Design,synthesis and activity evaluation of mannose-based DC-SIGN antagonists |
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| Authors: | Nataša Obermajer Sara Sattin Cinzia Colombo Michela Bruno Urban Švajger Marko Anderluh Anna Bernardi |
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| Institution: | 1.Department of Biotechnology,Jozef Stefan Institute,Ljubljana,Slovenia;2.Department of Pharmaceutical Biology, Faculty of Pharmacy,University of Ljubljana,Ljubljana,Slovenia;3.Dipartimento di Chimica Organica e Industriale and CISI,Università degli Studi di Milano,Milano,Italy;4.Blood Transfusion Center of Slovenia,Ljubljana,Slovenia;5.Department of Medicinal Chemistry, Faculty of Pharmacy,University of Ljubljana,Ljubljana,Slovenia |
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| 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. |
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