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Does Cysteine Rule (CysR) Complete the CendR Principle? Increase in Affinity of Peptide Ligands for NRP-1 Through the Presence of N-Terminal Cysteine

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cris.lastimport.scopus2024-02-12T19:43:02Z
dc.abstract.enThe structure-activity relationship of branched H-Lys(hArg)-Dab-Dhp-Arg-OH sequence analogues, modified with Cys-Asp or Cys at N-terminal amino acids (Lys, hArg), in VEGF-A165/Neuropilin-1 complex inhibition is presented. The addition of Cys residue led to a 100-fold decrease in the IC50 value, compared to the parent peptide. The change occurred regardless of coupling Cys to the free N-terminal amino group present in the main or the side chain. A few analogues extended by the attachment of Cys at the N-terminus of several potent NRP-1 peptide ligands documented in the literature are also presented. In all studied cases, the enhancement of inhibitory properties after the addition of Cys at the N-terminus is observed. It is particularly evident for the tetrapeptide derived from the C-terminus of VEGF-A165 (KPRR), suggesting that extending the K/RXXK/R motif (CendR) with the Cys moiety can significantly improve affinity to NRP-1 of CendR peptides.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorPuszko, Anna
dc.contributor.authorMisicka-Kęsik, Aleksandra
dc.contributor.authorRaynaud, Françoise
dc.contributor.authorSosnowski, Piotr
dc.contributor.authorLepelletier, Yves
dc.contributor.authorHermine, Olivier
dc.contributor.authorHopfgartner, Gérard
dc.date.accessioned2024-01-24T22:11:49Z
dc.date.available2024-01-24T22:11:49Z
dc.date.copyright2020-03-13
dc.date.issued2020
dc.description.accesstimeAT_PUBLICATION
dc.description.financeŚrodki finansowe przyznane na realizację projektu w zakresie badań naukowych lub prac rozwojowych
dc.description.number3
dc.description.versionFINAL_PUBLISHED
dc.description.volume10
dc.identifier.doi10.3390/BIOM10030448
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/105153
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofBiomolecules
dc.relation.pagesart.no. 448
dc.rightsCC-BY
dc.sciencecloudnosend
dc.subject.enNeuropilin-1
dc.subject.enVEGF-A165
dc.subject.enVEGF-A165/NRP-1 complex
dc.subject.enprotein-ligand interaction
dc.subject.enpeptide ligands
dc.titleDoes Cysteine Rule (CysR) Complete the CendR Principle? Increase in Affinity of Peptide Ligands for NRP-1 Through the Presence of N-Terminal Cysteine
dc.typeJournalArticle
dspace.entity.typePublication