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https://www.readbyqxmd.com/read/28165374/evaluation-of-epha2-and-ephb4-as-targets-for-image-guided-colorectal-cancer-surgery
#1
Marieke A Stammes, Hendrica A J M Prevoo, Meyke C Ter Horst, Stéphanie A Groot, Cornelis J H Van de Velde, Alan B Chan, Lioe-Fee de Geus-Oei, Peter J K Kuppen, Alexander L Vahrmeijer, Elena B Pasquale, Cornelis F M Sier
Targeted image-guided oncologic surgery (IGOS) relies on the recognition of cell surface-associated proteins, which should be abundantly present on tumor cells but preferably absent on cells in surrounding healthy tissue. The transmembrane receptor tyrosine kinase EphA2, a member of the A class of the Eph receptor family, has been reported to be highly overexpressed in several tumor types including breast, lung, brain, prostate, and colon cancer and is considered amongst the most promising cell membrane-associated tumor antigens by the NIH...
February 3, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28154322/non-canonical-activation-of-receptor-tyrosine-kinases-in-cancer-progression
#2
Hiroaki Sakurai
 Receptor tyrosine kinases (RTKs) are known to be key regulators of cancer cell proliferation, migration, invasion and metastatic spread. Ligand-binding to the extracellular domain triggers canonical activation of the intracellular tyrosine kinase domain. In contrast, it has become evident that RTKs are also regulated by non-canonical tyrosine kinase-independent mechanisms via phosphorylation of their serine/threonine residues. In this review, I mainly introduce our recent findings on the non-canonical regulation of epidermal growth factor receptor (EGFR), ErbB2 and erythropoietin-producing hepatocellular receptor A2 (EphA2), and discuss the roles of non-canonical activation of RTKs in cancer progression and resistance to targeted cancer agents...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28005388/metadynamics-for-perspective-drug-design-computationally-driven-synthesis-of-new-protein-protein-interaction-inhibitors-targeting-the-epha2-receptor
#3
Matteo Incerti, Simonetta Russo, Donatella Callegari, Daniele Pala, Carmine Giorgio, Ilaria Zanotti, Elisabetta Barocelli, Paola Vicini, Federica Vacondio, Silvia Rivara, Riccardo Castelli, Massimiliano Tognolini, Alessio Lodola
Metadynamics (META-D) is emerging as a powerful method for the computation of the multidimensional free-energy surface (FES) describing the protein-ligand binding process. Herein, the FES of unbinding of the antagonist N-(3α-hydroxy-5β-cholan-24-oyl)-l-β-homotryptophan (UniPR129) from its EphA2 receptor was reconstructed by META-D simulations. The characterization of the free-energy minima identified on this FES proposes a binding mode fully consistent with previously reported and new structure-activity relationship data...
January 5, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27994652/to-excavate-biomarkers-predictive-of-the-response-for-capecitabine-plus-rad001-through-nanostring-based-multigene-assay-in-advanced-gastric-cancer-patients
#4
Hansang Lee, Jeeyun Lee, Insuk Sohn, Se Hoon Park, Joon Oh Park, Young Suk Park, Kyoung-Mee Kim, Won Ki Kang, Seung Tae Kim
Comprehensive characterization of individual patients' tumour is important to realize personalized medicine. Here, we investigate to identify subsets that benefit from capecitabine plus RAD001 in advanced gastric cancer (GC) patients by comprehensive high-throughput genomic analysis (nCounter assay). Archival tumour tissue blocks, if possible, were collected at phase II trial of capecitabine plus RAD001 in 47 refractory GC patients (at clinicaltrials.gov NCT#01099527). A total of 42 formalin-fixed, paraffin-embedded (FFPE) tumour samples were available for nanostring based-multigene Assay...
2016: Journal of Cancer
https://www.readbyqxmd.com/read/27978884/-expressions-of-angiogenesis-related-factors-cd105-epha2-and-ephrina1-in-laryngeal-squamous-cell-carcinoma-and-clinical-implication
#5
J Su, X B Ji, J H Xie, W Li
Objective: To investigate the expressions of endoglin (CD105), erythropoietin-producing hepatocyte receptor A2 (EphA2) and its ligand ephrinA1 proteins in laryngeal squamous cell carcinoma (LSCC) and the relationship between their expressions and the clinicopathological factors of LSCC. Methods: The expressions of CD105, EphA2 and EphrinA1 proteins were detected with immunohistochemical staining in LSCC in 76 cases and adjacent normal laryngeal tissues (ANLT) (S-P) in 25 cases.SPSS 17.0 software was used to analyze the data...
