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Derivatization and combination therapy of current COVID-19 therapeutic agents: a review of mechanistic pathways, adverse effects, and binding sites.
Drug Discovery Today ( IF 6.5 ) Pub Date : 2020-08-12 , DOI: 10.1016/j.drudis.2020.08.002
Sally El Kantar 1 , Bilal Nehmeh 2 , Philippe Saad 2 , Gabie Mitri 2 , Celine Estephan 2 , Mohamad Mroueh 3 , Elias Akoury 1 , Robin I Taleb 2
Affiliation  

Current treatment of patients with coronavirus 2019 (COVID-19) involves repurposed drugs that inhibit viral infection by either binding to their respective targets or via modulating cellular signal transduction. However, there is still a great deal of efficacy enhancement through combination therapy and derivatization. Combination therapy should involve agents with significant activity and different mechanisms of action. The structural map of the interaction between a drug and its target protein will help guide drug discovery for devising safe and effective ways to treat COVID-19. Herein, we report numerous synthetic designs based on enhanced affinity to the viral carbohydrate-rich protein spikes and protein-binding sites of COVID-19.



中文翻译:

当前 COVID-19 治疗剂的衍生化和联合治疗:机制途径、不良反应和结合位点的综述。

目前对 2019 年冠状病毒 (COVID-19) 患者的治疗涉及改变用途的药物,这些药物通过结合各自的靶标或通过调节细胞信号转导来抑制病毒感染。然而,通过联合治疗和衍生化仍然有很大的疗效增强。联合治疗应涉及具有显着活性和不同作用机制的药物。药物与其靶蛋白之间相互作用的结构图将有助于指导药物发现,以设计安全有效的治疗 COVID-19 的方法。在此,我们报告了许多基于增强对 COVID-19 富含病毒碳水化合物的蛋白质尖峰和蛋白质结合位点的亲和力的合成设计。

更新日期:2020-08-12
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