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VEGFR methylation

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https://www.readbyqxmd.com/read/30098869/design-synthesis-and-preclinical-evaluation-of-5-methyl-n-4-aryl-furo-2-3-d-pyrimidines-as-single-agents-with-combination-chemotherapy-potential
#1
Ravi Kumar Vyas Devambatla, Shruti Choudhary, Michael Ihnat, Ernest Hamel, Susan L Mooberry, Aleem Gangjee
The design, synthesis and biological evaluation of 4-substituted 5-methyl-furo[2,3-d]pyrimidines is described. The Ullmann coupling of 5-methyl-furo[2,3-d]pyrimidine with aryl iodides was successfully optimized to synthesize these analogs. Compounds 6-10 showed single-digit nanomolar inhibition of EGFR kinase. Compounds 1 and 6-10 inhibited VEGFR-2 kinase better than or equal to sunitinib. Compounds 1 and 3-10 were more potent inhibitors of PDGFR-β kinase than sunitinib. In addition, compounds 4-11 had higher potency in the CAM angiogenesis assay than sunitinib...
October 1, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/30016964/rna-sequencing-in-non-small-cell-lung-cancer-shows-gene-downregulation-of-therapeutic-targets-in-tumor-tissue-compared-to-non-malignant-lung-tissue
#2
Kobe Reynders, Els Wauters, Matthieu Moisse, Herbert Decaluwé, Paul De Leyn, Stéphanie Peeters, Maarten Lambrecht, Kristiaan Nackaerts, Christophe Dooms, Wim Janssens, Johan Vansteenkiste, Diether Lambrechts, Dirk De Ruysscher
BACKGROUND: Gene expression of specific therapeutic targets in non-malignant lung tissue might play an important role in optimizing targeted therapies. This study aims to identify different expression patterns of fifteen genes important for targeted therapy in non-small cell lung cancer (NSCLC). METHODS: We prospectively collected tissue of NSCLC and non-malignant lung tissue from 25 primary resected patients. RNA-sequencing and 450 K methylation array profiling was applied to both NSCLC and non-malignant lung tissue and data were analyzed for 14 target genes...
July 17, 2018: Radiation Oncology
https://www.readbyqxmd.com/read/29616369/treatment-response-assessment-with-r-11-cpaq-pet-in-the-mmtv-pymt-mouse-model-of-breast-cancer
#3
T Tegnebratt, L Lu, S Eksborg, A Chireh, P Damberg, S Nikkhou-Aski, T Foukakis, H Rundqvist, S Holmin, R V Kuiper, E Samen
BACKGROUND: The goal of the study was to assess the potential of the vascular endothelial growth factor receptor (VEGFR)-2-targeting carbon-11 labeled (R)-N-(4-bromo-2-fluorophenyl)-6-methoxy-7-((1-methyl-3-piperidinyl)methoxy)-4-quinazolineamine ((R)-[11 C]PAQ) as a positron emission tomography (PET) imaging biomarker for evaluation of the efficacy of anticancer drugs in preclinical models. METHODS: MMTV-PyMT mice were treated with vehicle alone (VEH), murine anti-VEGFA antibody (B20-4...
April 3, 2018: EJNMMI Research
https://www.readbyqxmd.com/read/29400470/the-discovery-of-n-1-methyl-5-trifluoromethyl-1h-pyrazol-3-yl-5-6-methylamino-methyl-pyrimidin-4-yl-oxy-1h-indole-1-carboxamide-acrizanib-a-vegfr-2-inhibitor-specifically-designed-for-topical-ocular-delivery-as-a-therapy-for-neovascular-age-related-macular
#4
Christopher M Adams, Karen Anderson, Gerald Artman, Jean-Claude Bizec, Rosemarie Cepeda, Jason Elliott, Elizabeth Fassbender, Malay Ghosh, Shawn Hanks, Leo A Hardegger, Vinayak P Hosagrahara, Bruce Jaffee, Keith Jendza, Nan Ji, Leland Johnson, Wendy Lee, Donglei Liu, Fang Liu, Debby Long, Fupeng Ma, Nello Mainolfi, Erik L Meredith, Karl Miranda, Yao Peng, Stephen Poor, James Powers, Yubin Qiu, Chang Rao, Siyuan Shen, Jeremy M Sivak, Catherine Solovay, Peter Tarsa, Amber Woolfenden, Chun Zhang, Yiqin Zhang
A noninvasive topical ocular therapy for the treatment of neovascular or "wet" age-related macular degeneration would provide a patient administered alternative to the current standard of care, which requires physician administered intravitreal injections. This manuscript describes a novel strategy for the use of in vivo models of choroidal neovascularization (CNV) as the primary means of developing SAR related to efficacy from topical administration. Ultimately, this effort led to the discovery of acrizanib (LHA510), a small-molecule VEGFR-2 inhibitor with potency and efficacy in rodent CNV models, limited systemic exposure after topical ocular administration, multiple formulation options, and an acceptable rabbit ocular PK profile...
