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EPHA2

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https://www.readbyqxmd.com/read/29138859/17%C3%AE-estradiol-attenuates-ovariectomy%C3%A2-induced-bone-deterioration-through-the-suppression-of-the-epha2-ephrina2-signaling-pathway
#1
Lianyong Liu, Lin Zhou, Xiaorong Yang, Qi Liu, Ling Yang, Chao Zheng, Yongling Zhao, Zhenlin Zhang, Xiaohong Luo
The present study aimed to investigate whether 17β‑estradiol (E2) exerts protective effects on bone deterioration induced by ovariectomy (OVX) through the ephA2/ephrinA2 signaling pathway in rats. Female rats were subjected to OVX, sham surgeryor OVX+E2 treatment. Levels of biomarkers were measured in serum and urine. Hematoxylin and eosin staining was performed on paraffin‑embedded bone sections. Expression of genes and proteins was analyzed by reverse transcription‑quantitative polymerase chain reaction and western blotting, respectively...
November 14, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29133884/epha2-is-an-epithelial-cell-pattern-recognition-receptor-for-fungal-%C3%AE-glucans
#2
Marc Swidergall, Norma V Solis, Michail S Lionakis, Scott G Filler
Oral epithelial cells discriminate between pathogenic and non-pathogenic stimuli, and only induce an inflammatory response when they are exposed to high levels of a potentially harmful microorganism. The pattern recognition receptors (PRRs) in epithelial cells that mediate this differential response are poorly understood. Here, we demonstrate that the ephrin type-A receptor 2 (EphA2) is an oral epithelial cell PRR that binds to exposed β-glucans on the surface of the fungal pathogen Candida albicans. Binding of C...
November 13, 2017: Nature Microbiology
https://www.readbyqxmd.com/read/29132013/chimeric-antigen-receptor-modified-t-cells-redirected-to-epha2-for-the-immunotherapy-of-non-small-cell-lung-cancer
#3
Ning Li, Shaohui Liu, Mingjiao Sun, Wei Chen, Xiaogang Xu, Zhu Zeng, Yemin Tang, Yongquan Dong, Alex H Chang, Qiong Zhao
Erythropoietin-producing hepatocellular carcinoma A2 (EphA2) is overexpressed in more than 90% of non-small cell lung cancer (NSCLC) but not significantly in normal lung tissue. It is therefore an important tumor antigen target for chimeric antigen receptors (CAR)-T-based therapy in NSCLC. Here, we developed a specific CAR targeted to EphA2, and the anti-tumor effects of this CAR were investigated. A second generation CAR with co-stimulatory receptor 4-1BB targeted to EphA2 was developed. The functionality of EphA2-specific T cells in vitro was tested with flow cytometry and real-time cell electronic sensing system assays...
November 10, 2017: Translational Oncology
https://www.readbyqxmd.com/read/29129483/pharmacological-evaluation-of-new-bioavailable-small-molecules-targeting-eph-ephrin-interaction
#4
Carmine Giorgio, Matteo Incerti, Miriam Corrado, Marco Rusnati, Paola Chiodelli, Simonetta Russo, Donatella Callegari, Francesca Ferlenghi, Vigilio Ballabeni, Elisabetta Barocelli, Alessio Lodola, Massimiliano Tognolini
Eph/ephrin system is an emerging target for cancer therapy but the lack of potent, stable and orally bioavailable compounds is impairing the development of the field. Since 2009 our research group has been devoted to the discovery and development of small molecules targeting Eph/ephrin system and our research culminated with the synthesis of UniPR129, a potent but problematic Eph/ephrin antagonist. Herein, we describe the in vitro pharmacological properties of two derivatives (UniPR139 and UniPR502) stemmed from structure of UniPR129...
November 9, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29128116/design-and-synthesis-of-small-molecule-agonists-of-epha2-receptor
#5
Aaron Petty, Nethrie Idippily, Viharika Bobba, Werner J Geldenhuys, Bo Zhong, Bin Su, Bingcheng Wang
Ligand-independent activation of EphA2 receptor kinase promotes cancer metastasis and invasion. Activating EphA2 receptor tyrosine kinase with small molecule agonist is a novel strategy to treat EphA2 overexpressing cancer. In this study, we performed a lead optimization of a small molecule Doxazosin that was identified as an EphA2 receptor agonist. 33 new analogs were developed and evaluated; a structure-activity relationship was summarized based on the EphA2 activation of these derivatives. Two new derivative compounds 24 and 27 showed much improved activity compared to Doxazosin...
