A new class of RNA-binding oligomers: peptoid amide and ester analogues.
Replication of human immunodeficiency virus type 1 (HIV-1) requires specific interactions of Tat protein with the trans-activation responsive region (TAR) RNA, a 59-base stem-loop structure located at the 5'-end of all HIV mRNAs. Here we report the design, synthesis and in vitro activities of oligopeptoid amide and ester analogues which bind TAR RNA with high affinities. These results show that we have identified a new class of unnatural oligomers for RNA targeting.
Kesavan
Venkitasamy
V
Chemical Biology Program, Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, 364 Plantation Street, Worcester, Massachusetts 01605-2324, USA.
Tamilarasu
Natarajan
N
Cao
Hong
H
Rana
Tariq M
TM
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D000595:Amino Acid Sequence; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D001483:Base Sequence; D015195:Drug Design; D004952:Esters / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D031541:Fluorescence Resonance Energy Transfer; D006678:HIV / Q000187:drug effects / Q000235:genetics; D016325:HIV Long Terminal Repeat / Q000235:genetics; D009690:Nucleic Acid Conformation; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D012367:RNA, Viral / Q000235:genetics / Q000378:metabolism*; D013379:Substrate Specificity
D000577:Amides; D019380:Anti-HIV Agents; D004952:Esters; D010455:Peptides; D012367:RNA, Viral