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Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin
journal contribution
posted on 2020-01-10, 14:43 authored by Azzurra Stefanucci, Marilisa Pia Dimmito, Gabriela Molnar, John M. Streicher, Ettore Novellino, Gokhan Zengin, Adriano MollicaThe 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 δ-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.
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bioconjugatecharacterizationδ- opioid receptorprobebindingagentvivoDORmotifanaloguenmnovel opioid peptides fluorescentlydansyl-maleimideapplicationaffinitycompound 1 Dfluorescence emission spectrumsynthesisCyclic Opioid AnaloguesBiphalinimportancecontrol drug releasepotencyimaging1 Dcyclic biphalin derivativesFluorescently Labeled Bioconjugatestoxicity
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