About: Tanshinones as selective and slow-binding inhibitors for SARS-CoV cysteine proteases

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About: Tanshinones as selective and slow-binding inhibitors for SARS-CoV cysteine proteases Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Tanshinones as selective and slow-binding inhibitors for SARS-CoV cysteine proteases
Creator	Park, Su-Jin Kwon, Hyung-Jun Park, Ji-Young Jeong, Jae Kim, Dae Kim, Jang Kim, Young Lee, Woo Park, Ki Ryu, Young
Source	Elsevier; Medline; PMC
abstract	Abstract 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 mechanism through mixed-type simple reversible slow-binding inhibition. Furthermore, tanshinone I (5) exhibited the most potent nanomolar level inhibitory activity toward deubiquitinating (IC50 =0.7μM). Additionally, the inhibition is selective because these compounds do not exert significant inhibitory effects against other proteases including chymotrysin, papain, and HIV protease. These findings provide potential inhibitors for SARS-CoV viral infection and replication.
has issue date	2012-10-01(xsd:dateTime)
bibo:doi	10.1016/j.bmc.2012.07.038
bibo:pmid	22884354
has license	els-covid
sha1sum (hex)	2d308c06e6e9edcd5c843b9732133675e3bf4c9a
schema:url	https://doi.org/10.1016/j.bmc.2012.07.038
resource representing a document's title	Tanshinones as selective and slow-binding inhibitors for SARS-CoV cysteine proteases
has PubMed Central identifier	PMC7127169
has PubMed identifier	22884354
schema:publication	Bioorganic & Medicinal Chemistry
resource representing a document's body	covid:2d308c06e6e9edcd5c843b9732133675e3bf4c9a#body_text
is schema:about of	named entity 'identified' named entity 'derived' named entity 'CYSTEINE PROTEASES' named entity 'INHIBITORS' named entity 'SARS-COV' named entity 'MECHANISM' named entity 'BINDING' named entity 'LITERATURE SEARCH' named entity 'INHIBITORY' named entity 'ACTIVITY' named entity 'SIMPLE' named entity 'ISOLATED' named entity '0.7' named entity 'ENZYMES' named entity 'SEARCH' named entity 'ACT' named entity 'SLIGHTLY' named entity 'KINETIC' covid:arg/2d308c06e6e9edcd5c843b9732133675e3bf4c9a named entity 'SARS-COV' named entity '287' named entity 'SEVEN' named entity 'CHANGES' named entity 'SELECTIVE' named entity 'SELECTIVE' named entity 'SLOW' named entity 'STRUCTURE' named entity 'TIME' named entity 'IMPROVED' named entity 'TARGETING' named entity 'PRO' named entity 'POTENTIAL' named entity 'STUDIES' named entity 'FOLLOWING' named entity 'EXCEPT' named entity 'REVERSIBLE' named entity 'PRESENT' named entity 'INCLUDING' named entity 'REPLICATION' named entity 'INHIBITION' named entity 'THESE' named entity 'PAPAIN' named entity 'THEIR' named entity 'DERIVED' named entity 'INVOLVING' named entity 'FINDINGS' named entity 'INHIBITORY ACTIVITY' named entity 'BINDING' named entity 'MIXED' named entity 'HAVE' named entity 'IDENTIFIED' named entity 'EFFECTS' named entity 'CYSTEINE PROTEASES' named entity 'PROTEASE INHIBITORS' named entity 'TYPE' named entity 'INHIBITORS' named entity 'PROTEASES' named entity 'NANOMOLAR' named entity 'FOUND' named entity 'DEPENDENT' named entity 'SALVIA MILTIORRHIZA' named entity 'OBSERVED' named entity 'ENZYME' named entity 'DO NOT' named entity 'STUDY' named entity 'SIGNIFICANT' named entity 'HIV PROTEASE' named entity 'BUT' named entity 'DIFFERENT' named entity 'DEUBIQUITINATING' named entity 'SPECIFIC' named entity 'VIRAL'

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