Targefrin: A Potent Agent Targeting the Ligand Binding Domain of EphA2

A phase 1 safety and bioimaging trial of antibody DS-8895a against EphA2 in patients with advanced or metastatic EphA2 positive cancers

(2022) Hui K. Gan et al.   INVESTIGATIONAL NEW DRUGS

EphA2: A promising therapeutic target in breast cancer

(2021) Ping Zhao et al.   Journal of Genetics and Genomics

Effective Tumor Targeting by EphA2-Agonist-Biotin-Streptavidin Conjugates

(2021) Parima Udompholkul et al.   MOLECULES

Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads

(2020) Gemma E. Mudd et al.   JOURNAL OF MEDICINAL CHEMISTRY

Therapeutic Targeting of Pancreatic Cancer via EphA2 Dimeric Agonistic Agents

(2020) Ahmed F. Salem et al.   Pharmaceuticals

Prostate Cancer Metastases Are Strongly Inhibited by Agonistic Epha2 Ligands in an Orthotopic Mouse Model

(2020) Ahmed F. Salem et al.   Cancers

Pharmacological evaluation of new bioavailable small molecules targeting Eph/ephrin interaction

(2018) Carmine Giorgio et al.   BIOCHEMICAL PHARMACOLOGY

Design and synthesis of small molecule agonists of EphA2 receptor

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

Reduction of Circulating Cancer Cells and Metastases in Breast-Cancer Models by a Potent EphA2-Agonistic Peptide–Drug Conjugate

(2018) Ahmed F. Salem et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2018) Luca Gambini et al.   ACS Chemical Biology

Targeting Eph/ephrin system in cancer therapy

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

Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs

(2016) Stephanie Heinzlmeir et al.   ACS Chemical Biology

Novel anti-EPHA2 antibody, DS-8895a for cancer treatment

(2016) Jun Hasegawa et al.   CANCER BIOLOGY & THERAPY

EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer

(2016) Katherine R. Amato et al.   CANCER RESEARCH

Therapy of pancreatic cancer via an EphA2 receptor-targeted delivery of gemcitabine

(2016) Bridget A. Quinn et al.   Oncotarget

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

(2015) Bainan Wu et al.   CHEMISTRY & BIOLOGY

High-Throughput Screening by Nuclear Magnetic Resonance (HTS by NMR) for the Identification of PPIs Antagonists

(2015) Bainan Wu et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

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

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

Design, Synthesis and Bioevaluation of an EphA2 Receptor-Based Targeted Delivery System

(2014) Elisa Barile et al.   ChemMedChem

Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC

(2014) Katherine R. Amato et al.   JOURNAL OF CLINICAL INVESTIGATION

EPHA2 Is a Mediator of Vemurafenib Resistance and a Novel Therapeutic Target in Melanoma

(2014) B. Miao et al.   Cancer Discovery

HTS by NMR of Combinatorial Libraries: A Fragment-Based Approach to Ligand Discovery

(2013) Bainan Wu et al.   CHEMISTRY & BIOLOGY

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

(2013) Massimiliano Tognolini et al.   ChemMedChem

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

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

Design and Synthesis of Potent Bivalent Peptide Agonists Targeting the EphA2 Receptor

(2013) Srinivas Duggineni et al.   ACS Medicinal Chemistry Letters

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

(2012) Elena Binda et al.   CANCER CELL

Copy Number Variations of EphA3 Are Associated With Multiple Types of Hematologic Malignancies

(2012) Ming Guan et al.   Clinical Lymphoma Myeloma & Leukemia

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

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

Structure−Activity Relationship Analysis of Peptides Targeting the EphA2 Receptor

(2010) Sayantan Mitra et al.   BIOCHEMISTRY

EphA2 as a promoter of melanoma tumorigenicity

(2010) Naira V. Margaryan et al.   CANCER BIOLOGY & THERAPY

Emerging strategies for EphA2 receptor targeting for cancer therapeutics

(2010) Manish Tandon et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

EphA2Mutation in Lung Squamous Cell Carcinoma Promotes Increased Cell Survival, Cell Invasion, Focal Adhesions, and Mammalian Target of Rapamycin Activation

(2010) Leonardo Faoro et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Eph-ephrin bidirectional signaling comes into the context of lymphocyte transendothelial migration

(2010) Eva M. Trinidad et al.   Cell Adhesion & Migration

Over-Expression of EphA2 and EphrinA-1 in Human Gastric Adenocarcinoma and Its Prognostic Value for Postoperative Patients

(2008) Wei-Jie Yuan et al.   DIGESTIVE DISEASES AND SCIENCES

Expression profile of Eph receptors and ephrin ligands in healthy human B lymphocytes and chronic lymphocytic leukemia B-cells

(2008) Luis M. Alonso-C et al.   LEUKEMIA RESEARCH