Macrocyclic RGD-peptides with high selectivity for α_vβ₃ integrin in cancer imaging and therapy.

ABSTRACT: Integrins, particularly the α_vβ₃ subtype, are critical receptors involved in cell adhesion, migration, and signaling, playing a significant role in tumor progression and metastasis. Despite extensive research into integrin-targeted therapies, challenges remain in developing ligands that exhibit high selectivity for α_vβ₃ over other integrin subtypes, such as α_vβ₅. This study employs a one-pot sortase A-mediated on-resin peptide cleavage and in situ cyclization method to synthesize two generations of macrocyclic RGD-peptide libraries. Systematic screening through surface plasmon resonance and cell-based competition assays identified the lead compound, c-(G5RGDKcLPET), which demonstrated high affinity and selectivity for

SUBMITTER: Cheng X 

PROVIDER: S-EPMC12070224 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature