Journal
BIOCONJUGATE CHEMISTRY
Volume 30, Issue 9, Pages 2444-2451Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.9b00519
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Funding
- Italian Ministry of Research and Education [2015WX8Y5B_002]
- grant FAR 2018 (Fondo di Ateneo per la Ricerca Scientifica) from the University of Ferrara
- grant FFABR 2017 (Finanziamento delle attivita base di ricerca) from the University of Ferrara
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The general aim of the work was the validation of a new synthetic methodology designed for obtaining bifunctional heterotetrabranched peptide ligands. Applying an easily accessible synthetic route, we provided a small series of hetero-multimeric peptide conjugates targeting the nociceptin/orphanin FQ (N/OFQ) peptide receptors (NOP) and mu opioid receptors. Among these, H-PWT1-N/OFQ[Dmt(1)]dermorphin demonstrated a similar and high agonist potency at the NOP and mu receptors. The achieved results confirmed the robustness of the approach that is extremely versatile and virtually applicable to different peptide sequences whose pharmacological activity can be combined for generating dual acting multimeric compounds. These innovative pharmacological tools will be extremely helpful for investigating the consequences of the simultaneous activation and/or blockage of different peptidergic receptors.
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