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The Mathematics of a Successful Deconvolution: A Quantitative Assessment of Mixture-Based Combinatorial Libraries Screened Against Two Formylpeptide Receptors
In the past 20 years, synthetic combinatorial methods have fundamentally advanced the ability to synthesize and screen large numbers of compounds for drug discovery and basic research. Mixture-based libraries and positional scanning deconvolution combine two approaches for the rapid identification o...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4106117/ https://www.ncbi.nlm.nih.gov/pubmed/23722730 http://dx.doi.org/10.3390/molecules18066408 |
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author | Santos, Radleigh G. Appel, Jon R. Giulianotti, Marc A. Edwards, Bruce S. Sklar, Larry A. Houghten, Richard A. Pinilla, Clemencia |
author_facet | Santos, Radleigh G. Appel, Jon R. Giulianotti, Marc A. Edwards, Bruce S. Sklar, Larry A. Houghten, Richard A. Pinilla, Clemencia |
author_sort | Santos, Radleigh G. |
collection | PubMed |
description | In the past 20 years, synthetic combinatorial methods have fundamentally advanced the ability to synthesize and screen large numbers of compounds for drug discovery and basic research. Mixture-based libraries and positional scanning deconvolution combine two approaches for the rapid identification of specific scaffolds and active ligands. Here we present a quantitative assessment of the screening of 32 positional scanning libraries in the identification of highly specific and selective ligands for two formylpeptide receptors. We also compare and contrast two mixture-based library approaches using a mathematical model to facilitate the selection of active scaffolds and libraries to be pursued for further evaluation. The flexibility demonstrated in the differently formatted mixture-based libraries allows for their screening in a wide range of assays. |
format | Online Article Text |
id | pubmed-4106117 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-41061172014-07-22 The Mathematics of a Successful Deconvolution: A Quantitative Assessment of Mixture-Based Combinatorial Libraries Screened Against Two Formylpeptide Receptors Santos, Radleigh G. Appel, Jon R. Giulianotti, Marc A. Edwards, Bruce S. Sklar, Larry A. Houghten, Richard A. Pinilla, Clemencia Molecules Article In the past 20 years, synthetic combinatorial methods have fundamentally advanced the ability to synthesize and screen large numbers of compounds for drug discovery and basic research. Mixture-based libraries and positional scanning deconvolution combine two approaches for the rapid identification of specific scaffolds and active ligands. Here we present a quantitative assessment of the screening of 32 positional scanning libraries in the identification of highly specific and selective ligands for two formylpeptide receptors. We also compare and contrast two mixture-based library approaches using a mathematical model to facilitate the selection of active scaffolds and libraries to be pursued for further evaluation. The flexibility demonstrated in the differently formatted mixture-based libraries allows for their screening in a wide range of assays. MDPI 2013-05-30 /pmc/articles/PMC4106117/ /pubmed/23722730 http://dx.doi.org/10.3390/molecules18066408 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Santos, Radleigh G. Appel, Jon R. Giulianotti, Marc A. Edwards, Bruce S. Sklar, Larry A. Houghten, Richard A. Pinilla, Clemencia The Mathematics of a Successful Deconvolution: A Quantitative Assessment of Mixture-Based Combinatorial Libraries Screened Against Two Formylpeptide Receptors |
title | The Mathematics of a Successful Deconvolution: A Quantitative Assessment of Mixture-Based Combinatorial Libraries Screened Against Two Formylpeptide Receptors |
title_full | The Mathematics of a Successful Deconvolution: A Quantitative Assessment of Mixture-Based Combinatorial Libraries Screened Against Two Formylpeptide Receptors |
title_fullStr | The Mathematics of a Successful Deconvolution: A Quantitative Assessment of Mixture-Based Combinatorial Libraries Screened Against Two Formylpeptide Receptors |
title_full_unstemmed | The Mathematics of a Successful Deconvolution: A Quantitative Assessment of Mixture-Based Combinatorial Libraries Screened Against Two Formylpeptide Receptors |
title_short | The Mathematics of a Successful Deconvolution: A Quantitative Assessment of Mixture-Based Combinatorial Libraries Screened Against Two Formylpeptide Receptors |
title_sort | mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4106117/ https://www.ncbi.nlm.nih.gov/pubmed/23722730 http://dx.doi.org/10.3390/molecules18066408 |
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