The FGFR inhibitor PD173074 binds to the C-terminus of oncofetal HMGA2 and modulates its DNA-binding and transcriptional activation functions.
Sign Up to like & getrecommendations! Published in 2023 at "FEBS letters"
DOI: 10.1002/1873-3468.14675
Abstract: The architectural chromatin factor high-mobility group AT-hook 2 (HMGA2) is causally involved in several human malignancies and pathologies. HMGA2 is not expressed in most normal adult somatic cells, which renders the protein an attractive drug… read more here.
Keywords: fgfr inhibitor; dna binding; hmga2; inhibitor pd173074 ... See more keywords
DW14383 is an irreversible pan-FGFR inhibitor that suppresses FGFR-dependent tumor growth in vitro and in vivo.
Sign Up to like & getrecommendations! Published in 2020 at "Acta pharmacologica Sinica"
DOI: 10.1038/s41401-020-00567-3
Abstract: Fibroblast growth factor receptor (FGFR) is a promising anticancer target. Currently, most FGFR inhibitors lack sufficient selectivity and have nonnegligible activity against kinase insert domain receptor (KDR), limiting their feasibility due to the serious side… read more here.
Keywords: dw14383; fgfr; fgfr inhibitor; fgfr1 ... See more keywords
FGFR inhibitor, AZD4547, impedes the stemness of mammary epithelial cells in the premalignant tissues of MMTV-ErbB2 transgenic mice
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DOI: 10.1038/s41598-017-11751-7
Abstract: The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases (RTKs) regulates signaling pathways involved in cell proliferation and differentiation. Currently, the anti-tumor properties of FGFR inhibitors are being tested in preclinical and clinical… read more here.
Keywords: mammary epithelial; inhibitor; fgfr inhibitor; mmtv erbb2 ... See more keywords
EPCT-10. DEBIO1347, AN ORAL FGFR INHIBITOR: RESULTS FROM A SINGLE CENTER STUDY IN RECURRENT/REFRACTORY FGFR ALTERED PEDIATRIC GLIOMAS
Sign Up to like & getrecommendations! Published in 2021 at "Neuro-Oncology"
DOI: 10.1093/neuonc/noab090.196
Abstract: Abstract Background Oncogenic driver alterations in FGFR are present in a subset of pediatric gliomas. Debio1347 is an orally available, highly selective FGFR 1–3 inhibitor that had a favorable safety profile and encouraging preliminary clinical… read more here.
Keywords: gliomas; fgfr; fgfr inhibitor; patient ... See more keywords
FGFR Inhibitor Stymies Gastric Cancer.
Sign Up to like & getrecommendations! Published in 2021 at "Cancer discovery"
DOI: 10.1158/2159-8290.cd-nb2021-0312
Abstract: In the phase II FIGHT trial, adding bemarituzumab to chemotherapy led to longer progression-free survival and overall survival in patients with advanced FGFR2b-positive gastric or gastroesophageal junction cancers. However, the agent was also associated with… read more here.
Keywords: inhibitor stymies; fgfr inhibitor; cancer; gastric cancer ... See more keywords
Debio 1347, an oral FGFR inhibitor: Results from a first-in-human, phase I dose-escalation study in patients with FGFR genomically activated advanced solid tumors.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2017.35.15_suppl.2500
Abstract: 2500Background: Oncogenic alterations in fibroblast growth factor receptors (FGFR) are seen across multiple solid tumor malignancies. Debio 1347 is an orally available, highly selective panFGFR inh... read more here.
Keywords: debio 1347; fgfr inhibitor; oral fgfr; 1347 oral ... See more keywords
Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy
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DOI: 10.3390/cancers12082010
Abstract: Some colorectal cancer patients harboring FGFR (fibroblast growth factor receptor) genetic alterations, such as copy number gain, mutation, and/or mRNA overexpression, were selected for enrollment in several recent clinical trials of FGFR inhibitor, because these… read more here.
Keywords: inhibitor; fgfr inhibitor; colorectal cancer; cancer patients ... See more keywords
FGFR Inhibitors in Oncology: Insight on the Management of Toxicities in Clinical Practice
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DOI: 10.3390/cancers13122968
Abstract: Simple Summary FGFR inhibitors evolved as therapeutic options in cholangiocarcinoma and urothelial malignancies. Given the implications of FGFR pathway in various physiological functions, FGFR inhibitors are known to cause unique toxicities. In this review, we… read more here.
Keywords: fgfr; fgfr inhibitor; fgfr inhibitors; management ... See more keywords
BGJ398, A Pan-FGFR Inhibitor, Overcomes Paclitaxel Resistance in Urothelial Carcinoma with FGFR1 Overexpression
Sign Up to like & getrecommendations! Published in 2018 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms19103164
Abstract: Paclitaxel (PTX) is commonly used to treat urothelial carcinoma (UC) after platinum-based chemotherapy has failed. However, single-agent taxane therapy is not sufficient to inhibit tumor progression and drug resistance in advanced UC. Epithelial-to-mesenchymal transition (EMT)… read more here.
Keywords: fgfr inhibitor; ptx; fgfr1 overexpression; resistance ... See more keywords