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https://www.readbyqxmd.com/read/29137286/fibroblast-growth-factor-modulates-mast-cell-recruitment-in-a-murine-model-of-prostate-cancer
#1
Roberto Ronca, Roberto Tamma, Daniela Coltrini, Simona Ruggieri, Marco Presta, Domenico Ribatti
Mast cells are important modifiers of prostate tumor microenvironment. The fibroblast growth factor/fibroblast growth factor receptor (FGF/FGFR) system plays a non-redundant autocrine/paracrine role in the growth, vascularization and progression of prostate tumors. Accordingly, the FGF antagonist long pentraxin-3 (PTX3) and the PTX3-derived small molecule FGF-trap NSC12 have been shown to inhibit the growth and vascularization of different FGF-dependent tumor types, including prostate cancer. In this study, we show that recombinant FGF2 is able to cause mast cell recruitment in vivo in the Matrigel plug assay...
October 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29101463/a-drug-drug-interaction-study-to-assess-the-effect-of-the-cyp1a2-inhibitor-fluvoxamine-on-the-pharmacokinetics-of-dovitinib-tki258-in-patients-with-advanced-solid-tumors
#2
Vincent A de Weger, Sanjay Goel, Roger von Moos, Jan H M Schellens, Nicholas Mach, Eugene Tan, Suraj Anand, Jeffrey W Scott, Ulrik Lassen
PURPOSE: Dovitinib is an orally available multi tyrosine kinase inhibitor which inhibits VEGFR 1-3, FGFR 1-3, and PDGFR. This study was performed to investigate the potential drug-drug interaction of dovitinib with the CYP1A2 inhibitor fluvoxamine in patients with advanced solid tumors. METHODS: Non-smoking patients of ≥ 18 years with advanced solid tumors, excluding breast cancer, were included. Patients were treated with a dose of 300 mg in 5 days on/2 days off schedule...
November 3, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29094049/diagnostic-predictive-prognostic-and-therapeutic-molecular-biomarkers-in-third-millennium-a-breakthrough-in-gastric-cancer
#3
REVIEW
Nicola Carlomagno, Paola Incollingo, Vincenzo Tammaro, Gaia Peluso, Niccolò Rupealta, Gaetano Chiacchio, Maria Laura Sandoval Sotelo, Gianluca Minieri, Antonio Pisani, Eleonora Riccio, Massimo Sabbatini, Umberto Marcello Bracale, Armando Calogero, Concetta Anna Dodaro, Michele Santangelo
Introduction: Gastric cancer is the fifth most common cancer and the third cause of cancer death. The clinical outcomes of the patients are still not encouraging with a low rate of 5 years' survival. Often the disease is diagnosed at advanced stages and this obviously negatively affects patients outcomes. A deep understanding of molecular basis of gastric cancer can lead to the identification of diagnostic, predictive, prognostic, and therapeutic biomarkers. Main Body: This paper aims to give a global view on the molecular classification and mechanisms involved in the development of the tumour and on the biomarkers for gastric cancer...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29071223/an-alignment-independent-3d-qsar-study-of-fgfr2-tyrosine-kinase-inhibitors
#4
Behzad Jafari, Maryam Hamzeh-Mivehroud, Ali Akbar Alizadeh, Mehdi Sharifi, Siavoush Dastmalchi
Purpose: Receptor tyrosine kinase (RTK) inhibitors are widely used pharmaceuticals in cancer therapy. Fibroblast growth factor receptors (FGFRs) are members of RTK superfamily which are highly expressed on the surface of carcinoma associate fibroblasts (CAFs). The involvement of FGFRs in different types of cancer makes them promising target in cancer therapy and hence, the identification of novel FGFR inhibitors is of great interest. In the current study we aimed to develop an alignment independent three dimensional quantitative structure-activity relationship (3D-QSAR) model for a set of 26 FGFR2 kinase inhibitors allowing the prediction of activity and identification of important structural features for these inhibitors...
September 2017: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29068468/expression-of-the-fgfr2c-mesenchymal-splicing-variant-in-human-keratinocytes-inhibits-differentiation-and-promotes-invasion
#5
Danilo Ranieri, Benedetta Rosato, Monica Nanni, Francesca Belleudi, Maria Rosaria Torrisi
The altered isoform switching of the fibroblast growth factor receptor 2 (FGFR2) and aberrant expression of the mesenchymal FGFR2c isoform in epithelial cells is involved in cancer progression. We have recently described that the ectopic expression of FGFR2c in normal human keratinocytes induces epithelial-mesenchymal transition and leads to invasiveness and anchorage-independent growth. Here we extended our analysis to the effects of this FGFR2c forced expression on human keratinocyte differentiation and stratification...
