title: Iron(II) supramolecular helicates interfere with the HIV-1 Tat-TAR RNA interaction critical for viral replication.
abstract: The interaction between the HIV-1 transactivator protein Tat and TAR (transactivation responsive region) RNA, plays a critical role in HIV-1 transcription. Iron(II) supramolecular helicates were evaluated for their in vitro activity to inhibit Tat-TAR RNA interaction using UV melting studies, electrophoretic mobility shift assay, and RNase A footprinting. The results demonstrate that iron(II) supramolecular helicates inhibit Tat-TAR interaction at nanomolar concentrations by binding to TAR RNA. These studies provide a new insight into the biological potential of metallosupramolecular helicates.
authors.affiliation: Institute of Biophysics, Academy of Sciences of the Czech Republic, v.v.i., Kralovopolska 135, CZ-61265 Brno, Czech Republic.
authors.forename: Jaroslav
authors.initials: J
authors.lastname: Malina
authors.affiliation: School of Chemistry, University of Birmingham, Edgbaston, Birmingham B152TT, United Kingdom.
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Hannon
authors.affiliation: Institute of Biophysics, Academy of Sciences of the Czech Republic, v.v.i., Kralovopolska 135, CZ-61265 Brno, Czech Republic.|Department of Biophysics, Faculty of Science, Palacky University in Olomouc, Slechtitelu 27, CZ-78371 Olomouc, Czech Republic.
authors.forename: Viktor
authors.initials: V
authors.lastname: Brabec
mesh_terms: D005296:Ferrous Compounds / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000502:physiology*; D009690:Nucleic Acid Conformation; D011485:Protein Binding; D012367:RNA, Viral / Q000737:chemistry / Q000378:metabolism*; D014779:Virus Replication / Q000187:drug effects; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000378:metabolism*
chemical_list: D005296:Ferrous Compounds; D012367:RNA, Viral; D054322:tat Gene Products, Human Immunodeficiency Virus