keyword
MENU ▼
Read by QxMD icon Read
search

EPHA2

keyword
https://www.readbyqxmd.com/read/29334266/hyaluronic-acid-modified-daunorubicin-plus-honokiol-cationic-liposomes-for-the-treatment-of-breast-cancer-along-with-the-elimination-vasculogenic-mimicry-channels
#1
Rui-Jun Ju, Lan Cheng, Xiao Qiu, Shuang Liu, Xiao-Li Song, Xiao-Ming Peng, Teng Wang, Cui-Qing Li, Xue-Tao Li
BACKGROUND: Breast cancer is an alarming global public health problem and a main cause of cancer-related death in women. Systemic chemotherapy is the most widely used treatment for breast cancer. However, current chemotherapy treatments are far from desirable due to poor targeting specificity, severe side effects, and vasculogenic mimicry (VM). PURPOSE: Hyaluronic acid (HA) modified daunorubicin plus honokiol cationic liposomes were prepared and characterized for treatment of breast cancer by eliminating VM...
January 15, 2018: Journal of Drug Targeting
https://www.readbyqxmd.com/read/29318540/identification-of-proteolytic-cleavage-sites-of-epha2-by%C3%A2-membrane-type-1-matrix-metalloproteinase-on-the%C3%A2-surface-of-cancer-cells
#2
Keiji Kikuchi, Hiroko Kozuka-Hata, Masaaki Oyama, Motoharu Seiki, Naohiko Koshikawa
Proteolytic cleavage of membrane proteins can alter their functions depending on the cleavage sites. We recently demonstrated that membrane type 1 matrix metalloproteinase (MT1-MMP ) converts the tumor suppressor EphA2 into an oncogenic signal transducer through EphA2 cleavage. The cleaved EphA2 fragment that remains at the cell surface may be a better target for cancer therapy than intact EphA2. To analyze the cleavage site(s) of EphA2, we purified the fragments from tumor cells expressing MT1-MMP and Myc- and 6× His-tagged EphA2 by two-step affinity purification ...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29312631/proteomic-approach-toward-determining-the-molecular-background-of-pazopanib-resistance-in-synovial-sarcoma
#3
Zhiwei Qiao, Kumiko Shiozawa, Tadashi Kondo
Pazopanib, a multitarget tyrosine kinase (TK) inhibitor, has been approved for treatment of soft tissue sarcoma. Elucidation of the molecular background of pazopanib resistance should lead to improved clinical outcomes in sarcomas; accordingly, we investigated this in synovial sarcoma using a proteomic approach. Pazopanib sensitivity was examined in four synovial sarcoma cell lines: SYO-1, HS-SYII, 1273/99, and YaFuSS. The 1273/99 cell line showed significantly higher IC50 values than the others for pazopanib...
December 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29301020/discovery-of-internalizing-antibodies-to-basal-breast-cancer-cells
#4
Yu Zhou, Hao Zou, Christina Yau, Lequn Zhao, Steven C Hall, Daryl C Drummond, Shauna Farr-Jones, John W Park, Christopher C Benz, James D Marks
We present a strategy to discover recombinant monoclonal antibodies (mAbs) to specific cancers and demonstrate this approach using basal subtype breast cancers. A phage antibody library was depleted of antibodies to common cell surface molecules by incubation with luminal breast cancer cell lines, and then selected on a single basal-like breast cancer cell line (MDA-MB-231) for binding associated receptor-mediated endocytosis. Additional profiling against two luminal and four basal-like cell lines revealed 61 unique basal-specific mAbs from a pool of 1440 phage antibodies...
December 28, 2017: Protein Engineering, Design & Selection: PEDS
https://www.readbyqxmd.com/read/29299576/linking-invasive-motility-to-protein-expression-in-single-tumor-cells
#5
Jung-Ming G Lin, Chi-Chih Kang, Yun Zhou, Haiyan Huang, Amy E Herr, Sanjay Kumar
The invasion of malignant cells into tissue is a critical step in the progression of cancer. While it is increasingly appreciated that cells within a tumor differ in their invasive potential, it remains nearly unknown how these differences relate to cell-to-cell variations in protein expression. Here, we introduce a microfluidic platform that integrates measurements of invasive motility and protein expression for single cells, which we use to scrutinize human glioblastoma tumor-initiating cells (TICs). Our live-cell imaging microdevice is comprised of polyacrylamide microchannels that exhibit tissue-like stiffness and present chemokine gradients along each channel...
