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https://www.readbyqxmd.com/read/28905937/somcl-085-a-novel-multi-targeted-fgfr-inhibitor-displays-potent-anticancer-activity-in-fgfr-addicted-human-cancer-models
#1
Xi-Fei Jiang, Yang Dai, Xia Peng, Yan-Yan Shen, Yi Su, Man-Man Wei, Wei-Ren Liu, Zhen-Bin Ding, Ao Zhang, Ying-Hong Shi, Jing Ai
Aberrant fibroblast growth factor receptor (FGFR) activation is found across a diverse spectrum of malignancies, especially those lacking effective treatments. SOMCL-085 is a novel FGFR-dominant multi-target kinase inhibitor. Here, we explored the FGFR-targeting anticancer activity of SOMCL-085 both in vitro and in vivo. Among a panel of 20 tyrosine kinases screened, SOMCL-085 potently inhibited FGFR1, FGFR2 and FGFR3 kinase activity, with IC50 values of 1.8, 1.9 and 6.9 nmol/L, respectively. This compound simultaneously inhibited the angiogenesis kinases VEGFR and PDGFR, but without obvious inhibitory effect on other 12 tyrosine kinases...
September 14, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28900173/fgfr-inhibitor-azd4547-impedes-the-stemness-of-mammary-epithelial-cells-in-the-premalignant-tissues-of-mmtv-erbb2-transgenic-mice
#2
Qingxia Zhao, Amanda B Parris, Erin W Howard, Ming Zhao, Zhikun Ma, Zhiying Guo, Ying Xing, Xiaohe Yang
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 studies. Nevertheless, reports on FGFR inhibitor-mediated breast cancer prevention are sparse. In this study, we investigated the anti-cancer benefits of AZD4547, an FGFR1-3 inhibitor, in ErbB2-overexpressing breast cancer models. AZD4547 (1-5 µM) demonstrated potent anti-proliferative effects, inhibition of stemness, and suppression of FGFR/RTK signaling in ErbB2-overexpressing human breast cancer cells...
September 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28883546/api5-induces-cisplatin-resistance-through-fgfr-signaling-in-human-cancer-cells
#3
Han Sol Jang, Seon Rang Woo, Kwon-Ho Song, Hanbyoul Cho, Doo Byung Chay, Soon-Oh Hong, Hyo-Jung Lee, Se Jin Oh, Joon-Yong Chung, Jae-Hoon Kim, Tae Woo Kim
Most tumors frequently undergo initial treatment with a chemotherapeutic agent but ultimately develop resistance, which limits the success of chemotherapies. As cisplatin exerts a high therapeutic effect in a variety of cancer types, it is often used in diverse strategies, such as neoadjuvant, adjuvant and combination chemotherapies. However, cisplatin resistance has often manifested regardless of cancer type, and it represents an unmet clinical need. Since we found that API5 expression was positively correlated with chemotherapy resistance in several specimens from patients with cervical cancer, we decided to investigate whether API5 is involved in the development of resistance after chemotherapy and to explore whether targeting API5 or its downstream effectors can reverse chemo-resistance...
September 8, 2017: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/28882160/intrinsic-fluorescence-of-the-clinically-approved-multikinase-inhibitor-nintedanib-reveals-lysosomal-sequestration-as-resistance-mechanism-in-fgfr-driven-lung-cancer
#4
Bernhard Englinger, Sebastian Kallus, Julia Senkiv, Daniela Heilos, Lisa Gabler, Sushilla van Schoonhoven, Alessio Terenzi, Patrick Moser, Christine Pirker, Gerald Timelthaler, Walter Jäger, Christian R Kowol, Petra Heffeter, Michael Grusch, Walter Berger
BACKGROUND: Studying the intracellular distribution of pharmacological agents, including anticancer compounds, is of central importance in biomedical research. It constitutes a prerequisite for a better understanding of the molecular mechanisms underlying drug action and resistance development. Hyperactivated fibroblast growth factor receptors (FGFRs) constitute a promising therapy target in several types of malignancies including lung cancer. The clinically approved small-molecule FGFR inhibitor nintedanib exerts strong cytotoxicity in FGFR-driven lung cancer cells...
September 7, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28878133/exome-capture-rna-sequencing-of-decade-old-breast-cancers-and-matched-decalcified-bone-metastases
#5
Nolan Priedigkeit, Rebecca J Watters, Peter C Lucas, Ahmed Basudan, Rohit Bhargava, William Horne, Jay K Kolls, Zhou Fang, Margaret Q Rosenzweig, Adam M Brufsky, Kurt R Weiss, Steffi Oesterreich, Adrian V Lee
Bone metastases (BoM) are a significant cause of morbidity in patients with estrogen receptor-positive (ER-positive) breast cancer; yet, characterizations of human specimens are limited. In this study, exome-capture RNA sequencing (ecRNA-seq) on aged (8-12 years), formalin-fixed, paraffin-embedded (FFPE), and decalcified cancer specimens was evaluated. Gene expression values and ecRNA-seq quality metrics from FFPE or decalcified tumor RNA showed minimal differences when compared with matched flash-frozen or nondecalcified tumors...
