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Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules

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 s...

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Detalles Bibliográficos
Autores principales: Conole, Daniel, Chou, Yi‐Tai, Patsiarika, Anastasia, Nwabo, Valery, Dimitriou, Eleni, Soudy, Christelle, Mota, Filipa, Djordjevic, Snezana, Selwood, David L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley & Sons, Inc. 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7317715/
https://www.ncbi.nlm.nih.gov/pubmed/31958155
http://dx.doi.org/10.1002/ddr.21641
Descripción
Sumario: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.