ArticleMolecular pharmacology2013
Selective agonists and antagonists of formylpeptide receptors: duplex flow cytometry and mixture-based positional scanning libraries.
Article in Molecular pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 34 citations in OpenAlex.
- Novel Lipophagy Inducers as Potential Therapeutics for Lipid Metabolism Disorders.ACS chemical biology · 2025Article
- In Vivo Acute Toxicity Studies of Novel Anti-Melanoma Compounds Downregulators of hnRNPH1/H2.Biomolecules · 2023Article
- Malaria Parasite Plasmodium falciparum Proteins on the Surface of Infected Erythrocytes as Targets for Novel Drug Discovery.Biochemistry. Biokhimiia · 2022Review
- Chemotactic Ligands that Activate G-Protein-Coupled Formylpeptide Receptors.International journal of molecular sciences · 2019Review
- A Novel Probe for Spliceosomal Proteins that Induces Autophagy and Death of Melanoma Cells Reveals New Targets for Melanoma Drug Discovery.Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology · 2019Article
- Article
- The Formyl Peptide Receptors: Diversity of Ligands and Mechanism for Recognition.Molecules (Basel, Switzerland) · 2017Review
- SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes.Journal of medicinal chemistry · 2015Article
- Flow Cytometry: Impact on Early Drug Discovery.Journal of biomolecular screening · 2015Review
- 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
- Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).Journal of medicinal chemistry · 2014Article
- The University of New Mexico Center for Molecular Discovery.Combinatorial chemistry & high throughput screening · 2014Article
- Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis.Journal of medicinal chemistry · 2014Article
- Development of small molecule non-peptide formyl peptide receptor (FPR) ligands and molecular modeling of their recognition.Current medicinal chemistry · 2014Review
- Targeting GTPases in Parkinson's disease: comparison to the historic path of kinase drug discovery and perspectives.Frontiers in molecular neuroscience · 2014Review
- Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.Journal of medicinal chemistry · 2013Article
- Rapid scanning structure-activity relationships in combinatorial data sets: identification of activity switches.Journal of chemical information and modeling · 2013Article
- The mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors.Molecules (Basel, Switzerland) · 2013Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
The formylpeptide receptor (FPR1) and formylpeptide-like 1 receptor (FPR2) are G protein-coupled receptors that are linked to acute inflammatory responses, malignant glioma stem cell metastasis, and chronic inflammation. Although several N-formyl peptides are known to bind to these receptors, more selective small-molecule, high-affinity ligands are needed for a better understanding of the physiologic roles played by these receptors. High-throughput assays using mixture-based combinatorial libraries represent a unique, highly efficient approach for rapid data acquisition and ligand identification. We report the superiority of this approach in the context of the simultaneous screening of a diverse set of mixture-based small-molecule libraries. We used a single cross-reactive peptide ligand for a duplex flow cytometric screen of FPR1 and FPR2 in color-coded cell lines. Screening 37 different mixture-based combinatorial libraries totaling more than five million small molecules (contained in 5,261 mixture samples) resulted in seven libraries that significantly inhibited activity at the receptors. Using positional scanning deconvolution, selective high-affinity (low nM K(i)) individual compounds were identified from two separate libraries, namely, pyrrolidine bis-diketopiperazine and polyphenyl urea. The most active individual compounds were characterized for their functional activities as agonists or antagonists with the most potent FPR1 agonist and FPR2 antagonist identified to date with an EC₅₀ of 131 nM (4 nM K(i)) and an IC₅₀ of 81 nM (1 nM K(i)), respectively, in intracellular Ca²⁺ response determinations. Comparative analyses of other previous screening approaches clearly illustrate the efficiency of identifying receptor selective, individual compounds from mixture-based combinatorial libraries.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.