About: Thiopurine analogues inhibit papain-like protease of severe acute respiratory syndrome coronavirus

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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	Thiopurine analogues inhibit papain-like protease of severe acute respiratory syndrome coronavirus
Creator	Chang, Gu-Gang Chou, Chi-Yuan Turk, Boris Chen, Xin Chien, Chia-Hui Han, Yu-San Hsieh, Hsing-Pang Trstenjak Prebanda, Mojca
Source	Elsevier; Medline; PMC
abstract	Abstract The papain-like protease of severe acute respiratory syndrome coronavirus (PLpro) (EC 3.4.22.46) is essential for the viral life cycle and therefore represents an important antiviral target. We have identified 6MP and 6TG as reversible and slow-binding inhibitors of SARS-CoV PLpro, which is the first report about small molecule reversible inhibitors of PLpro. The inhibition mechanism was investigated by kinetic measurements and computer docking. Both compounds are competitive, selective, and reversible inhibitors of the PLpro with K is values ∼10 to 20μM. A structure–function relationship study has identified the thiocarbonyl moiety of 6MP or 6TG as the active pharmacophore essential for these inhibitions, which has not been reported before. The inhibition is selective because these compounds do not exert significant inhibitory effects against other cysteine proteases, including SARS-CoV 3CLpro and several cathepsins. Thus, our results present the first potential chemical leads against SARS-CoV PLpro, which might be used as lead compounds for further optimization to enhance their potency against SARS-CoV. Both 6MP and 6TG are still used extensively in clinics, especially for children with acute lymphoblastic or myeloblastic leukemia. In light of the possible inhibition against subset of cysteine proteases, our study has emphasized the importance to study in depth these drug actions in vivo.
has issue date	2008-04-15(xsd:dateTime)
bibo:doi	10.1016/j.bcp.2008.01.005
bibo:pmid	18313035
has license	els-covid
sha1sum (hex)	ca5bca39d98242b83a33252236335a766f0bb4bc
schema:url	https://doi.org/10.1016/j.bcp.2008.01.005
resource representing a document's title	Thiopurine analogues inhibit papain-like protease of severe acute respiratory syndrome coronavirus
has PubMed Central identifier	PMC7092826
has PubMed identifier	18313035
schema:publication	Biochemical Pharmacology
resource representing a document's body	covid:ca5bca39d98242b83a33252236335a766f0bb4bc#body_text
is schema:about of	named entity 'SEVERE ACUTE RESPIRATORY SYNDROME CORONAVIRUS' named entity 'resonance energy transfer' named entity 'proteinase' named entity 'N A' named entity 'V A' named entity 'SARS' named entity 'DEUBIQUITINATION' named entity 'A T' named entity 'CORONAVIRUS' named entity '6MP' named entity 'ABBREVIATIONS' named entity 'AMC' named entity 'D I' named entity 'FRET' named entity 'PROTEASE' named entity 'LIKE' named entity 'I E' named entity 'SEVERE ACUTE RESPIRATORY SYNDROME' named entity 'MATTER' named entity 'PROTEASE' named entity 'H O' named entity '7-AMINO-4-METHYLCOUMARIN' named entity 'THIOPURINE' named entity 'DUB' named entity 'L H' named entity 'C O' named entity 'PAPAIN-LIKE PROTEINASE 2' named entity '6-THIOGUANINE' named entity 'PAPAIN' named entity 'FLUORESCENCE RESONANCE ENERGY TRANSFER' named entity 'R M' named entity '2952' named entity 'ENZYME' named entity 'L S' named entity 'enzyme activity' named entity 'high-throughput' named entity 'deubiquitinating' named entity 'ligated' named entity 'AMC' named entity 'PLpro' named entity 'enzyme' named entity 'papain' named entity 'coronavirus' named entity 'papain' named entity 'severe acute respiratory syndrome coronavirus' named entity 'protease' named entity 'deubiquitinating' named entity 'PLpro' named entity 'thiocarbonyl' named entity 'enzymatic activity' named entity '6MP' named entity 'TPMT' named entity '6MP' named entity 'Novagen' named entity 'ubiquitin' named entity 'thio' named entity 'semi-log plot' named entity 'FRET' named entity '3CLpro' named entity 'PLpro' named entity 'enzyme' named entity 'RNA virus' named entity 'human clinical trials' named entity 'yeast' named entity 'Valencia, CA' named entity 'PLpro' named entity 'PLpro' named entity '6MP' named entity 'supernatant' named entity 'molecular modeling' named entity 'SARS-CoV' named entity 'allosteric site' named entity 'metabolically' named entity '6-Thioguanine'

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