February 22, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29328399/mir%C3%A2-378a-enhances-the-sensitivity-of-liver-cancer-to-sorafenib-by-targeting-vegfr-pdgfr%C3%AE-and-c%C3%A2-raf
#5
Hongxia Fu, Jicai Zhang, Tongshan Pan, Shuying Ai, Li Tang, Fengqin Wang
Liver cancer is a globally prevalent cancer with poor prognosis. The present study investigated the link between microRNA-378a (miR‑378a) expression and the sensitivity of hepatocellular carcinoma (HCC) and hepatoblastoma (HB) cancers to sorafenib therapy. miR‑378a expression was determined in liver tissue samples from healthy candidates and patients with liver cancer using the reverse transcription‑quantitative polymerase chain reaction. The antitumor effects of miR‑378a alone and in combination with sorafenib were investigated in the HB cell line HepG2 and the HCC cell line SMMC‑7721 with methyl thiazoyl tetrazolium, colony formation, flow cytometry and Transwell migration assays...
March 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29208290/synthesis-spectroscopic-thermal-and-molecular-modeling-studies-of-zn-2-cd-2-and-uo-2-2-complexes-of-schiff-bases-containing-triazole-moiety-antimicrobial-anticancer-antioxidant-and-dna-binding-studies
#6
Mohamed Gaber, Hoda A El-Ghamry, Shaimaa K Fathalla, Mohammed A Mansour
A novel series of Zn2+ , Cd2+ and UO2 2+ complexes of ligands namely 1-[(5-mercapto-1H-1,2,4-triazole-3-ylimino) methyl]naphthalene-2-ol (HL1 ) and [(1H-1,2,4-triazole-3-ylimino) methyl] naphthalene-2-ol (HL2 ) have been prepared and characterized by different analytical and spectral techniques. The stoichiometry, stereochemistry, conductivity measurements and mode of bonding of the complexes have been elucidated. Accurate comparison of the IR spectra of the ligands with their metal chelates proved the involvement of nitrogen atoms of the azomethine group and/or triazole ring in chelation in addition to the deprotonated hydroxyl oxygen...
February 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28774835/current-and-emerging-biomarkers-in-tumors-of-the-central-nervous-system-possible-diagnostic-prognostic-and-therapeutic-applications
#7
REVIEW
Ishaq N Khan, Najeeb Ullah, Deema Hussein, Kulvinder S Saini
Recent investments in research associated with the discovery of specific tumor biomarkers important for efficient diagnosis and prognosis are beginning to bear fruit. Key biomarkers could potentially outweigh traditional radiological or pathological methods by enabling specificity of early detection, when coupled with tumor molecular profiling and clinical associations. Only few biomarkers are approved by regulatory authorities for Central Nervous System Tumors (CNSTs), despite the evaluation of a large number of CNST related markers during clinical trials...
