Inhibition of SARS‐CoV 3C‐like Protease Activity by Theaflavin‐3,3′‐digallate (TF3)

Chen, Chia Nan; Lin, Coney Pei-Chen; Huang, Kuo Kuei; Chen, Wei Cheng; Hsieh, Hsin Pang; Liang, Po‐Huang; Hsu, John

doi:10.1093/ecam/neh081

Cited by 213 publications

(224 citation statements)

References 20 publications

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“…In addition to small molecules from chemical libraries, some research groups have turned to natural plant extracts such as Chinese herbs. Two research groups individually claimed that tannic acid, 3-isotheaflavin-3-gallate and theaflavin-3,3'-digallate from black tea and one plant-derived phenolic compound, hesperetin, are SARS-CoV M pro inhibitors [95,96].…”

Section: High-throughput Screeningmentioning

confidence: 99%

Drug Design Targeting the Main Protease, the Achilles Heel of Coronaviruses

Yang¹,

Bartlam²,

Rao

2006

CPD

169

144

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Coronaviruses (CoVs), a genus containing about 26 known species to date, cause highly prevalent diseases and are often severe or fatal in humans and animals. In 2003, a previously unknown coronavirus was identified to be the etiological agent of a global outbreak of a form of life-threatening pneumonia called severe acute respiratory syndrome (SARS). No efficacious therapy is currently available, and vaccines and drugs are under development to prevent SARS-CoV infection in many countries. The CoV main protease (M(pro)), which plays a pivotal role in viral gene expression and replication through a highly complex cascade involving the proteolytic processing of replicase polyproteins, is an attractive target for drug design. This review summarizes the recent advances in biological and structural studies, together with development of inhibitors targeting CoV M(pro)s. It is expected that inhibitors targeting CoV M(pro)s could be developed into wide-spectrum antiviral drugs against existing and possible future emerging CoV-associated diseases.

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Section: High-throughput Screeningmentioning

confidence: 99%

Drug Design Targeting the Main Protease, the Achilles Heel of Coronaviruses

Yang¹,

Bartlam²,

Rao

2006

CPD

169

144

View full text Add to dashboard Cite

show abstract

“…Therefore, it may be suggested that polyphenols (as supplements or in polyphenol-enriched diets) offer potential health benefits for HIV patients or could be promising candidates for the development of topical microbicides to reduce sexual HIV-1 transmission. Furthermore, antiviral activity of polyphenols has also been demonstrated for the severe acute respiratory syndrome-coronavirus infection [136] and herpes simplex virus (HSV-1 and HSV-2) infection [137]. However, increasing the local or systemic uptake of polyphenols might not be without risks.…”

Section: Enhancing the Cellular Antioxidant Defense As An Antiviral Smentioning

confidence: 99%

The role of cellular oxidoreductases in viral entry and virus infection-associated oxidative stress: potential therapeutic applications

Mathys

Balzarini

2015

Expert Opinion on Therapeutic Targets

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“…Through screening from a natural product library consisting of 720 compounds, Chen et al obtained two compounds, namely, tannic acid (IC 50 = 3 µM) and 3-isotheaflavin-3-gallate (TF2B) (IC 50 = 7 µM) as potent inhibitors of SARS 3CL pro [50]. These two compounds belong to a group of natural polyphenols in tea, and therefore Chen et al further investigated the 3CL pro inhibitory activities of the extracts from different types of tea including green tea, oolong tea, Puer tea, and black tea.…”

Section: A From High Throughput Screeningmentioning

confidence: 99%

Characterization and Inhibition of SARS-Coronavirus Main Protease

Liang

2006

CTMC

Self Cite

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Severe acute respiratory syndrome (SARS) is an emerging infectious disease caused by a novel human coronavirus (CoV). During the 2003 epidemic, the disease rapidly spread from its origin in southern China to other countries and affected almost 8000 patients, which resulted in about 800 fatalities. A chymotrypsin-like cysteine protease named 3C-like protease (3CLpro) is essential for the life cycle of the SARS-CoV. This main protease is responsible for maturation of functional proteins and represents a key anti-viral target. HPLC and fluorescence-based assays have been used to characterize the protease and to determine the potency of the inhibitors. The fluorogenic method monitoring the increase of fluorescence from the cleavage of a peptide substrate containing an Edans-Dabcyl fluorescence quenching pair at two ends has enabled the use of high throughput screening to speed up the drug discovery process. Several groups of inhibitors have been identified through high throughput screening and rational drug design approaches. Thus, alpha,beta-unsaturated peptidomimetics, anilides, metal-conjugated compounds, boronic acids, quinolinecarboxylate derivatives, thiophenecarboxylates, phthalhydrazide-substituted ketoglutamine analogues, isatin and natural products have been identified as potent inhibitors of the SARS-CoV main protease. The different classes of inhibitors reported in these studies are summarized in this review. Some of these inhibitors could be developed into potential drug candidates, which may provide a solution to combat possible reoccurrence of the SARS and other life-threatening viruses with 3CL proteases.

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Inhibition of SARS‐CoV 3C‐like Protease Activity by Theaflavin‐3,3′‐digallate (TF3)

Cited by 213 publications

References 20 publications

Drug Design Targeting the Main Protease, the Achilles Heel of Coronaviruses

Drug Design Targeting the Main Protease, the Achilles Heel of Coronaviruses

The role of cellular oxidoreductases in viral entry and virus infection-associated oxidative stress: potential therapeutic applications

Characterization and Inhibition of SARS-Coronavirus Main Protease

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