Given the ability of lithocholic acid to recognize FXR, TGR5 and EphA2 receptors, we hypothesized the structural requirements to bind each of these receptors might be similar. We selected a set of commercially available FXR or TGR5 ligands and tested them for their ability to inhibit EphA2 by targeting the EphA2–ephrin-A1 interface. Moreover, a small panel of GW4064 derivatives was synthesized.

Target Hopping as a Useful Tool for the Identification of Novel EphA2 Protein–Protein Antagonists / Tognolini, Massimiliano; Incerti, Matteo; Pala, Daniele; Russo, Simonetta; Castelli, Riccardo; HASSAN MOHAMED, Iftiin; Giorgio, Carmine; Lodola, Alessio. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 9:1(2014), pp. 67-72. [10.1002/cmdc.201300305]

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

TOGNOLINI, Massimiliano;INCERTI, Matteo;PALA, Daniele;RUSSO, Simonetta;CASTELLI, Riccardo;HASSAN MOHAMED, Iftiin;GIORGIO, Carmine;LODOLA, Alessio
2014-01-01

Abstract

Given the ability of lithocholic acid to recognize FXR, TGR5 and EphA2 receptors, we hypothesized the structural requirements to bind each of these receptors might be similar. We selected a set of commercially available FXR or TGR5 ligands and tested them for their ability to inhibit EphA2 by targeting the EphA2–ephrin-A1 interface. Moreover, a small panel of GW4064 derivatives was synthesized.
2014
Target Hopping as a Useful Tool for the Identification of Novel EphA2 Protein–Protein Antagonists / Tognolini, Massimiliano; Incerti, Matteo; Pala, Daniele; Russo, Simonetta; Castelli, Riccardo; HASSAN MOHAMED, Iftiin; Giorgio, Carmine; Lodola, Alessio. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 9:1(2014), pp. 67-72. [10.1002/cmdc.201300305]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/2645662
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