Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors
Covalent inhibitors have recently seen a revival in medicinal chemistry. Inhibitors addressing non-catalytic cysteine residues with weakly reactive electrophiles have been very successfully employed to target protein kinases, one of the major druggable protein families. Here we provide an overview...
| Main Authors: | , |
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| Format: | Article |
| Language: | deu |
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Swiss Chemical Society
2022-05-01
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| Series: | CHIMIA |
| Subjects: | |
| Online Access: | https://chimia.ch/chimia/article/view/6037 |
| _version_ | 1811328461789200384 |
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| author | Laura Hillebrand Matthias Gehringer |
| author_facet | Laura Hillebrand Matthias Gehringer |
| author_sort | Laura Hillebrand |
| collection | DOAJ |
| description |
Covalent inhibitors have recently seen a revival in medicinal chemistry. Inhibitors addressing non-catalytic cysteine residues with weakly reactive electrophiles have been very successfully employed to target protein kinases, one of the major druggable protein families. Here we provide an overview of irreversible and reversible covalent protein kinase inhibitors in clinical development and beyond. We further spotlight recent advances in targeting amino acids other than cysteine and the reactive groups utilized in covalent protein kinase inhibitors.
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| first_indexed | 2024-04-13T15:26:37Z |
| format | Article |
| id | doaj.art-4c84a2c9d3e549978e4e0c112c01cf58 |
| institution | Directory Open Access Journal |
| issn | 0009-4293 2673-2424 |
| language | deu |
| last_indexed | 2024-04-13T15:26:37Z |
| publishDate | 2022-05-01 |
| publisher | Swiss Chemical Society |
| record_format | Article |
| series | CHIMIA |
| spelling | doaj.art-4c84a2c9d3e549978e4e0c112c01cf582022-12-22T02:41:30ZdeuSwiss Chemical SocietyCHIMIA0009-42932673-24242022-05-0176510.2533/chimia.2022.435Never Gonna Give You Up – Current Developments in Covalent Protein Kinase InhibitorsLaura Hillebrand0Matthias Gehringer1aDepartment of Pharmaceutical & Medicinal Chemistry, Eberhard Karls University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, GermanyDepartment of Pharmaceutical & Medicinal Chemistry, Eberhard Karls University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany; Cluster of Excellence iFIT (EXC 2180) ‘Image-Guided & Functionally Instructed Tumor Therapies’, University of Tübingen, 72076 Tübingen, Germany Covalent inhibitors have recently seen a revival in medicinal chemistry. Inhibitors addressing non-catalytic cysteine residues with weakly reactive electrophiles have been very successfully employed to target protein kinases, one of the major druggable protein families. Here we provide an overview of irreversible and reversible covalent protein kinase inhibitors in clinical development and beyond. We further spotlight recent advances in targeting amino acids other than cysteine and the reactive groups utilized in covalent protein kinase inhibitors. https://chimia.ch/chimia/article/view/6037Covalent inhibitorsCysteine targetingProtein kinases |
| spellingShingle | Laura Hillebrand Matthias Gehringer Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors CHIMIA Covalent inhibitors Cysteine targeting Protein kinases |
| title | Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors |
| title_full | Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors |
| title_fullStr | Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors |
| title_full_unstemmed | Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors |
| title_short | Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors |
| title_sort | never gonna give you up current developments in covalent protein kinase inhibitors |
| topic | Covalent inhibitors Cysteine targeting Protein kinases |
| url | https://chimia.ch/chimia/article/view/6037 |
| work_keys_str_mv | AT laurahillebrand nevergonnagiveyouupcurrentdevelopmentsincovalentproteinkinaseinhibitors AT matthiasgehringer nevergonnagiveyouupcurrentdevelopmentsincovalentproteinkinaseinhibitors |