Table 5.

Aptamers application: in vitro therapeutic experiments and models in vivo.

Virus	Aptamer Name	Type	Target	Aptamer Application Method	Modification Enhancing Biostability	Inhibitory Effect	Kd/IC50	Refs.
Influenza H5N1	A22	DNA	HA	BALB/c mice were intranasally inoculated with the A22 solution	---	>90% decrease in viral loads in mice lungs	n/d	[80]
Influenza H9N2	C7-35M	DNA	HA	MDCK-infected culture cells incubated with aptamer	---	inhibition of viral infection in an aptamer-dose dependent manner (1000 pmole inhibits the viral infection by 55%)	n/d	[81]
Influenza H3N2	HA12-16	RNA	gHA1	MDCK-infected culture cells incubated with aptamer	none	efficient suppression of viral infection of the cells	n/d	[82]
HIV-1	B40, B40t77	RNA	gp120-CCR5	PBMC culture cells incubated with aptamer before infection	2'-fluoro modification	inhibition of viral infectivity (50% at 2 nM)	Kd B40 = 21 ± 2 nM Kd B40t77 = 31 ± 2 nM IC50 = 2 nM	[79]
	B40t77 iii_4		gp120-CCR5	PBMCs and blood monocyte-derived macrophages (BDMs)- infected cultures incubated with aptamer	inverted thymidine at the 3'-end; dimethoxyltrityloxy-(CH2)6-SS-(CH2)6-phospho linker at the 5'-end	inhibition of viral infectivity by 85%	n/d	[83]
	37 NT		HIV-RT	aptamer added to HIV-RT in vitro reaction	three 5'-nt and three loop-nt replaced by phosphothionucleosides	reaction rate decreased (100% by 50 nM of aptamer)	Kd = 0.66 nM IC50 = 2.5 nM	[84]
	DP6-12		Gag protein	293T cells transfected with plasmid encoding aptamer	---	20-fold inhibition of virus production	Kd = 130 ± 9 nM	[85]
	Ch A-1 (anti-gp120 aptamer-siRNA chimera)		gp120 (aptamer) tat/rev (siRNA)	RAG-Hu mice were injected with the chimera solution	2'-fluoro modification	reduction in tat/rev mRNA transcript level in mice T lymphocytes between 75% and 90%	n/d	[86]
	anti-gp120 aptamer- siRNA chmiera		gp120 (aptamer) tat/rev, CD4, transportin-3 (siRNA)	RAG-Hu mice were injected intravenously with chimera solution	2'-fluoro modification	significant decrease in viral loads level; stable level of CD4 T lymphocytes	n/d	[87]
	CD4-AsiCs		CD4 (aptamer) gag/vif CCR5 (siRNA)	NSG-BLT mice were administrated intravaginaly with aptamer	none	protection against HIV vaginal transmission	n/d	[88]
HCV	ODN 27v	DNA	NSB5	Huh7- JHF1 strain infected cells incubated with aptamer; aptamer enter cells without transfection reagent	none	reduction in virus mRNA levels (90% reduction at aptamer concentrations of 5 µM)	Kd = 132.2 ± 20 nM IC50 = 196 ± 16 nM	[74]
	B.2	RNA		aptamer added to HCV-NS5B in vitro reaction	---	inhibition of NS5B polymerase activity	Kd = 1.5 ± 0.2 nM IC50 = 10 ± 0.5 nM;	[89]
	NEO-35-s41 G925-s50		NS3	aptamer added to HCV-NS3 protease cleavage and helicase unwinding in vitro reactions	---	Inhibition of NS3 helicase and protease activity	protease/helicase NEO-35-s41 IC50 = 0.2 µM/20 nM G925-s50 IC50 = 0.2 µM/15 nM	[90]
	NEO-III-14U			HeLa-NS3-expressing cells were transfected with aptamer	---	protease activity inhibited in 60%	Kd = 4 nM	[91]
	AP30		(-)IRES domain I	aptamer preincubated with template and added to NS5B in vitro reaction	---	genetic material replication inhibited by 50%	Kd = 36 nM	[92]
HCMV	L13	RNA	glycoprotein B	virus particles preincubated with aptamer used to infect HFF cells	2'-amino-modified pyrimidines	infectivity reduction	IC50 = 125 ± 20 nM	[93]
	L19		glycoprotein H			100-fold reduction in viral yield blockade of viral entry	IC50 = 35 ± 7 nM
HSV	Aptamer-1	RNA	glycoprotein D	virus particles preincubated with aptamer used to infect VERO cells	2'-fluoro modification	blockade of viral entry	Kd = 109 nM IC50 = 0.8 µM	[75]
HBV	S9	RNA	P protein	HepG2.2.15 cells trasfected with plasmid encoding aptamer	---	reduction of replicative intermediates by about 80%–85%	n/d	[94]
SCV	ES15	RNA	NsP10	aptamer added to SCV helicase unwinding in vitro reaction	---	helicase unwinding activity inhibited in 85%	IC50 = 1.2 nM	[95]
Ebola	1G8-14 2F11-14	RNA	eVP35 IID	n/d	---	inhibition of EBOV polymerase activity and VP36-nucleoprotein interaction	Kd = 30-50 nM	[96]