Fluorescence Studies: A9 Peptide, Functionalized with a Fluorogenic Probe, Interacts with Its Receptor Model HER2-DIVMP.


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
12 May 2022
Historique:
received: 17 01 2022
accepted: 04 04 2022
entrez: 19 5 2022
pubmed: 20 5 2022
medline: 20 5 2022
Statut: epublish

Résumé

A recently developed synthetic protocol allowed for the functionalization of the active peptide A9 with a fluorogenic probe, which is useful for studying biomolecular interactions. Essentially, a nucleophilic attack on a halo-substituted benzofurazan is selectively performed by a cysteine sulfhydryl group. The process is assisted by the basic catalysis of activated zeolites (4 Å molecular sieves) and promoted by microwave irradiation. Fluorescence studies revealed that a donor-acceptor pair within the peptide sequence was introduced, thus allowing a deeper investigation on the interaction process between the peptide ligand and its receptor fragment. The obtained results allowed us to come full circle for all the currently understood structural determinants that were found to be involved in the binding process.

Identifiants

pubmed: 35586438
doi: 10.1021/acsmedchemlett.2c00026
pmc: PMC9109265
doi:

Types de publication

Journal Article

Langues

eng

Pagination

807-811

Informations de copyright

© 2022 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Valentina Verdoliva (V)

Institute of Biostructures and Bioimaging, National Research Council, 80134 Naples, Italy.
Institute of Crystallography, National Research Council, 70126 Bari, Italy.

Giuseppe Digilio (G)

Department of Science and Technological Innovation, Università del Piemonte Orientale "A. Avogadro", 15121 Alessandria, Italy.

Ivana Miletto (I)

Department of Science and Technological Innovation, Università del Piemonte Orientale "A. Avogadro", 15121 Alessandria, Italy.

Michele Saviano (M)

Institute of Crystallography, National Research Council, 70126 Bari, Italy.

Stefania De Luca (S)

Institute of Biostructures and Bioimaging, National Research Council, 80134 Naples, Italy.

Classifications MeSH