October 25, 2017: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/29067649/interplay-between-tgf-%C3%AE-signaling-and-receptor-tyrosine-kinases-in-tumor-development
#6
REVIEW
Qiaoni Shi, Ye-Guang Chen
Transforming growth factor-β (TGF-β) signaling regulates cell proliferation, differentiation, migration and death, and plays a critical role in embryogenesis and tissue homeostasis. Its deregulation results in various diseases including tumor formation. Receptor tyrosine kinases (RTKs), such as epidermal growth factor receptor (EGFR), fibroblast growth factor receptor (FGFR), vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR), also play key roles in the development and progression of many types of tumors...
October 23, 2017: Science China. Life Sciences
https://www.readbyqxmd.com/read/29061644/comprehensive-pharmacogenomic-profiling-of-malignant-pleural-mesothelioma-identifies-a-subgroup-sensitive-to-fgfr-inhibition
#7
Josine M Quispel-Janssen, Jitendra Badhai, Laurel Schunselaar, Stacey Price, Jonathan S Brammeld, Francesco Iorio, Krishna K Kolluri, Mathew J Garnett, Anton Berns, Paul Baas, Ultan McDermott, Jacques Neefjes, Constantine Alifrangis
PURPOSE: Despite intense research, treatment options for patients with mesothelioma are limited and offer only modest survival advantage. We screened a large panel of compounds in multiple mesothelioma models, and correlated sensitivity with a range of molecular features to detect biomarkers of drug response. EXPERIMENTAL DESIGN: We utilised a high-throughput chemical inhibitor screen in a panel of 889 cancer cell lines, including both immortalised and primary early passage mesothelioma lines, alongside comprehensive molecular characterisation using Illumina whole exome sequencing, copy number analysis and Affymetrix array whole transcriptome profiling...
October 23, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29048661/combination-of-fgfr4-inhibitor-blu9931-and-5-fluorouracil-effects-on-the-biological-characteristics-of-colorectal-cancer-cells
#8
Dongbao Jiang, Jingjing Li, Jie Li, Min Wang, Chao Han, Xinru Wang, Chunlin Zhao, Yanwei Ye
The aim of this study was to explore the effects of single agent treatments and combination of Blu9931 and 5-fluorouracil (5-FU) on the biological characteristics of colorectal cancer cells and its mechanism. Blu9931 is the first selective small molecule inhibitor of the fibroblast growth factor receptor 4 (FGFR4) and exquisitely selective for FGFR4 versus other FGFR family members and all other kinases. The colorectal cancer cells HCT116 and SW620 with high expression of FGFR4 were selected for a series of functional tests including cell viability, cell proliferation, apoptosis and cell cycle detection...
October 2, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/29017058/androgen-receptor-pathway-independent-prostate-cancer-is-sustained-through-fgf-signaling
#9
Eric G Bluemn, Ilsa M Coleman, Jared M Lucas, Roger T Coleman, Susana Hernandez-Lopez, Robin Tharakan, Daniella Bianchi-Frias, Ruth F Dumpit, Arja Kaipainen, Alexandra N Corella, Yu Chi Yang, Michael D Nyquist, Elahe Mostaghel, Andrew C Hsieh, Xiaotun Zhang, Eva Corey, Lisha G Brown, Holly M Nguyen, Kenneth Pienta, Michael Ittmann, Michael Schweizer, Lawrence D True, David Wise, Paul S Rennie, Robert L Vessella, Colm Morrissey, Peter S Nelson
Androgen receptor (AR) signaling is a distinctive feature of prostate carcinoma (PC) and represents the major therapeutic target for treating metastatic prostate cancer (mPC). Though highly effective, AR antagonism can produce tumors that bypass a functional requirement for AR, often through neuroendocrine (NE) transdifferentiation. Through the molecular assessment of mPCs over two decades, we find a phenotypic shift has occurred in mPC with the emergence of an AR-null NE-null phenotype. These "double-negative" PCs are notable for elevated FGF and MAPK pathway activity, which can bypass AR dependence...
October 9, 2017: Cancer Cell
https://www.readbyqxmd.com/read/29017052/cellular-origin-of-androgen-receptor-pathway-independent-prostate-cancer-and-implications-for-therapy
#10
W Nathaniel Brennen, John T Isaacs
In this issue of Cancer Cell, Bluemn et al. report that ∼20% of metastatic castration-resistant prostate cancers express neither AR nor neuroendocrine genes and show AR pathway-independent growth, driven instead by a FGFR/MAPK/ID1 signaling cascade. These results provide a strong rationale for co-targeting AR bypass pathways with initial AR antagonism.