October 2018: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28736316/early-actions-of-anti-vascular-endothelial-growth-factor-vascular-endothelial-growth-factor-receptor-drugs-on-angiogenic-blood-vessels
#8
Basel Sitohy, Sunghee Chang, Tracey E Sciuto, Elizabeth Masse, Mei Shen, Peter M Kang, Shou-Ching Jaminet, Laura E Benjamin, Rupal S Bhatt, Ann M Dvorak, Janice A Nagy, Harold F Dvorak
Tumors induce their heterogeneous vasculature by secreting vascular endothelial growth factor (VEGF)-A. Anti-VEGF/VEGF receptor (VEGFR) drugs treat cancer, but the underlying mechanisms remain unclear. An adenovirus expressing VEGF-A (Ad-VEGF-A164 ) replicates the tumor vasculature in mice without tumor cells. Mother vessels (MV) are the first angiogenic vessel type to form in tumors and after Ad-VEGF-A164 . Multiday treatments with a VEGF trap reverted MV back to normal microvessels. We now show that, within hours, a single dose of several anti-VEGF drugs collapsed MV to form glomeruloid microvascular proliferations (GMP), accompanied by only modest endothelial cell death...
October 2017: American Journal of Pathology
https://www.readbyqxmd.com/read/28718364/evaluation-of-epigenetic-inactivation-of-vascular-endothelial-growth-factor-receptors-in-head-and-neck-squamous-cell-carcinoma
#9
Yuki Misawa, Kiyoshi Misawa, Hideya Kawasaki, Atsushi Imai, Daiki Mochizuki, Ryuji Ishikawa, Shiori Endo, Masato Mima, Takeharu Kanazawa, Toshihide Iwashita, Hiroyuki Mineta
The aim of this study was to determine the methylation status of the genes encoding the vascular endothelial growth factor receptors and to evaluate the usefulness of VEGFR methylation as a prognostic indicator in head and neck squamous cell carcinoma. VEGFR messenger RNA expression and promoter methylation were examined in a panel of cell lines via quantitative reverse transcription and methylation-specific polymerase chain reaction, respectively. Promoter methylation was compared with clinical characteristics in 128 head and neck squamous cell carcinoma samples...
July 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/28001118/the-expression-of-vegf-receptor-genes-is-concurrently-influenced-by-epigenetic-gene-silencing-of-the-genes-and-vegf-activation
#10
Jee Yeon Kim, Jun Ha Whang, Wei Zhou, Jieun Shin, Seung Moo Noh, In Sang Song, Ji Yeon Kim, Suk Hoon Lee, Jei Kim
Vascular endothelial growth factor (VEGF) activates the VEGF-VEGF receptor (VEGFR) signaling pathway in angiogenesis. Some cancer cell lines show decreased expression of the two VEGFRs, Flt-1 and KDR, even though VEGF is uniformly expressed in cancer cell lines. Promoter methylation is a well-known cause of epigenetic gene silencing in cancer cells. Although VEGF, Flt-1 and KDR have typical CpG islands in their promoter regions, the epigenetic transcriptional alterations of these genes have not yet been described...
July 1, 2009: Epigenetics: Official Journal of the DNA Methylation Society
https://www.readbyqxmd.com/read/27904083/novel-sulfonamide-derivatives-carrying-a-biologically-active-3-4-dimethoxyphenyl-moiety-as-vegfr-2-inhibitors
#11
Mostafa Mohammed Ghorab, Mansour Sulaiman Alsaid, Yassin Mohammed Nissan, Abdelkader Elbadawy Ashour, Abdullah Abdulalrahman Al-Mishari, Ashok Kumar, Sheikh Fayaz Ahmed
Novel sulfonamides 3-19 with a biologically active 3,4-dimethoxyphenyl moiety were designed and synthesized. The structures of the synthesized compounds were established using elemental analyses, IR, (1)H-NMR, (13)C-NMR spectral data and mass spectroscopy. All the synthesized compounds were evaluated for their in vitro anticancer activity against four cancer cell lines, namely human hepatocellular carcinoma (HepG2), human medulloblastoma (Daoy), human cervical cancer (HeLa), and human colon cancer (HT-29), by using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and dasatinib as the reference drug...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27688180/design-and-discovery-of-4-anilinoquinazoline-urea-derivatives-as-dual-tk-inhibitors-of-egfr-and-vegfr-2
