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https://www.readbyqxmd.com/read/29150606/loss-of-hif-1%C3%AE-in-natural-killer-cells-inhibits-tumour-growth-by-stimulating-non-productive-angiogenesis
#1
Ewelina Krzywinska, Chahrazade Kantari-Mimoun, Yann Kerdiles, Michal Sobecki, Takayuki Isagawa, Dagmar Gotthardt, Magali Castells, Johannes Haubold, Corinne Millien, Thomas Viel, Bertrand Tavitian, Norihiko Takeda, Joachim Fandrey, Eric Vivier, Veronika Sexl, Christian Stockmann
Productive angiogenesis, a prerequisite for tumour growth, depends on the balanced release of angiogenic and angiostatic factors by different cell types within hypoxic tumours. Natural killer (NK) cells kill cancer cells and infiltrate hypoxic tumour areas. Cellular adaptation to low oxygen is mediated by Hypoxia-inducible factors (HIFs). We found that deletion of HIF-1α in NK cells inhibited tumour growth despite impaired tumour cell killing. Tumours developing in these conditions were characterised by a high-density network of immature vessels, severe haemorrhage, increased hypoxia, and facilitated metastasis due to non-productive angiogenesis...
November 17, 2017: Nature Communications
https://www.readbyqxmd.com/read/29146618/management-of-adverse-events-associated-with-cabozantinib-therapy-in-renal-cell-carcinoma
#2
REVIEW
Manuela Schmidinger, Romano Danesi
Cabozantinib was recently approved for the treatment of advanced renal cell carcinoma (RCC) after treatment with vascular endothelial growth factor (VEGF)-targeted therapy. Cabozantinib is a multikinase inhibitor targeting VEGF receptor (VEGFR) 2, mesenchymal-epithelial transition receptor, and "anexelekto" receptor tyrosine kinase. A 60-mg daily dose led to improved overall survival and progression-free survival (PFS) versus everolimus in advanced RCC patients as a second- or later-line treatment in the METEOR trial...
November 16, 2017: Oncologist
https://www.readbyqxmd.com/read/29146452/design-synthesis-and-biological-evaluation-of-thieno-2-3-d-pyrimidine-derivatives-as-novel-dual-c-met-and-vegfr-2-kinase-inhibitors
#3
Jieming Li, Weijie Gu, Xinzhou Bi, Huilan Li, Chen Liao, Chunxia Liu, Wenlong Huang, Hai Qian
Both c-Met and VEGFR-2 are important targets for cancer therapies. Here we report a series of potent dual c-Met and VEGFR-2 inhibitors bearing thieno[2,3-d]pyrimidine scaffold. The cell proliferation assay in vitro demonstrated that most target compounds had inhibition potency both on c-Met and VEGFR-2 with IC50 values in nanomolar range, especially compound 12j and 12m. Based on the further enzyme assay in vitro, compound 12j was considered as the most potent one, the IC50 values of which were 25 nM and 48 nM for c-Met and VEGFR-2, respectively...
November 4, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29143774/disrupting-vegf-vegfr1-interaction-de-novo-designed-linear-helical-peptides-to-mimic-the-vegf13-25-fragment
#4
Beatriz Balsera, M Ángeles Bonache, Marie Reille-Seroussi, Nathalie Gagey-Eilstein, Michel Vidal, Rosario González-Muñiz, María Jesús Pérez de Vega
The interaction between vascular endothelial growth factor (VEGF) and its receptors (VEGFR) has important implications in angiogenesis and cancer, which moved us to search for peptide derivatives able to block this protein-protein interaction. In a previous work we had described a collection of linear 13-mer peptides specially designed to adopt helical conformations (Ac-SSEEX⁵ARNX⁸AAX(12)N-NH₂), as well as the evaluation of seven library components for the inhibition of the interaction of VEGF with its Receptor 1 (VEGFR1)...
October 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29140979/ginsenoside-rg3-inhibits-angiogenesis-in-a-rat-model-of-endometriosis-through-the-vegfr-2-mediated-pi3k-akt-mtor-signaling-pathway
#5
Yang Cao, Qing Ye, Mengfei Zhuang, Shuwu Xie, Ruihua Zhong, Jingang Cui, Jieyun Zhou, Yan Zhu, Tingting Zhang, Lin Cao
OBJECTIVE: This study aimed to investigate the link between the inhibitory effect of ginsenoside Rg3 on the ectopic endometrium growth and the VEGFR-2-mediated PI3K/Akt/mTOR signaling pathway, a mechanism known to inhibit angiogenesis and induce ectopic endometrial cell apoptosis. MATERIALS AND METHODS: A model of endometriosis was established by allotransplantation in rats. The rats were randomly divided into 5 groups: the ginsenoside Rg3 low-dose group (group A,5mg/kgBW/d of ginsenoside Rg3), the ginsenoside Rg3 high-dose group (group B, 10mg/kgBW/d of ginsenoside Rg3), the gestrinone group (group C, 0...
