Inhibition of HIV-1 nuclear import via schiff base formation with arylene bis(methylketone) compounds.
Arylene bis(methylketone) compounds specifically block nuclear translocation of the HIV-1 pre-integration complex by forming Schiff-base adducts with contiguous lysines within nuclear localization signal.
Al-Abed
Yousef
Y
Laboratory of Medicinal Chemistry, North Shore-LIJ Research Institute, 350 Community Drive, Manhasset, NY, 11030, USA. yalabed@nshs.edu
Dubrovsky
Larisa
L
Ruzsicska
Bela
B
Seepersaud
Mohindra
M
Bukrinsky
Michael
M
D021581:Active Transport, Cell Nucleus / Q000187:drug effects*; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002467:Cell Nucleus / Q000737:chemistry / Q000187:drug effects / Q000821:virology*; D002478:Cells, Cultured; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D007202:Indicators and Reagents; D007659:Ketones / Q000138:chemical synthesis* / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects / Q000648:ultrastructure / Q000821:virology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D020133:Reverse Transcriptase Polymerase Chain Reaction; D012545:Schiff Bases / Q000737:chemistry*; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D007202:Indicators and Reagents; D007659:Ketones; D011743:Pyrimidines; D012545:Schiff Bases