#12
Hai-Qi Zhang, Fei-Hu Gong, Ji-Qing Ye, Chi Zhang, Xiao-Hong Yue, Chuan-Gui Li, Yun-Gen Xu, Li-Ping Sun
EGFR and VEGFR-2 are involved in pathological disorders and the progression of different kinds of tumors, the combined blockade of EGFR and VEGFR signaling pathways appears to be an attractive approach to cancer therapy. In this work, a series of 4-anilinoquinazoline derivatives containing substituted diaryl urea or glycine methyl ester moiety were designed and identified as EGFR and VEGFR-2 dual inhibitors. Compounds 19i, 19j and 19l exhibited the most potent inhibitory activities against EGFR (IC50 = 1 nM, 78 nM and 51 nM, respectively) and VEGFR-2 (IC50 = 79 nM, 14 nM and 14 nM, respectively), they showed good antiproliferative activities as well...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27236046/studies-on-some-metal-complexes-of-quinoxaline-based-unsymmetric-ligand-synthesis-spectral-characterization-in-vitro-biological-and-molecular-modeling-studies
#13
Chellaian Justin Dhanaraj, Jijo Johnson
Mononuclear Co(II), Ni(II), Cu(II) and Zn(II) complexes of an unsymmetric Schiff base ligand, 3-(-(3-(-3,5-dichloro-2-hydroxybenzylideneamino)propylimino)methyl)quinoxalin-2(1H) -one (L) were synthesized and characterized by various analytical and spectral techniques. The molar conductance values of metal complexes indicate non-electrolytic behavior of the metal complexes. The Schiff base act as tetra dentate ONNO donor ligand in Co(II), Ni(II), Zn(II) complexes and tridentate NNO donor in Cu(II) complex. Thermal stabilities of the newly synthesized compounds were determined by thermal analysis...
August 2016: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/27189674/retracted-design-synthesis-structure-activity-relationship-and-kinase-inhibitory-activity-of-substituted-3-methyl-1-phenyl-1h-pyrazolo-3-4-d-pyrimidin-4-ones
#14
Phoebe F Lamie
This article has been retracted: please see Elsevier Policy on Article Withdrawal (http://www.elsevier.com/locate/withdrawalpolicy). This article has been retracted at the request of the author who confirmed that the purity of some of the described compounds is below acceptable standards and thus the biochemical results reported in the paper have no validity.
July 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27018653/novel-application-assigned-to-toluquinol-inhibition-of-lymphangiogenesis-by-interfering-with-vegf-c-vegfr-3-signalling-pathway
#15
M García-Caballero, S Blacher, J Paupert, A R Quesada, M A Medina, A Noël
BACKGROUND AND PURPOSE: Lymphangiogenesis is an important biological process associated with the pathogenesis of several diseases, including metastatic dissemination, graft rejection, lymphoedema and other inflammatory disorders. The development of new drugs that block lymphangiogenesis has become a promising therapeutic strategy. In this study, we investigated the ability of toluquinol, a 2-methyl-hydroquinone isolated from the culture broth of the marine fungus Penicillium sp. HL-85-ALS5-R004, to inhibit lymphangiogenesis in vitro, ex vivo and in vivo...
June 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/26728997/regulation-of-soluble-flt-1-vegfr-1-production-by-hnrnp-d-and-protein-arginine-methylation
#16
Takayuki Ikeda, Yasuo Yoshitomi, Hidehito Saito, Takeo Shimasaki, Hideki Yamaya, Takashi Kobata, Yasuhito Ishigaki, Naohisa Tomosugi, Yoshino Yoshitake, Hideto Yonekura
Soluble fms-like tyrosine kinase-1 (sFlt-1) functions as a potent inhibitor of angiogenesis by trapping vascular endothelial growth factor (VEGF). However, the precise regulatory mechanism of sFlt-1 production is unknown. Here, we report that vascular sFlt-1 production is regulated by heterogeneous nuclear ribonucleoprotein D (hnRNP D) and arginine methylation. We showed that hnRNP D bound to Flt-1 pre-mRNA and that hnRNP D overexpression decreased sFlt-1 mRNA in human microvascular endothelial cells (HMVECs)...
