针对严重急性呼吸综合征冠状病毒主要蛋白酶设计的八肽抑制剂的合成与活性
Synthesis and activity of an octapeptide inhibitor designed for SARS coronavirus main proteinase.
作者信息
Gan Yi-Ru, Huang He, Huang Yong-Dong, Rao Chun-Ming, Zhao Yang, Liu Jin-Sheng, Wu Lei, Wei Dong-Qing
机构信息
School of Chemical Engineering & Technology, Tianjin University, Tianjin 300072, China.
出版信息
Peptides. 2006 Apr;27(4):622-5. doi: 10.1016/j.peptides.2005.09.006. Epub 2005 Oct 19.
The outbreak of SARS, a life-threatening disease, has spread over many countries around the world. So far there is no effective drug for the treatment of SARS. Stimulated by the binding mechanism of SARS-CoV Mpro with the octapeptide AVLQSGFR reported recently as well as the "Chou's distorted key" theory, we synthesized the octapeptide AVLQSGFR for conducting various biochemical experiments to investigate the antiviral potential of the octapeptide against SARS coronavirus (BJ-01). The results demonstrate that, compared with other compounds reported so far, AVLQSGFR is the most active in inhibiting replication of the SARS coronavirus, and that no detectable toxicity is observed on Vero cells under the condition of experimental concentration.
严重急性呼吸综合征（SARS）是一种危及生命的疾病，已在世界许多国家蔓延。到目前为止，尚无治疗SARS的有效药物。受最近报道的SARS-CoV Mpro与八肽AVLQSGFR的结合机制以及“周氏扭曲钥匙”理论的启发，我们合成了八肽AVLQSGFR，以进行各种生化实验，研究该八肽对SARS冠状病毒（BJ-01）的抗病毒潜力。结果表明，与目前报道的其他化合物相比，AVLQSGFR在抑制SARS冠状病毒复制方面活性最高，并且在实验浓度条件下对Vero细胞未观察到可检测到的毒性。
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