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DYRK1A inhibitors for disease therapy: Current status and perspectives

Tong Liu1, Yuxi Wang2, Jiaxing Wang3

  • 1Targeted Tracer Research and development laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Joint Institute for Altitude Health, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China; State Key Laboratory of Biotherapy and Cancer Center, Department of Respiratory and Critical Care Medicine, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China.

European Journal of Medicinal Chemistry
|December 26, 2021
PubMed

Insights

Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is crucial in Down syndrome, neurodegeneration, cancer, and diabetes. This review highlights novel DYRK1A inhibitors and their therapeutic potential for various diseases.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Genetics

Background:

  • Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a key protein kinase involved in numerous biological processes.
  • DYRK1A, located on chromosome 21q22.2, is implicated in Down syndrome pathogenesis.
  • DYRK1A dysregulation is linked to neurodegenerative diseases via amyloid beta accumulation and Tau hyperphosphorylation, as well as cancer and diabetes.

Purpose of the Study:

  • To review the latest therapeutic potential of DYRK1A for various human diseases.
  • To summarize recent discoveries in novel DYRK1A inhibitors.
  • To guide future DYRK1A inhibitor development and structural optimization.

Main Methods:

  • Literature review of recent scientific publications.
  • Analysis of DYRK1A's role in disease pathogenesis.
  • Summary of reported DYRK1A inhibitors and their therapeutic applications.

Main Results:

  • DYRK1A inhibitors show promise for treating Down syndrome, Alzheimer's disease, cancer, and diabetes.
  • Numerous novel DYRK1A inhibitors have been developed.
  • Understanding DYRK1A's function is critical for targeted therapeutic strategies.

Conclusions:

  • DYRK1A is a significant therapeutic target for multiple diseases.
  • Ongoing research into DYRK1A inhibitors is crucial for advancing treatment options.
  • This review provides a comprehensive overview of DYRK1A's therapeutic landscape.
Keywords:
CancerDSDYRK1ADYRK1A inhibitorDrug designStructure activity relationships

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