Abstract:
:In total, 47,500,000 people worldwide are affected by dementia and this number is estimated to double by 2030 and triple within 2050 resulting in a huge burden on public health. Alzheimer's disease (AD), a progressive neurodegenerative disorder, is the most common cause of dementia, accounting for 60-70% of all the cases. The cause of AD is still poorly understood but several brain abnormalities (e.g., loss of neuronal connections and neuronal death) have been identified in affected patients. In addition to the accumulation of β-amyloid plaques in the brain tissue, aberrant phosphorylation of tau proteins has proved to increase neuronal death. DYRK1A phosphorylates tau on 11 different Ser/Thr residues, resulting in the formation of aggregates called 'neurofibrillary tangles' which, together with amyloid plaques, could be responsible for dementia, neuronal degeneration and cell death. Small molecule inhibition of DYRK1A could thus represent an interesting approach toward the treatment of Alzheimer's and other neurodegenerative diseases. Herein we review the current progress in the identification and development of DYRK1A inhibitors.
journal_name
Future Med Chemjournal_title
Future medicinal chemistryauthors
Stotani S,Giordanetto F,Medda Fdoi
10.4155/fmc-2016-0013subject
Has Abstractpub_date
2016-04-01 00:00:00pages
681-96issue
6eissn
1756-8919issn
1756-8927journal_volume
8pub_type
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journal_title:Future medicinal chemistry
pub_type: 杂志文章
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journal_title:Future medicinal chemistry
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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journal_title:Future medicinal chemistry
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journal_title:Future medicinal chemistry
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更新日期:2016-12-01 00:00:00
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pub_type: 杂志文章
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2018-10-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.09.118
更新日期:2010-02-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2018-0586
更新日期:2019-07-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2019-0201
更新日期:2020-04-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.15.105
更新日期:2015-01-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.13.31
更新日期:2013-04-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.12.69
更新日期:2012-06-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2016-0041
更新日期:2016-06-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2017-0109
更新日期:2017-11-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.11.65
更新日期:2011-06-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2014-05-01 00:00:00
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doi:10.4155/fmc.14.9
更新日期:2014-03-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2018-01-01 00:00:00
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更新日期:2020-01-10 00:00:00
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journal_title:Future medicinal chemistry
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更新日期:2014-09-01 00:00:00
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journal_title:Future medicinal chemistry
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更新日期:2016-04-01 00:00:00
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更新日期:2015-01-01 00:00:00
abstract::CDK12 and CDK13 are Ser/Thr protein kinases that regulate transcription and co-transcriptional processes. Genetic silencing of CDK12 is associated with genomic instability in a variety of cancers, including difficult-to-treat breast, ovarian, colorectal, brain and pancreatic cancers, and is synthetic lethal with PARP,...
journal_title:Future medicinal chemistry
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更新日期:2021-01-01 00:00:00
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更新日期:2014-03-01 00:00:00
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journal_title:Future medicinal chemistry
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更新日期:2017-05-01 00:00:00
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journal_title:Future medicinal chemistry
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更新日期:2019-08-01 00:00:00