221554-84-3Relevant academic research and scientific papers
Cyclic PNA-based compound directed against HIV-1 TAR RNA: Modelling, liquid-phase synthesis and TAR binding
Depecker, Geoffrey,Patino, Nadia,Di Giorgio, Christophe,Terreux, Raphael,Cabrol-Bass, Daniel,Bailly, Christian,Aubertin, Anne-Marie,Condom, Roger
, p. 74 - 79 (2007/10/03)
A cyclic molecule including a hexameric PNA sequence has been designed and synthesized in order to target the TAR RNA loop of HIV-1 through the formation of a "kissing complex". For comparison, its linear analogue has also been investigated. The synthesis of the cyclic and linear PNA has been accomplished following a liquid-phase strategy using mixed PNA and fully N-protected (aminoethylglycinamide) fragments. The interactions of this cyclic PNA and its linear analogue with TAR RNA have been studied and the results indicate clearly that no interaction occurs between the cyclic antisense PNA and TAR RNA, whereas a tenuous interaction has been detected with its linear PNA analogue.
Cyclic PNA hexamer-based compound: Modelling, synthesis and inhibition of the HIV-1 RNA dimerization process
Schwergold, Caroline,Depecker, Geoffrey,Giorgio, Christophe Di,Patino, Nadia,Jossinet, Fabrice,Ehresmann, Bernard,Terreux, Raphael,Cabrol-Bass, Daniel,Condom, Roger
, p. 5675 - 5687 (2007/10/03)
A cyclic molecule constituted by (i) a hexameric PNA moiety complementary to six among the nine residues of the dimerization initiation site loop of HIV-1 and (ii) a spacer tethering the N- to the C-extremities of the PNA, has been elaborated to inhibit the dimerization process of HIV-1 genome. This compound has been synthesized following a liquid-phase procedure (fully protected backbone approach). Preliminary agarose gel electrophoresis analyses have shown that the cyclic PNA conjugate is able to inhibit the HIV-1 dimerization.
Liquid-phase combinatorial synthesis of diPNA-arginine conjugates
Leroux, Mary-Lorène,Di Giorgio, Christophe,Patino, Nadia,Condom, Roger
, p. 1641 - 1644 (2007/10/03)
Considering the promising anti HIV activity displayed by some diPNA-arginine conjugates, a library has been generated to determine the target(s) and mode(s) of action of these presumed multi targets drugs and to optimize the antiviral properties of lead compounds. This library has been prepared using a combinatorial liquid-phase strategy, involving easily available N-protected PNA dimeric backbones as building blocks.
Liquid-phase synthesis of polyamide nucleic acids (PNA)
Di Giorgio, Christophe,Pairot, Sandrine,Schwergold, Caroline,Patino, Nadia,Condom, Roger,Farese-Di Giorgio, Audrey,Guedj, Roger
, p. 1937 - 1958 (2007/10/03)
Three liquid-phase processes for the elaboration of short orthogonally protected PNA have been devised. Two of these methods are similar to the convergent and divergent approaches in peptide synthesis. The third process consists in building a fully protected polyamide backbone, by using as many different and orthogonal protecting groups as there are different types of nucleic bases in the targeted polyPNA. Simultaneous and selective cleavage of one kind of protecting group allows the simultaneous attachment of several identical nucleobase units.
