Target Information
| Target General Information | Top | |||||
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| Target ID |
T91323
(Former ID: TTDI00169)
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| Target Name |
Cytoplasmic DRAK1 (STK17A)
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| Synonyms |
Serine/threonine-protein kinase 17A; STK17A; DAP kinase-related apoptosis-inducing protein kinase 1
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| Gene Name |
STK17A
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Acts as a positive regulator of apoptosis. Also acts as a regulator of cellular reactive oxygen species.
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| BioChemical Class |
Kinase
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| UniProt ID | ||||||
| EC Number |
EC 2.7.11.1
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| Sequence |
MIPLEKPGSGGSSPGATSGSGRAGRGLSGPCRPPPPPQARGLLTEIRAVVRTEPFQDGYS
LCPGRELGRGKFAVVRKCIKKDSGKEFAAKFMRKRRKGQDCRMEIIHEIAVLELAQDNPW VINLHEVYETASEMILVLEYAAGGEIFDQCVADREEAFKEKDVQRLMRQILEGVHFLHTR DVVHLDLKPQNILLTSESPLGDIKIVDFGLSRILKNSEELREIMGTPEYVAPEILSYDPI SMATDMWSIGVLTYVMLTGISPFLGNDKQETFLNISQMNLSYSEEEFDVLSESAVDFIRT LLVKKPEDRATAEECLKHPWLTQSSIQEPSFRMEKALEEANALQEGHSVPEINSDTDKSE TKESIVTEELIVVTSYTLGQCRQSEKEKMEQKAISKRFKFEEPLLQEIPGEFIY 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: N-benzyl-7,10-dioxa-13,17,18,21-tetrazatetracyclo[12.5.2.12,6.017,20]docosa-1(20),2(22),3,5,14(21),15,18-heptaene-5-carboxamide | Ligand Info | |||||
| Structure Description | The STK17A (DRAK1) Kinase Domain Bound to CKJB68 | PDB:7QUE | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [2] |
| PDB Sequence |
SMVRTEPFQD
57 GYSLCPGREL67 GRGKFAVVRK77 CIKKDSGKEF87 AAKFMRKRRK97 GQDCRMEIIH 107 EIAVLELAQD117 NPWVINLHEV127 YETASEMILV137 LEYAAGGEIF147 AFKEKDVQRL 166 MRQILEGVHF176 LHTRDVVHLD186 LKPQNILLTS196 ESPLGDIKIV206 DFGLSRILKN 216 SEELREIMGT226 PEYVAPEILS236 YDPISMATDM246 WSIGVLTYVM256 LTGISPFLGN 266 DKQETFLNIS276 QMNLSYSEEE286 FDVLSESAVD296 FIRTLLVKKP306 EDRATAEECL 316 KHPWLT
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LEU67
3.134
GLY68
4.161
ARG69
4.032
GLY70
3.398
ALA73
3.216
VAL74
4.336
VAL75
3.743
ALA88
3.432
LYS90
2.874
GLU108
4.584
ILE122
4.304
LEU138
3.579
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| Ligand Name: N-tert-butyl-7,10-dioxa-13,17,18,21-tetrazatetracyclo[12.5.2.12,6.017,20]docosa-1(20),2(22),3,5,14(21),15,18-heptaene-5-carboxamide | Ligand Info | |||||
| Structure Description | The STK17A (DRAK1) Kinase Domain Bound to CK156 | PDB:7QUF | ||||
| Method | X-ray diffraction | Resolution | 2.60 Å | Mutation | No | [2] |
| PDB Sequence |
SMVRTEPFQD
57 GYSLCPGREL67 GRGKFAVVRK77 CIKKDSGKEF87 AAKFMRKRRK97 GQDCRMEIIH 107 EIAVLELAQD117 NPWVINLHEV127 YETASEMILV137 LEYAAGGEIF147 DQCVAFKEKD 162 VQRLMRQILE172 GVHFLHTRDV182 VHLDLKPQNI192 LLTSESPLGD202 IKIVDFGLSR 212 ILKNSEELRE222 IMGTPEYVAP232 EILSYDPISM242 ATDMWSIGVL252 TYVMLTGISP 262 FLGNDKQETF272 LNISQMNLSY282 SEEEFDVLSE292 SAVDFIRTLL302 VKKPEDRATA 312 EECLKHPWLT322
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LEU67
3.576
GLY68
3.979
ARG69
4.455
GLY70
4.067
ALA73
4.368
VAL75
3.481
ALA88
3.637
LYS90
2.278
ILE122
4.160
LEU138
3.893
GLU139
3.465
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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 Similarity Proteins
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| Chemical Structure based Activity Landscape of Target | Top |
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| References | Top | |||||
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| REF 1 | Cytoplasmic DRAK1 overexpressed in head and neck cancers inhibits TGF-1 tumor suppressor activity by binding to Smad3 to interrupt its complex for... Oncogene. 2015 Sep 24;34(39):5037-45. | |||||
| REF 2 | Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-a]pyrimidine-Based Macrocycles. J Med Chem. 2022 Jun 9;65(11):7799-7817. | |||||
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