2. Academic Validation
  3. Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin

Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin

  • ACS Med Chem Lett. 2020 Jan 8;11(5):720-726. doi: 10.1021/acsmedchemlett.9b00569.
Azzurra Stefanucci 1,  Marilisa Pia Dimmito 1,  Gabriela Molnar 2,  John M Streicher 2,  Ettore Novellino 3,  Gokhan Zengin 4,  Adriano Mollica 1
Affiliations

Affiliations

  • 1 Dipartimento di Farmacia, Università di Chieti-Pescara "G. d'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy.
  • 2 Department of Pharmacology, College of Medicine, University of Arizona, Tucson, Arizona 85721, United States.
  • 3 Dipartimento di Farmacia, Università di Napoli "Federico II", Via D. Montesano 49, 80131 Naples, Italy.
  • 4 Department of Biology, Science Faculty, Selcuk University, 42250 Konya, Turkey.
PMID: 32435376 DOI: 10.1021/acsmedchemlett.9b00569
Abstract

The 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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