2012
DOI: 10.1016/j.bmcl.2011.12.027
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Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor

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Cited by 95 publications
(37 citation statements)
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“…We now show that functional p38 signaling in pancreatic cancer is a predictive marker of outcome in resected pancreatic cancer. This is consistent with the findings by Koizumi et al who noted the necessity of p38 activity for gemcitabine-induced toxicity of pancreatic cancer cells (48), and that JNK inhibition suppressed pancreatic cancer cell growth in both in vitro assays and in a genetically engineered mouse model of pancreatic cancer (49), lending support to in human studies of JNK inhibition in the adjuvant setting and potentially in patients receiving first line therapy for newly diagnosed advanced stage disease as well (50). …”
Section: Discussionsupporting
confidence: 91%
“…We now show that functional p38 signaling in pancreatic cancer is a predictive marker of outcome in resected pancreatic cancer. This is consistent with the findings by Koizumi et al who noted the necessity of p38 activity for gemcitabine-induced toxicity of pancreatic cancer cells (48), and that JNK inhibition suppressed pancreatic cancer cell growth in both in vitro assays and in a genetically engineered mouse model of pancreatic cancer (49), lending support to in human studies of JNK inhibition in the adjuvant setting and potentially in patients receiving first line therapy for newly diagnosed advanced stage disease as well (50). …”
Section: Discussionsupporting
confidence: 91%
“…Immunoblotting confirmed enhanced JNK phosphorylation in XBP1Δ splenic cDC1s (Suppl Fig 5D). To explore whether JNK was mediating cell death of XBP1 deficient lung cDC1s, we treated the XBP1ΔDC mice with CC-930, a novel specific inhibitor of JNK phosphorylation ( 38 and validated in Suppl Fig 5E). As noticed in Fig 6E and F, CC-930 treatment was unable to rescue lung cDC1s and migratory counterparts in the MedLN.…”
Section: Resultsmentioning
confidence: 99%
“…Follow-up studies determined IC 50 values of 480 nM (MAPK2) and 379 nM (EGFR). The IC 50 values of JNK 1, 2, and 3 isomers were 52 nM, 5 nM and 5 nM, respectively 19. Dermal fibroblasts were incubated with CC-930 at concentrations from 0.1 to 10 µM for 24 h. For controls, fibroblasts were incubated with the solvent dimethyl sulphoxide in the same concentrations.…”
Section: Methodsmentioning
confidence: 99%