Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 129, Issue 25, Pages 7750-+Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ja072027p
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Funding
- NHLBI NIH HHS [N01-HV28185, N01HV28185] Funding Source: Medline
- NIH HHS [DP1 OD000663, DP1 OD000663-02] Funding Source: Medline
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The first chemical inhibitor of the 19S regulatory particle (RP) of the proteasome is described. The molecule was identified by screening a library of nucleoside-capped peptoids for binding to the yeast 26S proteasome in a crude extract. The hit was resynthesized and shown to block 19S RP-mediated protein unfolding in vitro and proteasome-mediated turnover of p27 in HeLa cells.
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