Dipartimento di Farmacia, Università di Parma , Viale delle Scienze 27/a, 43124 Parma, Italia.
ACS Chem Neurosci. 2014 Dec 17;5(12):1146-7. doi: 10.1021/cn500285h. Epub 2014 Nov 18.
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.
EphA4 受体被认为是神经退行性疾病的关键因素。在过去的几年中，几个研究小组致力于发现能够通过结合 EphA4 的细胞外结构域来阻断 EphA4 活性的小分子。然而，迄今为止鉴定的化合物都没有足够的化学和/或药理学特性来评估 EphA4 在动物模型中的“可药性”。需要新的努力来提供新一代合适的药理学工具。
