Synthetic N-acetylglucosamine based fully branched tetrasaccharide, a mimetic of the endogenous ligand for CD69, activates CD69+ NK cells and killer lymphocytes upon dimerization via a hydrophilic flexible linker

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14310%2F10%3A00044042" target="_blank" >RIV/00216224:14310/10:00044042 - isvavai.cz</a>

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

Synthetic N-acetylglucosamine based fully branched tetrasaccharide, a mimetic of the endogenous ligand for CD69, activates CD69+ NK cells and killer lymphocytes upon dimerization via a hydrophilic flexible linker

Original language description

Based on the highly branched ovomucoid-type undecasaccharide that has been shown previously to constitute a physiological ligand for CD69 leukocyte receptor, a systematic investigation of smaller oligosaccharide mimetics has been performed based on the linear and branched N-acetylhexosamine homooligomers prepared synthetically using hitherto unexplored reaction schemes. The systematic structure activity studies revealed the tetrasaccharide GlcNAcb1-3(GlcNAcb1-4)(GlcNAcb1-6)GlcNAc (compound 52) and its a-benzyl-derivative 49 as the best ligand for CD69 with IC50 as high as 10-9 M, thus approaching the affinity of the classical high-affinity ligand GlcNAc17BSA. Compound 68, GlcNAc tetrasaccharide dimerized through a hydrophilic flexible linker, turned out to be effective in activation of CD69+ lymphocytes. It also proved efficient in enhancing natural killing in vitro, decreasing the growth of tumors in vivo, and activating the CD69+ tumor infiltrating lymphocytes examined ex vivo.

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

CE - Biochemistry

OECD FORD branch

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Project

<a href="/en/project/LC06030" target="_blank" >LC06030: Biomolecular centre</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year

2010

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Journal of Medicinal Chemistry

ISSN

0022-2623

e-ISSN

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Volume of the periodical

53

Issue of the periodical within the volume

10

Country of publishing house

CZ - CZECH REPUBLIC

Number of pages

16

Pages from-to

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UT code for WoS article

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EID of the result in the Scopus database

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