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Scandium-44 Radiolabeled Peptide and Peptidomimetic Conjugates Targeting Neuropilin-1 Co-Receptor as Potential Tools for Cancer Diagnosis and Anti-Angiogenic Therapy

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cris.lastimport.scopus2024-02-12T19:39:37Z
dc.abstract.enPathological angiogenesis, resulting from an imbalance between anti- and pro-angiogenic factors, plays a pivotal role in tumor growth, development and metastasis. The inhibition of the angiogenesis process by the VEGF/VEGFR-2/NRP-1 pathway raises interest in the search for such interaction inhibitors for the purpose of the early diagnosis and treatment of angiogenesis-dependent diseases. In this work we designed and tested peptide-based radiocompounds that selectively bind to the neuropilin-1 co-receptor and prevent the formation of the pro-angiogenic VEGF-A165/NRP-1 complex. Three biomolecules, A7R and retro-inverso DR7A peptides, and the branched peptidomimetic Lys(hArg)-Dab-Pro-Arg (K4R), conjugated with macrocyclic chelator through two linkers’ types, were labeled with theranostic scandium-44 radionuclide, and studied in vitro as potential targeted radiopharmaceuticals. ELISA (enzyme-linked immunosorbent assay) studies showed no negative effect of the introduced biomolecules’ changes and high NRP-1 affinity in the case of A7R- and K4R-radiocompounds and a lack affinity for DR7A-radiocompounds. All radiopeptides showed a hydrophilic nature as well as high stability against ligand exchange reactions in cysteine/histidine solutions. Unfortunately, all radiocompounds showed unsatisfactory nano-scale stability in human serum, especially for use as therapeutic radioagents. Further work is ongoing and focused on the search for angiogenesis inhibitors that are more human serum stable.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorGniazdowska, Ewa
dc.contributor.authorMisicka-Kęsik, Aleksandra
dc.contributor.authorChoiński, Jarosław
dc.contributor.authorWalczak, Rafał
dc.contributor.authorTymecka, Dagmara
dc.contributor.authorWitkowska, Ewa
dc.contributor.authorHalik, Paweł Krzysztof
dc.contributor.authorRedkiewicz, Patrycja
dc.contributor.authorMasłowska, Katarzyna
dc.date.accessioned2024-01-25T19:43:40Z
dc.date.available2024-01-25T19:43:40Z
dc.date.copyright2023-02-15
dc.date.issued2023
dc.description.accesstimeAT_PUBLICATION
dc.description.financePublikacja bezkosztowa
dc.description.number2
dc.description.versionFINAL_PUBLISHED
dc.description.volume11
dc.identifier.doi10.3390/BIOMEDICINES11020564
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/119050
dc.identifier.weblinkhttps://www.mdpi.com/2227-9059/11/2/564/pdf
dc.languageeng
dc.pbn.affiliationphysical sciences
dc.relation.ispartofBiomedicines
dc.relation.pages564
dc.rightsCC-BY
dc.sciencecloudnosend
dc.subject.enangiogenesis
dc.subject.entheranostic 43,44,47Sc-radiopharmaceuticals
dc.subject.enanti-angiogenic therapy
dc.subject.enneuropilin-1
dc.subject.enVEGF-A165/NRP-1 complex inhibitor
dc.subject.enangiogenic factors
dc.subject.enA7R peptide
dc.subject.enretro-inverso isomer DR7A
dc.subject.enpeptidomimetics
dc.titleScandium-44 Radiolabeled Peptide and Peptidomimetic Conjugates Targeting Neuropilin-1 Co-Receptor as Potential Tools for Cancer Diagnosis and Anti-Angiogenic Therapy
dc.typeJournalArticle
dspace.entity.typePublication