December 7, 2016: Zhonghua Er Bi Yan Hou Tou Jing Wai Ke za Zhi, Chinese Journal of Otorhinolaryngology Head and Neck Surgery
https://www.readbyqxmd.com/read/27903608/progranulin-and-the-receptor-tyrosine-kinase-epha2-partners-in-crime
#6
Babykumari Chitramuthu, Andrew Bateman
Progranulin is a secreted protein with roles in tumorigenesis, inflammation, and neurobiology, but its signaling receptors have remained unclear. In this issue, Neill et al. (2016. J. Cell Biol https://doi.org/10.1083/jcb.201603079) identify the tyrosine kinase EphA2 as a strong candidate for such a receptor, providing insight into progranulin and EphA2 signaling.
December 5, 2016: Journal of Cell Biology
https://www.readbyqxmd.com/read/27903606/epha2-is-a-functional-receptor-for-the-growth-factor-progranulin
#7
Thomas Neill, Simone Buraschi, Atul Goyal, Catherine Sharpe, Elizabeth Natkanski, Liliana Schaefer, Andrea Morrione, Renato V Iozzo
Although the growth factor progranulin was discovered more than two decades ago, the functional receptor remains elusive. Here, we discovered that EphA2, a member of the large family of Ephrin receptor tyrosine kinases, is a functional signaling receptor for progranulin. Recombinant progranulin bound with high affinity to EphA2 in both solid phase and solution. Interaction of progranulin with EphA2 caused prolonged activation of the receptor, downstream stimulation of mitogen-activated protein kinase and Akt, and promotion of capillary morphogenesis...
December 5, 2016: Journal of Cell Biology
https://www.readbyqxmd.com/read/27882199/straightforward-glycoengineering-approach-to-site-specific-antibody-pyrrolobenzodiazepine-conjugates
#8
Pamela Thompson, Ebele Ezeadi, Ian Hutchinson, Ryan Fleming, Binyam Bezabeh, Jia Lin, Shenlan Mao, Cui Chen, Luke Masterson, Haihong Zhong, Dorin Toader, Philip Howard, Herren Wu, Changshou Gao, Nazzareno Dimasi
Antibody-drug conjugates (ADCs) have become a powerful platform to deliver cytotoxic agents selectively to cancer cells. ADCs have traditionally been prepared by stochastic conjugation of a cytotoxic drug using an antibody's native cysteine or lysine residues. Through strategic selection of the mammalian expression host, we were able to introduce azide-functionalized glycans onto a homogeneously glycosylated anti-EphA2 monoclonal antibody in one step. Conjugation with an alkyne-bearing pyrrolobenzodiazepine dimer payload (SG3364) using copper-catalyzed click chemistry yielded a site-specific ADC with a drug-to-antibody ratio (DAR) of four...
November 10, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27854239/kshv-entry-and-trafficking-in-target-cells-hijacking-of-cell-signal-pathways-actin-and-membrane-dynamics
#9
REVIEW
Binod Kumar, Bala Chandran
Kaposi's sarcoma associated herpesvirus (KSHV) is etiologically associated with human endothelial cell hyperplastic Kaposi's sarcoma and B-cell primary effusion lymphoma. KSHV infection of adherent endothelial and fibroblast cells are used as in vitro models for infection and KSHV enters these cells by host membrane bleb and actin mediated macropinocytosis or clathrin endocytosis pathways, respectively. Infection in endothelial and fibroblast cells is initiated by the interactions between multiple viral envelope glycoproteins and cell surface associated heparan sulfate (HS), integrins (α3β1, αVβ3 and αVβ5), and EphA2 receptor tyrosine kinase (EphA2R)...
