Unknown

Dataset Information

0

Development of an orally-administrable tumor vasculature-targeting therapeutic using annexin A1-binding D-peptides.


ABSTRACT: We previously reported that IF7 peptide, which binds to the annexin A1 (ANXA1) N-terminus, functions as a tumor vasculature-targeted drug delivery vehicle after intravenous injection. To enhance IF7 stability in vivo, we undertook mirror-image peptide phage display using a synthetic D-peptide representing the ANXA1 N-terminus as target. We then identified peptide sequences, synthesized them as D-amino acids, and designated the resulting peptide dTIT7, which we showed bound to the ANXA1 N-terminus. Whole body imaging of mouse brain tumor models injected with near infrared fluorescent IRDye-conjugated dTIT7 showed fluorescent signals in brain and kidney. Furthermore, orally-administered dTIT7/geldanamycin (GA) conjugates suppressed brain tumor growth. Ours is a proof-of-concept experiment showing that ANXA1-binding D-peptide can be developed as an orally-administrable tumor vasculature-targeted therapeutic.

SUBMITTER: Nonaka M 

PROVIDER: S-EPMC7787448 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature

altmetric image

Publications


We previously reported that IF7 peptide, which binds to the annexin A1 (ANXA1) N-terminus, functions as a tumor vasculature-targeted drug delivery vehicle after intravenous injection. To enhance IF7 stability in vivo, we undertook mirror-image peptide phage display using a synthetic D-peptide representing the ANXA1 N-terminus as target. We then identified peptide sequences, synthesized them as D-amino acids, and designated the resulting peptide dTIT7, which we showed bound to the ANXA1 N-terminu  ...[more]

Similar Datasets

| S-EPMC7053157 | biostudies-literature
| S-EPMC8293278 | biostudies-literature
| S-EPMC7809749 | biostudies-literature
| S-EPMC7272081 | biostudies-literature
| S-EPMC8006148 | biostudies-literature
| S-EPMC6001286 | biostudies-literature
| S-EPMC3150874 | biostudies-other
| S-EPMC7724756 | biostudies-literature
| S-EPMC7060371 | biostudies-literature
| S-EPMC7033200 | biostudies-literature