期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 9, 页码 1638-1641出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.03.042
关键词
Toll-like receptor 2; Pam(2)CSK(4); Structure-activity relationship; Lipopeptide
资金
- Mizutani Foundation for Glycoscience
- Mishima Kaiun Memorial Foundation
- Takeda Science Foundation
- Keio University Doctorate Student Grant-in-Aid Program
- [JP17H02207]
- [JP17H05800]
- [JP16H01162]
- [JP16K16638]
- Grants-in-Aid for Scientific Research [17H05800, 16K16638, 16H01162, 17H02207] Funding Source: KAKEN
Toll-like receptor 2 (TLR2), a member of the TLR innate immune receptor family, recognizes lipoproteins from bacteria and modulates the immune response by inducing the expression of various cytokines. TLR2 has a large hydrophobic pocket that recognizes long fatty acyl groups on TLR2 ligands. However, few studies have focused on the property of the hydrophobic TLR2 pocket. Based on the X-ray crystal structure of TLR2, small polar regions were found in the hydrophobic TLR2 pocket. Interactions between the polar residues and ligands were explored here by designing and synthesizing a Pam(2)CSK(4) derivative of the TLR2 ligands, containing an amide group within the lipid moiety. We evaluated the binding affinities and immunomodulatory activities of these ligands. Results suggested that the amide groups in the lipid chain interacted with the polar residues in the hydrophobic lipid-binding pocket of TLR2. (C) 2018 Elsevier Ltd. All rights reserved.
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