Target Information
| Target General Information | Top | |||||
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| Target ID |
T29728
(Former ID: TTDI03084)
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| Target Name |
Casein kinase I gamma-3 (CSNK1G3)
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| Synonyms |
Casein kinase I isoform gamma-3; CKI-gamma 3
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| Gene Name |
CSNK1G3
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Serine/threonine-protein kinase. Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. It can phosphorylate a large number of proteins. Participates in Wnt signaling. Regulates fast synaptic transmission mediated by glutamate (By similarity).
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| UniProt ID | ||||||
| EC Number |
EC 2.7.11.1
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| Sequence |
MENKKKDKDKSDDRMARPSGRSGHNTRGTGSSSSGVLMVGPNFRVGKKIGCGNFGELRLG
KNLYTNEYVAIKLEPMKSRAPQLHLEYRFYKQLGSGDGIPQVYYFGPCGKYNAMVLELLG PSLEDLFDLCDRTFSLKTVLMIAIQLISRMEYVHSKNLIYRDVKPENFLIGRPGNKTQQV IHIIDFGLAKEYIDPETKKHIPYREHKSLTGTARYMSINTHLGKEQSRRDDLEALGHMFM YFLRGSLPWQGLKADTLKERYQKIGDTKRATPIEVLCENFPEMATYLRYVRRLDFFEKPD YDYLRKLFTDLFDRKGYMFDYEYDWIGKQLPTPVGAVQQDPALSSNREAHQHRDKMQQSK NQSADHRAAWDSQQANPHHLRAHLAADRHGGSVQVVSSTNGELNTDDPTAGRSNAPITAP TEVEVMDETKCCCFFKRRKRKTIQRHK Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Cdk1/2 inhibitor III | Ligand Info | |||||
| Structure Description | Structure of casein kinase 1 gamma 3 | PDB:2CHL | ||||
| Method | X-ray diffraction | Resolution | 1.95 Å | Mutation | No | [2] |
| PDB Sequence |
VLMVGPNFRV
45 GKKIGCGNFG55 ELRLGKNLYT65 NEYVAIKLEP75 MKSRAPQLHL85 EYRFYKQLGS 95 GDGIPQVYYF105 GPCGKYNAMV115 LELLGPSLED125 LFDLCDRTFS135 LKTVLMIAIQ 145 LISRMEYVHS155 KNLIYRDVKP165 ENFLIGRPGN175 KTQQVIHIID185 FALAKEYIDP 195 ETKKHIPYRE205 HKSLTGTARY215 MSINTHLGKE225 QSRRDDLEAL235 GHMFMYFLRG 245 SLPWQGLKAD255 TLKERYQKIG265 DTKRATPIEV275 LCENFPEMAT285 YLRYVRRLDF 295 FEKPDYDYLR305 KLFTDLFDRK315 GYMFDYEYDW325 IGKQLPTP
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| Ligand Name: Purvalanol A | Ligand Info | |||||
| Structure Description | Structure of casein kinase gamma 3 in complex with inhibitor | PDB:2IZU | ||||
| Method | X-ray diffraction | Resolution | 1.85 Å | Mutation | No | [3] |
| PDB Sequence |
VLMVGPNFRV
45 GKKIGCFGEL57 RLGKNLYTNE67 YVAIKLEPMK77 SRAPQLHLEY87 RFYKQLGSGD 97 GIPQVYYFGP107 CGKYNAMVLE117 LLGPSLEDLF127 DLCDRTFSLK137 TVLMIAIQLI 147 SRMEYVHSKN157 LIYRDVKPEN167 FLIGRPGNKT177 QQVIHIIDFA187 LAKEYIDPET 197 KKHIPYREHK207 SLTGTARYMS217 INTHLGKEQS227 RRDDLEALGH237 MFMYFLRGSL 247 PWQGLKADTL257 KERYQKIGDT267 KRATPIEVLC277 ENFPEMATYL287 RYVRRLDFFE 297 KPDYDYLRKL307 FTDLFDRKGY317 MFDYEYDWIG327 KQLPTPV
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ILE49
3.602
GLY50
3.748
CYS51
4.150
LEU57
3.462
ALA70
3.579
LYS72
4.794
TYR90
4.030
PRO100
3.875
LEU116
3.776
GLU117
3.167
LEU118
3.894
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Hedgehog signaling pathway | hsa04340 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Chemical Structure based Activity Landscape of Target | Top |
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| References | Top | |||||
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| REF 1 | 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92. | |||||
| REF 2 | Structure of Casein Kinase 1 Gamma 3 | |||||
| REF 3 | Inhibitor Binding by Casein Kinases | |||||
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