LAUSR

Conformationally Constrained Sialyl Analogues as New Potential Binders of h‐CD22

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1 Published in 2022 at "Chembiochem"

DOI: 10.1002/cbic.202200076

Abstract: Here, two conformationally constrained sialyl analogues were synthesized and characterized in their interaction with the inhibitory Siglec, human CD22 (h‐CD22). An orthogonal approach, including biophysical assays (SPR and fluorescence), ligand‐based NMR techniques, and molecular modelling,… read more here.

Keywords: cd22; analogues new; conformationally constrained; sialyl analogues ... See more keywords

The importance of being Aib. Aggregation and self‐assembly studies on conformationally constrained oligopeptides

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0 Published in 2017 at "Journal of Peptide Science"

DOI: 10.1002/psc.2956

Abstract: The role of the conformationally constrained α‐aminoisobutyric acid (Aib) residue in the aggregation and self‐assembly properties of oligopeptides is discussed, critically reviewing our recent work in the field. In this connection, three significant case studies… read more here.

Keywords: aggregation; conformationally constrained; self assembly; aggregation self ... See more keywords

Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting.

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0 Published in 2020 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.0c01025

Abstract: HDACs are an attractive therapeutic target for a variety of human diseases. Currently, all four FDA-approved HDAC-targeting drugs are non-selective, pan-HDAC inhibitors, exhibiting adverse side-effects at therapeutic doses. While selective HDAC-inhibition has been proposed to… read more here.

Keywords: conformationally constrained; hdac8; benzanilide scaffolds; scaffolds potent ... See more keywords

The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors

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0 Published in 2021 at "ACS Medicinal Chemistry Letters"

DOI: 10.1021/acsmedchemlett.1c00391

Abstract: HCV NS5A inhibitors are the backbone of directly acting antiviral treatments against the hepatitis C virus (HCV). While these therapies are generally highly curative, they are less effective in some specific HCV patient populations. In… read more here.

Keywords: conformationally constrained; discovery conformationally; hcv; chemistry ... See more keywords

Achieving enhanced cell penetration of short conformationally constrained peptides through amphiphilicity tuning† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c7sc03614k

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0 Published in 2017 at "Chemical Science"

DOI: 10.1039/c7sc03614k

Abstract: We synthesized a panel of conformationally constrained peptides with either α-helix or β-hairpin conformations. We tuned the amphiphilicity of these constrained peptides with different distributions of charged or hydrophobic residues and compared their cellular uptake… read more here.

Keywords: amphiphilicity; conformationally constrained; enhanced cell; constrained peptides ... See more keywords