108783-01-3Relevant articles and documents
Recognition and inhibition of HIV integrase by novel dinucleotides
Taktakishvili, Michael,Neamati, Nouri,Pommier, Yves,Pal, Suresh,Nair, Vasu
, p. 5671 - 5677 (2000)
HIV integrase is involved in the integration of viral DNA into chromosomal DNA, a biological process that occurs by a sequence involving HIV DNA splicing and subsequent integration steps. In the quest for small nucleotide systems with nuclease stability of the internucleotide phosphate bond and critical structural features for recognition and inhibition of HIV-1 integrase, we have discovered novel, nuclease-resistant dinucleotides with defined base sequences that are inhibitors of this key viral enzyme. Synthetic methodologies utilized for the syntheses of the novel dinucleotides include an excellent new phosphorylating agent.
Oligo(2′-O-methylribonucleotides) and their derivatives: IV. Conjugates of oligo(2′-O-methylribonucleotides) with minor groove binders and intercalators: Synthesis, properties, and application
Novopashina,Sinyakov,Ryabinin,Perrouault,Giovannangeli,Venyaminova,Boutorine
, p. 138 - 152 (2013/08/23)
Triplex forming 3′-protected pyrimidine oligo(2′-O- methylribonucleotides) containing minor groove binders (MGB) and triplex specific intercalator, benzoindoloquinoline (BIQ), at the 5′-terminus were synthesized. The resulting conjugates formed stable complexes with a target dsDNA due to the simultaneous binding to the minor and major grooves and BIQ intercalation. The dissociation constants and the thermal stability were evaluated for the conjugate complexes with the model dsDNA corresponding to the polypurine tract (PPT) of the nef and pol genes from the HIV proviral genome. The conjugation of oligo(2′-O-methylribonucleotides) with MGB and BIQ was shown to increase the stability of the triple complexes with dsDNA at pH 7.2 and 37 C. Moreover, the intercalator accelerates the process of the complex formation. The dosedependent arrest of the in vitro transcription was demonstrated when a 780-bp DNA fragment containing the polypurine tract was transcribed under the control of T7 promoter in the presence of different concentrations of conjugates of oligo(2′-O-methylribonucleotides) containing MGB and BIQ.
A CHEMICAL 5'-PHOSPHORYLATION OF OLIGODEOXYRIBONUCLEOTIDES THAT CAN BE MONITORED BY TRITYL CATION RELEASE
Horn, Thomas,Urdea, Mickey S.
, p. 4705 - 4708 (2007/10/02)
A new phosphoramidite-derived reagent, (2-cyanoethoxy)-2-(2'-O-4,4'-dimethoxytrityloxyethylsulfonyl)ethoxy-N,N-diisopropylaminophosphine, for the 5'-phosphorylation of oligodeoxyribonucleotides has been developed.Phosphorylation efficiency can be determined by the release of 4,4'-dimethoxytrityl cation in acid.
