Interleukin-4 Receptor Targeting Peptide AP

Interleukin-4 Receptor Targeting Peptide AP

• COA/MS/HPLC Report
• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Batch to batch variation of the purity

H-CRKRLDRNC-OH

H-Cys-Arg-Lys-Arg-Leu-Asp-Arg-Asn-Cys-OH

9

95.2%

C₄₄H₈₂N₂₀O₁₃S₂

1163.37

Synthetic

Powder

Atherosclerotic plaque (AP) homing nonapeptide (CRKRLDRNC) was identified after cycles of ex vivo phage display screening on human atheroma tissue and further validated for homing to the atherosclerotic plaques in an in vivo murine model. A homology sequence search identified the AP binding sequence KRLDRN motif corresponding to the Interleukin-4 (IL-4) . Its receptor, IL-4R, is abundantly expressed by glioma cells thereby presenting the CRKRLDRNC as a promising tool for glioma targeting. Park et al. showed promising results with the AP peptide conjugated to doxorubicin containing microbubbles and nanoliposomes as a proof-of-concept for glioma targeted imaging and therapy using the U87MG in vitro models. AP peptide conjugated to doxorubicin containing liposomes showed also enhanced antitumor activity in in vivo model of human lung cancer.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual:Handling and Storage of Synthetic Peptides

• Hong HY, Lee HY, Kwak W, Yoo J, Na MH, So IS, et al. Phage display selection of peptides that home to atherosclerotic plaques: IL-4 receptor as a candidate target in atherosclerosis. J Cell Mol Med. 2008;12(5B):2003-14

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.