Design and synthesis of a novel peptidomimetic inhibitor of HIV-1 Tat-TAR interactions: squaryldiamide as a new potential bioisostere of unsubstituted guanidine.
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.
Lee
Chi-Wan
CW
Chemical Biology Program, Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, Worcester, MA 01605-2324, USA.
Cao
Hong
H
Ichiyama
Kozi
K
Rana
Tariq M
TM
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
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