September 7, 2017: JCI Insight
https://www.readbyqxmd.com/read/28877471/kif5b-ret-oncoprotein-signals-through-a-multi-kinase-signaling-hub
#6
Tirtha Kamal Das, Ross Leigh Cagan
Gene fusions are increasingly recognized as important cancer drivers. The KIF5B-RET gene has been identified as a primary driver in a subset of lung adenocarcinomas. Targeting human KIF5B-RET to epithelia in Drosophila directed multiple aspects of transformation, including hyperproliferation, epithelial-to-mesenchymal transition, invasion, and extension of striking invadopodia-like processes. The KIF5B-RET-transformed human bronchial cell line showed similar aspects of transformation, including invadopodia-like processes...
September 5, 2017: Cell Reports
https://www.readbyqxmd.com/read/28857247/fgfr2-regulation-by-picrasidine-q-inhibits-the-cell-growth-and-induces-apoptosis-in-esophageal-squamous-cell-carcinoma
#7
Yuanyuan Shi, Xuejiao Liu, Mangaladoss Fredimoses, Mengqiu Song, Hanyong Chen, Kangdong Liu, Mee-Hyun Lee, Zigang Dong
Fibroblast growth factor receptor (FGFR) 2 and its downstream signaling cascades, PI3K/AKT/mTOR is playing an important role in cell survival and proliferations. In this study, we firstly found that picrasidine Q (PQ), an alkaloid component extracted from Angelica keiskei species, has the capacity of anti-cell transformation and anti-cancer. After ligand shape similarity approach of PQ, we found that PQ targeted FGFR 2 and verified by FGFR2 kinase assay as well as computational docking model. FGFR2 highly expressed in esophageal cancer tissues and PQ inhibited fibroblast growth factor (FGF)-induced cell transformation...
August 31, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28855072/comparison-of-fibroblast-growth-factor-receptor-gene-alterations-at-the-dna-versus-messenger-rna-level-in-advanced-urothelial-cancer-insights-for-clinical-research
#8
Andrea Necchi, Daniele Raggi, Chiara C Volpi, Patrizia Giannatempo, Maurizio Colecchia, Annunziata Gloghini
Pan-fibroblast growth-factor receptor (FGFR) inhibitors hold promise in FGFR-altered patients, but such alterations are rare in advanced urothelial carcinoma. In order to assess whether we may increase the number of eligible patients by using different molecular techniques for detecting alterations, we pooled the results of the centralised FGFR mutation/translocation assays that were performed in Clinical Laboratory Improvement Amendments-certified laboratories within multiple phase 2 trials. At our centre, the same tissue blocks were used to analyse FGFR1-3 messenger RNA expression through messenger RNA in situ hybridisation (ISH; RNAscope 2...
August 27, 2017: European Urology Focus
https://www.readbyqxmd.com/read/28838394/molecular-profiling-in-italian-patients-with-advanced-non-small-cell-lung-cancer-an-observational-prospective-study
#9
Elisa Gobbini, Domenico Galetta, Marcello Tiseo, Paolo Graziano, Antonio Rossi, Emilio Bria, Massimo Di Maio, Giulio Rossi, Vanesa Gregorc, Ferdinando Riccardi, Vieri Scotti, Anna Ceribelli, Lucio Buffoni, Angelo Delmonte, Tindara Franchina, Maria Rita Migliorino, Diego Cortinovis, Salvatore Pisconti, Paola Bordi, Annamaria Catino, Evaristo Maiello, Francesca Arizio, Silvia Novello
OBJECTIVES: Molecular profiling of advanced non-small-cell lung cancer (NSCLC) is recommended according to European and Italian guidelines. However, molecular routine assessment remains still heterogeneous. This observational study aimed to take a picture of the real clinical practice in molecular testing and therapeutic choices in advanced Italian NSCLCs. MATERIALS AND METHODS: This study prospectively enrolled newly diagnosed advanced or recurrent NSCLCs referred to 38 Italian centres, from November 2014 to November 2015...
