About: Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic α,β-unsaturated esters

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About: Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic α,β-unsaturated esters Goto Sponge NotDistinct Permalink

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

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic α,β-unsaturated esters
Creator	Wong, Chi-Huey Jan, Jia-Tsrong Kuo, Chih-Jung Liang, Po-Huang Kuo, Tun-Hsun Fang, Jim-Min Shie, Jiun-Jie Huang, Hung-Jyun Wu, Yin-Ta Cheng, Yih-Shyun
Source	Elsevier; Medline; PMC
abstract	The proteolytic processing of polyproteins by the 3CL protease of severe acute respiratory syndrome coronavirus is essential for the viral propagation. A series of tripeptide α,β-unsaturated esters and ketomethylene isosteres, including AG7088, are synthesized and assayed to target the 3CL protease. Though AG7088 is inactive (IC(50) > 100 μM), the ketomethylene isosteres and tripeptide α,β-unsaturated esters containing both P1 and P2 phenylalanine residues show modest inhibitory activity (IC(50) = 11–39 μM). The Phe-Phe dipeptide inhibitors 18a–e are designed on the basis of computer modeling of the enzyme–inhibitor complex. The most potent inhibitor 18c with an inhibition constant of 0.52 μM is obtained by condensation of the Phe-Phe dipeptide α,β-unsaturated ester with 4-(dimethylamino)cinnamic acid. The cell-based assays also indicate that 18c is a nontoxic anti-SARS agent with an EC(50) value of 0.18 μM.
has issue date	2005-09-01(xsd:dateTime)
bibo:doi	10.1016/j.bmc.2005.05.065
bibo:pmid	15994085
has license	no-cc
sha1sum (hex)	96463d3d90503bf7cd329355bd942087c52e3de3
schema:url	https://doi.org/10.1016/j.bmc.2005.05.065
resource representing a document's title	Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic α,β-unsaturated esters
has PubMed Central identifier	PMC7119063
has PubMed identifier	15994085
schema:publication	Bioorg Med Chem
resource representing a document's body	covid:96463d3d90503bf7cd329355bd942087c52e3de3#body_text
is schema:about of	named entity 'BIRTHDAY' named entity 'KOJI' named entity 'ESTERS' named entity 'PROTEASE' named entity 'HONOR' named entity 'INHIBITION' named entity 'SEVERE ACUTE RESPIRATORY SYNDROME' named entity 'UNSATURATED' named entity 'PEPTIDOMIMETIC' named entity '80TH' named entity 'PROFESSOR' named entity 'RECEIVING' named entity 'PRIZE' named entity 'DEDICATED' named entity 'TETRAHEDRON' covid:arg/96463d3d90503bf7cd329355bd942087c52e3de3 named entity 'Tetrahedron Prize' named entity 'Professor' named entity 'China' named entity 'inverted microscope' named entity '3CL protease' named entity 'Western blotting' named entity 'protease' named entity 'acyl chloride' named entity 'DMF' named entity 'amine' named entity 'K i' named entity 'MgSO' named entity 'metabolic conversion' named entity 'cytopathogenic effect' named entity 'K i' named entity 'Phe' named entity 'Boc group' named entity 'THF' named entity 'LiCl' named entity 'SARS-CoV' named entity 'SARS' named entity 'PBS' named entity 'dipeptide' named entity 'Gly' named entity 'Thr' named entity 'glutamine' named entity 'protease inhibitors' named entity 'SARS-CoV' named entity 'alcohol' named entity '5.0' named entity 'hydrogen peroxide' named entity 'SARS virus' named entity 'SARS' named entity 'cinnamic acid' named entity 'Catalytic hydrogenation' named entity 'SARS-CoV' named entity 'hexapeptide' named entity 'infection' named entity 'SARS' named entity 'Phe' named entity 'mmol' named entity 'tert-butoxycarbonyl' named entity 'dimeric' named entity 'electrophoresis' named entity 'Phe' named entity 'Vero E6' named entity 'Phe' named entity 'oxygen' named entity 'valine' named entity 'steric effects' named entity 'PBS buffer' named entity 'crystal structure' named entity 'Gln' named entity 'esters' named entity 'glutamine' named entity 'protein'

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