October 9, 2017: Cancer Cell
https://www.readbyqxmd.com/read/28978722/acquired-resistance-to-fgfr-inhibitor-in-diffuse-type-gastric-cancer-through-an-akt-independent-pkc-mediated-phosphorylation-of-gsk3%C3%AE
#11
Wen Min Lau, Eileen Teng, Kie Kyon Huang, Jin Wei Tan, Kakoli Das, Zhijiang Zang, Tania Chia, Ming Teh, Koji Kono, Wei Peng Yong, Asim Shabbir, Amy Tay, Niam Sin Phua, Patrick Tan, Shing Leng Chan, Jimmy Bok Yan So
Preclinical models of diffuse type gastric cancer (DGC) that reliably predict clinical activity of novel compounds are lacking. To overcome the problem of poor tumor cellularity in DGC, we used cells from malignant ascites to establish diffuse type gastric cancer patient-derived xenograft (PDX) models that recapitulate the primary cancer. Cells in PDX model GAGA6 with FGFR2 amplification were sensitive to AZD4547, a potent FGFR inhibitor that is being clinically evaluated for FGFR-aberrant cancer types. Intermittent in vivo treatment of GAGA6 tumors with AZD4547 gave rise to PDX tumors with acquired resistance to AZD4547, GAGA6-R...
October 4, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28978721/the-irreversible-covalent-fibroblast-growth-factor-receptor-inhibitor-prn1371-exhibits-sustained-inhibition-of-fgfr-after-drug-clearance
#12
Eleni Venetsanakos, Ken A Brameld, Vernon T Phan, Erik Verner, Timothy D Owens, Yan Xing, Danny Tam, Jacob LaStant, Kwan Leung, Dane E Karr, Ronald J Hill, Mary E Gerritsen, David M Goldstein, Jens Oliver Funk, J Michael Bradshaw
An increasing number of cancers are known to harbor mutations, translocations, or amplifications in the fibroblast growth factor receptor (FGFR) family of kinases. The FGFR inhibitors evaluated in clinical trials to date have shown promise at treating these cancers. Here we describe PRN1371, an irreversible covalent inhibitor of FGFR1-4 targeting a cysteine within the kinase active site. PRN1371 demonstrated strong FGFR potency and excellent kinome-wide selectivity in a number of biochemical and cellular assays, including in various cancer cell lines exhibiting FGFR alterations...
October 4, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28975832/systemic-and-adjuvant-therapies-for-intrahepatic-cholangiocarcinoma
#13
Yun Shin Chun, Milind Javle
Intrahepatic cholangiocarcinoma represents the second most common primary liver cancer and is increasing in incidence. Most patients are diagnosed at an advanced, nonsurgical stage and only about 1 in 5 cases are surgically resectable. Despite surgery, the 5-year survival is low at only 30%. Multifocal, node- or margin-positive disease is at a higher risk of recurrence after resection. There is no level 1 evidence in support of postoperative adjuvant therapy. A recent adjuvant therapy phase III trial from the Partenariat de Recherche en Oncologie Digestive-Actions Concertées dans les Cancers Colo-Rectaux et Digestifs (PRODIGE) group reported no survival advantage with adjuvant gemcitabine and oxaliplatin therapy...
July 2017: Cancer Control: Journal of the Moffitt Cancer Center
https://www.readbyqxmd.com/read/28972963/a-phase-1-study-of-arq-087-an-oral-pan-fgfr-inhibitor-in-patients-with-advanced-solid-tumours
#14
K P Papadopoulos, B F El-Rayes, A W Tolcher, A Patnaik, D W Rasco, R D Harvey, P M LoRusso, J C Sachdev, G Abbadessa, R E Savage, T Hall, B Schwartz, Y Wang, J Kazakin, W L Shaib
BACKGROUND: ARQ 087 is an orally administered pan-FGFR inhibitor with multi-kinase activity. This Phase 1 study evaluated safety, pharmacokinetics, and pharmacodynamics of ARQ 087 and defined the recommended Phase 2 dose (RP2D). METHODS: Patients with advanced solid tumours received ARQ 087 administered initially at 25 mg every other day and dose-escalated from 25 to 425 mg daily (QD) continuous dosing. FGF19, 21, 23, and serum phosphate were assessed as potential biomarkers of target engagement...
October 3, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28968756/resistance-mediated-by-alternative-receptor-tyrosine-kinases-in-fgfr1-amplified-lung-cancer
#15
Yuta Adachi, Kazuyoshi Watanabe, Kenji Kita, Hidenori Kitai, Hiroshi Kotani, Yuki Sato, Naohiko Inase, Seiji Yano, Hiromichi Ebi
Fibroblast growth factor receptor 1 (FGFR1) amplification has been identified in 10-20% of patients with squamous non-small-cell lung cancer. Preclinical models showed promising activity of specific FGFR inhibitors, but early clinical trials showed that only a small fraction of patients with FGFR1-amplified lung cancer responded to FGFR inhibitors. These unsatisfactory results were partly explained by heterogeneous amplicons around the 8p11 genomic region, leading to false-positive amplification results. Furthermore, discrepancies in the gene amplification and protein expression of FGFR1 were also reported...
