NRP-1 binding inhibitory peptides and uses thereof

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NRP-1 binding inhibitory peptides and uses thereof

Grant US12590122B2 Kind: B2 Mar 31, 2026

Assignee

INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE)

Inventors

Yves Lepelletier, Françoise Raynaud, Aleksandra Misicka-Kesik, Anna Katarzyna Puszko, Olivier Hermine

Abstract

A number of anti-angiogenic strategies connected with the VEGF signalling pathway are used in current clinical treatment or trial phase, but they either cause adverse effects or are not specific. Various strategies were aimed at identifying peptides inhibiting the VEGF-A165/NRP-1 interaction. A well-known antiangiogenic peptide is the heptapeptide termed “A7R” having the amino acid sequence ATWLPPR, for which various derivatives have been synthesized, which include peptides having the general sequence Lys(hArg)-AA2-AA3-Arg. However, the ability of the known peptides to inhibit the VEGF-A165/NRP-1 interaction was too low for their use as candidate drugs for inhibiting angiogenesis in subjects in need thereof. The present inventors have now conceived a family of novel peptide-like compounds having a nanomolar affinity for NRP-1, which are thus endowed with a powerful capacity to inhibit the VEGF-A165/NRP-1 interaction. These novel peptide-like compounds may be relevantly used as antiangiogenic compounds, especially in subjects affected with cancer.

CPC Classifications

C07K 5/1019 C07K 5/0215 C07K 7/02 C07K 7/06 A61K 38/00

Filing Date

2020-06-10

Application No.

17618233

Claims

15

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