title: Design and synthesis of a novel peptidomimetic inhibitor of HIV-1 Tat-TAR interactions: squaryldiamide as a new potential bioisostere of unsubstituted guanidine.
abstract: By performing RNA-targeted structure-activity relationship studies, we discovered a novel peptidomimetic containing squaryldiamide as a potential bioisostere replacement for guanidine that binds transactivation responsive RNA with high affinity.
authors.affiliation: Chemical Biology Program, Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, Worcester, MA 01605-2324, USA.
authors.forename: Chi-Wan
authors.initials: CW
authors.lastname: Lee
authors.forename: Hong
authors.initials: H
authors.lastname: Cao
authors.forename: Kozi
authors.initials: K
authors.lastname: Ichiyama
authors.forename: Tariq M
authors.initials: TM
authors.lastname: Rana
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003503:Cyclobutanes; D003958:Diamide / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D015696:Gene Products, tat / Q000737:chemistry*; D019791:Guanidine; D016325:HIV Long Terminal Repeat / Q000187:drug effects*; D015497:HIV-1 / Q000737:chemistry*; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D016601:RNA-Binding Proteins / Q000737:chemistry; D013329:Structure-Activity Relationship; D054322:tat Gene Products, Human Immunodeficiency Virus
chemical_list: D019380:Anti-HIV Agents; D003503:Cyclobutanes; D015696:Gene Products, tat; D009842:Oligopeptides; D016601:RNA-Binding Proteins; D054322:tat Gene Products, Human Immunodeficiency Virus; D003958:Diamide; D019791:Guanidine; C030042:squaric acid