Optimization of the binding properties of PNA-(5')-DNA chimerae.
Bioorg Med Chem Lett
; 8(6): 663-8, 1998 Mar 17.
Article
en En
| MEDLINE
| ID: mdl-9871579
ABSTRACT
The synthesis and evaluation of PNA-(5')-DNA chimerae containing either a 5'-amide (i.e. 1a), a 5'-phosphodiester (i.e. 1b) or 5'-phosphonate linkages (i.e. 1c,d) at the junction site are described. The 5'-linkages could be installed using either 5'-amino-5'-deoxythymidine phosphoramidite 2, O-[2-(2-aminoethyl)-(thymin-1-ylacetyl)amino]ethyl phosphoramidite 3, N-(2-aminoethyl)-N-(thymin-1-ylacetyl)aminomethyl phosphonate 4 or N-(2-aminoethyl)-N-(allyloxycarbonyl)aminomethyl phosphonate 5 as building blocks, respectively. It is shown that PNA-(5')-DNA of type 1a-c have a higher binding affinity with complementary RNA than native DNA, and that the antisense activity is mainly due to RNase H.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
ADN
/
Ácidos Nucleicos de Péptidos
/
Ácidos Nucleicos Heterodúplex
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
1998
Tipo del documento:
Article
País de afiliación:
Países Bajos