Aptamer-targeted cell-specific RNA interference

Jiehua Zhou; John J Rossi

doi:10.1186/1758-907X-1-4

Silence

Table 1 Cell-internalizing aptamers for targeted delivery.

From: Aptamer-targeted cell-specific RNA interference

Cell-internalizing aptamers	Cargoes and strategy for targeted delivery
RNA aptamers against PSMA	1) siRNA (non-covalently conjugate siRNA with aptamer via a streptavidin connector [49]; aptamer-siRNA chimeras [17, 18] and bivalent aptamer-siRNA conjugates [77]).
	2) Toxin [73] (chemically covalently conjugate toxin with aptamer via SPDP reagent)
	3) Nanoparticles and chemotherapeutic agents [62–70] (cargoes such as dextran, docetaxel, Pt(IV) and doxorubicin were encapsulated into aptamer-coated nanoparticles; aptamer-Dox physical conjugates via intercalation interaction)
RNA aptamers against CD4	siRNA [25] (non-covalently assemble pRNA-siRNA chimera with pRNA-aptamer chimera into dimer or trimer)
RNA aptamers against HIV gp120	siRNA [19, 20] (aptamer-siRNA chimeras; non-covalently conjugate siRNA with aptamer via a 'sticky bridge')
RNA aptamers against TN-C	Radionuclide and fluorescent agents (chemically covalently conjugate ^99mTc or fluorescent agents with aptamers)
DNA aptamers against PTK7	1) Doxorubicin [93] (chemically covalently conjugate Dox with aptamer via an acid-labile linkage)
	2) Viral capsid [94] (chemically covalently conjugate MS2 viral capsid with aptamer via an oxidative coupling reaction)
DNA aptamers against TfR	Enzyme [74] (chemically covalently conjugate a-L-iduronidase with aptamer via an oxidative coupling reaction)
DNA aptamers against NCL	Liposomes and chemotherapeutic agents [71] (cisplatin was encapsulated into liposomes that was non-covalently coated with aptamers)
DNA aptamers against MUC1	Photodynamic therapy agents [72] (chemically covalently conjugate chlorine e6 with aptamer via EDC chemistry)

The RNA or DNA aptamers used as delivery vehicles for various cargoes via different strategies are listed in the table.
EDC, (1-ethyl-3-[3-dimethylaminopropyl]carbodiimide hydrochloride); gp120, glycoprotein 120 (envelope protein); MUC1, mucin protein (membrane-associated glycoprotein); NCL, nucleolin (a bcl-2 mRNA binding protein); pRNA, phage RNA; PSMA, prostate-specific membrane antigen; PTK7, protein tyrosine kinase 7 (a transmembrane receptor); siRNA, small interfering RNA; SPDP, N-[O-succinimdy]-3-(2-pyridyldithio) propionate; TfR, Transferrin receptor (in mouse); TN-C, tenasin-C (a hexameric glycoprotein).

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