Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin

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dc.contributor.authorStefanucci, A.
dc.contributor.authorDimmito, M. P.
dc.contributor.authorMolnar, G.
dc.contributor.authorStreicher, J. M.
dc.contributor.authorNovellino, E.
dc.contributor.authorZengin, Gökhan
dc.contributor.authorMollica, A.
dc.date.accessioned2020-03-26T20:20:46Z
dc.date.available2020-03-26T20:20:46Z
dc.date.issued2020
dc.departmentSelçuk Üniversitesien_US
dc.description.abstractThe development of bioconjugates is of pivotal importance in medicinal chemistry due to their potential applications as therapeutic agents to improve the targeting of specific diseases, decrease toxicity, or control drug release. In this work we achieved the synthesis and characterization of three novel opioid peptides fluorescently labeled, analogues of cyclic biphalin derivatives, namely 1D, 1C, and 2C. Among them, compound 1D, containing a dansyl-maleimide motif, exhibited an excellent binding affinity and functional potency for the ?-opioid receptor (DOR). 1D also demonstrated a strong fluorescence emission spectrum ranging from 300 to 700 nm. These features could be highly desirable for medical and biological applications needed for targeting the DOR, including in vivo imaging, and as a lead for the design of fluorescent probes. © 2020 American Chemical Society.en_US
dc.description.sponsorshipUniversity of Arizonaen_US
dc.description.sponsorshipThis study was funded in part by institutional funds from the University of Arizona to JMS.en_US
dc.identifier.doi10.1021/acsmedchemlett.9b00569en_US
dc.identifier.issn1948-5875en_US
dc.identifier.pmid32435376en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://dx.doi.org/10.1021/acsmedchemlett.9b00569
dc.identifier.urihttps://hdl.handle.net/20.500.12395/38663
dc.identifier.wosWOS:000535281200018en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherAmerican Chemical Societyen_US
dc.relation.ispartofACS Medicinal Chemistry Lettersen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.selcuk20240510_oaigen_US
dc.subjectbioconjugatesen_US
dc.subjectBiphalinen_US
dc.subjectfluorescent probesen_US
dc.subjectGPCRsen_US
dc.subjectopioidsen_US
dc.titleDeveloping Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalinen_US
dc.typeArticleen_US

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