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Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 1321 | 11q23.3 | SIK3 | SIK family kinase 3 | |
Mouse | - | 1311 | 9 A5.2 | Sik3 | SIK family kinase 3 |
Database Links ![]() |
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BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL6149 (Hs) |
Ensembl Gene | ENSG00000160584 (Hs), ENSMUSG00000034135 (Mm) |
Entrez Gene | 23387 (Hs), 70661 (Mm) |
Human Protein Atlas | ENSG00000160584 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:23387 (Hs), mmu:70661 (Mm) |
OMIM | 614776 (Hs) |
Pharos | Q9Y2K2 (Hs) |
RefSeq Nucleotide | NM_025164 (Hs), NM_027498 (Mm) |
RefSeq Protein | NP_079440 (Hs), NP_081774 (Mm) |
UniProtKB | Q9Y2K2 (Hs), Q6P4S6 (Mm) |
Wikipedia | SIK3 (Hs) |
Enzyme Reaction ![]() |
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Download all structure-activity data for this target as a CSV file
Inhibitors | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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DiscoveRx KINOMEscan® screen ![]() |
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A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 3,6 |
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Target used in screen: QSK | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
Inhibition of SIK2 and SIK3 to promote macrophage switch to a 'regulatory'-like phenotype that favours resolution of inflammation is considered a potential therapeutic strategy for the treatment of chronic inflammatory diseases [2,5]. |
1. Clark K, MacKenzie KF, Petkevicius K, Kristariyanto Y, Zhang J, Choi HG, Peggie M, Plater L, Pedrioli PG, McIver E et al.. (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc. Natl. Acad. Sci. U.S.A., 109 (42): 16986-91. [PMID:23033494]
2. Darling NJ, Toth R, Arthur JS, Clark K. (2017) Inhibition of SIK2 and SIK3 during differentiation enhances the anti-inflammatory phenotype of macrophages. Biochem. J., 474 (4): 521-537. [PMID:27920213]
3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]
4. Lombardi MS, Gilliéron C, Dietrich D, Gabay C. (2016) SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J. Leukoc. Biol., 99 (5): 711-21. [PMID:26590148]
5. Ozanne J, Prescott AR, Clark K. (2015) The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases. Biochem. J., 465 (2): 271-9. [PMID:25351958]
6. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]
QIK subfamily: SIK family kinase 3. Last modified on 23/05/2017. Accessed on 26/02/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2199.