Synthesis and Biological Properties of Novel Pyridinioalkanoyl Thiolesters (PATE) as Anti-HIV-1 Agents That Target the Viral Nucleocapsid Protein Zinc Fingers

1999 ◽  
Vol 42 (1) ◽  
pp. 67-86 ◽  
Author(s):  
Jim A. Turpin ◽  
Yongsheng Song ◽  
John K. Inman ◽  
Mingjun Huang ◽  
Anders Wallqvist ◽  
...  
2008 ◽  
Vol 8 (1) ◽  
pp. 24-35 ◽  
Author(s):  
Yves Mely ◽  
Hugues Rocquigny ◽  
Volodymyr Shvadchak ◽  
Sergiy Avilov ◽  
Chang Dong ◽  
...  

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

ChemInform ◽  
2010 ◽  
Vol 31 (14) ◽  
pp. no-no
Author(s):  
Hitoshi Takeuchi ◽  
Naoki Asai ◽  
Kazunori Tanabe ◽  
Teruya Kozaki ◽  
Masanori Fujita ◽  
...  

1999 ◽  
Vol 52 (11) ◽  
pp. 971-982 ◽  
Author(s):  
HITOSHI TAKEUCHI ◽  
NAOKI ASAI ◽  
KAZUNORI TANABE ◽  
TERUYA KOZAKI ◽  
MASANORI FUJITA ◽  
...  

2014 ◽  
Vol 58 (6) ◽  
pp. 3043-3052 ◽  
Author(s):  
Marika Tiberi ◽  
Cristina Tintori ◽  
Elisa Rita Ceresola ◽  
Roberta Fazi ◽  
Claudio Zamperini ◽  
...  

ABSTRACTWe report here the synthesis of 2-aminothiazolones along with their biological properties as novel anti-HIV agents. Such compounds have proven to act through the inhibition of the gp120-CD4 protein-protein interaction that occurs at the very early stage of the HIV-1 entry process. No cytotoxicity was found for these compounds, and broad antiviral activities against laboratory strains and pseudotyped viruses were documented. Docking simulations have also been applied to predict the mechanism, at the molecular level, by which the inhibitors were able to interact within the Phe43 cavity of HIV-1 gp120. Furthermore, a preliminary absorption, distribution, metabolism, and excretion (ADME) evaluation was performed. Overall, this study led the basis for the development of more potent HIV entry inhibitors.


Biochemistry ◽  
1990 ◽  
Vol 29 (34) ◽  
pp. 7786-7789 ◽  
Author(s):  
Terri L. South ◽  
Paul R. Blake ◽  
Raymond C. Sowder ◽  
Larry O. Arthur ◽  
Louis E. Henderson ◽  
...  

PLoS ONE ◽  
2014 ◽  
Vol 9 (7) ◽  
pp. e102150 ◽  
Author(s):  
Loussiné Zargarian ◽  
Carine Tisné ◽  
Pierre Barraud ◽  
Xiaoqian Xu ◽  
Nelly Morellet ◽  
...  

1992 ◽  
Vol 1 (5) ◽  
pp. 563-574 ◽  
Author(s):  
Michael F. Summers ◽  
Louis E. Henderson ◽  
Mark R. Chance ◽  
Terri L. South ◽  
Paul R. Blake ◽  
...  

2000 ◽  
Vol 74 (19) ◽  
pp. 8980-8988 ◽  
Author(s):  
Jianhui Guo ◽  
Tiyun Wu ◽  
Jada Anderson ◽  
Bradley F. Kane ◽  
Donald G. Johnson ◽  
...  

ABSTRACT The nucleocapsid protein (NC) of human immunodeficiency virus type 1 (HIV-1) has two zinc fingers, each containing the invariant metal ion binding residues CCHC. Recent reports indicate that mutations in the CCHC motifs are deleterious for reverse transcription in vivo. To identify reverse transcriptase (RT) reactions affected by such changes, we have probed zinc finger functions in NC-dependent RT-catalyzed HIV-1 minus- and plus-strand transfer model systems. Our approach was to examine the activities of wild-type NC and a mutant in which all six cysteine residues were replaced by serine (SSHS NC); this mutation severely disrupts zinc coordination. We find that the zinc fingers contribute to the role of NC in complete tRNA primer removal from minus-strand DNA during plus-strand transfer. Annealing of the primer binding site sequences in plus-strand strong-stop DNA [(+) SSDNA] to its complement in minus-strand acceptor DNA is not dependent on NC zinc fingers. In contrast, the rate of annealing of the complementary R regions in (−) SSDNA and 3′ viral RNA during minus-strand transfer is approximately eightfold lower when SSHS NC is used in place of wild-type NC. Moreover, unlike wild-type NC, SSHS NC has only a small stimulatory effect on minus-strand transfer and is essentially unable to block TAR-induced self-priming from (−) SSDNA. Our results strongly suggest that NC zinc finger structures are needed to unfold highly structured RNA and DNA strand transfer intermediates. Thus, it appears that in these cases, zinc finger interactions are important components of NC nucleic acid chaperone activity.


2010 ◽  
Vol 29 (4-6) ◽  
pp. 438-444 ◽  
Author(s):  
A. Miazga ◽  
P. Ziemkowski ◽  
M. A. Siwecka ◽  
A. Lipniacki ◽  
A. Piasek ◽  
...  
Keyword(s):  
Anti Hiv ◽  

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