Annexin A1-Targeted d-Peptide-Monomethyl Auristatin E Conjugate Enhanced Antitumor Effect of Monomethyl Auristatin E for Chemotherapy of Prostate Cancer.

ABSTRACT:

Background

N-terminus 15 amino acid (MC16) of Annexin A1 (ANXA1) is an effective therapeutic target for tumors and tumor vasculature as it specifically localizes to the cell surface of tumor cells and tumor vascular endothelial cells. We identified the d-type peptide (hpnevrs, dhp7) by mirror-image phage display targeting l-type MC16 and tested the hypothesis that intravenously injected c(vcMMAE)dhp7 eradicates prostate tumor in mice with less adverse side effects than that of mc-Val-Cit-PAB-monomethyl auristatin (vcMMAE) alone.

Methods

The binding affinity of dhp7 to MC16 of ANXA1 was analyzed by biolayer interferometry and in silico conformational analysis. c(vcMMAE)dhp7 was synthesized by coupling dhp7 to vcMMAE to evaluate the antitumor effects. A subcutaneous tumor mode

SUBMITTER: Ozaki K 

PROVIDER: S-EPMC12329190 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature