Document Report Card

ID: ALA1157069

Journal: J Nat Prod

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

Authors: Izumikawa M, Hashimoto J, Hirokawa T, Sugimoto S, Kato T, Takagi M, Shin-Ya K.

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.

CiteXplore: 20180542

DOI: 10.1021/np900788e