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Design, synthesis and activity evaluation of mannose-based DC-SIGN antagonists.
- Source :
-
Molecular diversity [Mol Divers] 2011 May; Vol. 15 (2), pp. 347-60. Date of Electronic Publication: 2010 Nov 14. - Publication Year :
- 2011
-
Abstract
- In this article, we describe the design, synthesis and activity evaluation of glycomimetic DC-SIGN antagonists, that use a mannose residue to anchor to the protein carbohydrate recognition domain (CRD). The molecules were designed from the structure of the known pseudo-mannobioside antagonist 1, by including additional hydrophobic groups, which were expected to engage lipophilic areas of DC-SIGN CRD. The results demonstrate that the synthesized compounds potently inhibit DC-SIGN-mediated adhesion to mannan coated plates. Additionally, in silico docking studies were performed to rationalize the results and to suggest further optimization.
- Subjects :
- Biological Assay
Models, Molecular
Protein Binding physiology
Reproducibility of Results
Structure-Activity Relationship
Cell Adhesion Molecules antagonists & inhibitors
Drug Design
Lectins, C-Type antagonists & inhibitors
Mannose chemistry
Receptors, Cell Surface antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1573-501X
- Volume :
- 15
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Molecular diversity
- Publication Type :
- Academic Journal
- Accession number :
- 21076980
- Full Text :
- https://doi.org/10.1007/s11030-010-9285-y