Target Binding Site Detail
Target General Information | Top | ||||
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Target ID | T04831 | Target Info | |||
Target Name | Tyrosine-protein kinase EIF2AK2 (p68) | ||||
Synonyms | p68 kinase; Proteinkinase RNA-activated; Interferon-inducible RNA-dependent protein kinase p68; Interferon-induced, double-stranded RNA-activated protein kinase p68 | ||||
Target Type | Patented-recorded Target | ||||
Gene Name | EIF2AK2 | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Ligand General Information | Top | ||||
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Ligand Name | Phosphonothreonine | Ligand Info | |||
Canonical SMILES | CC(C(C(=O)O)N)OP(=O)(O)O | ||||
InChI | 1S/C4H10NO6P/c1-2(3(5)4(6)7)11-12(8,9)10/h2-3H,5H2,1H3,(H,6,7)(H2,8,9,10)/t2-,3+/m1/s1 | ||||
InChIKey | USRGIUJOYOXOQJ-GBXIJSLDSA-N | ||||
PubChem Compound ID | 3246323 |
Drug Binding Sites of Target | Top | |||||
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PDB ID: 2A19 PKR kinase domain- eIF2alpha- AMP-PNP complex. | ||||||
Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | Yes | [1] |
PDB Sequence |
AHTVDKRFGM
265 DFKEIELIGS275 GGFGQVFKAK285 HRIDGKTYVI295 KRVKYNNEKA305 EREVKALAKL 315 DHVNIVHYNG325 CWDGFDYDRS357 KTKCLFIQME367 FCDKGTLEQW377 IEKRRGEKLD 387 KVLALELFEQ397 ITKGVDYIHS407 KKLINRDLKP417 SNIFLVDTKQ427 VKIGDFGLVT 437 SLKNDGKRRS448 KGTLRYMSPE458 QISSQDYGKE468 VDLYALGLIL478 AELLHVCDTA 488 FETSKFFTDL498 RDGIISDIFD508 KKEKTLLQKL518 LSKKPEDRPN528 TSEILRTLTV 538 WKK
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PDB ID: 7OBL Crystal structure of 14-3-3 sigma in complex with PKR phosphopeptide and stabilizer Fusicoccin-A | ||||||
Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [2] |
PDB Sequence |
ERHC
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References | Top | ||||
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REF 1 | Higher-order substrate recognition of eIF2alpha by the RNA-dependent protein kinase PKR. Cell. 2005 Sep 23;122(6):887-900. | ||||
REF 2 | IFN-alpha primes cancer cells for Fusicoccin-induced cell death via 14-3-3 PPI stabilization. Cell Chem Biol. 2023 Jun 15;30(6):573-590.e6. |
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