PEGylated RGD Peptide

What is PEGylated RGD Peptide?

PEGylated RGD peptide can change the nature and function of RGD peptide by combining polyethylene glycol and RGD. PEGylated RGD peptide has various characteristics, such as high stability, good solubility, strong targeting, and modulation of drug release. Therefore, it can be applied in the fields of drug delivery, tissue engineering, and biomaterials, etc. BOC Sciences, as a supplier of PEG copolymer materials and PEG services, not only provides customers with PEG preparation and modification services, but also provides customers with a wide range of types of PEGylated RGD peptide products. These products include modifications of various groups, such as amino, azide, MAL and NHS groups.

Fig. 1. Application of DSPE-PEG-cRGD in cancer cell transmission (Drug Delivery. 2021, 28(1): 995-1006).

Characterization of RGD Peptides

• Affinity - RGD peptides have a high degree of affinity, allowing them to selectively interact with integrin receptors on a cellular basis.
• Cell adhesion and recognition - RGD peptides can act as adhesion sites to mediate adhesion between cells and the matrix, and this adhesion can facilitate cellular localization, migration, and signaling.
• Targeting - The targeting of RGD peptides selectively recognizes and localizes cells overexpressing integrin receptors.
• Low immunogenicity - RGD peptides reduce recognition and rejection by the immune system and greatly increase stability and biological activity through binding to PEG.

Examples of PEGylated RGD Peptides

cRGD-PEG-DSPE

The cRGD-PEG-DSPE chain consists of a cRGD cyclic peptide and DSPE phospholipids at both ends. It is an active target substance and can be used as an antitumor drug carrier and an active target substance. cRGD peptide applications include inhibition of apoptosis, angiogenesis, and tumorigenesis. PEGylated RGD can be crosslinked to other molecules via reactive terminal groups on PEG and is used in a variety of biomedical studies.

RGD-PEG-N3

The RGD-PEG-N3 molecular chain has an RGD peptide and an azide moiety at each end. PEGylated RGDs can be crosslinked to azides via a reactive end group on PEG and can be used to modify proteins, peptides, and other materials via click chemistry. PEGylated RGDs can be crosslinked to other molecules via a reactive end group on PEG and are used in a variety of biomedical research applications.

RGD-PEG-SH

RGD-PEG-SH is one of the commonly used biodegradable copolymers of functional polymers and peptide amino acids. RGD-PEG-SH is soluble in certain organic solvents such as CH₂Cl₂ and CH₃Cl. It can be linked to antibodies and small molecules of drugs with COOH groups. RGD-PEG-SH has a wide range of applications for passive targeting of micelles and vesicles, RGD-PEG-SH can be used in a wide range of applications, such as passive and active targeting studies of micelles and vesicles, as well as the study of active compounds in cell culture, peptide synthesis support, grafted polymers, new materials, and PEG modified functional coatings.

How to Prepare PEGylated RGD Peptide in Bulk?

BOC Sciences offers capabilities and programs for batch preparation of PEGylated RGD peptide. The main steps are the following: First, a peptide chain with an RGD peptide sequence needs to be designed and synthesized. Second, the resulting RGD peptide is reacted with PEG. The activating reagent used is an active ester compound, such as N-hydroxysuccinimide. Then, the obtained RGD peptide-PEG conjugate was purified and separated to remove excess impurities of by-products. Finally, the pure product obtained was analyzed and validated to ensure the purity and quality of the batch product.

Precautions for PEGylated RGD Peptide

• Purity and quality control of peptide. During the use of the product, it is necessary to ensure that the purity and quality of the peptide meet the requirements, and any impurities or denaturation may affect the effect and stability of PEGylation.
• Biological activity verification. Prior to the use of the product, it is necessary to validate its biological activity to ensure that the conjugate binds to the target cell or receptor, and to evaluate its biological activity.

Reference

1. Yang, S. et al. cRGD peptide-conjugated polyethylenimine-based lipid nanoparticle for intracellular delivery of siRNA in hepatocarcinoma therapy. Drug Delivery. 2021, 28(1): 995-1006.