Thiopurine analogue inhibitors of severe acute respiratory syndrome-coronavirus papain-like protease, a deubiquitinating and deISGylating enzyme.
Identifieur interne : 000A77 ( 2020/Analysis ); précédent : 000A76; suivant : 000A78Thiopurine analogue inhibitors of severe acute respiratory syndrome-coronavirus papain-like protease, a deubiquitinating and deISGylating enzyme.
Auteurs : Xin Chen [Taïwan] ; Chi-Yuan Chou ; Gu-Gang ChangSource :
- Antiviral chemistry & chemotherapy [ 0956-3202 ] ; 2009.
Descripteurs français
- KwdFr :
- Cysteine endopeptidases (), Humains, Inhibiteurs de protéases (), Inhibiteurs de protéases (pharmacologie), Inhibiteurs de protéases (usage thérapeutique), Protéines virales (), Protéines virales (antagonistes et inhibiteurs), Syndrome respiratoire aigu sévère (traitement médicamenteux), Syndrome respiratoire aigu sévère (virologie), Tioguanine (), Tioguanine (pharmacologie), Tioguanine (usage thérapeutique), Virus du SRAS (enzymologie).
- MESH :
- antagonistes et inhibiteurs : Protéines virales.
- enzymologie : Virus du SRAS.
- pharmacologie : Inhibiteurs de protéases, Tioguanine.
- traitement médicamenteux : Syndrome respiratoire aigu sévère.
- usage thérapeutique : Inhibiteurs de protéases, Tioguanine.
- virologie : Syndrome respiratoire aigu sévère.
- Cysteine endopeptidases, Humains, Inhibiteurs de protéases, Protéines virales, Tioguanine.
English descriptors
- KwdEn :
- Cysteine Endopeptidases (chemistry), Humans, Mercaptopurine (chemistry), Mercaptopurine (pharmacology), Mercaptopurine (therapeutic use), Protease Inhibitors (chemistry), Protease Inhibitors (pharmacology), Protease Inhibitors (therapeutic use), SARS Virus (enzymology), Severe Acute Respiratory Syndrome (drug therapy), Severe Acute Respiratory Syndrome (virology), Thioguanine (chemistry), Thioguanine (pharmacology), Thioguanine (therapeutic use), Viral Proteins (antagonists & inhibitors), Viral Proteins (chemistry).
- MESH :
- chemical , antagonists & inhibitors : Viral Proteins.
- chemical , chemistry : Cysteine Endopeptidases, Mercaptopurine, Protease Inhibitors, Thioguanine, Viral Proteins.
- chemical , pharmacology : Mercaptopurine, Protease Inhibitors, Thioguanine.
- chemical , therapeutic use : Mercaptopurine, Protease Inhibitors, Thioguanine.
- drug therapy : Severe Acute Respiratory Syndrome.
- enzymology : SARS Virus.
- virology : Severe Acute Respiratory Syndrome.
- Humans.
Abstract
In the search for effective therapeutics against severe acute respiratory syndrome (SARS), 6-mercaptopurine (6MP) and 6-thioguanine (6TG) were found to be specific inhibitors for the SARS-coronavirus (CoV) papain-like protease (PLpro), a cysteine protease with deubiquitinating and deISGylating activity. 6MP and 6TG have long been used in cancer chemotherapy for treatment of acute lymphoblastic or myeloblastic leukaemia. Development and optimization of 6MP and 6TG will not only be important for antiviral studies, but also for further elucidating the biological functions of cellular deubiquitinating enzymes (DUBs) and deISGylating enzymes. So far, several crystal structures of cellular DUBs have been solved. Structure comparison has been carried out to search for DUBs with a similar structure to that of PLpro, and we have tried to dock 6MP and 6TG into these DUBs to investigate the potential use of 6MP and 6TG as cellular DUB inhibitors. The best docking score and binding energy for 6MP and 6TG is against ubiquitin-specific protease (USP)14, suggesting that 6MP and 6TG are potential inhibitors of USP14. Finding new usages for old drugs will speed up the process of drug discovery and substantially reduce the cost of drug development.
DOI: 10.1177/095632020901900402
PubMed: 19374142
Affiliations:
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pubmed:19374142Le document en format XML
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effective therapeutics against severe acute respiratory syndrome (SARS), 6-mercaptopurine (6MP) and 6-thioguanine (6TG) were found to be specific inhibitors for the SARS-coronavirus (CoV) papain-like protease (PLpro), a cysteine protease with deubiquitinating and deISGylating activity. 6MP and 6TG have long been used in cancer chemotherapy for treatment of acute lymphoblastic or myeloblastic leukaemia. Development and optimization of 6MP and 6TG will not only be important for antiviral studies, but also for further elucidating the biological functions of cellular deubiquitinating enzymes (DUBs) and deISGylating enzymes. So far, several crystal structures of cellular DUBs have been solved. Structure comparison has been carried out to search for DUBs with a similar structure to that of PLpro, and we have tried to dock 6MP and 6TG into these DUBs to investigate the potential use of 6MP and 6TG as cellular DUB inhibitors. The best docking score and binding energy for 6MP and 6TG is against ubiquitin-specific protease (USP)14, suggesting that 6MP and 6TG are potential inhibitors of USP14. Finding new usages for old drugs will speed up the process of drug discovery and substantially reduce the cost of drug development.</div></front></TEI><affiliations><list><country><li>Taïwan</li></country></list><tree><noCountry><name sortKey="Chang, Gu Gang" sort="Chang, Gu Gang" uniqKey="Chang G" first="Gu-Gang" last="Chang">Gu-Gang Chang</name><name sortKey="Chou, Chi Yuan" sort="Chou, Chi Yuan" uniqKey="Chou C" first="Chi-Yuan" last="Chou">Chi-Yuan Chou</name></noCountry><country name="Taïwan"><noRegion><name sortKey="Chen, Xin" sort="Chen, Xin" uniqKey="Chen X" first="Xin" last="Chen">Xin Chen</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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