About: Design, synthesis, and evaluation of 3C protease inhibitors as anti-enterovirus 71 agents

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About: Design, synthesis, and evaluation of 3C protease inhibitors as anti-enterovirus 71 agents Goto Sponge NotDistinct Permalink

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

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Design, synthesis, and evaluation of 3C protease inhibitors as anti-enterovirus 71 agents
Creator	Kuo, Chih-Jung Liang, Po-Huang Shih, Shin-Ru Liu, Hun-Ge Chang, Shih-Cheng Fang, Jim-Min Lee, Ching-Yin Shie, Jiun-Jie Tseng, Sung-Nain Yen, Guei-Rung Hsu, T.-A
Source	Elsevier; Medline; PMC
abstract	Abstract Human enterovirus (EV) belongs to the picornavirus family, which consists of over 200 medically relevant viruses. A peptidomimetic inhibitor AG7088 was developed to inhibit the 3C protease of rhinovirus (a member of the family), a chymotrypsin-like protease required for viral replication, by forming a covalent bond with the active site Cys residue. In this study, we have prepared the recombinant 3C protease from EV71 (TW/2231/98), a particular strain which causes severe outbreaks in Asia, and developed inhibitors against the protease and the viral replication. For inhibitor design, the P3 group of AG7088, which is not interacting with the rhinovirus protease, was replaced with a series of cinnamoyl derivatives directly linked to P2 group through an amide bond to simplify the synthesis. While the replacement caused decreased potency, the activity can be largely improved by substituting the α,β-unsaturated ester with an aldehyde at the P1′ position. The best inhibitor 10b showed EC50 of 18nM without apparent toxicity (CC50 >25μM). Our study provides potent inhibitors of the EV71 3C protease as anti-EV71 agents and facilitates the combinatorial synthesis of derivatives for further improving the inhibitory activity.
has issue date	2008-08-01(xsd:dateTime)
bibo:doi	10.1016/j.bmc.2008.06.015
bibo:pmid	18583140
has license	els-covid
sha1sum (hex)	9fe8c52bb7e6a43562b7196b366623df35eea5d9
schema:url	https://doi.org/10.1016/j.bmc.2008.06.015
resource representing a document's title	Design, synthesis, and evaluation of 3C protease inhibitors as anti-enterovirus 71 agents
has PubMed Central identifier	PMC7125518
has PubMed identifier	18583140
schema:publication	Bioorganic & Medicinal Chemistry
resource representing a document's body	covid:9fe8c52bb7e6a43562b7196b366623df35eea5d9#body_text
is schema:about of	named entity 'improved' named entity 'ester' named entity 'rhinovirus' named entity 'potent' named entity 'cinnamoyl' named entity 'inhibitor' named entity 'ESTER' named entity 'HAVE' named entity 'FAMILY' named entity 'REPLACED' named entity 'RHINOVIRUS' named entity 'HUMAN ENTEROVIRUS' named entity 'POTENCY' named entity 'AMIDE BOND' named entity 'MEMBER OF' named entity 'INHIBITOR' named entity 'CAUSES' named entity 'REPLACEMENT' named entity 'INHIBITORY ACTIVITY' named entity 'ACTIVITY' named entity 'RECOMBINANT' named entity 'INTERACTING' covid:arg/9fe8c52bb7e6a43562b7196b366623df35eea5d9 named entity 'CHYMOTRYPSIN-LIKE PROTEASE' named entity 'AG7088' named entity 'ACTIVE SITE' named entity '200' named entity 'SIMPLIFY' named entity 'GROUP' named entity 'PICORNAVIRUS' named entity 'CYS' named entity 'REQUIRED' named entity 'FORMING' named entity 'OUTBREAKS' named entity 'IMPROVED BY' named entity 'IMPROVING' named entity 'SYNTHESIS' named entity 'AN ALDEHYDE' named entity 'EVALUATION' named entity 'UNSATURATED' named entity 'POSITION' named entity 'DESIGN' named entity 'SYNTHESIS' named entity 'SEVERE' named entity '28A' named entity 'COVALENT BOND' named entity 'ASIA' named entity 'DECREASED' named entity 'OUR' named entity 'LARGELY' named entity 'STUDY' named entity 'VIRAL REPLICATION' named entity 'PEPTIDOMIMETIC' named entity 'PARTICULAR' named entity 'TO INHIBIT' named entity 'DIRECTLY' named entity 'COMBINATORIAL SYNTHESIS' named entity 'EV71' named entity 'ENTEROVIRUS 71' named entity 'PROTEASE INHIBITORS' named entity 'SERIES' named entity 'DESIGN' named entity 'PROTEASE' named entity 'PROVIDES' named entity 'BEST' named entity 'APPARENT' named entity 'TOXICITY' named entity 'RESIDUE' named entity 'STRAIN' named entity 'VIRUSES' named entity 'RELEVANT'

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