2017: PloS One
https://www.readbyqxmd.com/read/29137048/apatinib-for-the-treatment-of-pulmonary-epithelioid-hemangioendothelioma-a-case-report-and-literature-review
#6
Zhipeng Zheng, Hanying Wang, Hanliang Jiang, Enguo Chen, Jun Zhang, Xinyou Xie
RATIONALE: Pulmonary epithelioid hemangioendothelioma (P-EHE) is a rare tumor, with no established standard treatment. Overexpression of vascular endothelial growth factor receptor 2 (VEGFR-2) has been reported in some P-EHE patients. Apatinib, a new small molecule tyrosine kinase inhibitor that specifically targets VEGFR-2, has therapeutic benefits in some advanced tumors. However, its efficacy in P-EHE cases has not been reported. PATIENT CONCERNS: Herein, we presented a 44-year-old man with recurrent hemoptysis for approximately 9 years...
November 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29137038/quantification-of-stat3-and-vegf-expression-for-molecular-diagnosis-of-lymph-node-metastasis-in-breast-cancer
#7
Yujuan Chen, Ya Liu, Yu Wang, Wen Li, Xiaolu Wang, Xuejuan Liu, Yao Chen, Chibin Ouyang, Jing Wang
BACKGROUND: Axillary lymph node metastasis is associated with increased risk of regional recurrence, distant metastasis, and poor survival in breast malignant neoplasm. Expression of signal transducer and activator of transcription 3 (STAT3) is significantly associated with tumor formation, migration, and invasion in various cancers. In addition, vascular endothelial growth factor (VEGF) expression could promote angiogenesis and increase the risk of tumorigenesis. To determine correlations among STAT3 expression, VEGF, and clinicopathological data on lymph node involvement in breast cancer patients after surgery...
November 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29133058/design-and-synthesis-of-thienopyrimidine-urea-derivatives-with-potential-cytotoxic-and-pro-apoptotic-activity-against-breast-cancer-cell-line-mcf-7
#8
Eman F Abdelhaleem, Mohammed K Abdelhameid, Asmaa E Kassab, Manal M Kandeel
A series of novel tetrahydrobenzothieno[2,3-d]pyrimidine urea derivatives was synthesized according to fragment-based design strategy. They were evaluated for their anticancer activity against MCF-7 cell line. Three compounds 9c, 9d and 11b showed 1.5-1.03 folds more potent anticancer activity than doxorubicin. In this study, a promising multi-sited enzyme small molecule inhibitor 9c, which showed the most potent anti-proliferative activity, was identified. The anti-proliferative activity of this compound appears to correlate well with its ability to inhibit topoisomerase II (IC50 = 9...
October 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29131379/design-synthesis-molecular-docking-and-anticancer-activity-of-phthalazine-derivatives-as-vegfr-2-inhibitors
#9
Abdel-Ghany A El-Helby, Rezk R A Ayyad, Helmy Sakr, Khaled El-Adl, Mamdouh M Ali, Fathalla Khedr
Novel series of phthalazine derivatives 6-11 were designed, synthesized, and evaluated for their anticancer activity against two human tumor cell lines, HCT-116 human colon adenocarcinoma and MCF-7 breast cancer cells, targeting the VEGFR-2 enzyme. Compounds 7a,b and 8b,c showed the highest anticancer activities against both HCT116 human colon adenocarcinoma cells with IC50 of 6.04 ± 0.30, 13.22 ± 0.22, 18 ± 0.20, and 35 ± 0.45 μM, respectively, and MCF-7 breast cancer cells with IC50 of 8...
November 13, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29128359/ubiquitin-c-terminal-hydrolase-l1-plays-a-key-role-in-angiogenesis-by-regulating-hydrogen-peroxide-generated-by-nadph-oxidase-4
#10
In-Kang Song, Hyun Jung Kim, Venkataraman Magesh, Kong-Joo Lee
Ubiquitin C-terminal hydrolase-L1 (UCH-L1), which catalyzes the hydrolysis of ubiquitin esters and amides, is highly expressed in brain. Recently, UCH-L1 has been found to increase cancer cell migration and invasion by modulating hydrogen peroxide generated by NADPH oxidase 4 (NOX4). Because angiogenesis is also mediated by hydrogen peroxide, we explored the role of UCH-L1 in angiogenesis in human umbilical vein endothelial cells (HUVECs). Silencing UCH-L1 suppressed tubule formation in HUVECs, indicating that UCH-L1 promotes angiogenesis in vitro...
