Target specificity, in vivo pharmacokinetics, and efficacy of the putative STAT3 inhibitor LY5 in osteosarcoma, Ewing's sarcoma, and rhabdomyosarcoma

STAT3 is a transcription factor involved in cytokine and receptor kinase signal transduction that is aberrantly activated in a variety of sarcomas, promoting metastasis and chemotherapy resistance. The purpose of this work was to develop and test a novel putative STAT3 inhibitor, LY5. An in silico f...

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Veröffentlicht in:	PloS one 2017-07, Vol.12 (7), p.e0181885
Hauptverfasser:	Yu, Peter Y, Gardner, Heather L, Roberts, Ryan, Cam, Hakan, Hariharan, Seethalakshmi, Ren, Ling, LeBlanc, Amy K, Xiao, Hui, Lin, Jiayuh, Guttridge, Denis C, Mo, Xiaokui, Bennett, Chad E, Coss, Christopher C, Ling, Yonghua, Phelps, Mitch A, Houghton, Peter, London, Cheryl A
Format:	Artikel
Sprache:	eng
Schlagworte:	Aberration Aminopyridines - pharmacokinetics Aminopyridines - pharmacology Aminopyridines - therapeutic use Animal models Animals Anticancer properties Assaying Binding sites Bioavailability Biocompatibility Biological effects Biology Biology and Life Sciences Biomedical materials Biotechnology Bone cancer Cancer therapies Cell growth Cell Line, Tumor Cell proliferation Cell Proliferation - drug effects Cell Survival - drug effects Chemoresistance Chemotherapy Colorectal cancer Cytokines - pharmacology Dogs Drug development Drug therapy Enzyme inhibitors Ewing's sarcoma Ewings sarcoma Female Humans In vitro methods and tests In vivo methods and tests Inhibition Inhibitors Lung Neoplasms - secondary Medical research Medicine and Health Sciences Metastases Metastasis Mice Oncology Osteosarcoma Osteosarcoma - drug therapy Osteosarcoma - pathology Pediatrics Pharmaceuticals Pharmacokinetics Pharmacology Phosphorylation Phosphorylation - drug effects Phosphotyrosine Physiological aspects Research and Analysis Methods Rhabdomyosarcoma Rhabdomyosarcoma - drug therapy Rhabdomyosarcoma - pathology RNA-mediated interference Rodents Sarcoma Sarcoma, Ewing - drug therapy Sarcoma, Ewing - pathology Science Signal transduction Stat3 protein STAT3 Transcription Factor - antagonists & inhibitors STAT3 Transcription Factor - metabolism Sulfonamides - pharmacokinetics Sulfonamides - pharmacology Sulfonamides - therapeutic use Testing Treatment Outcome Tumor cell lines Tumors Veterinary medicine Xenograft Model Antitumor Assays Xenografts
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