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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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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
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author Conole, Daniel
Chou, Yi‐Tai
Patsiarika, Anastasia
Nwabo, Valery
Dimitriou, Eleni
Soudy, Christelle
Mota, Filipa
Djordjevic, Snezana
Selwood, David L.
author_facet Conole, Daniel
Chou, Yi‐Tai
Patsiarika, Anastasia
Nwabo, Valery
Dimitriou, Eleni
Soudy, Christelle
Mota, Filipa
Djordjevic, Snezana
Selwood, David L.
author_sort Conole, Daniel
collection PubMed
description 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.
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spelling pubmed-73177152020-06-29 Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules Conole, Daniel Chou, Yi‐Tai Patsiarika, Anastasia Nwabo, Valery Dimitriou, Eleni Soudy, Christelle Mota, Filipa Djordjevic, Snezana Selwood, David L. Drug Dev Res Research Articles 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. John Wiley & Sons, Inc. 2020-01-20 2020-06 /pmc/articles/PMC7317715/ /pubmed/31958155 http://dx.doi.org/10.1002/ddr.21641 Text en © 2020 The Authors. Drug Development Research published by Wiley Periodicals, Inc. This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Articles
Conole, Daniel
Chou, Yi‐Tai
Patsiarika, Anastasia
Nwabo, Valery
Dimitriou, Eleni
Soudy, Christelle
Mota, Filipa
Djordjevic, Snezana
Selwood, David L.
Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
title Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
title_full Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
title_fullStr Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
title_full_unstemmed Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
title_short Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
title_sort discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
topic Research Articles
url 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
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