0552049 - ÚOCHB 2022 RIV CN eng J - Článek v odborném periodiku
Cai, X. - Fu, G. - Lepšík, Martin - Paci, E. - Guo, Y. - Li, Z. - Li, Q.
Synthesis of a series of novel homo- and hetero-glycoclusters and their binding activities to DC-SIGN.
Journal of Chinese Pharmaceutical Sciences. Roč. 30, č. 11 (2021), s. 859-873. ISSN 1003-1057
Grant CEP: GA ČR(CZ) GBP208/12/G016
Institucionální podpora: RVO:61388963
Klíčová slova: synthesis * heteroglycoclusters * DC-SIGN * binging-activity * docking
Obor OECD: Biochemistry and molecular biology
Způsob publikování: Open access

As a dendritic cell-specific C-type lectin receptor, DC-SIGN plays 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 highly mannosylated and branched fucosylated oligosaccharides. Herein, we synthesized a new series of homo- and Man-Fuc heteroglycoclusters with diverse structures. The binding properties of these compounds to tetrameric extracellular DC-SIGN were assessed by surface plasmon resonance (SPR). Heteroglycocluster 17b showed high DC-SIGN-bnnding activity (KD = 2.6 µM). The structural determinants of this high affinity of 17b were rationalized by docking and compared with its much less potent isomer 17a. Therefore, 17b might serve as a base for the development of potent inhibitors of DC-SIGN-dependent viral infection.
Trvalý link: http://hdl.handle.net/11104/0327211