Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down Syndrome
Down syndrome (DS) is a complex genetic disorder associated with substantial physical, cognitive, and behavioral challenges. Due to better treatment options for the physical co-morbidities of DS, the life expectancy of individuals with DS is beginning to approach that of the general population. Howe...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-11-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/14/11/1170 |
| _version_ | 1797508828811493376 |
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| author | Wenche Stensen Ulli Rothweiler Richard Alan Engh Melissa R. Stasko Ilya Bederman Alberto C. S. Costa Anders Fugelli John S. Mjøen Svendsen |
| author_facet | Wenche Stensen Ulli Rothweiler Richard Alan Engh Melissa R. Stasko Ilya Bederman Alberto C. S. Costa Anders Fugelli John S. Mjøen Svendsen |
| author_sort | Wenche Stensen |
| collection | DOAJ |
| description | Down syndrome (DS) is a complex genetic disorder associated with substantial physical, cognitive, and behavioral challenges. Due to better treatment options for the physical co-morbidities of DS, the life expectancy of individuals with DS is beginning to approach that of the general population. However, the cognitive deficits seen in individuals with DS still cannot be addressed pharmacologically. In young individuals with DS, the level of intellectual disability varies from mild to severe, but cognitive ability generally decreases with increasing age, and all individuals with DS have early onset Alzheimer’s disease (AD) pathology by the age of 40. The present study introduces a novel inhibitor for the protein kinase DYRK1A, a key controlling kinase whose encoding gene is located on chromosome 21. The novel inhibitor is well characterized for use in mouse models and thus represents a valuable tool compound for further DYRK1A research. |
| first_indexed | 2024-03-10T05:10:25Z |
| format | Article |
| id | doaj.art-e08484b1821349199632d845ff4f1872 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T05:10:25Z |
| publishDate | 2021-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-e08484b1821349199632d845ff4f18722023-11-23T00:56:19ZengMDPI AGPharmaceuticals1424-82472021-11-011411117010.3390/ph14111170Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down SyndromeWenche Stensen0Ulli Rothweiler1Richard Alan Engh2Melissa R. Stasko3Ilya Bederman4Alberto C. S. Costa5Anders Fugelli6John S. Mjøen Svendsen7Department of Chemistry, UiT, The Arctic University of Norway, 9037 Tromsø, NorwayDepartment of Chemistry, UiT, The Arctic University of Norway, 9037 Tromsø, NorwayDepartment of Chemistry, UiT, The Arctic University of Norway, 9037 Tromsø, NorwayDepartments of Pediatrics, Psychiatry, Macromolecular Science and Engineering, Case Western Reserve University, 11100 Euclid Avenue, Cleveland, OH 44106, USADepartments of Pediatrics, Psychiatry, Macromolecular Science and Engineering, Case Western Reserve University, 11100 Euclid Avenue, Cleveland, OH 44106, USADepartments of Pediatrics, Psychiatry, Macromolecular Science and Engineering, Case Western Reserve University, 11100 Euclid Avenue, Cleveland, OH 44106, USAPharmasum Therapeutics AS, Gaustadalleen 21, 0349 Oslo, NorwayDepartment of Chemistry, UiT, The Arctic University of Norway, 9037 Tromsø, NorwayDown syndrome (DS) is a complex genetic disorder associated with substantial physical, cognitive, and behavioral challenges. Due to better treatment options for the physical co-morbidities of DS, the life expectancy of individuals with DS is beginning to approach that of the general population. However, the cognitive deficits seen in individuals with DS still cannot be addressed pharmacologically. In young individuals with DS, the level of intellectual disability varies from mild to severe, but cognitive ability generally decreases with increasing age, and all individuals with DS have early onset Alzheimer’s disease (AD) pathology by the age of 40. The present study introduces a novel inhibitor for the protein kinase DYRK1A, a key controlling kinase whose encoding gene is located on chromosome 21. The novel inhibitor is well characterized for use in mouse models and thus represents a valuable tool compound for further DYRK1A research.https://www.mdpi.com/1424-8247/14/11/1170protein kinase inhibitorDYRK1Adown syndromeneurodegenerationlearning and memory deficitsmouse models |
| spellingShingle | Wenche Stensen Ulli Rothweiler Richard Alan Engh Melissa R. Stasko Ilya Bederman Alberto C. S. Costa Anders Fugelli John S. Mjøen Svendsen Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down Syndrome Pharmaceuticals protein kinase inhibitor DYRK1A down syndrome neurodegeneration learning and memory deficits mouse models |
| title | Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down Syndrome |
| title_full | Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down Syndrome |
| title_fullStr | Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down Syndrome |
| title_full_unstemmed | Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down Syndrome |
| title_short | Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down Syndrome |
| title_sort | novel dyrk1a inhibitor rescues learning and memory deficits in a mouse model of down syndrome |
| topic | protein kinase inhibitor DYRK1A down syndrome neurodegeneration learning and memory deficits mouse models |
| url | https://www.mdpi.com/1424-8247/14/11/1170 |
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