Small-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate capture
We describe covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) and studies towards a strategy for photocapture of PHD2 substrates. Reversible active site binding of electrophile bearing compounds enables susbsequent covalent reaction with a lysine residue (K408...
| Main Authors: | , , , , , , , , , |
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| Format: | Journal article |
| Published: |
Royal Society of Chemistry
2018
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| _version_ | 1826268856945999872 |
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| author | Bush, J Lesniak, R Yeh, T Belle, R Kramer, H Tumber, A Chowdhury, R Flashman, E Mecinovic, J Schofield, C |
| author_facet | Bush, J Lesniak, R Yeh, T Belle, R Kramer, H Tumber, A Chowdhury, R Flashman, E Mecinovic, J Schofield, C |
| author_sort | Bush, J |
| collection | OXFORD |
| description | We describe covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) and studies towards a strategy for photocapture of PHD2 substrates. Reversible active site binding of electrophile bearing compounds enables susbsequent covalent reaction with a lysine residue (K408) in the flexible C-terminal region of PHD2 to give a modified protein that retains catalytic activity. |
| first_indexed | 2024-03-06T21:16:01Z |
| format | Journal article |
| id | oxford-uuid:3fcef202-cb23-4209-8d01-7298411b874a |
| institution | University of Oxford |
| last_indexed | 2024-03-06T21:16:01Z |
| publishDate | 2018 |
| publisher | Royal Society of Chemistry |
| record_format | dspace |
| spelling | oxford-uuid:3fcef202-cb23-4209-8d01-7298411b874a2022-03-26T14:34:17ZSmall-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate captureJournal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:3fcef202-cb23-4209-8d01-7298411b874aSymplectic Elements at OxfordRoyal Society of Chemistry2018Bush, JLesniak, RYeh, TBelle, RKramer, HTumber, AChowdhury, RFlashman, EMecinovic, JSchofield, CWe describe covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) and studies towards a strategy for photocapture of PHD2 substrates. Reversible active site binding of electrophile bearing compounds enables susbsequent covalent reaction with a lysine residue (K408) in the flexible C-terminal region of PHD2 to give a modified protein that retains catalytic activity. |
| spellingShingle | Bush, J Lesniak, R Yeh, T Belle, R Kramer, H Tumber, A Chowdhury, R Flashman, E Mecinovic, J Schofield, C Small-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate capture |
| title | Small-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate capture |
| title_full | Small-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate capture |
| title_fullStr | Small-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate capture |
| title_full_unstemmed | Small-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate capture |
| title_short | Small-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate capture |
| title_sort | small molecules that covalently react with a human prolyl hydroxylase towards activity modulation and substrate capture |
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