With no lysine kinase 3 (WNK3); A Target Enabling Package
A description of the materials and methods is included within the TEP datasheet. Kinases WNK1-4 regulate cation-chloride cotransporters via phosphorylation of SPAK and OSR1 and thereby control salt homeostasis, cell volume and blood pressure. Gain of function mutations in WNK kinases are found in Go...
| Автор: | |
|---|---|
| Формат: | Dataset |
| Опубліковано: |
University of Oxford
2018
|
| Предмети: |
| _version_ | 1826303573250539520 |
|---|---|
| author | Pinkas, D |
| author2 | Pinkas, D |
| author_facet | Pinkas, D Pinkas, D |
| author_sort | Pinkas, D |
| collection | OXFORD |
| description | A description of the materials and methods is included within the TEP datasheet. Kinases WNK1-4 regulate cation-chloride cotransporters via phosphorylation of SPAK and OSR1 and thereby control salt homeostasis, cell volume and blood pressure. Gain of function mutations in WNK kinases are found in Gordon’s hypertension syndrome suggesting the WNK pathway as a therapeutic target. WNK3 inhibition in particular has also been shown to reduce cerebral injury after Ischemic stroke. Here we present assays and crystal structures that define (i) the molecular basis for disease mutations; (ii) the multiple functional domains of WNK kinases and their protein interactions; (iii) the binding of small molecule kinase inhibitors and a potential allosteric pocket. |
| first_indexed | 2024-03-07T06:04:45Z |
| format | Dataset |
| id | oxford-uuid:ed741f58-fa45-44f6-b9b1-9c5b64d2e44a |
| institution | University of Oxford |
| last_indexed | 2024-03-07T06:04:45Z |
| publishDate | 2018 |
| publisher | University of Oxford |
| record_format | dspace |
| spelling | oxford-uuid:ed741f58-fa45-44f6-b9b1-9c5b64d2e44a2022-03-27T11:25:11ZWith no lysine kinase 3 (WNK3); A Target Enabling PackageDatasethttp://purl.org/coar/resource_type/c_ddb1uuid:ed741f58-fa45-44f6-b9b1-9c5b64d2e44aChemical BiologyStructural GenomicsDrug DiscoveryORA DepositUniversity of Oxford2018Pinkas, DPinkas, DBufton, JChen, ZDaubner, GSchumacher, FGeorghiou, GZhang, JKurz, TAlessi, DBartual, SA description of the materials and methods is included within the TEP datasheet. Kinases WNK1-4 regulate cation-chloride cotransporters via phosphorylation of SPAK and OSR1 and thereby control salt homeostasis, cell volume and blood pressure. Gain of function mutations in WNK kinases are found in Gordon’s hypertension syndrome suggesting the WNK pathway as a therapeutic target. WNK3 inhibition in particular has also been shown to reduce cerebral injury after Ischemic stroke. Here we present assays and crystal structures that define (i) the molecular basis for disease mutations; (ii) the multiple functional domains of WNK kinases and their protein interactions; (iii) the binding of small molecule kinase inhibitors and a potential allosteric pocket. |
| spellingShingle | Chemical Biology Structural Genomics Drug Discovery Pinkas, D With no lysine kinase 3 (WNK3); A Target Enabling Package |
| title | With no lysine kinase 3 (WNK3); A Target Enabling Package |
| title_full | With no lysine kinase 3 (WNK3); A Target Enabling Package |
| title_fullStr | With no lysine kinase 3 (WNK3); A Target Enabling Package |
| title_full_unstemmed | With no lysine kinase 3 (WNK3); A Target Enabling Package |
| title_short | With no lysine kinase 3 (WNK3); A Target Enabling Package |
| title_sort | with no lysine kinase 3 wnk3 a target enabling package |
| topic | Chemical Biology Structural Genomics Drug Discovery |
| work_keys_str_mv | AT pinkasd withnolysinekinase3wnk3atargetenablingpackage |