scholarly journals Selection of 2'-Deoxy-2'-Fluoroarabino Nucleic Acid (FANA) Aptamers that Bind HIV-1 Integrase with Picomolar Affinity

Author(s):  
Kevin M. Rose ◽  
Irani Alves Ferreira-Bravo ◽  
Min Li ◽  
Robert Craigie ◽  
Mark A Ditzler ◽  
...  
Keyword(s):  
Hiv 1 ◽  
Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3821
Author(s):  
Rita Meleddu ◽  
Angela Corona ◽  
Simona Distinto ◽  
Filippo Cottiglia ◽  
Serenella Deplano ◽  
...  

Current therapeutic protocols for the treatment of HIV infection consist of the combination of diverse anti-retroviral drugs in order to reduce the selection of resistant mutants and to allow for the use of lower doses of each single agent to reduce toxicity. However, avoiding drugs interactions and patient compliance are issues not fully accomplished so far. Pursuing on our investigation on potential anti HIV multi-target agents we have designed and synthesized a small library of biphenylhydrazo 4-arylthiazoles derivatives and evaluated to investigate the ability of the new derivatives to simultaneously inhibit both associated functions of HIV reverse transcriptase. All compounds were active towards the two functions, although at different concentrations. The substitution pattern on the biphenyl moiety appears relevant to determine the activity. In particular, compound 2-{3-[(2-{4-[4-(hydroxynitroso)phenyl]-1,3-thiazol-2-yl} hydrazin-1-ylidene) methyl]-4-methoxyphenyl} benzamide bromide (EMAC2063) was the most potent towards RNaseH (IC50 = 4.5 mM)- and RDDP (IC50 = 8.0 mM) HIV RT-associated functions.


2009 ◽  
Vol 200 (8) ◽  
pp. 1202-1206 ◽  
Author(s):  
Cédric F. Invernizzi ◽  
Dimitrios Coutsinos ◽  
Maureen Oliveira ◽  
Daniela Moisi ◽  
Bluma G. Brenner ◽  
...  

2017 ◽  
Vol 130 ◽  
pp. 137-145 ◽  
Author(s):  
Maria C. Bewley ◽  
Lisa Reinhart ◽  
Matthew S. Stake ◽  
Shorena Nadaraia-Hoke ◽  
Leslie J. Parent ◽  
...  

2014 ◽  
Vol 41 (1) ◽  
pp. 8-8 ◽  
Author(s):  
Michael Chudy ◽  
Julia Kress ◽  
Jochen Halbauer ◽  
Margarethe Heiden ◽  
Markus B. Funk ◽  
...  

2002 ◽  
Vol 296 (5) ◽  
pp. 1228-1237 ◽  
Author(s):  
Andrew G Stephen ◽  
Karen M Worthy ◽  
Eric Towler ◽  
Judy A Mikovits ◽  
Shizuko Sei ◽  
...  

2011 ◽  
Vol 7 (2) ◽  
pp. e1001273 ◽  
Author(s):  
Guido Ferrari ◽  
Bette Korber ◽  
Nilu Goonetilleke ◽  
Michael K. P. Liu ◽  
Emma L. Turnbull ◽  
...  

Biochemistry ◽  
2018 ◽  
Vol 57 (30) ◽  
pp. 4562-4573 ◽  
Author(s):  
Volodymyr Shvadchak ◽  
Sarwat Zgheib ◽  
Beata Basta ◽  
Nicolas Humbert ◽  
Johannes Langedijk ◽  
...  

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