Ephrin or not? Six tough questions on Eph targeting

Genetically Encoded FRET Biosensor for Visualizing EphA4 Activity in Different Compartments of the Plasma Membrane

(2019) Yijia Pan et al.   ACS Sensors

The Small Molecule Ephrin Receptor Inhibitor, GLPG1790, Reduces Renewal Capabilities of Cancer Stem Cells, Showing Anti-Tumour Efficacy on Preclinical Glioblastoma Models

(2019) Giovanni Gravina et al.   Cancers

Inhibition of Eph/ephrin interaction with the small molecule UniPR500 improves glucose tolerance in healthy and insulin-resistant mice

(2019) C. Giorgio et al.   PHARMACOLOGICAL RESEARCH

Dose escalation and expansion cohort study for DS-8895a in patients with advanced solid tumors.

(2019) Taroh Satoh et al.   JOURNAL OF CLINICAL ONCOLOGY

First-in-human, phase I study of PF-06647263, an anti-EFNA4 calicheamicin antibody-drug conjugate, in patients with advanced solid tumors

(2019) Ignacio Garrido-Laguna et al.   INTERNATIONAL JOURNAL OF CANCER

Eph receptor signalling: from catalytic to non-catalytic functions

(2019) Lung-Yu Liang et al.   ONCOGENE

Co-targeting ephrin receptor tyrosine kinases A2 and A3 in cancer stem cells reduces growth of recurrent glioblastoma.

(2018) Maleeha A Qazi et al.   CANCER RESEARCH

Design and synthesis of small molecule agonists of EphA2 receptor

(2018) Aaron Petty et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

EPHB6 augments both development and drug sensitivity of triple-negative breast cancer tumours

(2018) Behzad M. Toosi et al.   ONCOGENE

UniPR1331, a small molecule targeting Eph/ephrin interaction, prolongs survival in glioblastoma and potentiates the effect of antiangiogenic therapy in mice

(2018) Claudio Festuccia et al.   Oncotarget

Differential Expression Patterns of Eph Receptors and Ephrin Ligands in Human Cancers

(2018) Chung-Ting Jimmy Kou et al.   Biomed Research International

Targeting Cancer Stemness in the Clinic: From Hype to Hope

(2018) Caner Saygin et al.   Cell Stem Cell

Targeting Eph/ephrin system in cancer therapy

(2017) Alessio Lodola et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Pharmacological targeting of the ephrin receptor kinase signalling by GLPG1790 in vitro and in vivo reverts oncophenotype, induces myogenic differentiation and radiosensitizes embryonal rhabdomyosarcoma cells

(2017) Francesca Megiorni et al.   Journal of Hematology & Oncology

Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein–Protein Interaction Inhibitors Targeting the EphA2 Receptor

(2017) Matteo Incerti et al.   JOURNAL OF MEDICINAL CHEMISTRY

Comment on “KB004, a first in class monoclonal antibody targeting the receptor tyrosine kinase EphA3, in patients with advanced hematologic malignancies: Results from a phase 1 study”

(2017) Amy Hughes et al.   LEUKEMIA RESEARCH

Intra-tumor heterogeneity from a cancer stem cell perspective

(2017) Pramudita R. Prasetyanti et al.   Molecular Cancer

ADAM10-mediated ephrin-B2 shedding promotes myofibroblast activation and organ fibrosis

(2017) David Lagares et al.   NATURE MEDICINE

Dysregulation of EGFR Pathway in EphA2 Cell Subpopulation Significantly Associates with Poor Prognosis in Colorectal Cancer

(2016) Mariangela De Robertis et al.   CLINICAL CANCER RESEARCH

EphB4 promotes the proliferation, invasion, and angiogenesis of human colorectal cancer

(2016) JingHuan Lv et al.   EXPERIMENTAL AND MOLECULAR PATHOLOGY

Exosomes mediate cell contact–independent ephrin-Eph signaling during axon guidance

(2016) Jingyi Gong et al.   JOURNAL OF CELL BIOLOGY

EphA3 as a target for antibody immunotherapy in acute lymphoblastic leukemia

(2016) S Charmsaz et al.   LEUKEMIA

Proteolysis of EphA2 Converts It from a Tumor Suppressor to an Oncoprotein

(2015) N. Koshikawa et al.   CANCER RESEARCH

Anti-EFNA4 Calicheamicin Conjugates Effectively Target Triple-Negative Breast and Ovarian Tumor-Initiating Cells to Result in Sustained Tumor Regressions

(2015) M. Damelin et al.   CLINICAL CANCER RESEARCH

Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors

(2015) Massimiliano Tognolini et al.   CURRENT DRUG TARGETS

Δ5-Cholenoyl-amino acids as selective and orally available antagonists of the Eph–ephrin system

(2015) Riccardo Castelli et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

EphA2 Is a Therapy Target in EphA2-Positive Leukemias but Is Not Essential for Normal Hematopoiesis or Leukemia

(2015) Sara Charmsaz et al.   PLoS One

UniPR129 is a competitive small molecule Eph-ephrin antagonist blockingin vitroangiogenesis at low micromolar concentrations

