Target General Infomation
Target ID
T82720 (Former ID: TTDI03163)
Target Name
Dual-specificity tyrosine-phosphorylation regulated kinase 1B (DYRK1B)
Synonyms
Minibrain-related kinase; MIRK; Dual specificity tyrosine-phosphorylation-regulated kinase 1B
Gene Name
DYRK1B
Target Type
Patented-recorded target
[1]
Function
Enhances the transcriptional activity of TCF1/HNF1A and FOXO1. Inhibits epithelial cell migration. Mediates colon carcinoma cell survival in mitogen-poor environments. Inhibits the SHH and WNT1 pathways, thereby enhancing adipogenesis. In addition, promotes expression of the gluconeogenic enzyme glucose-6-phosphatase (G6PC). Dual-specificity kinase which possesses both serine/threonine and tyrosine kinase activities.
BioChemical Class
Kinase
UniProt ID
DYR1B_HUMAN
EC Number
EC 2.7.12.1
Sequence
MAVPPGHGPFSGFPGPQEHTQVLPDVRLLPRRLPLAFRDATSAPLRKLSVDLIKTYKHIN
EVYYAKKKRRAQQAPPQDSSNKKEKKVLNHGYDDDNHDYIVRSGERWLERYEIDSLIGKG
SFGQVVKAYDHQTQELVAIKIIKNKKAFLNQAQIELRLLELMNQHDTEMKYYIVHLKRHF
MFRNHLCLVFELLSYNLYDLLRNTHFRGVSLNLTRKLAQQLCTALLFLATPELSIIHCDL
KPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGTPYDLAIDMWSLG
CILVEMHTGEPLFSGSNEVDQMNRIVEVLGIPPAAMLDQAPKARKYFERLPGGGWTLRRT
KELRKDYQGPGTRRLQEVLGVQTGGPGGRRAGEPGHSPADYLRFQDLVLRMLEYEPAARI
SPLGALQHGFFRRTADEATNTGPAGSSASTSPAPLDTCPSSSTASSISSSGGSSGSSSDN
RTYRYSNRYCGGPGPPITDCEMNSPQVPPSQPLRPWAGGDVPHKTHQAPASASSLPGTGA
QLPPQPRYLGRPPSPTSPPPPELMDVSLVGGPADCSPPHPAPAPQHPAASALRTRMTGGR
PPLPPPDDPATLGPHLGLRGVPQSTAASS
Mode of Action [+] 1 Modes of Action +
Inhibitor [+] 21 Inhibitor drugs +
1 PMID28766366-Compound-Scheme14BINDY Drug Info [1]
2 PMID28766366-Compound-Scheme21Left Drug Info [1]
3 PMID28766366-Compound-Scheme21Right Drug Info [1]
4 PMID28766366-Compound-Scheme25-2 Drug Info [1]
5 PMID28766366-Compound-Scheme25-3 Drug Info [1]
6 PMID28766366-Compound-Scheme25-4 Drug Info [1]
7 PMID28766366-Compound-Scheme2WO2012/098065bottom Drug Info [1]
8 PMID28766366-Compound-Scheme2WO2012/098065upper Drug Info [1]
9 PMID28766366-Compound-Scheme4Bottom Drug Info [1]
10 PMID28766366-Compound-Scheme4Upper Drug Info [1]
11 PMID28766366-Compound-Scheme5 Drug Info [1]
12 PMID28766366-Compound-Scheme7WO2012/098070bottom Drug Info [1]
13 PMID28766366-Compound-Scheme7WO2012/098070upper Drug Info [1]
14 PMID28766366-Compound-Scheme9EHT1610 Drug Info [1]
15 PMID28766366-Compound-Scheme9EHT3356 Drug Info [1]
16 PMID28766366-Compound-Scheme9EHT5372 Drug Info [1]
17 PMID28766366-Compound-Scheme9EHT6840 Drug Info [1]
18 PMID28766366-Compound-Scheme9EHT9851 Drug Info [1]
19 PMID23642479C17 Drug Info [2]
20 PMID24900699C68 Drug Info [3]
21 WO2013026806C72 Drug Info [4]
Target Regulators
Target-interacting Proteins
References
REF 1 Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors: a survey of recent patent literature.Expert Opin Ther Pat. 2017 Nov;27(11):1183-1199.
REF 2 Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. Bioorg Med Chem Lett. 2013 Jun15;23(12):3654-61.
REF 3 Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down's Syndrome or Alzheimer's Disease. ACS Med Chem Lett. 2013 Apr 26;4(6):502-3.
REF 4 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2010).

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