November 14, 2016: Viruses
https://www.readbyqxmd.com/read/27854147/improving-the-developability-of-an-anti-epha2-single-chain-variable-fragment-for-nanoparticle-targeting
#10
Melissa L Geddie, Neeraj Kohli, Dmitri B Kirpotin, Maja Razlog, Yang Jiao, Tad Kornaga, Rachel Rennard, Lihui Xu, Birgit Schoerberl, James D Marks, Daryl C Drummond, Alexey A Lugovskoy
Antibody-targeted nanoparticles have great promise as anti-cancer drugs; however, substantial developmental challenges of antibody modules prevent many candidates from reaching the clinic. Here, we describe a robust strategy for developing an EphA2-targeting antibody fragment for immunoliposomal drug delivery. A highly bioactive single-chain variable fragment (scFv) was engineered to overcome developmental liabilities, including low thermostability and weak binding to affinity purification resins. Improved thermostability was achieved by modifying the framework of the scFv, and complementarity-determining region (CDR)-H2 was modified to increase binding to protein A resins...
January 2017: MAbs
https://www.readbyqxmd.com/read/27851002/1366-clinical-implications-of-the-plasma-epha2-receptor-level-in-patients-with-sepsis
#11
Kyung Soo Chung, Chi Young Kim, Su Hwan Lee, Se Kyu Kim, Joon Chang, Youngsam Kim
No abstract text is available yet for this article.
December 2016: Critical Care Medicine
https://www.readbyqxmd.com/read/27850642/1004-the-effect-of-blocking-epha2-ephrina1-pathway-in-hyperoxia-induced-lung-injury
#12
Kyung Soo Chung, Chi Young Kim, Ju Hye Shin, Moo Suk Park, Se Kyu Kim, Joon Chang, Youngsam Kim
No abstract text is available yet for this article.
December 2016: Critical Care Medicine
https://www.readbyqxmd.com/read/27815408/epha2-proteomics-in-human-keratinocytes-reveals-a-novel-association-with-afadin-and-epidermal-tight-junctions
#13
Bethany E Perez White, Rosa Ventrella, Nihal Kaplan, Calvin J Cable, Paul M Thomas, Spiro Getsios
EphA2 is a receptor tyrosine kinase that helps to maintain epidermal tissue homeostasis. A proximity-dependent biotin identification (BioID) approach was used to identify proteins in close proximity to EphA2 within primary human keratinocytes and three-dimensional (3D) reconstituted human epidermis (RHE) cultures to map a putative protein interaction network for this membrane receptor that exhibits a polarized distribution in stratified epithelia. Although a subset of known EphA2 interactors were identified in the BioID screen, >97% were uniquely detected in keratinocytes with over 50% of these vicinal proteins only present in 3D human epidermal culture...
January 1, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/27804871/the-sam-domain-of-epha2-receptor-and-its-relevance-to-cancer-a-novel-challenge-for-drug-discovery
#14
REVIEW
Flavia A Mercurio, Marilisa Leone
BACKGROUND: Eph receptors play important functions in developmental processes and diseases and among them EphA2 is well known for its controversial role in cancer. Drug discovery strategies are mainly centered on EphA2 extracellular ligand-binding domain however, the receptor also contains a largely unexplored cytosolic Sam (Sterile alpha motif) domain at the C-terminus. EphA2-Sam binds the Sam domain from the lipid phosphatase Ship2 and the first Sam domain of Odin. Sam-Sam interactions may be important to regulate ligand-induced receptor endocytosis and degradation i...
2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27802842/defective-anks1a-disrupts-the-export-of-receptor-tyrosine-kinases-from-the-endoplasmic-reticulum
#15
Soochul Park
EphA2 has been implicated in amplifying ErbB2 tumorigenic signaling. One protein that interacts with EphA2 is the Anks1a PTB adaptor. However, the precise role of Anks1a in EphA2-mediated tumorigenesis is unclear. We demonstrated that Anks1a localizes to the ER upon phosphorylation and that the Ankyrin repeats and PTB of Anks1a bind to EphA2 and Sec23, respectively. Thus, Anks1a facilitates the selective packaging of EphA2 into COPII vesicles. Additionally, Anks1a knockout mice, a phenocopy of EphA2 knockout mice, exhibited markedly reduced ErbB2-induced breast tumorigenesis...
