HSP90 Inhibition Drives Degradation of FGFR2 Fusion Proteins: Implications for Treatment of Cholangiocarcinoma
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DOI: 10.1002/hep.30127
Abstract: About 15% of intrahepatic cholangiocarcinomas (ICCs) express constitutively active fibroblast growth factor receptor 2 (FGFR2) fusion proteins (FFs) generated by chromosomal translocations. FFs have been nominated as oncogenic drivers because administration of FGFR tyrosine kinase… read more here.
Keywords: hsp90; fusion proteins; fgfr2 fusion; bgj398 ... See more keywords
Akt Activation Mediates Acquired Resistance to Fibroblast Growth Factor Receptor Inhibitor BGJ398
Sign Up to like & getrecommendations! Published in 2017 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.mct-15-1010
Abstract: Activation of FGFR signaling through mutations, amplifications, or fusions involving FGFR1, 2, 3, or 4 is seen in multiple tumors, including lung, bladder, and cholangiocarcinoma. Currently, several clinical trials are evaluating the role of novel… read more here.
Keywords: bgj398; cell lines; acquired resistance; resistance ... See more keywords
Inhibition of FGFR Signaling Partially Rescues Hypophosphatemic Rickets in HMWFGF2 Tg Male Mice
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DOI: 10.1210/en.2016-1617
Abstract: &NA; Transgenic mice harboring high molecular weight fibroblast growth factor (FGF)2 isoforms (HMWTg) in osteoblast lineage cells phenocopy human X‐linked hypophosphatemic rickets (XLH) and Hyp murine model of XLH demonstrating increased FGF23/FGF receptor signaling and… read more here.
Keywords: nvp bgj398; bgj398; bone; fgfr signaling ... See more keywords
Targeting FGFR with BGJ398 in Breast Cancer: Effect on Tumor Growth and Metastasis.
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DOI: 10.2174/1568009618666171214114706
Abstract: BACKGROUND Endocrine resistance and metastatic dissemination comprise major clinical challenges for breast cancer treatment. The fibroblast growth factor receptor family (FGFR) consists of four tyrosine kinase transmembrane receptors, involved in key biological processes. Genomic alterations… read more here.
Keywords: cancer; bgj398; tumor growth; breast cancer ... See more keywords
Selective FGFR inhibitor BGJ398 inhibits phosphorylation of AKT and STAT3 and induces cytotoxicity in sphere-cultured ovarian cancer cells.
Sign Up to like & getrecommendations! Published in 2017 at "International journal of oncology"
DOI: 10.3892/ijo.2017.3913
Abstract: Epithelial ovarian cancer is the most aggressive and lethal among the gynecological malignancies, which is often found disseminated to peritoneal cavity at the time of diagnosis. There is accumulating evidence on the existence of genetic… read more here.
Keywords: sphere cultured; skov3ip1 cells; bgj398; ovarian cancer ... See more keywords