Protein-Protein Interaction Inhibitors Targeting the Eph-Ephrin System with a Focus on Amino Acid Conjugates of Bile Acids

Cholenic acid derivative UniPR1331 impairs tumor angiogenesis via blockade of VEGF/VEGFR2 in addition to Eph/ephrin

(2021) Marco Rusnati et al.   CANCER GENE THERAPY

Optimization of EphA2 antagonists based on a lithocholic acid core led to the identification of UniPR505, a new 3α-carbamoyloxy derivative with antiangiogenetic properties

(2020) Matteo Incerti et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Radiopharmacologist’s and Radiochemist’s View on Targeting the Eph/Ephrin Receptor Tyrosine Kinase System

(2020) Christin Neuber et al.   ACS Omega

Safety, tolerability, pharmacokinetics, and pharmacodynamics of the afucosylated, humanized anti-EPHA2 antibody DS-8895a: a first-in-human phase I dose escalation and dose expansion study in patients with advanced solid tumors

(2019) Kohei Shitara et al.   Journal for ImmunoTherapy of Cancer

ATIM-23. PRELIMINARY FINDINGS OF A PHASE I SAFETY AND BIOIMAGING TRIAL OF KB004 (IFABOTUZUMAB) IN PATIENTS WITH GLIOBLASTOMA

(2019) Hui Gan et al.   NEURO-ONCOLOGY

Drug-gut microbiota metabolic interactions: the case of UniPR1331, selective antagonist of the Eph-ephrin system, in mice

(2019) Francesca Ferlenghi et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

EphrinB2/EphB4 signaling regulates non‐sprouting angiogenesis by VEGF

(2018) Elena Groppa et al.   EMBO REPORTS

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

Structure-Based Design of Novel EphA2 Agonistic Agents with Nanomolar Affinity in Vitro and in Cell

(2018) Luca Gambini et al.   ACS Chemical Biology

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

Eph-ephrin signaling modulated by polymerization and condensation of receptors

(2017) Samuel Ojosnegros et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Regulation of EBV LMP1-triggered EphA4 downregulation in EBV-associated B lymphoma and its impact on patients survival

(2016) Y.-C. Huang et al.   BLOOD

Three stories on Eph kinase inhibitors: From in silico discovery to in vivo validation

(2016) Andrea Unzue et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2016) Ronan T. Swords et al.   LEUKEMIA RESEARCH

Mechanisms of ephrin–Eph signalling in development, physiology and disease

(2016) Artur Kania et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Eph Receptors and Ephrins: Therapeutic Opportunities

(2015) Antonio Barquilla et al.   Annual Review of Pharmacology and Toxicology

Design and Characterization of Novel EphA2 Agonists for Targeted Delivery of Chemotherapy to Cancer Cells

(2015) Bainan Wu et al.   CHEMISTRY & BIOLOGY

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

(2015) Massimiliano Tognolini et al.   CURRENT DRUG TARGETS

Targeting the Eph System with Peptides and Peptide Conjugates

(2015) Stefan Riedl 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

Malaria parasites target the hepatocyte receptor EphA2 for successful host infection

(2015) A. Kaushansky et al.   SCIENCE

Are We Using the Right Pharmacological Tools to Target EphA4?

(2014) Massimiliano Tognolini et al.   ACS Chemical Neuroscience

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

NMR-Based Approaches for the Identification and Optimization of Inhibitors of Protein–Protein Interactions

(2014) Elisa Barile et al.   CHEMICAL REVIEWS

Ephs and Ephrins in malignant gliomas

(2014) Sara Ferluga et al.   GROWTH FACTORS

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

On the Use of 2,5-Dimethyl-Pyrrol-1-yl-Benzoic Acid Derivatives as EPH-Ephrin Antagonists

(2014) A. Lodola et al.   JOURNAL OF VIROLOGY

Homotypic receptor-receptor interactions regulating Eph signaling

(2014) Dimitar B Nikolov et al.   Cell Adhesion & Migration

Specific tumor delivery of paclitaxel using glycolipid-like polymer micelles containing gold nanospheres

(2013) Jian You et al.   BIOMATERIALS

EphA3 Maintains Tumorigenicity and Is a Therapeutic Target in Glioblastoma Multiforme

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

Amino Acid Conjugates of Lithocholic Acid As Antagonists of the EphA2 Receptor

(2013) Matteo Incerti et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2012) Elena Binda et al.   CANCER CELL

Structure-Activity Relationships and Mechanism of Action of Eph-ephrin Antagonists: Interaction of Cholanic Acid with the EphA2 Receptor

(2012) Massimiliano Tognolini et al.   ChemMedChem

Expression of EphrinB2 and EphB4 in glioma tissues correlated to the progression of glioma and the prognosis of glioblastoma patients

(2012) Yanyang Tu et al.   Clinical & Translational Oncology

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

Structural and Functional Characterization of Monomeric EphrinA1 Binding Site to EphA2 Receptor

(2012) Carla M. Lema Tomé et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Concepts and consequences of Eph receptor clustering

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

Structural and Functional Characterization of an Agonistic Anti-Human EphA2 Monoclonal Antibody

(2011) Li Peng et al.   JOURNAL OF MOLECULAR BIOLOGY

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Lithocholic Acid Is an Eph-ephrin Ligand Interfering with Eph-kinase Activation

(2011) Carmine Giorgio et al.   PLoS One

PEGylation Potentiates the Effectiveness of an Antagonistic Peptide That Targets the EphB4 Receptor with Nanomolar Affinity

(2011) Roberta Noberini et al.   PLoS One

Proteomic profiling of secretome and adherent plasma membranes from distinct mammary epithelial cell subpopulations

(2011) Hong Ji et al.   PROTEOMICS

EphA2 Targeted Chemotherapy Using an Antibody Drug Conjugate in Endometrial Carcinoma

(2010) J. W. Lee et al.   CLINICAL CANCER RESEARCH

Ephrins Negatively Regulate Cell Proliferation in the Epidermis and Hair Follicle

(2010) Maria Genander et al.   STEM CELLS

Eph Receptors and Ephrin Ligands: Important Players in Angiogenesis and Tumor Angiogenesis

(2010) Birgit Mosch et al.   Journal of Oncology

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

Ligand recognition by A-class Eph receptors: crystal structures of the EphA2 ligand-binding domain and the EphA2/ephrin-A1 complex

(2009) Juha P Himanen et al.   EMBO REPORTS

Eph-Ephrin Bidirectional Signaling in Physiology and Disease

(2008) Elena B. Pasquale   CELL