December 2016: BMB Reports
https://www.readbyqxmd.com/read/27776928/the-sam-domain-inhibits-epha2-interactions-in-the-plasma-membrane
#16
Deo R Singh, Fozia Ahmed, Michael D Paul, Manasee Gedam, Elena B Pasquale, Kalina Hristova
All members of the Eph receptor family of tyrosine kinases contain a SAM domain near the C terminus, which has been proposed to play a role in receptor homotypic interactions and/or interactions with binding partners. The SAM domain of EphA2 is known to be important for receptor function, but its contribution to EphA2 lateral interactions in the plasma membrane has not been determined. Here we use a FRET-based approach to directly measure the effect of the SAM domain on the stability of EphA2 dimers on the cell surface in the absence of ligand binding...
January 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27768280/chemical-proteomics-and-structural-biology-define-epha2-inhibition-by-clinical-kinase-drugs
#17
Stephanie Heinzlmeir, Denis Kudlinzki, Sridhar Sreeramulu, Susan Klaeger, Santosh Lakshmi Gande, Verena Linhard, Mathias Wilhelm, Huichao Qiao, Dominic Helm, Benjamin Ruprecht, Krishna Saxena, Guillaume Médard, Harald Schwalbe, Bernhard Kuster
The receptor tyrosine kinase EPHA2 (Ephrin type-A receptor 2) plays important roles in oncogenesis, metastasis, and treatment resistance, yet therapeutic targeting, drug discovery, or investigation of EPHA2 biology is hampered by the lack of appropriate inhibitors and structural information. Here, we used chemical proteomics to survey 235 clinical kinase inhibitors for their kinase selectivity and identified 24 drugs with submicromolar affinities for EPHA2. NMR-based conformational dynamics together with nine new cocrystal structures delineated drug-EPHA2 interactions in full detail...
December 16, 2016: ACS Chemical Biology
https://www.readbyqxmd.com/read/27763725/targeting-epha2-sam-and-its-interactome-design-and-evaluation-of-helical-peptides-enriched-in-charged-residues
#18
Flavia A Mercurio, Daniela Marasco, Concetta Di Natale, Luciano Pirone, Susan Costantini, Emilia M Pedone, Marilisa Leone
The EphA2 receptor controls diverse physiological and pathological conditions and its levels are often upregulated in cancer. Targeting receptor overexpression, through modulation of endocytosis and consequent degradation, appears to be an appealing strategy for attacking tumor malignancy. In this scenario, the Sam domain of EphA2 plays a pivotal role because it is the site where protein regulators of endocytosis and stability are recruited by means of heterotypic Sam-Sam interactions. Because EphA2-Sam heterotypic complexes are largely based on electrostatic contacts, we have investigated the possibility of attacking these interactions with helical peptides enriched in charged residues...
October 20, 2016: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/27746866/mir-26b-enhances-radiosensitivity-of-hepatocellular-carcinoma-cells-by-targeting-epha2
#19
Qiao Jin, Xiang Jun Li, Pei Guo Cao
OBJECTIVES: Although low-dose radiotherapy (RT) that involves low collateral damage is more suitable for hepatocellular carcinoma (HCC) than traditional high-dose RT, but to achieve satisfactory therapeutic effect with low-dose RT, it is necessary to sensitize HCC cells to irradiation. This study was aimed to determine whether radiosensitivity of HCC cells can be enhanced using miR-26b by targeting erythropoietin producing human hepatocelluar A2 (EphA2). MATERIALS AND METHODS: The levels of miR-26b and EphA2 expression in multiple HCC cell lines were assessed by qPCR and western blotting, respectively, and compared with those in a hepatic cell line...
August 2016: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/27742560/regulation-of-endothelial-migration-and-proliferation-by-ephrin-a1
#20
Elisa Wiedemann, Stefanie Jellinghaus, Georg Ende, Antje Augstein, Ronny Sczech, Ben Wielockx, Sönke Weinert, Ruth H Strasser, David M Poitz
Endothelial migration and proliferation are fundamental processes in angiogenesis and wound healing of injured or inflamed vessels. The present study aimed to investigate the regulation of the Eph/ephrin-system during endothelial proliferation and the impact of the ligand ephrin-A1 on proliferation and migration of human umbilical venous (HUVEC) and arterial endothelial cells (HUAEC). Endothelial cells that underwent contact inhibition showed a massive induction of ephrin-A1. In contrast, an injury to a confluent endothelial layer, associated with induction of migration and proliferation, showed reduced ephrin-A1 levels...
January 2017: Cellular Signalling
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