A Potent Agent Targeting the Ligand Binding Domain of EphA2

We report on a novel agent, targefrin, that binds to EphA2-LBD with a 21 nM dissociation constant by isothermal titration calorimetry and presents an IC 50 ...

Overexpression of the receptor tyrosine kinase EphA2 is invariably associated with poor prognosis and development of aggressive metastatic ...

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

The extraordinary affinity of targefrin for the LBD of EphA2 makes this agent an unprecedented pharmacological tool to study this receptor ...

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

Overexpression of the receptor tyrosine kinase EphA2 is invariably associated with poor prognosis and development of aggressive metastatic ...

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

A novel agent, targefrin, is reported on that binds to EphA2-LBD with a 21 nM dissociation constant by isothermal titration calorimetry and presents an IC50 ...

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

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Abstract 3911: Targeting the EphA2-ligand binding domain for the ...

In addition, due to its ability to endocytose upon activation, EphA2 could also be used as a carrier of cytotoxic agents, particularly in ...

Targeting EphA2 in cancer | Journal of Hematology & Oncology

Eph receptors are grouped into A and B categories according to their extracellular domains, which determine the binding affinity for ligands ( ...

Ligands with different dimeric configurations potently activate the ...

The extracellular region of EphA2 contains an N-terminal ligand-binding domain (LBD), a cysteine-rich region and two fibronectin type III ...

Design and Characterization of Novel EphA2 Agonists for Targeted ...

123B9 is a potent and selective EphA2 agonist targeting its ligand-binding domain ... agent targets both the human and mouse receptor ...

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

... a potent synthetic agent, 135H11, that selectively targets the receptor tyrosine kinase, EphA2 ... ligand-binding domain of EphA2 (Kd~130 ...

Unveiling the therapeutic promise of EphA2 in glioblastoma

This framework encompasses a conserved N-terminal globular ligand-binding domain ... Hence, the concomitant targeting of these four receptors ...

The EphA2 receptor is activated through induction of distinct, ligand ...

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

Dimeric and tetrameric EphA2 agonistic ligands ... - ResearchGate

Targefrin: A Potent Agent Targeting the Ligand Binding Domain of EphA2. Article. Full-text available. Nov 2022; J MED CHEM. Carlo Baggio ...

Therapeutic Targeting of Pancreatic Cancer via EphA2 Dimeric ...

Very recently, we developed novel and more potent synthetic agents, which target the EphA2-LBD (ligand binding domain) at nanomolar concentrations, as ...

(Open Access) Targefrin: A Potent Agent Targeting the Ligand ...

DOI: 10.1021/acs.jmedchem.2c01391) Overexpression of the receptor tyrosine kinase EphA2 is invariably associated with poor prognosis and development of ...

Structure-Based Design of Novel EphA2 Agonistic Agents with ...

Recent efforts from our laboratories identified a number of agonistic peptides targeting the ligand-binding domain of the EphA2 receptor. The individual agents, ...

Affinity of EphA2-LBD-targeting agents as detected by ITC (panels A ...

Targefrin: A Potent Agent Targeting the Ligand Binding Domain of EphA2. Article. Full-text available. Nov 2022; J MED CHEM. Carlo Baggio ...

Ki Summary - BindingDB

... A Potent Agent Targeting the Ligand Binding Domain of EphA2. J Med Chem 65 ... receptor | Epithelial cell kinase | Tyrosine-protein kinase receptor ECK.

iScience - Cell Press

The EphA2 receptor tyrosine kinase activates signaling pathways with different, and sometimes opposite, effects in cancer and other ...