期刊
JOURNAL OF NATURAL PRODUCTS
卷 73, 期 4, 页码 628-631出版社
AMER CHEMICAL SOC
DOI: 10.1021/np900788e
关键词
-
资金
- New Energy and Industrial Technology Department Organization (NEDO) of Japan
Proteasome assembling chaperone (PAC) 3 acts as a homodimer and plays an important role in proteasome formation. We screened JBIR-22 (1) as an inhibitor for protein protein interaction (PPI) of PAC3 homodimer from our natural product library using a protein fragment complementation assay (PCA) with monomeric Kusabira-Green fluorescent protein (mKG) in vitro and found that 1 exhibited potent inhibitory activity against PAC3 homodimerization. Compound 1 showed long-term cytotoxicity against the human cervical carcinoma cell line, HeLa. This is the first report of a PPI inhibitor for proteasome assembly factors.
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