Discovery of JSI-124 (cucurbitacin I), a selective Janus kinase/signal transducer and activator of transcription 3 signaling pathway inhibitor with potent antitumor activity against human and murine…

By M. Blaskovich, Jiazhi Sun, A. Cantor, J. Turkson, R. Jove, S. Sebti. Cancer Research, 2003

620 citations recorded by the source corpus.

View Paper: https://www.semanticscholar.org/paper/cbd89bc2919a5dab76bca3e74ee87db8241d94ca

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Citations in the corpus

Drug discovery from medicinal plants. (2005, methodology): “Three examples are cucurbitacin I, obtained from the National Cancer Institute (NCI) Diversity Set of known compounds and found to be highly selective in inhibiting the JAK/STAT3 pathway in tumors with activated STAT3 (Blaskovich et al., 2003), h-lapachone, which selectively kills cancer cells over ”
gp130-mediated Stat3 activation in enterocytes regulates cell survival and cell-cycle progression during colitis-associated tumorigenesis. (2009, result): “Finally, cucurbitacin I-mediated inhibition of Stat3 (Blaskovich et al., 2003) induces cell-cycle arrest at the G2/M transition in cell lines derived from either laryngeal squamous cell carcinoma or glioblastoma multiforme, which, similar to our observations in lesions from Stat3DIEC mice, is…”
Mechanism regulating reactive oxygen species in tumor induced myeloid-derived suppressor cells (2009, background): “We therefore asked whether JSI-124 mediates its effect via ROS down-regulation in MDSC. MDSC were isolated from spleens of 3-wk MC38 tumor-bearing mice and treated with JSI-124 in the presence of TCCM. Twenty-four hour treatment with the STAT3 inhibitor dramatically ( p 0.01) reduced the level of RO”
Interleukin-6 induces an epithelial–mesenchymal transition phenotype in human breast cancer cells (2009, background): “To determine whether STAT3 was required for the EMT phenotypes in human breast cancer cells, we inhibited STAT3 activation in MCF7IL 6 and MCF-7Twist cells with JSI-124, a highly selective smallmolecular inhibitor of the Jak/STAT3 signaling pathway (Blaskovich et al., 2003).”
Interleukin-6 in aging and chronic disease: a magnificent pathway. (2006, background): “The binding of IL-6 to IL-6r is followed by the homodimerization of gp130 and activation of two distinct signaling pathways: 1) the gp130-associated cytoplasmatic Janus and tyrosine kinases (JAK1, JAK2, and TYK2) signal transducers and activators of transcription (STATs, particularly STAT 1 and 3), ”
Stattic: a small-molecule inhibitor of STAT3 activation and dimerization. (2006, background): “STAT3 signaling inhibitors with unknown targets [21, 22] include members of the cucurbitacin family of natural products [23-25].”