A recent study revealed that Perillaldehyde (PAE), a natural compound from Perilla frutescens, characterized by claimed neuroprotective, antiallergic, antinflammatory, antimicrobial, antitumor, gastroprotective and antidiabetic activities, acts as a ligand of the EphA2 receptor, modulating its signaling through the inhibition of ephrin-A1-EphA2 binding. In this study, we investigated the interaction between PAE and EphA2 with binding and functional assays. Our data demonstrate that PAE neither interferes with ephrin-A1-EphA2 interaction, nor significantly affects ephrin-A1-induced EphA2 activation. PAE is just one of many instances that teaches how difficult and challenging it is to identify natural compounds characterized by selectivity and specificity towards a molecular target.

Target validation of natural compounds: Perillaldehyde case study / Blesio, A.; Giorgio, C.; Sala, S.; Cavazzoni, A.; Zanotti, I.; Tognolini, M.. - In: INTERNATIONAL IMMUNOPHARMACOLOGY. - ISSN 1567-5769. - 172:(2026). [10.1016/j.intimp.2026.116178]

Target validation of natural compounds: Perillaldehyde case study

Blesio A.
Investigation
;
Giorgio C.;Sala S.;Cavazzoni A.;Zanotti I.;Tognolini M.
2026-01-01

Abstract

A recent study revealed that Perillaldehyde (PAE), a natural compound from Perilla frutescens, characterized by claimed neuroprotective, antiallergic, antinflammatory, antimicrobial, antitumor, gastroprotective and antidiabetic activities, acts as a ligand of the EphA2 receptor, modulating its signaling through the inhibition of ephrin-A1-EphA2 binding. In this study, we investigated the interaction between PAE and EphA2 with binding and functional assays. Our data demonstrate that PAE neither interferes with ephrin-A1-EphA2 interaction, nor significantly affects ephrin-A1-induced EphA2 activation. PAE is just one of many instances that teaches how difficult and challenging it is to identify natural compounds characterized by selectivity and specificity towards a molecular target.
2026
Target validation of natural compounds: Perillaldehyde case study / Blesio, A.; Giorgio, C.; Sala, S.; Cavazzoni, A.; Zanotti, I.; Tognolini, M.. - In: INTERNATIONAL IMMUNOPHARMACOLOGY. - ISSN 1567-5769. - 172:(2026). [10.1016/j.intimp.2026.116178]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/3055473
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