September 2017: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
https://www.readbyqxmd.com/read/28835367/fgfr2-amplification-in-colorectal-adenocarcinoma
#10
Jamal H Carter, Catherine E Cottrell, Samantha McNulty, Katinka A Vingh-Conrad, Stephen Lamp, Jonathan W Heusel, Eric J Duncavage
FGFR2 is recurrently amplified in 5% of gastric cancers and 1-4% of breast cancers; however, this molecular alteration has never been reported in a primary colorectal cancer specimen. Preclinical studies indicate that several FGFR tyrosine-kinase inhibitors (TKI), such as AZD4547, have in vitro activity against the FGFR2-amplified colorectal cell line, NCI-H716. The efficacy of these inhibitors is currently under investigation in clinical trials for breast and gastric cancer. Thus, better characterizing colorectal tumors for FGFR2 amplification could identify a subset of patients who may benefit from FGFR TKI therapies...
August 23, 2017: Cold Spring Harbor Molecular Case Studies
https://www.readbyqxmd.com/read/28818953/new-horizons-for-precision-medicine-in-biliary-tract-cancers
#11
REVIEW
Juan W Valle, Angela Lamarca, Lipika Goyal, Jorge Barriuso, Andrew X Zhu
Biliary tract cancers (BTC), including cholangiocarcinoma and gallbladder cancer, are poor-prognosis and low-incidence cancers, although the incidence of intrahepatic cholangiocarcinoma is rising. A minority of patients present with resectable disease but relapse rates are high; benefit from adjuvant capecitabine chemotherapy has been demonstrated. Cisplatin/gemcitabine combination chemotherapy has emerged as the reference first-line treatment regimen; there is no standard second-line therapy. Selected patients may be suitable for liver-directed therapy (e...
September 2017: Cancer Discovery
https://www.readbyqxmd.com/read/28796141/therapeutic-potential-for-fgfr-inhibitors-in-sox9-fgfr2-coexpressing-pancreatic-cancer
#12
Hazel OʼSullivan, Fergal C Kelleher, Máire Lavelle, Brianan McGovern, Jean Murphy, Niall Swan, Ray McDermott
No abstract text is available yet for this article.
September 2017: Pancreas
https://www.readbyqxmd.com/read/28794627/in-situ-imaging-of-quantum-dot-azd4547-conjugates-for-tracking-the-dynamic-behavior-of-fibroblast-growth-factor-receptor-3
#13
Gyoyeon Hwang, Hyeonhye Kim, Hojong Yoon, Chiman Song, Dong-Kwon Lim, Taebo Sim, Jiyeon Lee
Fibroblast growth factor receptors (FGFRs) play an important role in determining cell proliferation, differentiation, migration, and survival. Although a variety of small-molecule FGFR inhibitors have been developed for cancer therapeutics, the interaction between FGFRs and FGFR inhibitors has not been well characterized. The FGFR-inhibitor interaction can be characterized using a new imaging probe that has strong, stable signal properties for in situ cellular imaging of the interaction without quenching. We developed a kinase-inhibitor-modified quantum dot (QD) probe to investigate the interaction between FGFR and potential inhibitors...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28783178/fibroblast-growth-factor-receptor-is-a-mechanistic-link-between-visceral-adiposity-and-cancer
#14
D Chakraborty, V Benham, B Bullard, T Kearney, H C Hsia, D Gibbon, E Y Demireva, S Y Lunt, J J Bernard
Epidemiological evidence implicates excess adipose tissue in increasing cancer risk. Despite a steeply rising global prevalence of obesity, how adiposity contributes to transformation (stage a non-tumorigenic cell undergoes to become malignant) is unknown. To determine the factors in adipose tissue that stimulate transformation, we used a novel ex vivo system of visceral adipose tissue (VAT)-condition medium-stimulated epithelial cell growth in soft agar. To extend this system in vivo, we used a murine lipectomy model of ultraviolet light B-induced, VAT-promoted skin tumor formation...
August 7, 2017: Oncogene
https://www.readbyqxmd.com/read/28769084/antibody-induced-dimerization-of-fgfr1-promotes-receptor-endocytosis-independently-of-its-kinase-activity
#15
Łukasz Opaliński, Aleksandra Sokołowska-Wędzina, Martyna Szczepara, Małgorzata Zakrzewska, Jacek Otlewski
Fibroblast growth factors (FGFs) and their plasma membrane-localized receptors (FGFRs) play a key role in the regulation of developmental processes and metabolism. Aberrant FGFR signaling is associated with the progression of serious metabolic diseases and human cancer. Binding of FGFs to FGFRs induces receptor dimerization and transphosphorylation of FGFR kinase domains that triggers activation of intracellular signaling pathways. Following activation, FGFRs undergo internalization and subsequent lysosomal degradation, which terminates transmission of signals...
