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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Main Authors: Lorenzo Guidetti (Author), Riccardo Castelli (Author), Laura Scalvini (Author), Francesca Ferlenghi (Author), Miriam Corrado (Author), Carmine Giorgio (Author), Massimiliano Tognolini (Author), Alessio Lodola (Author)
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Published: MDPI AG, 2022-01-01T00:00:00Z.
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001 doaj_0b82201a259e4962b13fbf700c20e7b4
042 |a dc 
100 1 0 |a Lorenzo Guidetti  |e author 
700 1 0 |a Riccardo Castelli  |e author 
700 1 0 |a Laura Scalvini  |e author 
700 1 0 |a Francesca Ferlenghi  |e author 
700 1 0 |a Miriam Corrado  |e author 
700 1 0 |a Carmine Giorgio  |e author 
700 1 0 |a Massimiliano Tognolini  |e author 
700 1 0 |a Alessio Lodola  |e author 
245 0 0 |a Protein-Protein Interaction Inhibitors Targeting the Eph-Ephrin System with a Focus on Amino Acid Conjugates of Bile Acids 
260 |b MDPI AG,   |c 2022-01-01T00:00:00Z. 
500 |a 10.3390/ph15020137 
500 |a 1424-8247 
520 |a 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. 
546 |a EN 
690 |a Eph receptor 
690 |a ephrin 
690 |a bile acids 
690 |a protein-protein interaction 
690 |a small molecules 
690 |a antagonist 
690 |a Medicine 
690 |a R 
690 |a Pharmacy and materia medica 
690 |a RS1-441 
655 7 |a article  |2 local 
786 0 |n Pharmaceuticals, Vol 15, Iss 2, p 137 (2022) 
787 0 |n https://www.mdpi.com/1424-8247/15/2/137 
787 0 |n https://doaj.org/toc/1424-8247 
856 4 1 |u https://doaj.org/article/0b82201a259e4962b13fbf700c20e7b4  |z Connect to this object online.