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Cell penetrating peptides (CPPs), also known as protein transduction domains (PTDs) or membrane transduction peptides (MTPs), are small molecular peptides that consist of 5-30 amino acid residues, which not only penetrate the cell membrane by themselves, but also carry a variety of exogenous substances such as RNA/DNA, peptides, proteins, nucleic acids, PNA, radioisotopes, nanoparticles and even large proteins in a covalent or non-covalent binding manner into cells. CPPs have a wide range of transmembrane targets and can enter a variety of cell types, even through the blood-brain barrier when applied in vivo.
Creative Peptides can provide CPPs from stock or as custom synthesis. Our stock cell penetrating peptides include TAT and Penetratin peptides as standard purified peptides, tagged with a fluorophore or in activated format ready for conjugation.
As an effective bioactive molecular intracellular transport tool, CPPs have broad application prospects in cell biology and cellular immunology, especially in the fields of drug development, gene biotherapy and tumor targeted therapy.
CPPs have been successfully used for the intracellular delivery of different cargos, including protein, siRNA, antisense oligonucleotide, nanoparticles, PNA, liposomes and nucleic acids, both in vitro and in vivo. The most common method is covalent conjugation between the cargo and CPP.
Covalent conjugations by chemical or genetic methods
A. Conjugate CPP with a cargo directly through carboxyl group and amide group reactions
B. Disulfide bonds are added to benefit rapid reductions in the intracellular environment, enabling release of the cargo
C. Other stable covalent linkages that have been employed include thioether, thiolmalmeide, thiazolidine, oxmine and hydrazine linkages
D. Bi-functional cross-linkers such as SMCC
E. Expressed CPP-cargo complex through genetically encoded approach
CPPs play a significantly important role in the delivery of imaging agents, due to their excellent permeability, high affinity, and high stability. Many researchers also devoted to the study of CPPs as imaging agents for diagnosis, obtaining a certain advancement in preclinical and clinical. CPPs can be conjugated to fluorophores, activatable probes, radioisotopes or contrast agents for imaging tissues, such as tumors.
The CPPs can be conjugated to specific bactericidal substances and enter into cells by direct transport or endocytosis, and the specific bactericidal substances play a selective therapeutic effect in the cells.
Every step of peptide synthesis is subject to Creative Peptides' stringent quality control. Typical delivery specifications include:
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