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Relations between effects and structure of small bicyclic molecules on the complex model system saccharomyces cerevisiae
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Brilli, Matteo, Trabocchi, Andrea, Weil, Tobias, Cavalieri, Duccio and Stefanini, Irene (2017) Relations between effects and structure of small bicyclic molecules on the complex model system saccharomyces cerevisiae. Frontiers in Pharmacology, 8 . 170. doi:10.3389/fphar.2017.00170
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Official URL: http://dx.doi.org/10.3389/fphar.2017.00170
Abstract
The development of compounds able to modify biological functions largely took advantage of parallel synthesis to generate a broad chemical variance of compounds to be tested for the desired effect(s). The budding yeast Saccharomyces cerevisiae is a model for pharmacological studies since a long time as it represents a relatively simple system to explore the relations among chemical variance and bioactivity. To identify relations between the chemical features of the molecules and their activity, we delved into the effects of a library of small compounds on the viability of a set of S. cerevisiae strains. Thanks to the high degree of chemical diversity of the tested compounds and to the measured effect on the yeast growth rate, we were able to scale-down the chemical library and to gain information on the most effective structures at the substituent level. Our results represent a valuable source for the selection, rational design, and optimization of bioactive compounds.
| Item Type: | Journal Article | ||||||
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| Subjects: | Q Science > QK Botany R Medicine > RM Therapeutics. Pharmacology |
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| Divisions: | Faculty of Medicine > Warwick Medical School > Biomedical Sciences > Cell & Developmental Biology Faculty of Medicine > Warwick Medical School |
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| Library of Congress Subject Headings (LCSH): | Drug development, Saccharomyces cerevisiae -- Molecular aspects, Principal components analysis, High throughput screening (Drug development) | ||||||
| Journal or Publication Title: | Frontiers in Pharmacology | ||||||
| Publisher: | Frontiers Research Foundation | ||||||
| ISSN: | 1663-9812 | ||||||
| Official Date: | 30 March 2017 | ||||||
| Dates: |
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| Date of first compliant deposit: | 3 April 2017 | ||||||
| Volume: | 8 | ||||||
| Article Number: | 170 | ||||||
| DOI: | 10.3389/fphar.2017.00170 | ||||||
| Status: | Peer Reviewed | ||||||
| Publication Status: | Published | ||||||
| Access rights to Published version: | Open Access | ||||||
| Funder: | Wellcome Trust (London, England), University of Warwick |
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