RGD Reference Report - Synthesis, characterization, and preliminary assessment of anti-Flt1 peptide-hyaluronate conjugate for the treatment of corneal neovascularization. - Rat Genome Database

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Synthesis, characterization, and preliminary assessment of anti-Flt1 peptide-hyaluronate conjugate for the treatment of corneal neovascularization.

Authors: Oh, EJ  Park, K  Choi, JS  Joo, CK  Hahn, SK 
Citation: Oh EJ, etal., Biomaterials. 2009 Oct;30(30):6026-34. doi: 10.1016/j.biomaterials.2009.07.024. Epub 2009 Jul 31.
RGD ID: 10402147
Pubmed: (View Article at PubMed) PMID:19647313
DOI: Full-text: DOI:10.1016/j.biomaterials.2009.07.024

Anti-Flt1 peptide of GNQWFI has been reported to inhibit vascular endothelial growth factor receptor 1 (VEGFR1) - mediated endothelial cell migration and tube formation. In this work, a protocol to synthesize anti-Flt1 peptide-hyaluronate (HA) conjugate was successfully developed for the treatment of corneal neovascularization. Using tetrabutyl ammonium salt of HA (HA-TBA), water-insoluble anti-Flt1 peptide could be conjugated with HA in dimethyl sulfoxide (DMSO) by the amide bond formation between carboxyl groups of HA and N-terminal amine groups of GGNQWFI. The formation of anti-Flt1 peptide-HA conjugate was confirmed by (1)H NMR and fluorometric analyses. The average number of grafted peptide molecules in anti-Flt1 peptide-HA conjugates could be controlled from 3 to 30 per single HA chain by changing the feeding amount of peptide for the conjugation reaction. According to in vitro biological activity tests, anti-Flt1 peptide-HA conjugate exhibited a significant inhibition effect on the binding of Flt1-Fc to VEGF(165) coated on the well. Furthermore, in vivo biological activity of anti-Flt1 peptide-HA conjugate was confirmed from the inhibitory effect on corneal neovascularization in silver nitrate cauterized corneas of SD rats. The VEGF receptor 2 expression was also reduced after treatment with anti-Flt1 peptide-HA conjugate. The water-soluble anti-Flt1 peptide-HA conjugate was thought to have a potential to be developed as anti-angiogenic therapeutics for the treatment of corneal neovascularization.

Annotation

Disease Annotations    

Objects Annotated

Genes (Rattus norvegicus)
Flt1  (Fms related receptor tyrosine kinase 1)

Genes (Mus musculus)
Flt1  (FMS-like tyrosine kinase 1)

Genes (Homo sapiens)
FLT1  (fms related receptor tyrosine kinase 1)


Additional Information