Inhibition of the HIV-1 rev-RRE complex formation by unfused aromatic cations.
RNA viruses cause a wide range of human diseases. Development of new agents to target such viruses is an active area of research. Towards this goal, a series of diphenylfuran cations as potential inhibitors of the Rev-RRE complex have been designed and synthesized. Analysis of the interaction of the diphenylfurans with RRE and TAR RNA model systems by gel shift assays indicates that they exhibit both sequence and structure-dependent binding modes. Our results show a strong interaction between the diphenylfuran ring system and RRE bases, while the TAR interactions are much weaker with the compounds that are the best inhibitors of Rev-RRE.
Xiao
G
G
Department of Chemistry, Georgia State University, Atlanta, GA 30303, USA.
Kumar
A
A
Li
K
K
Rigl
C T
CT
Bajic
M
M
Davis
T M
TM
Boykin
D W
DW
Wilson
W D
WD
D000617:Aminoglycosides / Q000494:pharmacology; D002412:Cations / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D005663:Furans / Q000138:chemical synthesis / Q000494:pharmacology*; D015694:Gene Products, rev / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D015752:Genes, env / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D016325:HIV Long Terminal Repeat / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D046911:Macromolecular Substances; D008954:Models, Biological; D011489:Protein Denaturation / Q000528:radiation effects; D054321:rev Gene Products, Human Immunodeficiency Virus
D000617:Aminoglycosides; D002412:Cations; D005663:Furans; D015694:Gene Products, rev; D046911:Macromolecular Substances; D054321:rev Gene Products, Human Immunodeficiency Virus