High-Throughput Screening for Small-Molecule Activators of Neutrophils: Identification of NovelN-Formyl Peptide Receptor Agonists

2007 ◽  
Vol 71 (4) ◽  
pp. 1061-1074 ◽  
Author(s):  
Igor A. Schepetkin ◽  
Liliya N. Kirpotina ◽  
Andrei I. Khlebnikov ◽  
Mark T. Quinn
Keyword(s):  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Formyl Peptide Receptor ◽  
Peptide Receptor ◽  
Receptor Agonists ◽  
Formyl Peptide

scholarly journals Molecular docking of 2-(benzimidazol-2-ylthio)-N-phenylacetamide-derived small-molecule agonists of human formyl peptide receptor 1

2011 ◽  
Vol 18 (6) ◽  
pp. 2831-2843 ◽  
Author(s):  
Andrei I. Khlebnikov ◽  
Igor A. Schepetkin ◽  
Liliya N. Kirpotina ◽  
Lars Brive ◽  
Claes Dahlgren ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Small Molecule ◽  
Formyl Peptide Receptor ◽  
Peptide Receptor ◽  
Formyl Peptide

scholarly journals Using the BioAssay Ontology for Analyzing High-Throughput Screening Data

2014 ◽  
Vol 20 (3) ◽  
pp. 402-415 ◽  
Author(s):  
Linda Zander Balderud ◽  
David Murray ◽  
Niklas Larsson ◽  
Uma Vempati ◽  
Stephan C. Schürer ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Method Comparison ◽  
Formyl Peptide Receptor ◽  
The Public ◽  
Starting Point ◽  
Technology Gaps ◽  
Formyl Peptide ◽  
Assay Methods ◽  
Hit Identification

High-throughput screening (HTS) is the main starting point for hit identification in drug discovery programs. This has led to a rapid increase of available screening data both within pharmaceutical companies and the public domain. We have used the BioAssay Ontology (BAO) 2.0 for assay annotation within AstraZeneca to enable comparison with external HTS methods. The annotated assays have been analyzed to identify technology gaps, evaluate new methods, verify active hits, and compare compound activity between in-house and PubChem assays. As an example, the binding of a fluorescent ligand to formyl peptide receptor 1 (FPR1, involved in inflammation, for example) in an in-house HTS was measured by fluorescence intensity. In total, 155 active compounds were also tested in an external ligand binding flow cytometry assay, a method not used for in-house HTS detection. Twelve percent of the 155 compounds were found active in both assays. By the annotation of assay protocols using BAO terms, internal and external assays can easily be identified and method comparison facilitated. They can be used to evaluate the effectiveness of different assay methods, design appropriate confirmatory and counterassays, and analyze the activity of compounds for identification of technology artifacts.

Conformational Aspects of Human Formyl-peptide Receptor Agonists

2011 ◽  
Vol 53 (11) ◽  
pp. 793-798
Author(s):  
Alessandro Dalpiaz ◽  
Gianni Vertuani ◽  
Angelo Scatturin ◽  
Federica Vitali ◽  
Katia Varani ◽  
...  
Keyword(s):  
Formyl Peptide Receptor ◽  
Peptide Receptor ◽  
Receptor Agonists ◽  
Formyl Peptide

scholarly journals Synthesis of Five- and Six-MemberedN-Phenylacetamido Substituted Heterocycles as Formyl Peptide Receptor Agonists

2016 ◽  
Vol 78 (1) ◽  
pp. 49-62 ◽  
Author(s):  
Claudia Vergelli ◽  
Igor A. Schepetkin ◽  
Giovanna Ciciani ◽  
Agostino Cilibrizzi ◽  
Letizia Crocetti ◽  
...  
Keyword(s):  
Formyl Peptide Receptor ◽  
Peptide Receptor ◽  
Receptor Agonists ◽  
Formyl Peptide

scholarly journals Development of Small Molecule Non-peptide Formyl Peptide Receptor (FPR) Ligands and Molecular Modeling of Their Recognition

2014 ◽  
Vol 21 (13) ◽  
pp. 1478-1504 ◽  
Author(s):  
I.A. Schepetkin ◽  
A.I. Khlebnikov ◽  
M.P. Giovannoni ◽  
L.N. Kirpotina ◽  
A. Cilibrizzi ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Small Molecule ◽  
Formyl Peptide Receptor ◽  
Peptide Receptor ◽  
Formyl Peptide

scholarly journals High-throughput screening campaign identifies a small molecule agonist of the relaxin family peptide receptor 4

2020 ◽  
Vol 41 (10) ◽  
pp. 1328-1336
Author(s):  
Guang-yao Lin ◽  
Lin Lin ◽  
Xiao-qing Cai ◽  
An-tao Dai ◽  
Yue Zhu ◽  
...  
Keyword(s):  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Peptide Receptor ◽  
Relaxin Family

Substituted Pyridazin-3(2H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists

2019 ◽  
Vol 62 (10) ◽  
pp. 5242-5248 ◽  
Author(s):  
Girdhar Singh Deora ◽  
Cheng Xue Qin ◽  
Elizabeth A. Vecchio ◽  
Aaron J. Debono ◽  
Daniel L. Priebbenow ◽  
...  
Keyword(s):  
Formyl Peptide Receptor ◽  
Peptide Receptor ◽  
Receptor Agonists ◽  
Formyl Peptide
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