title: Are we using the right pharmacological tools to target EphA4?
abstract: The EphA4 receptor has been proposed to be a key actor in neurodegenerative diseases. In the last years, several research groups focused their efforts on the discovery of small molecules capable of blocking EphA4 activity by binding its extracellular domain. However, none of the compounds so far identified possess adequate chemical and/or pharmacological profiles to assess the "druggability" of EphA4 in animal models. New efforts are required to deliver a new generation of suitable pharmacological tools.
authors.affiliation: Dipartimento di Farmacia, Università di Parma , Viale delle Scienze 27/a, 43124 Parma, Italia.
authors.forename: Massimiliano
authors.initials: M
authors.lastname: Tognolini
authors.forename: Matteo
authors.initials: M
authors.lastname: Incerti
authors.forename: Alessio
authors.initials: A
authors.lastname: Lodola
mesh_terms: D000818:Animals; D006801:Humans; D026121:Indole Alkaloids / Q000737:chemistry / Q000627:therapeutic use; D008958:Models, Molecular; D019636:Neurodegenerative Diseases / Q000188:drug therapy / Q000378:metabolism*; D000078183:Oxindoles; D011758:Pyrroles / Q000737:chemistry / Q000627:therapeutic use; D036122:Receptor, EphA4 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D012459:Salicylates / Q000737:chemistry / Q000627:therapeutic use; D015398:Signal Transduction / Q000187:drug effects
chemical_list: C579419:4-(2,5-dimethylpyrrol-1-y1)-2-hydroxybenzoic acid; D026121:Indole Alkaloids; D000078183:Oxindoles; D011758:Pyrroles; D012459:Salicylates; C052714:rhyncophylline; D036122:Receptor, EphA4
keywords: Eph-ephrin antagonist; EphA4; Rhynchophylline; UniPR129; compound 1