FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3207584688> ?p ?o ?g. }

• W3207584688 endingPage "17478" @default.
• W3207584688 startingPage "17465" @default.
• W3207584688 abstract "The C-type lectin receptor DC-SIGN is a pattern recognition receptor expressed on macrophages and dendritic cells. It has been identified as a promiscuous entry receptor for many pathogens, including epidemic and pandemic viruses such as SARS-CoV-2, Ebola virus, and HIV-1. In the context of the recent SARS-CoV-2 pandemic, DC-SIGN-mediated virus dissemination and stimulation of innate immune responses has been implicated as a potential factor in the development of severe COVID-19. Inhibition of virus binding to DC-SIGN, thus, represents an attractive host-directed strategy to attenuate overshooting innate immune responses and prevent the progression of the disease. In this study, we report on the discovery of a new class of potent glycomimetic DC-SIGN antagonists from a focused library of triazole-based mannose analogues. Structure-based optimization of an initial screening hit yielded a glycomimetic ligand with a more than 100-fold improved binding affinity compared to methyl α-d-mannopyranoside. Analysis of binding thermodynamics revealed an enthalpy-driven improvement of binding affinity that was enabled by hydrophobic interactions with a loop region adjacent to the binding site and displacement of a conserved water molecule. The identified ligand was employed for the synthesis of multivalent glycopolymers that were able to inhibit SARS-CoV-2 spike glycoprotein binding to DC-SIGN-expressing cells, as well as DC-SIGN-mediated trans-infection of ACE2+ cells by SARS-CoV-2 spike protein-expressing viruses, in nanomolar concentrations. The identified glycomimetic ligands reported here open promising perspectives for the development of highly potent and fully selective DC-SIGN-targeted therapeutics for a broad spectrum of viral infections." @default.
• W3207584688 created "2021-10-25" @default.
• W3207584688 creator A5008798618 @default.
• W3207584688 creator A5009077999 @default.
• W3207584688 creator A5015481785 @default.
• W3207584688 creator A5033535150 @default.
• W3207584688 creator A5036344035 @default.
• W3207584688 creator A5038752800 @default.
• W3207584688 creator A5065053750 @default.
• W3207584688 creator A5073528182 @default.
• W3207584688 creator A5080896513 @default.
• W3207584688 creator A5086012510 @default.
• W3207584688 creator A5086571646 @default.
• W3207584688 creator A5090058563 @default.
• W3207584688 creator A5091596746 @default.
• W3207584688 creator A5043448626 @default.
• W3207584688 date "2021-10-15" @default.
• W3207584688 modified "2023-10-01" @default.
• W3207584688 title "Sweet Drugs for Bad Bugs: A Glycomimetic Strategy against the DC-SIGN-Mediated Dissemination of SARS-CoV-2" @default.
• W3207584688 cites W1523739221 @default.
• W3207584688 cites W1964521930 @default.
• W3207584688 cites W1971849220 @default.
• W3207584688 cites W1985588649 @default.
• W3207584688 cites W1988066093 @default.
• W3207584688 cites W1996466627 @default.
• W3207584688 cites W2020871710 @default.
• W3207584688 cites W2025021056 @default.
• W3207584688 cites W2028035578 @default.
• W3207584688 cites W2041922739 @default.
• W3207584688 cites W2072874236 @default.
• W3207584688 cites W2076595001 @default.
• W3207584688 cites W2082081313 @default.
• W3207584688 cites W2083608791 @default.
• W3207584688 cites W2086155380 @default.
• W3207584688 cites W2098576769 @default.
• W3207584688 cites W2109204917 @default.
• W3207584688 cites W2110808180 @default.
• W3207584688 cites W2124239064 @default.
• W3207584688 cites W2144081223 @default.
• W3207584688 cites W2144822303 @default.
• W3207584688 cites W2147874841 @default.
• W3207584688 cites W2154714625 @default.
• W3207584688 cites W2162884941 @default.
• W3207584688 cites W2163341755 @default.
• W3207584688 cites W2164545523 @default.
• W3207584688 cites W2168112834 @default.
• W3207584688 cites W2169252930 @default.
• W3207584688 cites W2170995846 @default.
• W3207584688 cites W2180229411 @default.
• W3207584688 cites W2222589778 @default.
• W3207584688 cites W2321635162 @default.
• W3207584688 cites W2597943218 @default.
• W3207584688 cites W2607277738 @default.
• W3207584688 cites W2615305549 @default.
• W3207584688 cites W2776480460 @default.
• W3207584688 cites W2793311671 @default.
• W3207584688 cites W2794127862 @default.
• W3207584688 cites W2939138733 @default.
• W3207584688 cites W2953747453 @default.
• W3207584688 cites W2953814967 @default.
• W3207584688 cites W2970471625 @default.
• W3207584688 cites W2980488195 @default.
• W3207584688 cites W2981726292 @default.
• W3207584688 cites W3016246963 @default.
• W3207584688 cites W3021484935 @default.
• W3207584688 cites W3023376619 @default.
• W3207584688 cites W3023982717 @default.
• W3207584688 cites W3025932081 @default.
• W3207584688 cites W3034615197 @default.
• W3207584688 cites W3041243551 @default.
• W3207584688 cites W3045836602 @default.
• W3207584688 cites W3093073619 @default.
• W3207584688 cites W3162168784 @default.
• W3207584688 cites W3163383906 @default.
• W3207584688 cites W3174184935 @default.
• W3207584688 cites W3198689144 @default.
• W3207584688 cites W4248872320 @default.
• W3207584688 doi "https://doi.org/10.1021/jacs.1c06778" @default.
• W3207584688 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34652144" @default.
• W3207584688 hasPublicationYear "2021" @default.
• W3207584688 type Work @default.
• W3207584688 sameAs 3207584688 @default.
• W3207584688 citedByCount "18" @default.
• W3207584688 countsByYear W32075846882022 @default.
• W3207584688 countsByYear W32075846882023 @default.
• W3207584688 crossrefType "journal-article" @default.
• W3207584688 hasAuthorship W3207584688A5008798618 @default.
• W3207584688 hasAuthorship W3207584688A5009077999 @default.
• W3207584688 hasAuthorship W3207584688A5015481785 @default.
• W3207584688 hasAuthorship W3207584688A5033535150 @default.
• W3207584688 hasAuthorship W3207584688A5036344035 @default.
• W3207584688 hasAuthorship W3207584688A5038752800 @default.
• W3207584688 hasAuthorship W3207584688A5043448626 @default.
• W3207584688 hasAuthorship W3207584688A5065053750 @default.
• W3207584688 hasAuthorship W3207584688A5073528182 @default.
• W3207584688 hasAuthorship W3207584688A5080896513 @default.
• W3207584688 hasAuthorship W3207584688A5086012510 @default.
• W3207584688 hasAuthorship W3207584688A5086571646 @default.

• next