PMC:7352545 / 72677-75481 JSONTXT 10 Projects

Annnotations TAB TSV DIC JSON TextAE

Id Subject Object Predicate Lexical cue
T705 0-4 Sentence denotes 7.1.
T706 5-84 Sentence denotes N-Glycosylation Inhibition by Chloroquine (CLQ) and Hydroxychloroquine (CLQ-OH)
T707 85-164 Sentence denotes CLQ and CLQ-OH are under investigation worldwide to treat COVID-19 (Figure 10).
T708 165-309 Sentence denotes CLQ and its derivative CLQ-OH block CoV replication, amplification and spread in in vitro culture via inhibition of ACE2 receptor glycosylation.
T709 310-454 Sentence denotes In HCoVs, interaction of the S glycoprotein with gangliosides initially occur as the first entry step during the replication cycle of the virus.
T710 455-600 Sentence denotes CLQ and CLQ-OH have been alternative drugs for RA and several autoimmune diseases for 70 years, although they are anti-malaria prophylaxis drugs.
T711 601-657 Sentence denotes CLQ-OH is an aminoquinoline with less toxicity than CLQ.
T712 658-754 Sentence denotes CLQ-OH bears an N-hydroxyethyl side chain, which increases its solubility compared to CLQ [141].
T713 755-857 Sentence denotes CLQ-OH modulates activated immune cells via downregulation of TLR signaling and IL-6 production [142].
T714 858-946 Sentence denotes Clinical trials are also under consideration for the efficacy and safety of these drugs.
T715 947-1063 Sentence denotes Regarding the action mechanism(s), CLQ and CLQ-OH-mediated inhibition of ACE2 terminal glycosylation was considered.
T716 1064-1250 Sentence denotes In in vitro Vero E6 cells, CLQ significantly inhibits SARS-CoV spread by interfering with ACE2 function, acting at the entry and post-entry steps of SARS-CoV-2 replication and infection.
T717 1251-1357 Sentence denotes The binding affinity of ACE2 to S glycoprotein is simulated to be lowered by treatment with CLQ-OH or CLQ.
T718 1358-1479 Sentence denotes CLQ may modify the binding affinity between ACE2 and S glycoprotein by alterations in ACE2 glycosylation or modification.
T719 1480-1551 Sentence denotes CLQ-OH (EC50 0.72 μM) and CLQ (EC50, 5.47 μM) inhibit SARS-CoV-2 [143].
T720 1552-1789 Sentence denotes Using computer simulation techniques, CLQ and CLQ-OH have been suggested to recognize the enzymatic active site of the UDP-GlcNAc 2-epimerase, known as an essential enzyme in SA biosynthesis [144], blocking the sialylation of host cells.
T721 1790-1995 Sentence denotes The mechanism underlying the glycosylation inhibition may support the antiviral properties of CLQ and CLQ-OH through interactions of CLQ or CLQ-OH with NDP-saccharide mutases or glycosyltransferases [145].
T722 1996-2140 Sentence denotes CLQ was reported to inhibit quinone reductase 2 [146], known as a catalytic mimetic or structural neighbor of UDP-GlcNAc 2-epimerases [147,148].
T723 2141-2332 Sentence denotes If CLQ or CLQ-OH inhibits SA synthesis, the inhibitory properties may support the antiviral activity of CLQ or CLQ-OH against SARS-CoVs because the SARS-CoV receptor ACE2 contains SA species.
T724 2333-2451 Sentence denotes In fact, CLQ exhibits in vitro anti-SARS-CoV-1 activity via defective glycosylation of viral ACE2 in Vero cells [149].
T725 2452-2645 Sentence denotes In addition. the interference of CLQ or CLQ-OH with SA synthesis may broadly be applicable as an antiviral because the HcoVs or other orthomyxoviruses also utilize SAs as entry molecules [150].
T726 2646-2708 Sentence denotes However, the detailed mechanisms should be further elucidated.
T727 2709-2804 Sentence denotes The CLQ treatment efficacy in Covid-19 patients has, however, not been conclusively determined.