February 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/26458588/the-role-of-the-vascular-endothelial-growth-factor-vascular-endothelial-growth-factor-receptors-axis-mediated-angiogenesis-in-curcumin-loaded-nanostructured-lipid-carriers-induced-human-hepg2-cells-apoptosis
#17
Fengling Wang, Zhengmin He, Wenting Dai, Qi Li, Xiuzhen Liu, Zhengsheng Zhang, Dandan Zhai, Jin Chen, Weidong Chen
BACKGROUND: Curcumin (diferuloylmethane), the active constituent of turmeric extract has potent anti-cancer properties have been demonstrated in hepatocellular carcinoma (HCC). However, its underlying molecular mechanism of therapeutic effects remains unclear. Vascular endothelial growth factor (VEGF) and its receptors (VEGFRs) have crucial roles in tumor angiogenesis. PURPOSE: The goal of this study was to investigate the role of the VEGF/VEGFRs mediated angiogenesis during the proliferation and apoptosis of human HepG2 hepatoma cell line and the effect of curcumin-loaded nanostructured lipid carriers (Cur-NLC)...
July 2015: Journal of Cancer Research and Therapeutics
https://www.readbyqxmd.com/read/26380584/decreased-efficacy-of-drugs-targeting-the-vascular-endothelial-growth-factor-pathway-by-the-epigenetic-silencing-of-flt1-in-renal-cancer-cells
#18
Jee Yeon Kim, Junha Hwang, Seo Hyun Lee, Hyo Jin Lee, Jaroslav Jelinek, Hyeseon Jeong, Jae Sung Lim, Jin Man Kim, Kyu Sang Song, Byung Hoon Kim, Sukhoon Lee, Jei Kim
BACKGROUND: The vascular endothelial growth factor (VEGF)-VEGF receptor (VEGFR) signaling pathway is involved in cancer-related biological functions and is a therapeutic target in cancer. However, the influence of epigenetic regulation of VEGF-VEGFR signaling-related genes remains unclear. Here, we evaluated the effects of FLT1 and KDR promoter hypermethylation combined with drugs targeting VEGF-VEGFR signaling on cancer-related phenotypes in renal cancer cells (RCCs) and examined changes in FLT1 and KDR promoter hypermethylation in tissues from patients with renal cancer...
2015: Clinical Epigenetics
https://www.readbyqxmd.com/read/26203967/impaired-endothelium-dependent-vasodilation-does-not-initiate-the-development-of-sunitinib-associated-hypertension
#19
Anna M J Thijs, Carla M L van Herpen, Vivienne Verweij, Jeanne Pertijs, Petra H H van den Broek, Winette T A van der Graaf, Gerard A Rongen
BACKGROUND: Tyrosine kinase inhibitors targeting angiogenesis have become an important part of the treatment of patients with several types of cancer. One of the most reported side effects of vascular endothelial growth factor receptor (VEGFR)-targeted therapies is hypertension. In this study, we hypothesized that the development of hypertension in patients treated with sunitinib, a multitargeted tyrosine kinase inhibitor, is preceded by reduced endothelium-dependent vasodilation. Moreover, we hypothesized that this endothelial dysfunction is a result of impaired nitric oxide release...
October 2015: Journal of Hypertension
https://www.readbyqxmd.com/read/25940601/rosuvastatin-improves-hepatopulmonary-syndrome-through-inhibition-of-inflammatory-angiogenesis-of-lung
#20
Ching-Chih Chang, Sun-Sang Wang, Hsian-Guey Hsieh, Wen-Shin Lee, Chiao-Lin Chuang, Han-Chieh Lin, Fa-Yauh Lee, Shou-Dong Lee, Hui-Chun Huang
The hepatopulmonary syndrome (HPS) is characterized by hypoxia and increased intrapulmonary shunts in cirrhotic patients. Emerging evidence showed promising results of treating HPS by abolishment of intrapulmonary inflammation and angiogenesis. Rosuvastatin is a kind of 3-hydroxy-methyl-3-glutamyl coenzyme A reductase inhibitor. In addition to lipid-lowering effects, it has anti-inflammation and anti-angiogenesis properties. We postulated that rosuvastatin treatment can ameliorate HPS. Common bile duct ligation (CBDL) was applied in an experimental HPS animal model...
September 2015: Clinical Science (1979-)
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