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

The role of the Eph-ephrin system in the etiology of pathological conditions has been consolidated throughout the years. In this context, approaches directed against this signaling system, intended to modulate its activity, can be strategic therapeutic opportunities. Currently, the most promising cl...

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Bibliographic Details
Published in:Pharmaceuticals (Basel, Switzerland) Switzerland), 2022-01, Vol.15 (2), p.137
Main Authors: Guidetti, Lorenzo, Castelli, Riccardo, Scalvini, Laura, Ferlenghi, Francesca, Corrado, Miriam, Giorgio, Carmine, Tognolini, Massimiliano, Lodola, Alessio
Format: Article
Language:English
Subjects:
Amino acids
antagonist
bile acids
Cancer therapies
Eph receptor
ephrin
Kinases
Ligands
Medical research
Metabolism
Monoclonal antibodies
Nanoparticles
Peptides
Phosphorylation
protein-protein interaction
Proteins
Review
Signal transduction
small molecules
Tumors
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Summary:The role of the Eph-ephrin system in the etiology of pathological conditions has been consolidated throughout the years. In this context, approaches directed against this signaling system, intended to modulate its activity, can be strategic therapeutic opportunities. Currently, the most promising class of compounds able to interfere with the Eph receptor-ephrin protein interaction is composed of synthetic derivatives of bile acids. In the present review, we summarize the progresses achieved, in terms of chemical expansions and structure-activity relationships, both in the steroidal core and the terminal carboxylic acid group, along with the pharmacological characterization for the most promising Eph-ephrin antagonists in in vivo settings.
ISSN:1424-8247
1424-8247
DOI:10.3390/ph15020137