Di Stasi Rossella, De Rosa Lucia, D'Andrea Luca D
Istituto di Biostrutture e Bioimmagini, CNR, Via Mezzocannone 16, 80134 Napoli, Italy.
Istituto di Biostrutture e Bioimmagini, CNR, Via Nizza 52, 10126 Torino, Italy.
Drug Discov Today. 2020 Dec;25(12):2130-2148. doi: 10.1016/j.drudis.2020.09.022. Epub 2020 Sep 28.
Axl receptor tyrosine kinase (RTK) and its ligand, growth arrest-specific protein 6 (Gas6), are involved in several biological functions and participate in the development and progression of a range of malignancies and autoimmune disorders. In this review, we present this molecular system from a drug discovery perspective, highlighting its therapeutic implications and challenges that need to be addressed. We provide an update on Axl/Gas6 axis biology, exploring its role in fields ranging from angiogenesis, cancer development and metastasis, immune response and inflammation to viral infection. Finally, we summarize the molecules that have been developed to date to target the Axl/Gas6 molecular system for therapeutic and diagnostic applications.
Axl受体酪氨酸激酶(RTK)及其配体生长停滞特异性蛋白6(Gas6)参与多种生物学功能,并在一系列恶性肿瘤和自身免疫性疾病的发生发展中发挥作用。在本综述中,我们从药物发现的角度介绍这个分子系统,强调其治疗意义以及需要应对的挑战。我们提供了Axl/Gas6轴生物学的最新进展,探讨了其在从血管生成、癌症发生与转移、免疫反应和炎症到病毒感染等领域中的作用。最后,我们总结了迄今为止已开发出的针对Axl/Gas6分子系统用于治疗和诊断应用的分子。