Laboratory for Drug Design and Synthesis, Department of Pharmaceutical Sciences and Natural Products, School of Basic and Applied Sciences, Central University of Punjab, Bathinda, 151001, India.
Curr Top Med Chem. 2020;20(12):1105-1123. doi: 10.2174/1568026620666200207100227.
The EGFR is overexpressed in numerous cancers. So, it becomes one of the most favorable drug targets. Single-acting EGFR inhibitors on prolong use induce resistance and side effects. Inhibition of EGFR and/or its interacting proteins by dual/combined/multitargeted therapies can deliver more efficacious drugs with less or no resistance.
The review delves deeper to cover the aspects of EGFR mediated endocytosis, leading to its trafficking, internalization, and crosstalk(s) with HDACs.
This review is put forth to congregate relevant literature evidenced on EGFR, its impact on cancer prognosis, inhibitors, and its trafficking regulation by acetylation along with the current strategies involved in targeting these proteins (EGFR and HDACs) successfully by involving dual/hybrid/combination chemotherapy.
The current information on cross-talk of EGFR and HDACs would likely assist researchers in designing and developing dual or multitargeted inhibitors through combining the required pharmacophores.
表皮生长因子受体 (EGFR) 在许多癌症中过度表达，因此成为最有利的药物靶点之一。单作用 EGFR 抑制剂长期使用会诱导耐药性和副作用。通过双重/联合/多靶点治疗抑制 EGFR 及其相互作用蛋白可以提供更有效的药物，而耐药性更小或没有。
本综述深入探讨 EGFR 介导的内吞作用及其导致的转位、内化和与 HDACs 的串扰。
提出本综述以汇集有关 EGFR 的相关文献，包括其对癌症预后的影响、抑制剂以及乙酰化对其转运的调节，以及目前通过双重/混合/联合化疗成功靶向这些蛋白（EGFR 和 HDACs）的策略。
目前关于 EGFR 和 HDACs 串扰的信息可能有助于研究人员通过结合所需的药效团设计和开发双重或多靶点抑制剂。
