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Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
Author(s) -
Conole Daniel,
Chou YiTai,
Patsiarika Anastasia,
Nwabo Valery,
Dimitriou Eleni,
Soudy Christelle,
Mota Filipa,
Djordjevic Snezana,
Selwood David L.
Publication year - 2020
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21641
Subject(s) - neuropilin 1 , small molecule , fluorescence , chemistry , molecule , biophysics , microbiology and biotechnology , combinatorial chemistry , nanotechnology , biochemistry , biology , materials science , cancer research , vegf receptors , physics , quantum mechanics , organic chemistry , vascular endothelial growth factor
Neuropilin‐1 (NRP1) is emerging as an important molecule in immune signaling where it has been shown to modulate the actions of TGF‐β1 in macrophages and regulatory T cells. The development of cost‐effective and reliable assays for NRP1 binding is therefore important. We synthesized three new NRP1 small molecule fluorophores and examined their performance as fluorescent polarization probes. One molecule DS108 exhibited favorable binding and fluorescent characteristics and allowed us to establish a simple assay suitable for medium to high throughput screening of small molecules.