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Discovery of Dermorphin-Based Affinity Labels with Subnanomolar Affinity for Mu Opioid Receptors+
dc.contributor.author | Sinha, Bhaswati | |
dc.contributor.author | Cao, Zhengyu | |
dc.contributor.author | Murray, Thomas F. | |
dc.contributor.author | Aldrich, Jane V. | |
dc.date.accessioned | 2017-04-06T16:45:34Z | |
dc.date.available | 2017-04-06T16:45:34Z | |
dc.date.issued | 2009-12-10 | |
dc.identifier.citation | Sinha, B., Cao, Z., Murray, T. F., & Aldrich, J. V. (2009). Discovery of Dermorphin-Based Affinity Labels with Subnanomolar Affinity for Mu Opioid Receptors. Journal of Medicinal Chemistry, 52(23), 7372–7375. http://doi.org/10.1021/jm9007592 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/23589 | |
dc.description.abstract | A series of potent electrophilic affinity labels (IC50 = 0.1-5 nM) containing either a bromoacetamide or isothiocyanate based on the mu opioid receptor (MOR) selective peptide dermorphin were prepared. All four analogs exhibited wash resistant inhibition of [3H]DAMGO binding at subnanomolar to nanomolar concentrations, suggesting that these analogs bind covalently to MOR. To our knowledge these peptides are the highest affinity peptide-based affinity labels for MOR reported to date. | en_US |
dc.publisher | American Chemical Society | en_US |
dc.rights | This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/jm9007592. | en_US |
dc.title | Discovery of Dermorphin-Based Affinity Labels with Subnanomolar Affinity for Mu Opioid Receptors+ | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Sinha, Bhaswati | |
kusw.kuauthor | Aldrich, Jane V. | |
kusw.kudepartment | Medicinal Chemistry | en_US |
dc.identifier.doi | 10.1021/jm9007592 | en_US |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.rights.accessrights | openAccess |