title: Inhibition of the 26S proteasome by peptide mimics of the coiled-coil region of its ATPase subunits.
abstract: Regulation of proteasomal degradation is an indispensable tool for biomedical studies. Thus, there is demand for novel proteasome inhibitors. Proteasomal degradation requires formation of coiled-coil structure by the N-terminal region of ATPase subunits of the proteasome cap. Here we show that peptides that mimic the N-terminal coiled-coil region of ATPase subunits interfere with proteasome function. These results suggest that coiled-coil peptides represent promising new proteasome inhibitors and that N-terminal coiled-coil regions of ATPase subunits are targets for proteasome inhibition.
authors.affiliation: Frontier Research Core for Life Sciences, University of Toyama, 3190 Gofuku, Toyama-shi, Toyama 930-8555, Japan. Electronic address: inobe@ctg.u-toyama.ac.jp.
authors.forename: Tomonao
authors.initials: T
authors.lastname: Inobe
authors.affiliation: Frontier Research Core for Life Sciences, University of Toyama, 3190 Gofuku, Toyama-shi, Toyama 930-8555, Japan.
authors.forename: Reiko
authors.initials: R
authors.lastname: Genmei
mesh_terms: D000251:Adenosine Triphosphatases / Q000737:chemistry / Q000378:metabolism; D000595:Amino Acid Sequence; D006801:Humans; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology*; D046988:Proteasome Endopeptidase Complex / Q000737:chemistry / Q000378:metabolism*; D061988:Proteasome Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015003:Yeasts / Q000187:drug effects / Q000201:enzymology / Q000254:growth & development
chemical_list: D010455:Peptides; D061988:Proteasome Inhibitors; D046988:Proteasome Endopeptidase Complex; C061553:ATP dependent 26S protease; D000251:Adenosine Triphosphatases
keywords: Coiled-coil; Inhibitor; Peptide; Proteasome; Protein degradation; Rpt subunit