2010
DOI: 10.1021/np900788e
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JBIR-22, An Inhibitor for Protein−Protein Interaction of the Homodimer of Proteasome Assembly Factor 3

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 ca… Show more

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Cited by 29 publications
(25 citation statements)
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“…Another spongederived compound, JBIR-22, was later found to be an analogue of equisetin, an antibiotic compound produced by Fusarium spp. 256 . JBIR-22 was shown to be cytotoxic to HeLa cells 256 , but it was not otherwise characterized for biological activity.…”
Section: Protein Protein Interactions Protein Protein Interactions Amentioning
confidence: 99%
See 1 more Smart Citation
“…Another spongederived compound, JBIR-22, was later found to be an analogue of equisetin, an antibiotic compound produced by Fusarium spp. 256 . JBIR-22 was shown to be cytotoxic to HeLa cells 256 , but it was not otherwise characterized for biological activity.…”
Section: Protein Protein Interactions Protein Protein Interactions Amentioning
confidence: 99%
“…256 . JBIR-22 was shown to be cytotoxic to HeLa cells 256 , but it was not otherwise characterized for biological activity.…”
Section: Protein Protein Interactions Protein Protein Interactions Amentioning
confidence: 99%
“…JBIR-22, specifically inhibiting proteasome assembling chaperone homodimerization in vitro, could be a useful primary compound for developing anticancer drugs [58,59]. Due to its important bioactivity and unsolved stereochemical assignment, Healy et al developed an elegant synthetic route (Scheme 6) [27].…”
Section: C3-decalinoyl Ta (Jbir-22)mentioning
confidence: 99%
“…24) and JBIR-22, which inhibits homodimer formation of proteasome assembly factor 3 (Ref. 25). Many of these natural products have intrinsic antitumour properties, although it is not clear whether this is solely attributable to their proteasome inhibitory capacities.…”
Section: Targeting Proteasome Subsets For Inhibition – Reducing Overamentioning
confidence: 99%