title: PPG peptide nucleic acids that promote DNA guanine quadruplexes.
abstract: Recent studies have shown that guanine-rich (G-rich) sequences with the potential to form quadruplexes might play a role in normal transcription as well as overexpression of oncogenes. Chemical tools that allow examination of the specific roles of G-quadruplex formation in vivo, and their association with gene regulation will be essential to understanding the functions of these quadruplexes and might lead to beneficial therapies. Properly designed peptide nucleic acids (PNAs) can invade G-rich DNA duplexes and induce the formation of a G-quadruplex in the free DNA strand. Replacing guanines in the PNA sequence with pyrazolo[3,4-d]pyrimidine guanine (PPG) nucleobases eliminates G-quadruplex formation with PNA and promotes invasion of the target DNA.
authors.affiliation: Laboratory of Bioorganic Chemistry, NIDDK, NIH, DHHS, 8 Center Drive, Bethesda, MD 20892 (USA).
authors.forename: Ethan A
authors.initials: EA
authors.lastname: Englund
authors.forename: Pankaj
authors.initials: P
authors.lastname: Gupta
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Micklitsch
authors.forename: Mykola I
authors.initials: MI
authors.lastname: Onyshchenko
authors.forename: Evgenia
authors.initials: E
authors.lastname: Remeeva
authors.forename: Ronald D
authors.initials: RD
authors.lastname: Neumann
authors.forename: Igor G
authors.initials: IG
authors.lastname: Panyutin
authors.forename: Daniel H
authors.initials: DH
authors.lastname: Appella
mesh_terms: D004247:DNA / Q000187:drug effects; D054856:G-Quadruplexes / Q000187:drug effects*; D006147:Guanine / Q000031:analogs & derivatives* / Q000737:chemistry; D020135:Peptide Nucleic Acids / Q000138:chemical synthesis*; D010957:Plasmids; D011720:Pyrazoles / Q000737:chemistry*
chemical_list: D020135:Peptide Nucleic Acids; D011720:Pyrazoles; D006147:Guanine; D004247:DNA
keywords: DNA recognition; G-quadruplexes; nucleic acids; nucleobases; peptide nucleic acids