Gersizangitide peptide

• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Batch to batch variation of the purity

Gersizangitide (AXT107) is a 20-amino acid peptide derived from collagen IV, functioning as an angiogenic inhibitor. It exhibits dual activity by inhibiting VEGF-A and VEGF-C while activating the Tie2 receptor. This peptide effectively blocks VEGF receptor signaling, thereby suppressing vascular leakage in ischemic retinopathy and choroidal neovascularization models. Gersizangitide demonstrates potential in inhibiting neovascularization, vascular leakage, and inflammation, offering a promising approach for treating neovascular retinal diseases with a potential dosing interval of once per year.

• Mirando AC, Shen J, Silva RLE, Chu Z, Sass NC, Lorenc VE, Green JJ, Campochiaro PA, Popel AS, Pandey NB. A collagen IV-derived peptide disrupts α5β1 integrin and potentiates Ang2/Tie2 signaling. JCI Insight. 2019 Feb 21;4(4):e122043. doi: 10.1172/jci.insight.122043. PMID: 30668550; PMCID: PMC6478425.

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.