Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases.
Protein kinases are involved in many essential cellular processes and their deregulation can lead to a variety of diseases, including cancer. The pharmaceutical industry has invested heavily in the identification of kinase inhibitors to modulate these disease-promoting pathways, resulting in several...
| Main Authors: | , , |
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| Format: | Journal article |
| Sprog: | English |
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Future Science
2014
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| _version_ | 1826258609295589376 |
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| author | Cowan-Jacob, S Jahnke, W Knapp, S |
| author_facet | Cowan-Jacob, S Jahnke, W Knapp, S |
| author_sort | Cowan-Jacob, S |
| collection | OXFORD |
| description | Protein kinases are involved in many essential cellular processes and their deregulation can lead to a variety of diseases, including cancer. The pharmaceutical industry has invested heavily in the identification of kinase inhibitors to modulate these disease-promoting pathways, resulting in several successful drugs. However, the field is challenging as it is difficult to identify novel selective inhibitors with good pharmacokinetic/pharmacodynamic properties. In addition, resistance to kinase inhibitor treatment frequently arises. The identification of non-ATP site targeting ('allosteric') inhibitors, the identification of kinase activators and the expansion of kinase target space to include the less studied members of the family, including atypical- and pseudo-kinases, are potential avenues to overcome these challenges. In this perspective, the opportunities and challenges of following these approaches and others will be discussed. |
| first_indexed | 2024-03-06T18:36:40Z |
| format | Journal article |
| id | oxford-uuid:0b7ace66-6e5c-4b4e-b8c4-d069c308eb2c |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-06T18:36:40Z |
| publishDate | 2014 |
| publisher | Future Science |
| record_format | dspace |
| spelling | oxford-uuid:0b7ace66-6e5c-4b4e-b8c4-d069c308eb2c2022-03-26T09:29:35ZNovel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:0b7ace66-6e5c-4b4e-b8c4-d069c308eb2cEnglishSymplectic Elements at OxfordFuture Science2014Cowan-Jacob, SJahnke, WKnapp, SProtein kinases are involved in many essential cellular processes and their deregulation can lead to a variety of diseases, including cancer. The pharmaceutical industry has invested heavily in the identification of kinase inhibitors to modulate these disease-promoting pathways, resulting in several successful drugs. However, the field is challenging as it is difficult to identify novel selective inhibitors with good pharmacokinetic/pharmacodynamic properties. In addition, resistance to kinase inhibitor treatment frequently arises. The identification of non-ATP site targeting ('allosteric') inhibitors, the identification of kinase activators and the expansion of kinase target space to include the less studied members of the family, including atypical- and pseudo-kinases, are potential avenues to overcome these challenges. In this perspective, the opportunities and challenges of following these approaches and others will be discussed. |
| spellingShingle | Cowan-Jacob, S Jahnke, W Knapp, S Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. |
| title | Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. |
| title_full | Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. |
| title_fullStr | Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. |
| title_full_unstemmed | Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. |
| title_short | Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. |
| title_sort | novel approaches for targeting kinases allosteric inhibition allosteric activation and pseudokinases |
| work_keys_str_mv | AT cowanjacobs novelapproachesfortargetingkinasesallostericinhibitionallostericactivationandpseudokinases AT jahnkew novelapproachesfortargetingkinasesallostericinhibitionallostericactivationandpseudokinases AT knapps novelapproachesfortargetingkinasesallostericinhibitionallostericactivationandpseudokinases |