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- Title
Synthesis of a series of novel homo- and hetero-glycoclusters and their binding activities to DC-SIGN.
- Authors
Xueni Cai; Ge Fu; Lepšik, Martin; Paci, Emanuele; Yuan Guo; Zhongjun Li; Qing Li
- Abstract
As a dendritic cell-specific C-type lectin receptor, DC-SIGN plrs an important role in the early stages of many viral infections, including HIV and Ebola, making it an interesting therapeutic target. It has been found that DC-SIGN can recognize both hiily manno seated and branched fucosjdated oligosaccharides. Herein we synthesized a new series of homo- and Man-Fuc heteroycoclusters with &verse structures. The binding properties of these compounds to tetrameric extracellular DC-SIGN were assessed by surface plasmon resonance (SPR). Heteroycoduster 17b diowed hii DC-SIGN-binding activity (KD = 2.6 pM). The structural determinants of this higi affinity of 17b were rationalized ty docking and compared with its much less potent isomer 17a. Therefore, 17b might serve as a base for the development of potent inhibitors of D C-SIGN-dependent viral infection.
- Subjects
LECTINS; SURFACE plasmon resonance; VIRUS diseases; OLIGOSACCHARIDES
- Publication
Journal of Chinese Pharmaceutical Sciences, 2021, Vol 30, Issue 11, p859
- ISSN
1003-1057
- Publication type
Article
- DOI
10.5246/jcps.2021.11.074