dc.contributor.authorThakur, Ganesh A.
dc.contributor.authorLai, Yvonne Y.
dc.contributor.authorHohmann, Andrea G.
dc.contributor.departmentDepartment of Biochemistry and Molecular Biology, IU School of Medicineen_US
dc.date.accessioned2016-12-08T23:30:38Z
dc.date.available2016-12-08T23:30:38Z
dc.date.issued2015-10
dc.description.abstractAberrant increases in NMDA receptor (NMDAR) signaling contributes to central nervous system sensitization and chronic pain by activating neuronal nitric oxide synthase (nNOS) and generating nitric oxide (NO). Because the scaffolding protein postsynaptic density 95kDA (PSD95) tethers nNOS to NMDARs, the PSD95-nNOS complex represents a therapeutic target. Small molecule inhibitors IC87201 (EC5O: 23.94 µM) and ZL006 (EC50: 12.88 µM) directly inhibited binding of purified PSD95 and nNOS proteins in AlphaScreen without altering binding of PSD95 to ErbB4. Bothen_US
dc.eprint.versionAccepted Manuscripten_US
dc.identifier.citationLee, W.-H., Xu, Z., Ashpole, N. M., Hudmon, A., Kulkarni, P. M., Thakur, G. A., … Hohmann, A. G. (2015). Small molecule inhibitors of PSD95-nNOS protein-protein interactions as novel analgesics. Neuropharmacology, 97, 464–475. https://doi.org/10.1016/j.neuropharm.2015.05.038
dc.identifier.issn0028-3908 1873-7064en_US
dc.identifier.urihttps://hdl.handle.net/1805/11575
dc.language.isoen_USen_US
dc.publisherElsevieren_US
dc.relation.isversionof10.1016/j.neuropharm.2015.05.038en_US
dc.relation.journalNeuropharmacologyen_US
dc.rightsPublisher Policyen_US
dc.sourcePMCen_US
dc.subjectAllodyniaen_US
dc.subjectCentral sensitizationen_US
dc.subjectComplete Freund's adjuvanten_US
dc.subjectNMDARen_US
dc.subjectNeuronal nitric oxide synthaseen_US
dc.subjectNeuropathic painen_US
dc.subjectPostsynaptic density 95en_US
dc.subjectmotor ataxiaen_US
dc.subjectpaclitaxelen_US
dc.titleSmall molecule inhibitors of PSD95-nNOS protein-protein interactions as novel analgesics.en_US
dc.typeArticleen_US
Files
Original bundle
Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
nihms699154.pdf
Size:
3.48 MB
Format:
Adobe Portable Document Format