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cRGD-10R-siRNA
- Development stage
- Preclinical
- Lead developer
- Hamad Bin Khalifa University
- Modality
- Chemically Modified siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Peptides, Conjugated siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous
01
Overview
cRGD-10R-siRNA (specifically cRGD-10R:siLDHC) is a cell-penetrating peptide (CPP)-siRNA nanocomplex designed for the tumor-targeted delivery of small interfering RNA (siRNA) targeting Lactate Dehydrogenase C (LDHC). The nanocomplex consists of a cyclic RGD (cRGD) peptide conjugated to a polyarginine (10R) cell-penetrating peptide, which complexes with the negatively charged LDHC siRNA. The cRGD moiety targets integrin alpha-V/beta-3, which is highly expressed on tumor cells and tumor neovasculature, facilitating receptor-mediated endocytosis and tumor-specific homing. The 10R peptide facilitates cell penetration and endosomal escape. Silencing of LDHC by this nanocomplex suppresses tumor growth, reduces clonogenicity, and enhances sensitivity to DNA damage response-related drugs, such as the PARP inhibitor olaparib, in triple-negative breast cancer (TNBC) models.
- Other names
- cRGD-10R:siLDHCcRGD-10R:siRNAcyclicRGD-10R:siRNA
02
Targets
αVβ3 (Integrin αVβ3)
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