Discovery, Synthesis, and Evaluation of Small-Molecule Signal Transducer and Activator of Transcription 3 Inhibitors
نویسندگان
چکیده
منابع مشابه
Preclinical characterization of signal transducer and activator of transcription 3 small molecule inhibitors for primary and metastatic brain cancer therapy.
Signal transducer and activator of transcription 3 (STAT3) has been implicated as a hub for multiple oncogenic pathways. The constitutive activation of STAT3 is present in several cancers, including gliomas (GBMs), and is associated with poor therapeutic responses. Phosphorylation of STAT3 triggers its dimerization and nuclear transport, where it promotes the transcription of genes that stimula...
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Angiotensin II (Ang II) is known to promote vascular disease and hypertension in part by formation of cytokines, such as interleukin-6. However, the role of signal transducer and activator of transcription 3 (STAT3) in these processes and Ang II/interleukin-6 signaling is unclear. Using 2 models, we tested the hypothesis that STAT3 is essential for Ang II-induced vascular dysfunction and hypert...
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Constitutively activated STAT3 protein has been found to be a key regulator of pancreatic cancer and a target for molecular therapeutic intervention. In this study, PG-S3-001, a small molecule derived from the SH-4-54 class of STAT3 inhibitors, was found to inhibit patient-derived pancreatic cancer cell proliferation in vitro and in vivo in the low micromolar range. PG-S3-001 binds the STAT3 pr...
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15 صفحه اولEvaluation of quantitative assays for the identification of direct signal transducer and activator of transcription 3 (STAT3) inhibitors
In many forms of cancer the signal transducer and activator of transcription 3 (STAT3) transcription factor remains constitutively active, driving cancer survival and progression. The critical role of STAT3 in tumorigenesis has prompted a campaign of drug discovery programs to identify small molecules that disrupt the function of STAT3, with more recent efforts focusing on direct STAT3 inhibiti...
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ژورنال
عنوان ژورنال: CHEMICAL & PHARMACEUTICAL BULLETIN
سال: 2012
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.c12-00745