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Synthesis, Radiolabeling, and In Vitro and In Vivo Characterization of Heterobivalent Peptidic Agents for Bispecific EGFR and Integrin αvβ3 Targeting.


ABSTRACT: Radiolabeled heterobivalent peptidic ligands (HBPLs) are a highly promising compound class for the sensitive and specific visualization of tumors as they often exhibit superior properties compared to their monospecific counterparts and are able to concomitantly or complementarily address different receptor types. The combination of two receptor-specific agents targeting the epidermal growth factor receptor (EGFR) and the integrin αvβ3 in one HBPL would constitute a synergistic combination of binding motifs as these two receptor types are concurrently overexpressed on several human tumor types and are closely associated with disease progression and metastasis. Here, we designed and synthesized two heterobivalent radioligands consisting of the EGFR-specific peptide GE11

SUBMITTER: Braun D 

PROVIDER: S-EPMC9850772 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature