Vanda Pharmaceuticals, 2200 Pennsylvania NW, Suite 300-E, Washington, DC 20037, United States.
Vanda Pharmaceuticals, 2200 Pennsylvania NW, Suite 300-E, Washington, DC 20037, United States.
Int J Antimicrob Agents. 2020 Jun;55(6):106004. doi: 10.1016/j.ijantimicag.2020.106004. Epub 2020 Apr 30.
SARS-coronavirus 2 is the causal agent of the COVID-19 outbreak. SARS-Cov-2 entry into a cell is dependent upon binding of the viral spike (S) protein to cellular receptor and on cleavage of the spike protein by the host cell proteases such as Cathepsin L and Cathepsin B. CTSL/B are crucial elements of lysosomal pathway and both enzymes are almost exclusively located in the lysosomes. CTSL disruption offers potential for CoVID-19 therapies. The mechanisms of disruption include: decreasing expression of CTSL, direct inhibition of CTSL activity and affecting the conditions of CTSL environment (increase pH in the lysosomes). We have conducted a high throughput drug screen gene expression analysis to identify compounds that would downregulate the expression of CTSL/CTSB. One of the top significant results shown to downregulate the expression of the CTSL gene is amantadine (10uM). Amantadine was approved by the US Food and Drug Administration in 1968 as a prophylactic agent for influenza and later for Parkinson's disease. It is available as a generic drug. Amantadine in addition to downregulating CTSL appears to further disrupt lysosomal pathway, hence, interfering with the capacity of the virus to replicate. It acts as a lysosomotropic agent altering the CTSL functional environment. We hypothesize that amantadine could decrease the viral load in SARS-CoV-2 positive patients and as such it may serve as a potent therapeutic decreasing the replication and infectivity of the virus likely leading to better clinical outcomes. Clinical studies will be needed to examine the therapeutic utility of amantadine in COVID-19 infection.
严重急性呼吸综合征冠状病毒 2 是 COVID-19 爆发的病原体。SARS-CoV-2 进入细胞依赖于病毒刺突 (S) 蛋白与细胞受体的结合,以及宿主细胞蛋白酶(如组织蛋白酶 L 和组织蛋白酶 B)对刺突蛋白的切割。CTSL/B 是溶酶体途径的关键要素,两种酶几乎都仅位于溶酶体中。CTSL 的破坏为 COVID-19 治疗提供了潜力。破坏的机制包括:降低 CTSL 的表达、直接抑制 CTSL 活性以及影响 CTSL 环境的条件(增加溶酶体中的 pH 值)。我们进行了高通量药物筛选基因表达分析,以确定可下调 CTSL/CTSB 表达的化合物。显示下调 CTSL 基因表达的最重要结果之一是金刚烷胺(10uM)。金刚烷胺于 1968 年被美国食品和药物管理局批准作为流感的预防剂,后来也被批准用于帕金森病。它是一种通用药物。除了下调 CTSL 外,金刚烷胺似乎还进一步破坏了溶酶体途径,从而干扰了病毒复制的能力。它作为一种溶酶体趋向性药物改变了 CTSL 的功能环境。我们假设金刚烷胺可以降低 SARS-CoV-2 阳性患者的病毒载量,因此它可能作为一种有效的治疗方法,降低病毒的复制和感染力,从而带来更好的临床结果。需要进行临床研究来检查金刚烷胺在 COVID-19 感染中的治疗效用。