LitCovid-sentences  

PMC:7074424 / 22996-25250 JSONTXT 11 Projects

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Id Subject Object Predicate Lexical cue
T134 0-9 Sentence denotes Proteases
T135 10-59 Sentence denotes The SERS-CoV genome encodes a number of proteins.
T136 60-265 Sentence denotes The replicase gene, which is a major component of the CoV genome encoded for 16 NSPs in the form of two large PPs (PP1a and PP1ab).[74] Two types of cysteine proteases act on these PPs to release the NSPs.
T137 266-654 Sentence denotes The C-terminal end of these PPs is cleaved by chymotrypsin-like cysteine protease (main protease [Mpro] or 3C-like protease [3CLpro]) and the N-terminal end is processed by the Mpro (also known as papain-like protease [PLpro]).[74] The first three cleavage sites of the PPs is cut by PLpro while the rest 11 sites are cleaved by CLpro, and this cleavage results in release of 16 NSPs.[75]
T138 656-672 Sentence denotes 3C-like protease
T139 673-879 Sentence denotes The 3CLpro is present in homodimer form and has cys-his dyad on active site which shows protease activity.[27] If mutated on the Ser139 and phe140 positions, it abolishes the dimerization of 3CLPro (PDB ID:
T140 880-1089 Sentence denotes 3F9G).[76] This protease can cleave 11 sites in the p1 position of PP1a and PP1ab and can produce a mature protein that anchors the replication/transcription complex[377] and also releases the mature NSPs.[78]
T141 1090-1213 Sentence denotes N-(benzo[1,2,3]triazol-1-yl)-N-(benzyl) acetamido) phenyl) carboxamides are also found to be important inhibitors of CLPro.
T142 1214-1292 Sentence denotes The structure of CLPro inhibitor is with ML188 (IC50 1.5 μM) is reported (CID:
T143 1293-1310 Sentence denotes 46897844, PDB ID:
T144 1311-1377 Sentence denotes 3V3M).[7980] Another structure with CLPro inhibitor ML300 (PDB ID:
T145 1378-1389 Sentence denotes 4MDS, IC50:
T146 1390-1897 Sentence denotes 6.2 μM) is reported.[79] Some metal-conjugated and peptidomimetic compounds showed inhibitory activity against 3CLpro.[77] Some of the small molecules also act as an inhibitor that is arylboronic acids, quinolinecarboxylate derivatives, thiophenecarboxylate, and phthalhydrazide-substituted ketoglutamine analogs.[77] Some flavonoids are also reported to inhibit Mpro.[75] GC376 also has protease inhibitor activity.[81] A crystal structure of Mpro with small molecule inhibitor N3 is also reported (PDB ID:
T147 1898-2254 Sentence denotes 2AMQ).[82] Lopinavir and ritonavir, which are the inhibitors of HIV protease, also inhibit Mpro.[83] In silico studies directed that among commercially available drugs, colistin, valrubicin, icatibant, bepotastine, epirubicin, epoprostenol, vapreotide, aprepitant, caspofungin, and perphenazine also bind to the lopinavir/ritonavir-binding site on CoV.[83]