January 4, 2018: Lab on a Chip
https://www.readbyqxmd.com/read/29290990/molecular-and-functional-crosstalk-between-extracellular-hsp90-and-ephrin-a1-signaling
#6
Abdelkader Daoud, Udhayakumar Gopal, Jasmine Kaur, Jennifer S Isaacs
The Eph receptor tyrosine kinase family member EphA2 plays a pivotal role in modulating cytoskeletal dynamics to control cancer cell motility and invasion. EphA2 is frequently upregulated in diverse solid tumors and has emerged as a viable druggable target. We previously reported that extracellular Hsp90 (eHsp90), a known pro-motility and invasive factor, collaborates with EphA2 to regulate tumor invasion in the absence of its cognate ephrin ligand. Here, we aimed to further define the molecular and functional relationship between EphA2 and eHsp90...
December 5, 2017: Oncotarget
https://www.readbyqxmd.com/read/29273006/mir-302b-inhibits-tumorigenesis-by-targeting-epha2-via-wnt-%C3%AE-catenin-emt-signaling-cascade-in-gastric-cancer
#7
Jin Huang, Yijing He, Howard L Mcleod, Yanchun Xie, Desheng Xiao, Huabin Hu, Pan Chen, Liangfang Shen, Shan Zeng, Xianli Yin, Jie Ge, Li Li, Lanhua Tang, Jian Ma, Zihua Chen
BACKGROUND: EphA2 is a crucial oncogene in gastric cancer (GC) development and metastasis, this study aims to identify microRNAs that target it and serve as key regulators of gastric carcinogenesis. METHODS: We identified several potential microRNAs targeting EphA2 by bioinformatics websites and then analyzed the role of miR-302b in modulating EphA2 in vitro and in vivo of GC, and it's mechanism. RESULTS: Our analysis identified miR-302b, a novel regulator of EphA2, as one of the most significantly downregulated microRNA (miRNA) in GC tissues...
December 22, 2017: BMC Cancer
https://www.readbyqxmd.com/read/29242524/clinical-implications-of-the-plasma-epha2-receptor-level-in-critically-ill-patients-with-septic-shock
#8
Su Hwan Lee, Ju Hye Shin, Joo Han Song, Ah Young Leem, Moo Suk Park, Young Sam Kim, Joon Chang, Kyung Soo Chung
The Eph/ephrin receptor ligand system is known to play a role in inflammation induced by infection, injury, and inflammatory diseases. The present study aimed to evaluate plasma EphA2 receptor levels in critically ill patients with sepsis. This study was a prospective cohort study evaluating samples and clinical data from the medical intensive care unit (MICU) of a 2000-bed university tertiary referral hospital in South Korea. Positive correlations of the plasma EphA2 receptor level with the acute physiology and chronic health evaluation (APACHE) II score and the sequential organ failure assessment (SOFA) score were observed...
December 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29234063/the-sam-sam-interaction-between-ship2-and-the-epha2-receptor-design-and-analysis-of-peptide-inhibitors
#9
Flavia Anna Mercurio, Concetta Di Natale, Luciano Pirone, Roberta Iannitti, Daniela Marasco, Emilia Maria Pedone, Rosanna Palumbo, Marilisa Leone
The lipid phosphatase Ship2 represents a drug discovery target for the treatment of different diseases, including cancer. Its C-terminal sterile alpha motif domain (Ship2-Sam) associates with the Sam domain from the EphA2 receptor (EphA2-Sam). This interaction is expected to mainly induce pro-oncogenic effects in cells therefore, inhibition of the Ship2-Sam/EphA2-Sam complex may represent an innovative route to discover anti-cancer therapeutics. In the present work, we designed and analyzed several peptide sequences encompassing the interaction interface of EphA2-Sam for Ship2-Sam...
December 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29228713/cell-surface-thomsen-friedenreich-proteome-profiling-of-metastatic-prostate-cancer-cells-reveals-potential-link-with-cancer-stem-cell-like-phenotype
#10
Feng Li, Olga V Glinskii, Brian P Mooney, Kate Rittenhouse-Olson, Kenneth J Pienta, Vladislav V Glinsky
The tumor-associated Thomsen-Friedenreich glycoantigen (TF-Ag) plays an important role in hematogenous metastasis of multiple cancers. The LTQ Orbitrap LC-MS/MS mass spectrometry analysis of cell surface TF-Ag proteome of metastatic prostate cancer cells reveals that several cell surface glycoproteins expressing this carbohydrate antigen in prostate cancer (CD44, α2 integrin, β1 integrin, CD49f, CD133, CD59, EphA2, CD138, transferrin receptor, profilin) are either known as stem cell markers or control important cancer stem-like cell functions...
