Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor.
The quinoline-5,8 dicarboxylic acid scaffold has been identified by fragment-based approach as new potential lead compound for the development of JMJD3 inhibitors. Among them, compound 3 shows low micromolar inhibitory activity against JMJD3. The experimental evaluation of inhibition activity vs. re...
| Main Authors: | , , , , , |
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| Format: | Journal article |
| Language: | English |
| Published: |
Wiley
2018
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| _version_ | 1797073957331927040 |
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| author | Giordano, A Del Gaudio, F Johansson, C Riccio, R Oppermann, U Di Micco, S |
| author_facet | Giordano, A Del Gaudio, F Johansson, C Riccio, R Oppermann, U Di Micco, S |
| author_sort | Giordano, A |
| collection | OXFORD |
| description | The quinoline-5,8 dicarboxylic acid scaffold has been identified by fragment-based approach as new potential lead compound for the development of JMJD3 inhibitors. Among them, compound 3 shows low micromolar inhibitory activity against JMJD3. The experimental evaluation of inhibition activity vs. related seven isoforms of JMJD3 highlighted an unprecedented selectivity towards the biological target of interest. |
| first_indexed | 2024-03-06T23:29:22Z |
| format | Journal article |
| id | oxford-uuid:6b7c0653-cada-4dff-9680-39e20b525b12 |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-06T23:29:22Z |
| publishDate | 2018 |
| publisher | Wiley |
| record_format | dspace |
| spelling | oxford-uuid:6b7c0653-cada-4dff-9680-39e20b525b122022-03-26T19:04:21ZVirtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:6b7c0653-cada-4dff-9680-39e20b525b12EnglishSymplectic Elements at OxfordWiley2018Giordano, ADel Gaudio, FJohansson, CRiccio, ROppermann, UDi Micco, SThe quinoline-5,8 dicarboxylic acid scaffold has been identified by fragment-based approach as new potential lead compound for the development of JMJD3 inhibitors. Among them, compound 3 shows low micromolar inhibitory activity against JMJD3. The experimental evaluation of inhibition activity vs. related seven isoforms of JMJD3 highlighted an unprecedented selectivity towards the biological target of interest. |
| spellingShingle | Giordano, A Del Gaudio, F Johansson, C Riccio, R Oppermann, U Di Micco, S Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor. |
| title | Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor. |
| title_full | Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor. |
| title_fullStr | Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor. |
| title_full_unstemmed | Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor. |
| title_short | Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor. |
| title_sort | virtual fragment screening identification of a novel quinoline 5 8 dicarboxylic acid derivative as selective jmjd3 inhibitor |
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