(2014) I Hassan-Mohamed et al.   BRITISH JOURNAL OF PHARMACOLOGY

Targeting EphA3 Inhibits Cancer Growth by Disrupting the Tumor Stromal Microenvironment

(2014) M. E. Vail et al.   CANCER RESEARCH

Combining Ligand- and Structure-Based Approaches for the Discovery of New Inhibitors of the EPHA2–ephrin-A1 Interaction

(2014) Daniele Pala et al.   Journal of Chemical Information and Modeling

The role of proteases in regulating Eph/ephrin signaling

(2014) Lakmali Atapattu et al.   Cell Adhesion & Migration

EphA3 Maintains Tumorigenicity and Is a Therapeutic Target in Glioblastoma Multiforme

(2013) Bryan W. Day et al.   CANCER CELL

Target Hopping as a Useful Tool for the Identification of Novel EphA2 Protein-Protein Antagonists

(2013) Massimiliano Tognolini et al.   ChemMedChem

U.S. Food and Drug Administration Approval: Vismodegib for Recurrent, Locally Advanced, or Metastatic Basal Cell Carcinoma

(2013) M. Axelson et al.   CLINICAL CANCER RESEARCH

Pharmacological inhibition of Eph receptors enhances glucose-stimulated insulin secretion from mouse and human pancreatic islets

(2013) R. Jain et al.   DIABETOLOGIA

ADAM12-cleaved ephrin-A1 contributes to lung metastasis

(2013) K Ieguchi et al.   ONCOGENE

Attenuation of Eph Receptor Kinase Activation in Cancer Cells by Coexpressed Ephrin Ligands

(2013) Giulia Falivelli et al.   PLoS One

Design, synthesis and characterization of novel small molecular inhibitors of ephrin-B2 binding to EphB4

(2012) Srinivas Duggineni et al.   BIOCHEMICAL PHARMACOLOGY

The EphA2 Receptor Drives Self-Renewal and Tumorigenicity in Stem-like Tumor-Propagating Cells from Human Glioblastomas

(2012) Elena Binda et al.   CANCER CELL

Phase 1, open-label study of MEDI-547 in patients with relapsed or refractory solid tumors

(2012) Christina M. Annunziata et al.   INVESTIGATIONAL NEW DRUGS

Novel Targeted System To Deliver Chemotherapeutic Drugs to EphA2-Expressing Cancer Cells

(2012) Si Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

EphrinA1 Is Released in Three Forms from Cancer Cells by Matrix Metalloproteases

(2012) A. Beauchamp et al.   MOLECULAR AND CELLULAR BIOLOGY

HGF induces novel EGFR functions involved in resistance formation to tyrosine kinase inhibitors

(2012) S Gusenbauer et al.   ONCOGENE

A Small Molecule Agonist of EphA2 Receptor Tyrosine Kinase Inhibits Tumor Cell Migration In Vitro and Prostate Cancer Metastasis In Vivo

(2012) Aaron Petty et al.   PLoS One

Concepts and consequences of Eph receptor clustering

(2012) Peter W. Janes et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

The Intestinal Stem Cell Signature Identifies Colorectal Cancer Stem Cells and Predicts Disease Relapse

(2011) Anna Merlos-Suárez et al.   Cell Stem Cell

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Structure−Activity Relationship Analysis of Peptides Targeting the EphA2 Receptor

(2010) Sayantan Mitra et al.   BIOCHEMISTRY

EphB Signaling Controls Lineage Plasticity of Adult Neural Stem Cell Niche Cells

(2010) Tadashi Nomura et al.   Cell Stem Cell

Crosstalk of the EphA2 receptor with a serine/threonine phosphatase suppresses the Akt-mTORC1 pathway in cancer cells

(2010) Nai-Ying Yang et al.   CELLULAR SIGNALLING

Ephrins and Eph receptors in stem cells and cancer

(2010) Maria Genander et al.   CURRENT OPINION IN CELL BIOLOGY

Vasculogenensis, angiogenesis and special features of tumor blood vessels

(2010) Sachie Hiratsuka   Frontiers in Bioscience-Landmark

Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors

(2009) Yongmun Choi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

EphA2 Mediates Ligand-Dependent Inhibition and Ligand-Independent Promotion of Cell Migration and Invasion via a Reciprocal Regulatory Loop with Akt

(2009) Hui Miao et al.   CANCER CELL

Loss of EphA2 receptor tyrosine kinase reducesApcmin/+tumorigenesis

(2008) Christina Bogan et al.   INTERNATIONAL JOURNAL OF CANCER

The receptor tyrosine kinase EphA2 promotes mammary adenocarcinoma tumorigenesis and metastatic progression in mice by amplifying ErbB2 signaling

(2008) Dana M. Brantley-Sieders et al.   JOURNAL OF CLINICAL INVESTIGATION

Soluble monomeric EphrinA1 is released from tumor cells and is a functional ligand for the EphA2 receptor

(2008) J Wykosky et al.   ONCOGENE