Article
Structural studies and biological evaluation of T30695 variants modified with single chiral glycerol-T reveal the importance of LEDGF/p75 for the aptamer anti-HIV-integrase activities.
Biochimica et biophysica acta. General subjects - 1 Feb 2019
Rivieccio Elisa, Tartaglione Luciana, Esposito Veronica, Dell'Aversano Carmela, Koneru P C, Scuotto Maria, Virgilio Antonella, Mayol Luciano, Kvaratskhelia Mamuka, Varra Michela
Abstract excerpt
Some G-quadruplex (GQ) forming aptamers, such as T30695, exhibit particularly promising properties among the potential anti-HIV drugs. T30695 G-quadruplex binds to HIV-1 integrase (IN) and inhibits its activity during 3'-end processing at nanomolar concentrations. Herein we report a study concerning six T30695-GQ variants, in which the R or S chiral glycerol T, singly replaced the thymine residues at the...
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