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RKKRRQRRR is a 9-amino acid peptide derived from the HIV-1 Tat protein (trans-activator of transcription). It is widely recognized as a cell-penetrating peptide (CPP) that can translocate across cell membranes and facilitate the intracellular delivery of biomolecules such as nucleic acids, proteins, and nanoparticles.
Upon binding to NRP-1, RPARPAR activates an endocytic pathway that enhances the permeability of blood vessels, allowing for deeper tissue penetration. This mechanism is particularly valuable in targeting tumor vasculature, as it enables the delivery of therapeutic agents directly into tumor tissues.
Functional & Experimental Applications
- Intracellular Delivery: Conjugation to proteins, peptides, DNA, RNA, or small molecules for delivery into mammalian cells.
- Gene Therapy & Nucleic Acid Research: Facilitates transfection and siRNA/shRNA delivery.
- Therapeutic Development: Used in experimental therapeutics to transport drugs or imaging agents into target cells.
- Fluorescent or FAM Conjugates: Modified versions (e.g., FAM-RKKRRQRRR) enable visualization of cellular uptake.
Mechanism of Action: Cell-penetrating via electrostatic interactions with cell surface GAGs, endocytosis, and direct translocation
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