November 8, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29123118/substrate-microarchitecture-shapes-the-paracrine-crosstalk-of-stem-cells-with-endothelial-cells-and-osteoblasts
#11
Francisco Martín-Saavedra, Lara Crespo, Clara Escudero-Duch, Laura Saldaña, Enrique Gómez-Barrena, Nuria Vilaboa
We examined the hypothesis that substrate microarchitecture regulates the crosstalk between human mesenchymal stem cells (hMSC) and cell types involved in bone regeneration. Compared with polyester flat substrates having uniformly distributed homogenous pores (2D), three-dimensional polystyrene substrates with randomly oriented and interconnected pores of heterogeneous size (3D) stimulated the stromal secretion of IGF-1 while lessened the production of VEGFR-1, MCP-1 and IL-6. The medium conditioned by hMSC cultured in 3D substrates stimulated tube formation by human endothelial cells (hEC) to a higher extent than medium from 2D cultures...
November 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29122006/single-nucleotide-polymorphisms-in-the-angiogenic-and-lymphangiogenic-pathways-are-associated-with-lymphedema-caused-by-wuchereria-bancrofti
#12
Linda Batsa Debrah, Anna Albers, Alexander Yaw Debrah, Felix F Brockschmidt, Tim Becker, Christine Herold, Andrea Hofmann, Jubin Osei-Mensah, Yusif Mubarik, Holger Fröhlich, Achim Hoerauf, Kenneth Pfarr
BACKGROUND: Lymphedema (LE) is a chronic clinical manifestation of filarial nematode infections characterized by lymphatic dysfunction and subsequent accumulation of protein-rich fluid in the interstitial space-lymphatic filariasis. A number of studies have identified single nucleotide polymorphisms (SNPs) associated with primary and secondary LE. To assess SNPs associated with LE caused by lymphatic filariasis, a cross-sectional study of unrelated Ghanaian volunteers was designed to genotype SNPs in 285 LE patients as cases and 682 infected patients without pathology as controls...
November 9, 2017: Human Genomics
https://www.readbyqxmd.com/read/29113263/artesunate-inhibits-proliferation-and-invasion-of-mouse-hemangioendothelioma-cells-in-vitro-and-of-tumor-growth-in-vivo
#13
Ning Wang, Hongxia Chen, Yinping Teng, Xionghui Ding, Huan Wu, Xianqing Jin
Artesunate has been demonstrated to be a novel potential antitumor agent in numerous studies. However, its efficacy in infantile hemangioma is unknown. The aim of the present study was to investigate the role of artesunate in the control of vascular tumor biological behavior and molecular mechanism using mouse hemangioendothelioma endothelial (EOMA) cells and a nude mouse model. Cell viability, apoptosis and invasion were determined by an MTT assay, flow cytometric analysis and Transwell invasion assay, respectively...
November 2017: Oncology Letters
https://www.readbyqxmd.com/read/29107421/discovery-of-novel-pyrrolo-pyridine-pyrimidine-derivatives-bearing-pyridazinone-moiety-as-c-met-kinase-inhibitors
#14
Lin Xiao Wang, Xiaobo Liu, Shan Xu, Qidong Tang, Yongli Duan, Zhen Xiao, Jia Zhi, Liwen Jiang, Pengwu Zheng, Wufu Zhu
In continue to our previous research, eight series of pyrrolo[2,3-b]pyridine and pyrrolo[2,3-d]pyrimidine derivatives bearing pyridazinone moiety were designed, synthesized, and the in vitro antitumor activity was evaluated against four cancer cell lines (A549, HepG2, MCF-7 and PC-3). Some selected compounds (22f, 22g, 26c and 26e) were evaluated for the activity against c-Met kinase, and according to the results of kinase inhibitory activity, the compound 22g was further evaluated for other four tyrosine kinases (Flt-3, VEGFR-2, c-Kit and EGFR) to test the enzyme-based selectivity...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29104145/the-dual-effects-of-a-novel-peptibody-on-angiogenesis-inhibition-and-m2-macrophage-polarization-on-sarcoma
#15
Xiaoqing Zhu, Jiali Yang, Yanfeng Gao, Chunjing Wu, Lili Yi, Guodong Li, Yuanming Qi
Inhibition of the VEGF/VEGF receptor (VEGFR) and angiopoietin-2 (Ang-2)/TEK receptor tyrosine kinase (Tie-2) pathway is a potential target for tumor angiogenesis. We previously showed that a peptide AS16 which dually inhibits VEGFR/Ang-2 could reduce the tumor growth and decrease the number of microvessels in tumor. However, its short circulating half-life in the serum limits its clinical applications. In this study, as an effort to prolong the short in vivo half-life of AS16, we designed a fusion protein containing peptide AS16 and an IgG Fc fragment...
