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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...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley & Sons, Inc.
2020
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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. |
format | Online Article Text |
id | pubmed-7317715 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | John Wiley & Sons, Inc. |
record_format | MEDLINE/PubMed |
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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