JTE-607 is a pro-drug, which carboxylic form (JTE-607-COOH) is a potent cytokine release inhibitor. JTE-607 reduces the production of proinflammatory cytokines in models of acute injury, septic shock and endotoxemia. It also inhibits proliferation of AML cell in vitro and in xenograft model. JTE-607 is an inhibitor of CPSF3 (pre-messenger RNA endonuclease cleavage and polyadenylation specificity factor 3) that directly binds to CPSF3 and blocks the release of newly synthesized pre-mRNAs.
pro-drug of cytokine release inhibitor JTE-607-COOH; inhibitor of CPSF3
Proinflammatory cytokines and growth factors have been thought to play crucial roles in the pathology of acute myelogenous leukemia (AML) by supporting the proliferation and survival of AML cells in an autocrine and paracrine manner, although further elucidation is required.
Biochemical and biophysical research communications, 518(1), 32-37 (2019-08-11)
JTE-607 is a small molecule that was developed as an inflammatory cytokine inhibitor and also as an anti-leukemia reagent for monocytic leukemia. However, the mode of action of JTE-607 remains unknown. In this study, we identified JTE-607 to be a
Nature chemical biology, 16(1), 50-59 (2019-12-11)
The post-genomic era has seen many advances in our understanding of cancer pathways, yet resistance and tumor heterogeneity necessitate multiple approaches to target even monogenic tumors. Here, we combine phenotypic screening with chemical genetics to identify pre-messenger RNA endonuclease cleavage
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