November 2, 2017: Cancer Letters
https://www.readbyqxmd.com/read/29103026/effect-of-minocycline-on-vascular-proliferation-after-corneal-alkaline-burn-a-mechanism-study
#16
Haijun Wu, Xin Dai, Hui Li, Chunying Lv
Impairment of vision or blindness always occurs in the progress of corneal neovascularization (CNV). CNV may cause corneal graft rejection at corneal transplant status. Thus, intervention of CNV is of concern to clinical treatment. Given minocycline was reported with inhibiting effect on CNV, our study was focused on specific effect of minocycline on CNV after corneal alkaline burn. Seventy-five male Sprague Dawley rats were randomly assigned into three groups with an equal number (25). Sodium hydroxide (NaOH) solution was used to establish corneal alkaline burn model...
October 20, 2017: Cancer Biomarkers: Section A of Disease Markers
https://www.readbyqxmd.com/read/29102175/discovery-of-novel-anti-angiogenesis-agents-part-7-multitarget-inhibitors-of-vegfr-2-tie-2-and-ephb4
#17
Chuansheng Li, Yuanyuan Shan, Ying Sun, Ru Si, Liyuan Liang, Xiaoyan Pan, Binghe Wang, Jie Zhang
Herein, we embarked on a structural optimization campaign aiming at the discovery of second generation anti-angiogenesis agents with our previously reported BPS-7 as lead compound. A library of 27 compounds has been afforded based on the highly conserved ATP-binding pocket of VEGFR-2, Tie-2, and EphB4. Several title compounds exhibited simultaneous inhibitory effects against three angiogenic RTKs. These compounds with a 'triplet' inhibition profile have been identified as novel anti-angiogenic and anticancer agents...
December 1, 2017: European Journal of Medicinal Chemistry
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
#18
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/29095088/vegf-a121a-binding-to-neuropilins-a-concept-revisited
#19
Sarvenaz Sarabipour, Feilim Mac Gabhann
All known splice isoforms of vascular endothelial growth factor A (VEGF-A) can bind to the receptor tyrosine kinases VEGFR-1 and VEGFR-2. We focus here on VEGF-A121a and VEGF-A165a, two of the most abundant VEGF-A splice isoforms in human tissue (1) , and their ability to bind the Neuropilin co-receptors NRP1 and NRP2. The Neuropilins are key vascular, immune, and nervous system receptors on endothelial cells, neuronal axons, and regulatory T cells respectively. They serve as co-receptors for the Plexins in Semaphorin binding on neuronal and vascular endothelial cells, and for the VEGFRs in VEGF binding on vascular and lymphatic endothelial cells, and thus regulate the initiation and coordination of cell signaling by Semaphorins and VEGFs...
November 2, 2017: Cell Adhesion & Migration
https://www.readbyqxmd.com/read/29095068/pro-angiogenic-gene-expression-is-associated-with-better-outcome-on-sunitinib-in-metastatic-clear-cell-renal-cell-carcinoma
#20
Benoit Beuselinck, Annelies Verbiest, Gabrielle Couchy, Sylvie Job, Aurélien de Reynies, Clément Meiller, Maarten Albersen, Virginie Verkarre, Evelyne Lerut, Arnaud Méjean, Jean-Jacques Patard, Brigitte Laguerre, Nathalie Rioux-Leclercq, Patrick Schöffski, Stéphane Oudard, Jessica Zucman-Rossi
OBJECTIVES: Clear-cell renal cell carcinomas (ccRCC) are characterized by hyper-vascularization and can respond to vascular endothelial growth factor receptor (VEGFR) inhibitors such as sunitinib. We aimed to study the predictive value of the expression of genes in the hypoxia induced factor (HIF) - vascular endothelial growth factor (VEGF) - VEGFR-pro-angiogenic pathway in metastatic ccRCC (m-ccRCC) patients treated with sunitinib and the correlation between the expression of these genes and the molecular ccrcc-classification, the expression of genes involved in the immune-suppressive microenvironment and Von Hippel-Lindau (VHL) - and Polybromo-1 (PBRM1) - mutational status...
November 2, 2017: Acta Oncologica
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