Target Information
| Target General Information | Top | |||||
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| Target ID |
T08198
(Former ID: TTDI03428)
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| Target Name |
Oxidative stress responsive 1 (OXSR1)
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| Synonyms |
Serine/threonine-protein kinase OSR1; Oxidative stress-responsive 1 protein; KIAA1101
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| Gene Name |
OXSR1
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Phosphorylates RELL1, RELL2 and RELT. Phosphorylates PAK1. Phosphorylates PLSCR1 in the presence of RELT.
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| UniProt ID | ||||||
| EC Number |
EC 2.7.11.1
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| Sequence |
MSEDSSALPWSINRDDYELQEVIGSGATAVVQAAYCAPKKEKVAIKRINLEKCQTSMDEL
LKEIQAMSQCHHPNIVSYYTSFVVKDELWLVMKLLSGGSVLDIIKHIVAKGEHKSGVLDE STIATILREVLEGLEYLHKNGQIHRDVKAGNILLGEDGSVQIADFGVSAFLATGGDITRN KVRKTFVGTPCWMAPEVMEQVRGYDFKADIWSFGITAIELATGAAPYHKYPPMKVLMLTL QNDPPSLETGVQDKEMLKKYGKSFRKMISLCLQKDPEKRPTAAELLRHKFFQKAKNKEFL QEKTLQRAPTISERAKKVRRVPGSSGRLHKTEDGGWEWSDDEFDEESEEGKAAISQLRSP RVKESISNSELFPTTDPVGTLLQVPEQISAHLPQPAGQIATQPTQVSLPPTAEPAKTAQA LSSGSGSQETKIPISLVLRLRNSKKELNDIRFEFTPGRDTAEGVSQELISAGLVDGRDLV IVAANLQKIVEEPQSNRSVTFKLASGVEGSDIPDDGKLIGFAQLSIS 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: AMP-PNP | Ligand Info | |||||
| Structure Description | Structure of the OSR1 kinase, a hypertension drug target | PDB:2VWI | ||||
| Method | X-ray diffraction | Resolution | 2.15 Å | Mutation | No | [2] |
| PDB Sequence |
NRDDYELQEV
22 IGTAVVQAAY35 CEKVAIKRIN49 AMSQCHHPNI75 VSYYTSFVVK85 DELWLVMKLL 95 SGGSVLDIIK105 HIVAKGEHKS115 GVLDESTIAT125 ILREVLEGLE135 YLHKNGQIHR 145 DVKAGNILLG155 EDGSVQIADF165 GVSAFLAGTP190 CWMAPEVMEQ200 VRGYDFKADI 210 WSFGITAIEL220 ATGAAPYHKY230 PPMKVLMLTL240 QNDPPSLETE255 MLKKYGKSFR 265 KMISLCLQKD275 PEKRPTAAEL285 LRHKFFQ
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| 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 Similarity Proteins
Human Tissue Distribution
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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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| References | Top | |||||
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| REF 1 | Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. Eur J Med Chem. 2014 Jun 10;80:364-82. | |||||
| REF 2 | Structure of the OSR1 kinase, a hypertension drug target. Proteins. 2008 Dec;73(4):1082-7. | |||||
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