November 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29216437/epha2-modulation-associates-with-protective-effect-of-prone-position-in-ventilator-induced-lung-injury
#11
Byung Hoon Park, Mi Hwa Shin, Ivor S Douglas, Kyung Soo Chung, Joo Han Song, Song Yee Kim, Eun Young Kim, Ji Ye Jung, Young Ae Kang, Joon Chang, Young Sam Kim, Moo Suk Park
The erythropoietin-producing hepatoma receptor tyrosine kinase A2 (EphA2) and its ligand ephrinA1 play a pivotal role in inflammation and tissue injury by modulating the epithelial and endothelial barrier integrity. Therefore, EphA2 receptor may be a potential therapeutic target for modulating ventilator-induced lung injury (VILI). To support this hypothesis, here we analyzed EphA2/ephrinA1 signaling in the process of VILI and determined the role of EphA2/ephrinA1 signaling in the protective mechanism of prone positioning in a VILI model...
December 7, 2017: American Journal of Respiratory Cell and Molecular Biology
https://www.readbyqxmd.com/read/29208682/the-receptor-tyrosine-kinase-epha2-promotes-glutamine-metabolism-in-tumors-by-activating-the-transcriptional-coactivators-yap-and-taz
#12
Deanna N Edwards, Verra M Ngwa, Shan Wang, Eileen Shiuan, Dana M Brantley-Sieders, Laura C Kim, Albert B Reynolds, Jin Chen
Malignant tumors reprogram cellular metabolism to support cancer cell proliferation and survival. Although most cancers depend on a high rate of aerobic glycolysis, many cancer cells also display addiction to glutamine. Glutamine transporters and glutaminase activity are critical for glutamine metabolism in tumor cells. We found that the receptor tyrosine kinase EphA2 activated the TEAD family transcriptional coactivators YAP and TAZ (YAP/TAZ), likely in a ligand-independent manner, to promote glutamine metabolism in cells and mouse models of HER2-positive breast cancer...
December 5, 2017: Science Signaling
https://www.readbyqxmd.com/read/29197141/the-human-blood-brain-barrier-internalizes-cryptococcus-neoformans-via-the-epha2-tyrosine-kinase-receptor
#13
Phylicia A Aaron, Mantana Jamklang, John P Uhrig, Angie Gelli
Cryptococcus neoformans is an opportunistic fungal pathogen that causes life-threatening meningitis most commonly in populations with impaired immunity. Here we resolved the transcriptome of the human brain endothelium challenged with C. neoformans to establish whether C. neoformans invades the CNS by co-opting particular signaling pathways as a means to promote its own entry. Among the 5 major pathways targeted by C. neoformans, the EPH-EphrinA1 (EphA2) tyrosine kinase receptor-signaling pathway was examined further...
December 2, 2017: Cellular Microbiology
https://www.readbyqxmd.com/read/29167336/an-insight-into-the-role-of-e3-ubiquitin-ligase-c-cbl-escrt-machinery-and-host-cell-signaling-in-kaposi-s-sarcoma-associated-herpesvirus-kshv-entry-and-trafficking
#14
Binod Kumar, Arunava Roy, Mohanan Valiya Veettil, Bala Chandran
Kaposi's sarcoma-associated herpesvirus (KSHV) in vitro infection of dermal endothelial cell begins with its binding to host cell surface receptor molecules such as heparan sulfate (HS), integrins (α3β1, αVβ3 and αVβ5), xCT and EphA2 receptor tyrosine kinase (EphA2R). These initial events initiate dynamic host protein-protein interactions involving a multi-molecular complex of receptors, signal molecules (FAK, Src, PI3-K, RhoA-GTPase), adaptors (c-Cbl, CIB1, Crk, p130Cas and GEF-C3G), and actin/myosin II light chain that leads to virus entry via macropinocytosis...
November 22, 2017: Journal of Virology
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
keyword
keyword
27139
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"