期刊名称：International Journal of Fundamental and Applied Sciences
印刷版ISSN：2278-1404
出版年度：2017
卷号：6
期号：4
页码：34-39
出版社：BioMedAsia
摘要：Bacillus anthracis is a notorious occupational zoonotic agent causing anthrax to veterinarians. Anthrax infection is
highly lethal in its most virulent form and produces a combination of three endotoxins namely Protective antigen,
Lethal factor and Edema factor. Protective antigen binds to target cells and eases the transfer of either Edema factor
or Lethal factor into the cytosol. One possible protein target is Furin, an endogenous, membrane-associated, trypsinlike
serine endoprotease which is utilized by B. anthracis as a means of activating Protective Antigen (PA). In this
study, for the purpose of lead development, Dehydro Andrographolide Succinic acid Monoester (DASM) inhibitor of
Furin was selected as a template. Furin is involved in other diseases, DASM was modified by adding anti-cancer, anti
-inflammatory, anti-tuberculosis and anti-viral groups. It was found that modification with each group like
Pyrazofurin, Ethanol, Dimethyl, Dimethylbutyl, Mercaptopurine, Sulfacetamide, Ethambutol, Isoniazid to DASM
showed a better interaction. The ligand with Pyrazofurin as the modification group showed high affinity with Furin
involving the active site residue SER 368. The results suggest that DASM containing pyrazofurin (compound2) as
side group can be an appropriate lead for the development of Furin inhibitors.