October 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29111705/one-bead-two-compound-thioether-bridged-macrocyclic-%C3%AE-aapeptide-screening-library-against-epha2
#6
Yan Shi, Sridevi Challa, Peng Sang, Fengyu She, Chunpu Li, Geoffrey M Gray, Alekhya Nimmagadda, Peng Teng, Timothy Odom, Yan Wang, Arjan van der Vaart, Qi Li, Jianfeng Cai
Identification of molecular ligands that recognize peptides or proteins is significant but poses a fundamental challenge in chemical biology and biomedical sciences. Development of cyclic peptidomimetic library is scarce, and thus discovery of cyclic peptidomimetic ligands for protein targets is rare. Herein we report the unprecedented one-bead-two-compound (OBTC) combinatorial library based on a novel class of the macrocyclic peptidomimetics γ-AApeptides. In the library, we utilized the coding peptide tags synthesized with Dde-protected α-amino acids, which were orthogonal to solid phase synthesis of γ-AApeptides...
November 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29110283/epha2-targeted-doxorubicin-nanoliposomes-for-osteosarcoma-treatment
#7
Fateme Haghiralsadat, Ghasem Amoabediny, Samira Naderinezhad, Kamran Nazmi, Jantine Posthuma De Boer, Behrouz Zandieh-Doulabi, Tymour Forouzanfar, Marco N Helder
PURPOSE: To employ Doxorubicin-loaded liposomes, modified with YSA-peptide to target EphA2, to reduce adverse effects against primary bone cells and maximize toxicity against Saos-2 osteosarcoma cells. METHODS: PEGylated liposomes were prepared by thin film method using Dipalmitoylphosphatidylcholine (DPPC), cholesterol and distearylphosphatidylethanolamine-polyethyleneglycol conjugate (DSPE-mPEG) in 67.9:29.1:3 M ratios, and loaded with DOX (L-DOX) by pH-gradient method...
November 6, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/29072678/specific-detection-of-soluble-epha2-fragments-in-blood-as-a-new-biomarker-for-pancreatic-cancer
#8
Naohiko Koshikawa, Tomoko Minegishi, Hirofumi Kiyokawa, Motoharu Seiki
Because membrane type 1-matrix metalloproteinase 1 (MT1-MMP) and erythropoietin-producing hepatocellular receptor 2 (EphA2) expression are upregulated by the Ras/mitogen-activated protein kinase pathway, they are frequently coexpressed in malignant tumors. MT1-MMP cleaves the N-terminal ligand-binding domain of EphA2 and inactivates its ligand-dependent tumor-suppressing activity. Therefore, specific detection of the cleaved N-terminal EphA2 fragment in blood might be an effective biomarker to diagnose malignant tumors...
October 26, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/29067091/identifying-key-genes-in-glaucoma-based-on-a-benchmarked-dataset-and-the-gene-regulatory-network
#9
Xi Chen, Qiao-Ling Wang, Meng-Hui Zhang
The current study aimed to identify key genes in glaucoma based on a benchmarked dataset and gene regulatory network (GRN). Local and global noise was added to the gene expression dataset to produce a benchmarked dataset. Differentially-expressed genes (DEGs) between patients with glaucoma and normal controls were identified utilizing the Linear Models for Microarray Data (Limma) package based on benchmarked dataset. A total of 5 GRN inference methods, including Zscore, GeneNet, context likelihood of relatedness (CLR) algorithm, Partial Correlation coefficient with Information Theory (PCIT) and GEne Network Inference with Ensemble of Trees (Genie3) were evaluated using receiver operating characteristic (ROC) and precision and recall (PR) curves...
October 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29048432/silencing-fli-or-targeting-cd13-anpep-lead-to-dephosphorylation-of-epha2-a-mediator-of-braf-inhibitor-resistance-and-induce-growth-arrest-or-apoptosis-in-melanoma-cells
#10
Alireza Azimi, Rainer Tuominen, Fernanda Costa Svedman, Stefano Caramuta, Maria Pernemalm, Marianne Frostvik Stolt, Lena Kanter, Pedram Kharaziha, Janne Lehtiö, Carolina Hertzman Johansson, Veronica Höiom, Johan Hansson, Suzanne Egyhazi Brage
A majority of patients with BRAF-mutated metastatic melanoma respond to therapy with BRAF inhibitors (BRAFi), but relapses are common owing to acquired resistance. To unravel BRAFi resistance mechanisms we have performed gene expression and mass spectrometry based proteome profiling of the sensitive parental A375 BRAF V600E-mutated human melanoma cell line and of daughter cell lines with induced BRAFi resistance. Increased expression of two novel resistance candidates, aminopeptidase-N (CD13/ANPEP) and ETS transcription factor FLI1 was observed in the BRAFi-resistant daughter cell lines...
