Peptide Information
General Information of This Peptide
| Peptide ID |
PEP01077
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| Peptide Name |
iRGD
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| Sequence |
CRGDKGPDC
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| Peptide Type |
Cyclic
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| PDC Transmembrane Types | Cell-penetrating peptides (CPPs) | |||||
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
diCPTiRGD [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | Tumer volume |
0 mm3
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| Administration Time | 30 days | ||||
| MOA of PDC |
In this context, we developed a drug-bearing supramolecular hydrogel system to intratumourally (i.t.) deliver CDNs against malignant tumours to achieve cancer chemoimmunotherapy. Our strategy was to chemically conjugate the hydrophilic pep-tide moiety iRGD (a tumour-penetrating peptide that can bind to neuropilin-1 (NRP-1) and trigger tumour tissue penetration) to the hydrophobic anticancer drug CPT to form a self-assembling and self-formulating peptide-drug conjugate (diCPT-iRGD). In aqueous solution, the designed drug amphiphile spontaneously assembles into supramolecular nanotubes (NTs). The negatively charged STING agonist (c-di-AMP (CDA)) can condense on the surface of these positively charged NTs through electrostatic complexations. After injection into the tumour site, the CDA-NT solution can immediately form a hydrogel, functioning as a local reservoir for extended localized release of CDA and CPT to awaken both the innate and adaptive immune systems.
Click to Show/Hide
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| Description |
When using the diCPT-iRGD NT hydrogel, the CDA-NT treatment led to substantial tumour regression (Fig. 3c-e) and demonstrated a 100% survival rate in mice (Fig. 3f).
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| In Vivo Model | GL-261 brain cancer C57BL/6 mice. | ||||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | Survival rate |
100.00%
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| Administration Time | 30 days | ||||
| MOA of PDC |
In this context, we developed a drug-bearing supramolecular hydrogel system to intratumourally (i.t.) deliver CDNs against malignant tumours to achieve cancer chemoimmunotherapy. Our strategy was to chemically conjugate the hydrophilic pep-tide moiety iRGD (a tumour-penetrating peptide that can bind to neuropilin-1 (NRP-1) and trigger tumour tissue penetration) to the hydrophobic anticancer drug CPT to form a self-assembling and self-formulating peptide-drug conjugate (diCPT-iRGD). In aqueous solution, the designed drug amphiphile spontaneously assembles into supramolecular nanotubes (NTs). The negatively charged STING agonist (c-di-AMP (CDA)) can condense on the surface of these positively charged NTs through electrostatic complexations. After injection into the tumour site, the CDA-NT solution can immediately form a hydrogel, functioning as a local reservoir for extended localized release of CDA and CPT to awaken both the innate and adaptive immune systems.
Click to Show/Hide
|
||||
| Description |
When using the diCPT-iRGD NT hydrogel, the CDA-NT treatment led to substantial tumour regression (Fig. 3c-e) and demonstrated a 100% survival rate in mice (Fig. 3f).
|
||||
| In Vivo Model | GL-261 brain cancer C57BL/6 mice. | ||||
References