Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives; International Immunopharmacology; Vol. 37

Bibliografiske detaljer
Parent link:International Immunopharmacology
Vol. 37.— 2016.— [P. 43–58]
Institution som forfatter: Национальный исследовательский Томский политехнический университет Институт физики высоких технологий Кафедра биотехнологии и органической химии
Andre forfattere: Schepetkin (Shchepyotkin) I. A. Igor Aleksandrovich, Khlebnikov A. I. Andrey Ivanovich, Kirpotina L. N. Liliya Nikolaevna, Quinn M. T.
Summary:Title screen
Formyl peptide receptor 1 (FPR1) regulates a wide variety of neutrophil functional responses and plays an important role in inflammation and the pathogenesis of various diseases. To date, a variety of natural and synthetic molecules have been identified as FPR1 ligands. Here, we review current knowledge on natural products and natural product-inspired small molecules reported to antagonize and/or inhibit the FPR1-mediated responses. Based on this literature, additional screening of selected commercially available natural compounds for their ability to inhibit fMLF-induced Ca2 + mobilization in human neutrophils and FPR1 transfected HL-60 cells, and pharmacophore modeling, natural products with potential as FPR1 antagonists are considered and discussed in this review. The identification and characterization of natural products that antagonize FPR1 activity may have potential for the development of novel therapeutics to limit or alter the outcome of inflammatory processes.
Режим доступа: по договору с организацией-держателем ресурса
Sprog:engelsk
Udgivet: 2016
Fag:
Online adgang:http://dx.doi.org/10.1016/j.intimp.2015.08.036
Format: Electronisk Book Chapter
KOHA link:https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=650219
Beskrivelse
Summary:Title screen
Formyl peptide receptor 1 (FPR1) regulates a wide variety of neutrophil functional responses and plays an important role in inflammation and the pathogenesis of various diseases. To date, a variety of natural and synthetic molecules have been identified as FPR1 ligands. Here, we review current knowledge on natural products and natural product-inspired small molecules reported to antagonize and/or inhibit the FPR1-mediated responses. Based on this literature, additional screening of selected commercially available natural compounds for their ability to inhibit fMLF-induced Ca2 + mobilization in human neutrophils and FPR1 transfected HL-60 cells, and pharmacophore modeling, natural products with potential as FPR1 antagonists are considered and discussed in this review. The identification and characterization of natural products that antagonize FPR1 activity may have potential for the development of novel therapeutics to limit or alter the outcome of inflammatory processes.
Режим доступа: по договору с организацией-держателем ресурса
DOI:10.1016/j.intimp.2015.08.036