August 31, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/29039721/a-recurrent-splice-site-mutation-in-epha2-causing-congenital-posterior-nuclear-cataract
#11
Vanita Berry, Nikolas Pontikos, Monica Albarca-Aguilera, Vincent Plagnol, Andreas Massouras, DeQuincy Prescott, Anthony T Moore, Gavin Arno, Michael E Cheetham, Michel Michaelides
Intoduction: Inherited cataract, opacification of the lens, is the most common worldwide cause of blindness in children. We aimed to identify the genetic cause of autosomal dominant (AD) posterior nuclear cataract in a four generation British family. METHODS: Whole genome sequence (WGS) was performed on two affected and one unaffected individual of the family and further validated by direct sequencing. Haplotype analysis was performed via genotying. RESULTS: A splice-site mutation c...
October 17, 2017: Ophthalmic Genetics
https://www.readbyqxmd.com/read/29029445/microrna-200c-increases-radiosensitivity-of-human-cancer-cells-with-activated-egfr-associated-signaling
#12
Taeryool Koo, Bong Jun Cho, Dan Hyo Kim, Ji Min Park, Eun Jung Choi, Hans H Kim, David J Lee, In Ah Kim
MicroRNA-200c (miR-200c) recently was found to have tumor-suppressive properties by inhibiting the epithelial-mesenchymal transition (EMT) in several cancers. miR-200c also interacts with various cellular signaling molecules and regulates many important signaling pathways. In this study, we investigated the radiosensitizing effect of miR-200c and its mechanism in a panel of human cancer cell lines. Malignant glioma (U251, T98G), breast cancer (MDA-MB-468), and lung carcinoma (A549) cells were transfected with control pre-microRNA, pre-miR-200c, or anti-miR-200c...
September 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29024629/the-role-of-wt1-isoforms-in-vasculogenic-mimicry-and-metastatic-potential-of-human-triple-negative-breast-cancer-cells
#13
Rassanee Bissanum, Kriengsak Lirdprapamongkol, Jisnuson Svasti, Raphatphorn Navakanitworakul, Kanyanatt Kanokwiroon
Triple negative breast cancer (TNBC) is highly aggressive and has a few therapeutic treatments, so new targeted therapy and biomarkers are required to provide alternative choices for treating TNBC patients. Recent studies showed that vasculogenic mimicry (VM), the formation of blood channels by aggressive cancer cells that mimic endothelial cells, is a factor contributing to poor prognosis in TNBC. Wilms' tumor 1 (WT1) gene has been found to be highly expressed in TNBC, and has 4 major distinct isoforms; isoform A (-17AA/-KTS; -/-), isoform B (+17AA/-KTS; +/-), isoform C (-17AA/+KTS; -/+) and isoform D (+17AA/+KTS; +/+)...
October 9, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29016929/trivalent-car-t-cells-overcome-interpatient-antigenic-variability-in-glioblastoma
#14
Kevin Bielamowicz, Kristen Fousek, Tiara T Byrd, Hebatalla Samaha, Malini Mukherjee, Nikita Aware, Meng-Fen Wu, Jordan S Orange, Pavel Sumazin, Tsz-Kwong Man, Sujith K Joseph, Meenakshi Hegde, Nabil Ahmed
Background: Glioblastoma (GBM) is the most common primary malignant brain cancer, and is currently incurable. Chimeric Antigen Receptor (CAR) T-cells have shown promise in GBM treatment. While we have shown that combinatorial targeting of two glioma antigens offsets antigen escape and enhances T-cell effector functions, the inter-patient variability in surface antigen expression between patients hinders the clinical impact of targeting two antigen pairs. This study addresses targeting 3 antigens using a single CAR T-cell product for broader application...
