Literature DB >> 20180542

JBIR-22, an inhibitor for protein-protein interaction of the homodimer of proteasome assembly factor 3.

Miho Izumikawa1, Junko Hashimoto, Takatsugu Hirokawa, Satoshi Sugimoto, Taira Kato, Motoki Takagi, Kazuo Shin-Ya.   

Abstract

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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Year:  2010        PMID： 20180542     DOI： 10.1021/np900788e

Source DB:  PubMed          Journal:  J Nat Prod        ISSN： 0163-3864            Impact factor:   4.050


  8 in total

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  8 in total

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