Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors
The 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl hydroxylases (PHDs) are targets for treatment of anaemia and other ischaemia related diseases. PHD inhibitors are in clinical trials; however, the number of reported templates for PHD inhibition is limited. We report structure–...
| Egile Nagusiak: | , , , , , , , |
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| Formatua: | Journal article |
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Royal Society of Chemistry
2019
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| _version_ | 1826257608902705152 |
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| author | Holt-Martyn, J Tumber, A Rahman, M Lippl, K Figg, W McDonough, M Chowdhury, R Schofield, C |
| author_facet | Holt-Martyn, J Tumber, A Rahman, M Lippl, K Figg, W McDonough, M Chowdhury, R Schofield, C |
| author_sort | Holt-Martyn, J |
| collection | OXFORD |
| description | The 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl hydroxylases (PHDs) are targets for treatment of anaemia and other ischaemia related diseases. PHD inhibitors are in clinical trials; however, the number of reported templates for PHD inhibition is limited. We report structure–activity relationship and crystallographic studies on spiro[4.5]decanone containing PHD inhibitors. Together with other studies, our results reveal spiro[4.5]decanones as useful templates for generation of potent and selective 2OG oxygenase inhibitors. |
| first_indexed | 2024-03-06T18:20:53Z |
| format | Journal article |
| id | oxford-uuid:063de5c2-f147-41cd-babe-e20d8673d91e |
| institution | University of Oxford |
| last_indexed | 2024-03-06T18:20:53Z |
| publishDate | 2019 |
| publisher | Royal Society of Chemistry |
| record_format | dspace |
| spelling | oxford-uuid:063de5c2-f147-41cd-babe-e20d8673d91e2022-03-26T09:01:32ZStudies on spiro[4.5]decanone prolyl hydroxylase domain inhibitorsJournal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:063de5c2-f147-41cd-babe-e20d8673d91eSymplectic Elements at OxfordRoyal Society of Chemistry2019Holt-Martyn, JTumber, ARahman, MLippl, KFigg, WMcDonough, MChowdhury, RSchofield, CThe 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl hydroxylases (PHDs) are targets for treatment of anaemia and other ischaemia related diseases. PHD inhibitors are in clinical trials; however, the number of reported templates for PHD inhibition is limited. We report structure–activity relationship and crystallographic studies on spiro[4.5]decanone containing PHD inhibitors. Together with other studies, our results reveal spiro[4.5]decanones as useful templates for generation of potent and selective 2OG oxygenase inhibitors. |
| spellingShingle | Holt-Martyn, J Tumber, A Rahman, M Lippl, K Figg, W McDonough, M Chowdhury, R Schofield, C Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors |
| title | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors |
| title_full | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors |
| title_fullStr | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors |
| title_full_unstemmed | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors |
| title_short | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors |
| title_sort | studies on spiro 4 5 decanone prolyl hydroxylase domain inhibitors |
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