ArticleThe Biochemical journal2013
V101L of human formyl peptide receptor 1 (FPR1) increases receptor affinity and augments the antagonism mediated by cyclosporins.
Article in The Biochemical journal, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 13 citations in OpenAlex.
- Development of ADS051, an oral, gut-restricted, small molecule neutrophil modulator for the treatment of neutrophil-mediated inflammatory diseases.FEBS open bio · 2023Article
- Annexin A1 and its receptor gene polymorphisms in systemic lupus erythematosus in the Tunisian population.Clinical rheumatology · 2022Article
- Antibiotic-chemoattractants enhance neutrophil clearance of Staphylococcus aureus.Nature communications · 2021Article
- The Role of Formyl Peptide Receptor 1 Gene Polymorphisms in Human Colorectal Cancer.Journal of Cancer · 2020Article
- 4-Aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-ones as N-formyl peptide receptor 1 (FPR1) antagonists.Biochemical pharmacology · 2017Article
- Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives.International immunopharmacology · 2016Review
- The role of formylated peptides and formyl peptide receptor 1 in governing neutrophil function during acute inflammation.The American journal of pathology · 2015Review
- Antagonism of human formyl peptide receptor 1 (FPR1) by chromones and related isoflavones.Biochemical pharmacology · 2014Article
- Development of small molecule non-peptide formyl peptide receptor (FPR) ligands and molecular modeling of their recognition.Current medicinal chemistry · 2014Review
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
Abstract
Genetic variation plays a major role in drug response variability. CsA (cyclosporin A), a widely used immunosuppressive agent, is a specific antagonist for FPR1 (formyl peptide receptor 1), which is an important G-protein-coupled chemoattractant receptor in the innate immune system. In order to study the variable responses of cyclosporins to different FPR1 mutants, we investigated the distribution of human FPR1 haplotypes among 209 healthy Han Chinese subjects. The haplotype pattern in Han Chinese were characterized on the basis of five SNPs (single nucleotide polymorphisms), including rs5030878 (p.T11I), rs2070745 (p.V101L), rs5030880 (p.R190W), rs1042229 (p.N192K) and rs867228 (p.A346E). Receptor binding affinity of cyclosporins to FPR1 haplotypes was assessed using N-formyl-Nle-Leu-Phe-Nle-Tyr-Lys-FITC in CHO-G(α16) cells stably transfected with cDNAs encoding the top 12 FPR1 haplotypes in the Han Chinese. Variants of FPR1 carrying a single amino acid substitution of leucine for valine at position 101 (p.Leu(101)) displayed significantly higher pK(i) values for CsA and CsH (cyclosporin H), indicative of an improved receptor affinity. The polymorphism of FPR1 p.Leu(101) also enhanced the inhibitory effects of cyclosporins on fMLF (N-formyl-methionyl-leucyl-phenylalanine)-induced activities, including calcium mobilization, cell chemotaxis and MAPK (mitogen-activated protein kinase) phosphorylation. These results point to a possible complication for clinical use of CsA in patients carrying the p.Leu(101) allele of FPR1.
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