| Literature DB >> 25019313 |
Marian M J H P Willems1, Gijs G Zom, Selina Khan, Nico Meeuwenoord, Cornelis J M Melief, Mario van der Stelt, Herman S Overkleeft, Jeroen D C Codée, Gijsbert A van der Marel, Ferry Ossendorp, Dmitri V Filippov.
Abstract
New analogues (UPam) of triacylated lipopeptide Pam3CysSK4, a popular agonist of Toll-like receptor 2 (TLR2), were designed making use of the cocrystal structure of a TLR2 heterodimer (with TLR1) with Pam3CysSK4. 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.Entities:
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Year: 2014 PMID: 25019313 DOI: 10.1021/jm500722p
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446