September 16, 2017: Neuro-oncology
https://www.readbyqxmd.com/read/28966234/emerging-and-diverse-functions-of-the-epha2-noncanonical-pathway-in-cancer-progression
#15
Yue Zhou, Hiroaki Sakurai
Erythropoietin-producing hepatocellular receptor A2 (EphA2) receptor tyrosine kinase controls multiple physiological processes to maintain homeostasis in normal cells. In many types of solid tumors, it has been reported that EphA2 is overexpressed and plays a critical role in oncogenic signaling. However, in recent years, the opposing functions of EphA2 have been explained by the canonical and noncanonical signaling pathways. Ligand- and tyrosine kinase-dependent EphA2 activation (the canonical pathway) inhibits cancer cell proliferation and motility...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28957431/male-hormones-activate-epha2-to-facilitate-kaposi-s-sarcoma-associated-herpesvirus-infection-implications-for-gender-disparity-in-kaposi-s-sarcoma
#16
Xing Wang, Zhe Zou, Zhaohui Deng, Deguang Liang, Xin Zhou, Rui Sun, Ke Lan
There is increasing consensus that males are more vulnerable than females to infection by several pathogens. However, the underlying mechanism needs further investigation. Here, it was showed that knockdown of androgen receptor (AR) expression or pre-treatment with 5α-dihydrotestosterone, the AR agonist, led to a considerably dysregulated Kaposi's sarcoma-associated herpesvirus (KSHV) infection. In endothelial cells, membrane-localized AR promoted the endocytosis and nuclear trafficking of KSHV. The AR interacted with ephrin receptor A2 (EphA2) and increased its phosphorylation at residue Ser897, which was specifically upregulated upon KSHV infection...
September 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28911167/in-utero-exposure-to-a-high-fat-diet-programs-hepatic-hypermethylation-and-gene-dysregulation-and-development-of-metabolic-syndrome-in-male-mice
#17
Yoshinori Seki, Masako Suzuki, Xingyi Guo, Alan Scott Glenn, Patricia M Vuguin, Ariana Fiallo, Quan Du, Yi-An Ko, Yiting Yu, Katalin Susztak, Deyou Zheng, John M Greally, Ellen B Katz, Maureen J Charron
Exposure to a high-fat (HF) diet in utero is associated with increased incidence of cardiovascular disease, diabetes, and metabolic syndrome later in life. However, the molecular basis of this enhanced susceptibility for metabolic disease is poorly understood. Gene expression microarray and genome-wide DNA methylation analyses of mouse liver revealed that exposure to a maternal HF milieu activated genes of immune response, inflammation, and hepatic dysfunction. DNA methylation analysis revealed 3360 differentially methylated loci, most of which (76%) were hypermethylated and distributed preferentially to hotspots on chromosomes 4 [atherosclerosis susceptibility quantitative trait loci (QTLs) 1] and 18 (insulin-dependent susceptibility QTLs 21)...
September 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28883622/socs2-binds-to-and-regulates-epha2-through-multiple-mechanisms
#18
Carissa Pilling, Jonathan A Cooper
Suppressors of cytokine signaling (SOCS) proteins inhibit signaling by serving as substrate receptors for the Cullin5-RING E3 ubiquitin ligase (CRL5) and through a variety of CRL5-independent mechanisms. CRL5, SOCS2 and SOCS6 are implicated in suppressing transformation of epithelial cells. We identified cell proteins that interact with SOCS2 and SOCS6 using two parallel proteomics techniques: BioID and Flag affinity purification mass spectrometry. The receptor tyrosine kinase ephrin type-A receptor 2 (EphA2) was identified as a SOCS2-interacting protein...
September 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28881807/associations-of-high-altitude-polycythemia-with-polymorphisms-in-epha2-and-agt-in-chinese-han-and-tibetan-populations
#19
Lijun Liu, Yao Zhang, Zhiying Zhang, Yiduo Zhao, Xiaowei Fan, Lifeng Ma, Yuan Zhang, Haijin He, Longli Kang
High altitude polycythemia (HAPC) refers to the long-term living in the plateau of the hypoxia environment is not accustomed to cause red blood cell hyperplasia. The pathological changes are mainly the various organs and tissue congestion, blood stasis and hypoxia damage. Although chronic hypoxia is the main cause of HAPC, the related molecular mechanisms remain largely unclear. This study aims to explore the genetic basis of HAPC in the Chinese Han and Tibetan populations. We enrolled 100 patients (70 Han, 30 Tibetan) with HAPC and 100 healthy control subjects (30 Han, 70 Tibetan)...
August 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28855599/functional-non-coding-polymorphism-in-an-epha2-promoter-pax2-binding-site-modifies-expression-and-alters-the-mapk-and-akt-pathways
#20
Xiaoyin Ma, Zhiwei Ma, Xiaodong Jiao, J Fielding Hejtmancik
To identify possible genetic variants influencing expression of EPHA2 (Ephrin-receptor Type-A2), a tyrosine kinase receptor that has been shown to be important for lens development and to contribute to both congenital and age related cataract when mutated, the extended promoter region of EPHA2 was screened for variants. SNP rs6603883 lies in a PAX2 binding site in the EPHA2 promoter region. The C (minor) allele decreased EPHA2 transcriptional activity relative to the T allele by reducing the binding affinity of PAX2...
August 30, 2017: Scientific Reports
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