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DSPE-PEG2000-iRGD Peptide Conjugate is based on the cyclic tumor-penetrating peptide iRGD, CRGDKGPDC. iRGD was developed as a tumor-homing peptide capable of combining integrin recognition with a proteolytically activated tissue-penetration mechanism.
iRGD Tumor-Homing Mechanism
The iRGD sequence contains an RGD motif that can bind alpha-v integrins enriched on tumor vasculature and in several tumor-associated cellular compartments. After initial tumor localization, proteolytic processing can expose a C-terminal C-end rule (CendR) motif that interacts with neuropilin-1, promoting tissue and cellular penetration in experimental tumor models.
The two cysteines of CRGDKGPDC form an intramolecular disulfide bond that cyclizes the peptide. Cyclization helps constrain the peptide conformation and is an important feature of the canonical iRGD design.
DSPE-PEG2000 Conjugation
LT8677 incorporates iRGD into a DSPE-PEG2000 conjugate through an added Lys(N3) chemical handle. DSPE is a phospholipid anchor commonly used to insert targeting ligands into liposomes, lipid nanoparticles, micelles, and other lipid-based assemblies. PEG2000 provides a hydrophilic spacer that can project the peptide away from the particle surface.
This architecture is useful for studies in which an iRGD ligand needs to be displayed on a lipid membrane or nanoparticle surface while preserving the cyclic iRGD core.
Potential Research Applications
- Targeted liposome development
- Lipid nanoparticle surface functionalization
- Tumor-homing studies
- Neuropilin-1 pathway research
- Integrin-binding experiments
- Nanoparticle biodistribution studies
- Ligand-density optimization
Published Sequence and Product Configuration
iRGD: CRGDKGPDC, cyclic disulfide between the two cysteines.
LT8677: {DSPE-PEG2000}-Lys(N3)-CRGDKGPDC-NH2
References
Sugahara KN, et al. Tissue-penetrating delivery of compounds and nanoparticles into tumors. Cancer Cell. 2009;16(6):510-520.
Public source / publication
Karmali PP, et al. Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment. Mol Pharm. 2016.
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Research Use Only. Not for human, diagnostic, clinical, or therapeutic use.
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