研究动态
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Arf6 作为治疗靶点:结构、机制和抑制剂。

Arf6 as a therapeutic target: Structure, mechanism, and inhibitors.

发表日期:2023 Oct
作者: Dejuan Sun, Yuanyuan Guo, Piyu Tang, Hua Li, Lixia Chen
来源: Acta Pharmaceutica Sinica B

摘要:

ADP-核糖基化因子 6 (Arf6) 是 Ras 超家族的一种小 G 蛋白,在多种细胞事件中发挥着关键作用,包括胞吐作用、内吞作用、肌动蛋白重塑、质膜重组和囊泡运输。 Arf6 通过激活细胞运动和侵袭来调节癌症的进展。 Arf6 的异常激活是一个潜在的治疗靶点。本综述旨在了解 Arf6 对未来癌症治疗的综合功能。总结了 Arf6 GEF、蛋白质结构和在癌症中的作用。了解 Arf6 介导的癌细胞生长和存活的机制至关重要。讨论了 Arf6 的结构特征及其努力,并可能有助于发现未来新型蛋白质-蛋白质相互作用抑制剂。此外,Arf6抑制剂及其作用机制列于表中。本综述进一步强调了 Arf6 在耐药性中的关键作用,并试图展望 Arf6 在癌症治疗中的前景。© 2023 中国药学会和中国医学科学院药物研究所。由 Elsevier B.V. 制作和主持
ADP-ribosylation factor 6 (Arf6), a small G-protein of the Ras superfamily, plays pivotal roles in multiple cellular events, including exocytosis, endocytosis, actin remodeling, plasma membrane reorganization and vesicular transport. Arf6 regulates the progression of cancer through the activation of cell motility and invasion. Aberrant Arf6 activation is a potential therapeutic target. This review aims to understand the comprehensive function of Arf6 for future cancer therapy. The Arf6 GEFs, protein structure, and roles in cancer have been summarized. Comprehending the mechanism underlying Arf6-mediated cancer cell growth and survival is essential. The structural features of Arf6 and its efforts are discussed and may be contributed to the discovery of future novel protein-protein interaction inhibitors. In addition, Arf6 inhibitors and mechanism of action are listed in the table. This review further emphasizes the crucial roles in drug resistance and attempts to offer an outlook of Arf6 in cancer therapy.© 2023 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.