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Модификация SELEX/Aptamer

Nucleotides by Application  /  ... in Drug Discovery - SELEX/Aptamer Modification

Aptamers are short single-stranded DNA or RNA oligonucleotides (< 100 nt). They gained increasing importance in drug discovery due to their inherent ability to form defined three-dimensional structures that enables them to bind to various targets (e.g. proteins) with antibody-antigen-like affinity and specificity[1].

Aptamers with the highest binding affinity and specificity against a given target molecule are generated by an multi-step in vitro selection and enzymatic amplification process called "systematic evolution of ligands by exponential enrichment (SELEX) (for detailed information please refer to the references below[2,3]).

The main advantages of aptamers compared to antibodies are heat stability, the lack of immunogenicity and minimal interbatch variability. Their usage in diagnostics however, is often hampered by nuclease-mediated degradation.

Enzymatic incorporation of fluoro-, amino- or O-methyl- 2'-ribose-modified nucleotides (1) by generating an initially modified combinatorial library or (2) post-SELEX markedly improve the nuclease resistance of aptamers (Tab. 1) [3-12]. Furthermore, a number of modified nucleotides suitable for the selection of cross-linking capable aptamers (Photo-SELEX) are available as well (Tab. 1)[13-15].
 


Table 1: SELEX-compatible modified nucleotides.

n/a: not applicable


NucleotideModificationDNA aptamer selection
(DNA SELEX)
RNA aptamer selection
(RNA SELEX)
ribose moiety2'F-dUTPSubstitution of 2'-OH by fluor (F)[5][6,7]
2'F-dCTP[5][6,7]
2'F-dATP[5][6]
2'F-dGTP[5]
2'OMe-UTPModification of 2'-OH by a methyl group (CH3)
[8,9,10,11]
2'OMe-CTP
[8,9,11]
2'OMe-ATP
[8]
2'OMe-GTP
[8]
2'NH2-dUTPSubstitution of 2'-OH by an amino group (NH2)
[6,12]
2'NH2-dCTP
[12]
2'NH2-dATP

2'NH2-dGTP

base moiety5Br-dUTPModification of C-5 by Bromine (Br)[13]n/a
5I-UTPModification of C-5 by Iodine (I)n/a[14]
4-Thio-UTPSubstitution of 4-O by Sulfur (S)n/a[15]
 


 
 

Datasheet
НазваниеКодЦена Количество
L pack NU-151L 48113.47 руб. 5 x 50 µl
(100 mM)
S pack NU-151S 12437.18 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-1214L 48113.47 руб. 5 x 50 µl
(100 mM)
S pack NU-1214S 12437.18 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-1216L 48113.47 руб. 5 x 50 µl
(100 mM)
S pack NU-1216S 12437.18 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
4 x 5 µmol pack NU-10405-20 46827.22 руб. 4 x 5 µmol
(4 x 50 µl 100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-1215L 48113.47 руб. 5 x 50 µl
(100 mM)
S pack NU-1215S 12437.18 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-244L 41417.25 руб. 5 x 50 µl
(100 mM)
S pack NU-244S 12133.63 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-243L 41417.25 руб. 5 x 50 µl
(100 mM)
S pack NU-243S 12133.63 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-245L 41417.25 руб. 5 x 50 µl
(100 mM)
S pack NU-245S 12133.63 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-242L 41417.25 руб. 5 x 50 µl
(100 mM)
S pack NU-242S 12133.63 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-1184L 46939.55 руб. 5 x 50 µl
(100 mM)
S pack NU-1184S 12133.63 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-1211L 46939.55 руб. 5 x 50 µl
(100 mM)
S pack NU-1211S 12133.63 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-1127L 46939.55 руб. 5 x 50 µl
(100 mM)
S pack NU-1127S 12133.63 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-1212L 46939.55 руб. 5 x 50 µl
(100 mM)
S pack NU-1212S 12133.63 руб. 50 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-1156L 46731.18 руб. 5 x 10 µl
(100 mM)
S pack NU-1156S 10706.75 руб. 10 µl
(100 mM)



Datasheet
НазваниеКодЦена Количество
L pack NU-122L 47899.09 руб. 5 x 50 Units
S pack NU-122S 16352.53 руб. 50 Units



Datasheet
НазваниеКодЦена Количество
L pack NU-119L 40036.68 руб. 5 x 50 Units
S pack NU-119S 9850.1 руб. 50 Units




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