Challenges and Opportunities for Small Molecule Aptamer Development

Table 3

A listing of RNA aptamers reported in the open literature* (up until July 2012) that have been confirmed to bind to small molecule targets. The dissociation constant (𝐾_𝑑), a measure of binding affinity, is included as well as the year of aptamer development.

Target	Binding affinity (𝐾𝑑)	Year	Reference
Organic dyes	100–600 μM	1990	[158]
D-tryptophan	18 μM	1992	[46]
L-valine	2.9 mM	1994	[159]
Theophylline	100 nM	1994	[44]
Cyanocobalamin	88 nM	1994	[160]
L-citrulline	62–68 μM	1994	[47]
Flavin mononucleotide	0.5 μM	1994	[161]
Flavin adenine dinucleotide	137–273 μM	1994	[161]
Kanamycin A	≤300 nM	1995	[162]
Neomycin	100 nM	1995	[163]
Tobramycin	2–3 nM	1995	[164]
Lividomycin	≤300 nM	1995	[162]
Nicotinamide adenine dinucleotide	2.5 μM	1995	[165]
Riboflavin	1–5 μM	1995	[165]
Biotin	5 μM	1995	[166]
L-arginine	330 nM	1996	[48]
Dopamine	2.8 μM	1997	[167]
7-methyl-guanosine	5 μM	1997	[168]
CCdApPuro	10 nM	1997	[169]
Chloramphenicol	25–65 μM	1997	[170]
Viomycin	11–21 μM	1997	[171]
Sulforhodamine B	310 nM	1998	[172]
Streptomycin	1–10 μM	1998	[173]
L-isoleucine	200–500 μM	1998	[174]
7,8-dihydro-8-hydroxy-2′-deoxyguanosine (8-oxodG)	0.27–2.8 μM	1998	[134]
Xanthine	3.3 μM	1998	[175]
Guanine	1.3 μM	1998	[175]
Malachite green	≤1 μM	1999	[176]
Phosphatidylcholine	≥100 μM	1999	[177]
Cyclic adenosine monophosphate	10 μM	2000	[178]
Adenosine triphosphate	127–223 μM	2000	[179]
L-tyrosine	35 μM	2000	[180]
S-adenosyl homocysteine	0.2–0.8 μM	2000	[181]
Neomycin	1.8 μM	2000	[182]
Moenomycin A	300–400 nM	2001	[183]
Sialyl Lewis X	0.085–10 nM	2001	[184]
Tetracycline	1 μM	2001	[185]
Kanamycin B	180 nM	2001	[186]
Adenine	10 μM	2002	[187]
Flavin adenine dinucleotide	50 μM	2002	[188]
L-isoleucine	1–7 mM	2003	[189]
Adenosine triphosphate	2 μM	2003	[190]
Morpholine-based GTP analog	20, 33 μM	2003	[191]
4,4′-methylenedianiline	0.45–15 μM	2004	[192]
Tobramycin	30–100 nM	2004	[34]
Kanamycin	10–30 nM	2004	[34]
Adenosine triphosphate	5 μM	2004	[193]
Isoleucine	0.9 mM	2005	[194]
L-histidine	8–54 μM	2005	[195]
Codeine	2.5–4 μM	2006	[33]
Mesomesoprotoporphyrin IX	188–445 nM	2006	[87]
Thyroxine	50 μM	2007	[196]
Tobramycin	16 μM	2007	[197]
10-carboxy-2,7-di-t-butyl-trans-12c,12d-dimethyl-12c,12d-dihydrobenzo[e]pyrene	2.7 μM	2007	[198]
Dimethylindole red	87 nM	2008	[199]
Cyanine 3 dye	60 μM	2010	[200]
Aniline-substituted sulforhodamine analogue	3.5 μM	2010	[201]
Atrazine	2 μM	2010	[202]
Sphingosylphosphorylcholine	20–250 nM	2010	[203]
Black hole quencher	4.7 μM	2011	[204]
4-dimethylaminobenzylidene imidazolinone	464 nM	2011	[205]
Glutathione	41.8, 48.9 nM	2011	[206]
Heteroaryldihydropyrimidine	50 nM	2011	[207]

∗Only aptamer sequences that have experimentally determined 𝐾_𝑑 values were included in this table.