October 26, 2017: Carcinogenesis
https://www.readbyqxmd.com/read/28968431/breast-cancer-cell-derived-fibroblast-growth-factors-enhance-osteoclast-activity-and-contribute-to-the-formation-of-metastatic-lesions
#16
Kelly Aukes, Cynthia Forsman, Nicholas J Brady, Kristina Astleford, Nicholas Blixt, Deepali Sachdev, Eric D Jensen, Kim C Mansky, Kathryn L Schwertfeger
Fibroblast growth factors (FGFs) and their receptors (FGFRs) have been implicated in promoting breast cancer growth and progression. While the autocrine effects of FGFR activation in tumor cells have been extensively studied, little is known about the effects of tumor cell-derived FGFs on cells in the microenvironment. Because FGF signaling has been implicated in the regulation of bone formation and osteoclast differentiation, we hypothesized that tumor cell-derived FGFs are capable of modulating osteoclast function and contributing to growth of metastatic lesions in the bone...
2017: PloS One
https://www.readbyqxmd.com/read/28965421/safety-and-efficacy-of-nintedanib-for-the-treatment-of-metastatic-colorectal-cancer
#17
REVIEW
Maria Carmen Riesco-Martinez, Ana Sanchez-Torre, Rocio Garcia-Carbonero
Nintedanib (BIBF 1200) is an oral tyrosine kinase inhibitor that targets the vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR) and fibroblast growth factor (FGFR) receptors. It is approved in Europe in combination with docetaxel for patients with advanced lung adenocarcinoma who have progressed to first-line chemotherapy. However, its role in the treatment of metastatic colorectal cancer (mCRC) is uncertain. Recent results from the LUME-Colon 1 pivotal phase III trial showed only a marginal increase in progression free survival over placebo in refractory mCRC patients, with a toxicity profile similar to other antiangiogenic agents, and no benefit in overall survival...
November 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28945747/establishment-of-primary-mixed-cell-cultures-from-spontaneous-canine-mammary-tumors-characterization-of-classic-and-new-cancer-associated-molecules
#18
Luciana B Gentile, Marcia K Nagamine, Luiz R Biondi, Daniel S Sanches, Fábio Toyota, Tatiane M Giovani, Isis P de Jesus, Ivone I M da Fonseca, Nicolle Queiroz-Hazarbassanov, Bruno L Diaz, Cristina de O Massoco Salles Gomes, Maria Lucia Z Dagli
There are many factors which make canine cancer like cancer in humans. The occurrence of spontaneous mammary tumors in pet dogs, tumor genetics, molecular targets and exposure to the same environmental risk factors are among these factors. Therefore, the study of canine cancer can provide useful information to the oncology field. This study aimed to establish and characterize a panel of primary mixed cell cultures obtained from spontaneous canine mammary tumors. Eight established cell cultures obtained from one normal mammary gland, one complex adenoma, one mixed adenoma, two complex carcinomas and two mixed carcinomas were analyzed...
2017: PloS One
https://www.readbyqxmd.com/read/28938491/inhibition-of-fgfr-signaling-partially-rescues-hypophosphatemic-rickets-in-hmwfgf2-tg-male-mice
#19
Liping Xiao, Erxia Du, Collin Homer-Bouthiette, Marja M Hurley
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 hypophosphatemic rickets. Because HMWFGF2 was upregulated in bones of Hyp mice and abnormal FGF receptor (FGFR) signaling is important in XLH, HMWTg mice were used to examine the effect of the FGFR inhibitor NVP-BGJ398, now in clinical trials for cancer therapy, on hypophosphatemic rickets...
October 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28930565/role-of-fibroblast-growth-factor-receptor-2-splicing-in-normal-and-cancer-cells
#20
Toshiyuki Ishiwata
Types 1-4 of fibroblast growth factor receptors (FGFR) are all expressed in various cancers. Because of its prominent role in carcinogenesis and cancer progression, FGFR-2, is being considered as a novel target in cancer treatment. Owing to the alternative splicing of its extracellular domain, FGFR-2 exists in two variants: IIIb and IIIc. FGFR-2 IIIb is mainly expressed in normal epithelial cells, as well as in oral mucosal, esophageal, gastric, colorectal, pancreatic, pulmonary, breast, endometrial, cervical, and prostate cancers...
January 1, 2018: Frontiers in Bioscience (Landmark Edition)
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