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10.1002/chem.202004112

http://scihub22266oqcxt.onion/10.1002/chem.202004112
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32915473!7756435!32915473
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suck abstract from ncbi


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pmid32915473      Chemistry 2020 ; 26 (66): 15140-15144
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  • Gold Metallodrugs to Target Coronavirus Proteins: Inhibitory Effects on the Spike-ACE2 Interaction and on PLpro Protease Activity by Auranofin and Gold Organometallics* #MMPMID32915473
  • Gil-Moles M; Basu U; Bussing R; Hoffmeister H; Turck S; Varchmin A; Ott I
  • Chemistry 2020[Nov]; 26 (66): 15140-15144 PMID32915473show ga
  • Gold complexes have a long tradition in medicine and for many examples antirheumatic, anticancer or anti-infective effects have been confirmed. Herein, we evaluated the lead compound Auranofin and five selected gold organometallics as inhibitors of two relevant drug targets of severe acute respiratory syndrome coronaviruses (SARS-CoV). The gold metallodrugs were effective inhibitors of the interaction of the SARS-CoV-2 spike protein with the angiotensin converting enzyme 2 (ACE2) host receptor and might thus interfere with the viral entry process. The gold metallodrugs were also efficient inhibitors of the papain-like protease (PLpro) of SARS-CoV-1 and SARS-CoV-2, which is a key enzyme in the viral replication. Regarding PLpro from SARS-CoV-2, the here reported inhibitors are among the very first experimentally confirmed examples with activity against this target enzyme. Importantly, the activity of the complexes against both PLpro enzymes correlated with the ability of the inhibitors to remove zinc ions from the labile zinc center of the enzyme. Taken together, the results of this pilot study suggest further evaluation of gold complexes as SARS-CoV antiviral drugs.
  • |*COVID-19 Drug Treatment[MESH]
  • |Angiotensin-Converting Enzyme 2/*antagonists & inhibitors/metabolism[MESH]
  • |Antiviral Agents/pharmacology[MESH]
  • |Auranofin/chemistry/*pharmacology[MESH]
  • |COVID-19/virology[MESH]
  • |Coronavirus 3C Proteases/*antagonists & inhibitors/metabolism[MESH]
  • |Gold/*chemistry/pharmacology[MESH]
  • |Humans[MESH]
  • |Molecular Targeted Therapy[MESH]
  • |Organometallic Compounds/chemistry/*pharmacology[MESH]
  • |SARS-CoV-2/*drug effects/enzymology/metabolism[MESH]


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