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Design, synthesis and characterization of fMLF-mimicking AApeptides
Hu Y.2; Cheng N.1; Wu H.2; Kang S.1; Ye R.D.2; Cai J.2
2014-11-03
Source PublicationChemBioChem
ISSN14397633 14394227
Volume15Issue:16Pages:2420-2426
AbstractThe tripeptide N-formyl-Met-Leu-Phe (fMLF) is a potent neutrophil chemoattractant and the reference agonist for the G protein-coupled N-formylpeptide receptor (FPR). As it plays a very important role in host defense and inflammation, there has been considerable interest in the development of fMLF analogues in the hope of identifying potential therapeutic agents. Herein we report the design, synthesis, and evaluation of AA-peptides that mimic the structure and function of fMLF. The lead AApeptides induced calcium mobilization and mitogen-activated protein kinase (MAPK) signal transduction pathways in FPR-transfected rat basophilic leukemic (RBL) cells. More in-triguingly, at high concentrations, certain AApeptides were more effective than fMLF in the induction of calcium mobilization. Their agonistic activity is further supported by their ability to stimulate chemotaxis and the production of superoxide in HL-60 cells. Similarly to fMLF, these AApeptides are much more selective towards FPR1 than FPR2. These results suggest that the fMLF-mimicking AApeptides might emerge as a new class of therapeutic agents that target FPRs.
KeywordAApeptides Calcium Chemotaxis FMLF Peptidomimetics
DOI10.1002/cbic.201402396
URLView the original
Language英語
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Cited Times [WOS]:7   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.University of Illinois College of Medicine
2.University of South Florida, Tampa
3.Shanghai Jiao Tong University
Recommended Citation
GB/T 7714
Hu Y.,Cheng N.,Wu H.,et al. Design, synthesis and characterization of fMLF-mimicking AApeptides[J]. ChemBioChem,2014,15(16):2420-2426.
APA Hu Y.,Cheng N.,Wu H.,Kang S.,Ye R.D.,&Cai J..(2014).Design, synthesis and characterization of fMLF-mimicking AApeptides.ChemBioChem,15(16),2420-2426.
MLA Hu Y.,et al."Design, synthesis and characterization of fMLF-mimicking AApeptides".ChemBioChem 15.16(2014):2420-2426.
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