August 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28753560/enhancement-of-the-anti-tumor-activity-of-fgfr1-inhibition-in-squamous-cell-lung-cancer-by-targeting-downstream-signaling-involved-in-glucose-metabolism
#16
Claudia Fumarola, Daniele Cretella, Silvia La Monica, Mara A Bonelli, Roberta Alfieri, Cristina Caffarra, Federico Quaini, Denise Madeddu, Angela Falco, Andrea Cavazzoni, Graziana Digiacomo, Giulia Mazzaschi, Valentina Vivo, Elisabetta Barocelli, Marcello Tiseo, Pier Giorgio Petronini, Andrea Ardizzoni
Fibroblast Growth Factor Receptor (FGFR) signaling is a complex pathway which controls several processes, including cell proliferation, survival, migration, and metabolism. FGFR1 signaling is frequently deregulated via amplification/over-expression in NSCLC of squamous histotype (SQCLC), however its inhibition has not been successfully translated in clinical setting. We determined whether targeting downstream signaling implicated in FGFR1 effects on glucose metabolism potentiates the anti-tumor activity of FGFR1 inhibition in SQCLC...
July 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/28752189/impact-of-tissue-based-genomic-profiling-on-clinical-decision-making-in-the-management-of-patients-with-metastatic-breast-cancer-at-academic-centers
#17
Cesar A Santa-Maria, Megan Kruse, Paola Raska, Mia Weiss, April Swoboda, Martin B Mutonga, Jame Abraham, Sarika Jain, Rita Nanda, Alberto J Montero
BACKGROUND: Genomic profiling can identify targetable mutations; however, the impact of tissue-based genomic profiling on clinical decision making for patients with metastatic breast cancer has not been well characterized. METHODS: Patients with stage IV breast cancer who had undergone genomic profiling between 7/2013 and 3/2015 were identified at three academic cancer centers. Genomic analysis was determined to have impacted clinical decision if (A) a patient was enrolled onto a genotype-matched clinical trial or (B) prescribed off-label an FDA-approved therapy targeting an identified mutation...
July 27, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28751448/association-of-fgfr1-with-er%C3%AE-maintains-ligand-independent-er-transcription-and-mediates-resistance-to-estrogen-deprivation-in-er-breast-cancer
#18
Luigi Formisano, Kimberly Mae Stauffer, Christian D Young, Neil E Bhola, Angel L Guerrero-Zotano, Valerie M Jansen, Monica M Estrada, Katherine E Hutchinson, Jennifer M Giltnane, Luis J Schwarz, Yao Lu, Justin M Balko, Olivier Deas, Stefano Cairo, Jean-Gabriel Judde, Ingrid A Mayer, Melinda Sanders, Teresa C Dugger, Roberto Bianco, Thomas Stricker, Carlos L Arteaga
FGFR1 amplification occurs in ~15% of ER+ human breast cancers. We investigated mechanisms by which FGFR1 amplification confers antiestrogen resistance to ER+ breast cancer.<br /><br />Experimental Design: ER+ tumors from patients treated with letrozole before surgery were subjected to Ki67 immunohistochemistry, FGFR1 FISH, and RNA-sequencing. ER+/FGFR1 amplified breast cancer cells and patient-derived xenografts (PDXs) were treated with FGFR1 siRNA or the FGFR tyrosine kinase inhibitor lucitanib...
July 27, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28747655/strategies-to-mitigate-variability-in-engineering-human-nasal-cartilage
#19
Stephen H J Andrews, Melanie Kunze, Aillette Mulet-Sierra, Lynn Williams, Khalid Ansari, Martin Osswald, Adetola B Adesida
Skin cancer and its associated treitments can have devastating consequences for survivors; this is particularly true when cancer occurs on the nose. Recent work has applied cell-based tissue engineering (TE) strategies to develop nasal cartilage constructs for reconstruction of the nose. In this study, we have generated human nasal cartilage on a clinically approved collagen scaffold to investigate the donor-to-donor variability of TE cartilage and evaluated strategies to mitigate it. We also evaluated the gene expression of the family of fibroblast growth factor receptors (FGFR1-4) and their association with tissue quality...
July 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28736639/promising-therapeutics-of-gastrointestinal-cancers-in-clinical-trials
#20
REVIEW
Lingling Du, Zheng Che, Andrea Wang-Gillam
Many novel therapeutics are being developed for patients with cancers along the gastrointestinal (GI) tract. These emerging agents are frequently classified by their biological targets such as tumor growth pathways, tumor metabolism, microenvironment, etc. Some agents targeting cancer growth pathways are based on existing clinically validated therapeutic targets, such as regorafenib for hepatocellular carcinoma (HCC), while other agents focus on newly identified targets, such as FGFR fusions in cholangiocarcinoma...
June 2017: Journal of Gastrointestinal Oncology
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