Zhang Rui, Wei Dong-Qing, Du Qi-Shi, Chou Kuo-Chen
Tianjin Institute of Bioinformatics and Drug Discoveries and Tianjin Normal University, China.
Med Chem. 2006 May;2(3):309-14. doi: 10.2174/157340606776930736.
Flexible alignment and docking studies were conducted for the three octapeptides, ATLQANEV, AVLQSGFR, and ATLQAIAS, that were cleavable by SARS-CoV Mpro. It has been observed that all pharmacophores of the three peptides overlap very well, and that ATLQANEV binds best with the receptor, followed by AVLQSGFR, and then ATLQAIAS. During the process of docking the octapeptides to the SARS enzyme, the residues of the catalytic dyad, i.e., His-41 and Cys-145 are actively involved in forming the hydrogen bonds, so is the center residue (Gln) of all the three octapeptides. The findings are fully consistent with experimental observations. The present studies suggest that the octapeptides ATLQANEV and ATLQAIAS, like AVLQSGFR, might also be the good starting points for designing potential drugs against SARS.
对可被严重急性呼吸综合征冠状病毒(SARS-CoV)M蛋白酶切割的三种八肽ATLQANEV、AVLQSGFR和ATLQAIAS进行了柔性比对和对接研究。据观察,这三种肽的所有药效基团重叠得非常好,并且ATLQANEV与受体的结合最佳,其次是AVLQSGFR,然后是ATLQAIAS。在将八肽与SARS酶对接的过程中,催化二元组的残基,即His-41和Cys-145积极参与形成氢键,所有三种八肽的中心残基(Gln)也是如此。这些发现与实验观察结果完全一致。目前的研究表明,八肽ATLQANEV和ATLQAIAS与AVLQSGFR一样,也可能是设计抗SARS潜在药物的良好起点。