Identification of c[D-Trp-Phe-β-Ala-β-Ala], the First κ-Opioid Receptor-Specific Negative Allosteric Modulator.


Journal

ACS pharmacology & translational science
ISSN: 2575-9108
Titre abrégé: ACS Pharmacol Transl Sci
Pays: United States
ID NLM: 101721411

Informations de publication

Date de publication:
11 Oct 2024
Historique:
received: 19 06 2024
revised: 25 08 2024
accepted: 28 08 2024
pmc-release: 11 09 2025
medline: 17 10 2024
pubmed: 17 10 2024
entrez: 17 10 2024
Statut: epublish

Résumé

Recently, the fungus secondary metabolite cyclotetrapetide c[Trp-Phe-D-Pro-Phe] (CJ-15,208) and its derivatives deserved some attention for their unusual structure and distinctive in vitro and in vivo activity. These tryptophan-containing noncationic opioid peptides can be truly regarded as versatile picklocks capable of activating all opioid receptors. Intriguingly, minimal modification of the potent κ-opioid receptor (KOR) agonist c[D-Trp-Phe-Gly-β-Ala] (

Identifiants

pubmed: 39416958
doi: 10.1021/acsptsci.4c00372
pmc: PMC11475277
doi:

Types de publication

Journal Article

Langues

eng

Pagination

3192-3204

Informations de copyright

© 2024 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

Auteurs

Junwei Zhao (J)

Dept. of Chemistry "G. Ciamician", University of Bologna, Campus Navile - Ue4, via Gobetti 83, Bologna 40129, Italy.

Monica Baiula (M)

Department of Pharmacy and Biotechnology, University of Bologna, Bologna 40126, Italy.

Elisabetta Cuna (E)

Department of Pharmacy and Biotechnology, University of Bologna, Bologna 40126, Italy.

Marco Francescato (M)

Dept. of Chemistry "G. Ciamician", University of Bologna, Campus Navile - Ue4, via Gobetti 83, Bologna 40129, Italy.

Joanna Matalińska (J)

Department of Neuropeptides, Mossakowski Medical Research Institute, Polish Academy of Sciences, 5 Pawinskiego Street, Warsaw 02-106, Poland.

Piotr F J Lipiński (PFJ)

Department of Neuropeptides, Mossakowski Medical Research Institute, Polish Academy of Sciences, 5 Pawinskiego Street, Warsaw 02-106, Poland.

Andrea Bedini (A)

Department of Pharmacy and Biotechnology, University of Bologna, Bologna 40126, Italy.

Luca Gentilucci (L)

Dept. of Chemistry "G. Ciamician", University of Bologna, Campus Navile - Ue4, via Gobetti 83, Bologna 40129, Italy.
Health Sciences & Technologies (HST) CIRI, University of Bologna, Ozzano Emilia 40064, Italy.

Classifications MeSH