MMP-2-sensitive peptide

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

Batch to batch variation of the purity

• PVGLIG peptide is a remarkable molecule with significant potential in the field of drug delivery and cancer treatment. It is an MMP-2-sensitive peptide that plays a crucial role in the design of novel drug delivery systems.
• This peptide is designed to be combined with cell-penetrating peptides (CPPs), such as SynB3, to form a dual-functional peptide. The combination with SynB3 allows for enhanced permeability across the blood-brain barrier (BBB), making it a promising candidate for treating glioblastomas (GBM) and other brain tumors. PVGLIG serves as a linker between the CPP and the drug, enabling targeted release of the loaded drug at sites with high MMP-2 expression, which is characteristic of GBM cells. It can be conjugated to drugs like paclitaxel (PTX) to create a drug-peptide nanocomplex, such as SynB3-PVGLIG-PTX. This complex exhibits excellent solubility properties and can release the drug upon cleavage by MMP-2. Overall, PVGLIG peptide offers a novel approach to improving the efficacy and specificity of drug delivery in the treatment of brain tumors.

• Hua D, Tang L, Wang W, Tang S, Yu L, Zhou X, Wang Q, Sun C, Shi C, Luo W, Jiang Z, Li H, Yu S. Improved Antiglioblastoma Activity and BBB Permeability by Conjugation of Paclitaxel to a Cell-Penetrative MMP-2-Cleavable Peptide. Adv Sci (Weinh). 2020 Dec 21;8(3):2001960. doi: 10.1002/advs.202001960. PMID: 33552853; PMCID: PMC7856885.

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.