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Application of An Improved HPLC-FL Method to Screen Serine Palmitoyl Transferase Inhibitors

In this work, we reported the application and validation of an improved high-performance liquid chromatography method coupled with a fluorimetric detector (HPLC-FL) to screen the activity of two heterocyclic derivatives reported as serine palmitoyl transferase (SPT) inhibitors. The analytical condit...

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Autores principales: Bertini, Simone, Saccomanni, Giuseppe, Del Carlo, Sara, Digiacomo, Maria, Gargini, Claudia, Piano, Ilaria, Campisi, Giuseppe Matteo, Ghidoni, Riccardo, Macchia, Marco, Manera, Clementina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152383/
https://www.ncbi.nlm.nih.gov/pubmed/28714922
http://dx.doi.org/10.3390/molecules22071198
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author Bertini, Simone
Saccomanni, Giuseppe
Del Carlo, Sara
Digiacomo, Maria
Gargini, Claudia
Piano, Ilaria
Campisi, Giuseppe Matteo
Ghidoni, Riccardo
Macchia, Marco
Manera, Clementina
author_facet Bertini, Simone
Saccomanni, Giuseppe
Del Carlo, Sara
Digiacomo, Maria
Gargini, Claudia
Piano, Ilaria
Campisi, Giuseppe Matteo
Ghidoni, Riccardo
Macchia, Marco
Manera, Clementina
author_sort Bertini, Simone
collection PubMed
description In this work, we reported the application and validation of an improved high-performance liquid chromatography method coupled with a fluorimetric detector (HPLC-FL) to screen the activity of two heterocyclic derivatives reported as serine palmitoyl transferase (SPT) inhibitors. The analytical conditions were optimized in terms of the derivatization procedure, chromatographic condition, extraction procedure, and method validation according to EMEA guidelines. Once fully optimized, the method was applied to assess the SPT-inhibitory activity of the above-mentioned derivatives and of the reference inhibitor myriocin. The obtained results, expressed as a percentage of residual SPT activity, were compared to those obtained with the reference radio immune assay (RIA). The good correlation between the two types of assay demonstrated that the improved HPLC-FL method is suitable for a preliminary and rapid screening of potential SPT-inhibitors.
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spelling pubmed-61523832018-11-13 Application of An Improved HPLC-FL Method to Screen Serine Palmitoyl Transferase Inhibitors Bertini, Simone Saccomanni, Giuseppe Del Carlo, Sara Digiacomo, Maria Gargini, Claudia Piano, Ilaria Campisi, Giuseppe Matteo Ghidoni, Riccardo Macchia, Marco Manera, Clementina Molecules Communication In this work, we reported the application and validation of an improved high-performance liquid chromatography method coupled with a fluorimetric detector (HPLC-FL) to screen the activity of two heterocyclic derivatives reported as serine palmitoyl transferase (SPT) inhibitors. The analytical conditions were optimized in terms of the derivatization procedure, chromatographic condition, extraction procedure, and method validation according to EMEA guidelines. Once fully optimized, the method was applied to assess the SPT-inhibitory activity of the above-mentioned derivatives and of the reference inhibitor myriocin. The obtained results, expressed as a percentage of residual SPT activity, were compared to those obtained with the reference radio immune assay (RIA). The good correlation between the two types of assay demonstrated that the improved HPLC-FL method is suitable for a preliminary and rapid screening of potential SPT-inhibitors. MDPI 2017-07-17 /pmc/articles/PMC6152383/ /pubmed/28714922 http://dx.doi.org/10.3390/molecules22071198 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Bertini, Simone
Saccomanni, Giuseppe
Del Carlo, Sara
Digiacomo, Maria
Gargini, Claudia
Piano, Ilaria
Campisi, Giuseppe Matteo
Ghidoni, Riccardo
Macchia, Marco
Manera, Clementina
Application of An Improved HPLC-FL Method to Screen Serine Palmitoyl Transferase Inhibitors
title Application of An Improved HPLC-FL Method to Screen Serine Palmitoyl Transferase Inhibitors
title_full Application of An Improved HPLC-FL Method to Screen Serine Palmitoyl Transferase Inhibitors
title_fullStr Application of An Improved HPLC-FL Method to Screen Serine Palmitoyl Transferase Inhibitors
title_full_unstemmed Application of An Improved HPLC-FL Method to Screen Serine Palmitoyl Transferase Inhibitors
title_short Application of An Improved HPLC-FL Method to Screen Serine Palmitoyl Transferase Inhibitors
title_sort application of an improved hplc-fl method to screen serine palmitoyl transferase inhibitors
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152383/
https://www.ncbi.nlm.nih.gov/pubmed/28714922
http://dx.doi.org/10.3390/molecules22071198
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