作者
Ji-Young Park, Jang Hoon Kim, Young Min Kim, Hyung Jae Jeong, Dae Wook Kim, Ki Hun Park, Hyung-Jun Kwon, Su-Jin Park, Woo Song Lee, Young Bae Ryu
发表日期
2012/10/1
期刊
Bioorganic & medicinal chemistry
卷号
20
期号
19
页码范围
5928-5935
出版商
Pergamon
简介
In the search for anti-SARS-CoV, tanshinones derived from Salvia miltiorrhiza were found to be specific and selective inhibitors for the SARS-CoV 3CLpro and PLpro, viral cysteine proteases. A literature search for studies involving the seven isolated tanshinone hits showed that at present, none have been identified as coronaviral protease inhibitors. We have identified that all of the isolated tanshinones are good inhibitors of both cysteine proteases. However, their activity was slightly affected by subtle changes in structure and targeting enzymes. All isolated compounds (1–7) act as time dependent inhibitors of PLpro, but no improved inhibition was observed following preincubation with the 3CLpro. In a detail kinetic mechanism study, all of the tanshinones except rosmariquinone (7) were identified as noncompetitive enzyme isomerization inhibitors. However, rosmariquinone (7) showed a different kinetic …
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JY Park, JH Kim, YM Kim, HJ Jeong, DW Kim, KH Park… - Bioorganic & medicinal chemistry, 2012