期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 57, 期 15, 页码 6873-6878出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm500722p
关键词
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资金
- Dutch Cancer Society (KWF) [UL2007-3906]
- TI Pharma project
New analogues (UPam) of triacylated lipopeptide Pam(3)CysSK(4), a popular agonist of Toll-like receptor 2 (TLR2), were designed making use of the cocrystal structure of a TLR2 heterodimer (with TLR1) with Pam(3)CysSK(4). Twenty-two UPam derivatives that feature an N-tetradecylcarbamyl chain to mimic the native N-palmitoyl moiety and various small amino acids residues at the penultimate N-terminal position were prepared via solid-phase synthesis. In vitro evaluation of immunostimulatory properties revealed new potent TLR2 ligands.
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