Target Information
| Target General Information | Top | |||||
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| Target ID |
T43289
(Former ID: TTDR00461)
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| Target Name |
Neuropsin (KLK8)
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| Synonyms |
hK8; UNQ283/PRO322; Tumor-associated differentially expressed gene-14 protein; Tumor-associated differentially expressed gene 14 protein; TADG14; Serine protease TADG-14; Serine protease 19; PRSS19; Ovasin; Neuropsin (M(r) 25032); NRPN; NP; Kallikrein-8; Kallikrein 8; KLK8 (neuropsin/ovasin)
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| Gene Name |
KLK8
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Cleaves L1CAM in response to increased neural activity. Induces neurite outgrowth and fasciculation of cultured hippocampal neurons. Plays a role in the formation and maturation of orphan and small synaptic boutons in the Schaffer-collateral pathway, regulates Schaffer-collateral long-term potentiation in the hippocampus and is required for memory acquisition and synaptic plasticity. Involved in skin desquamation and keratinocyte proliferation. Plays a role in the secondary phase of pathogenesis following spinal cord injury. Serine protease which is capable of degrading a number of proteins such as casein, fibrinogen, kininogen, fibronectin and collagen type IV.
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| BioChemical Class |
Peptidase
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| UniProt ID | ||||||
| EC Number |
EC 3.4.21.118
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| Sequence |
MGRPRPRAAKTWMFLLLLGGAWAGHSRAQEDKVLGGHECQPHSQPWQAALFQGQQLLCGG
VLVGGNWVLTAAHCKKPKYTVRLGDHSLQNKDGPEQEIPVVQSIPHPCYNSSDVEDHNHD LMLLQLRDQASLGSKVKPISLADHCTQPGQKCTVSGWGTVTSPRENFPDTLNCAEVKIFP QKKCEDAYPGQITDGMVCAGSSKGADTCQGDSGGPLVCDGALQGITSWGSDPCGRSDKPG VYTNICRYLDWIKKIIGSKG Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| 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: 2-Methyl-2-Propanol | Ligand Info | |||||
| Structure Description | Kallikrein-related peptidase 8 leupeptin inhibitor complex | PDB:5MS4 | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | No | [2] |
| PDB Sequence |
VLGGHECQPH
25 SQPWQAALFQ35 GQQLLCGGVL46 VGGNWVLTAA56 HCKKPKYTVR66 LGDHSLQNKD 77 GPEQEIPVVQ87 SIPHPCYNSS95B DVEDHNHDLM104 LLQLRDQASL114 GSKVKPISLA 124 DHCTQPGQKC136 TVSGWGTVTS146 PRENFPDTLN156 CAEVKIFPQK166 KCEDAYPGQI 176 TDGMVCAGSS186 KGADTCQGDS195 GGPLVCDGAL209 QGITSWGSDP219 CGRSDKPGVY 228 TNICRYLDWI238 KKIIGSKG
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| Ligand Name: amino{[(4S)-4-amino-5,5-dihydroxypentyl]amino}methaniminium | Ligand Info | |||||
| Structure Description | Kallikrein-related peptidase 8 leupeptin inhibitor complex | PDB:5MS4 | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | No | [2] |
| PDB Sequence |
VLGGHECQPH
25 SQPWQAALFQ35 GQQLLCGGVL46 VGGNWVLTAA56 HCKKPKYTVR66 LGDHSLQNKD 77 GPEQEIPVVQ87 SIPHPCYNSS95B DVEDHNHDLM104 LLQLRDQASL114 GSKVKPISLA 124 DHCTQPGQKC136 TVSGWGTVTS146 PRENFPDTLN156 CAEVKIFPQK166 KCEDAYPGQI 176 TDGMVCAGSS186 KGADTCQGDS195 GGPLVCDGAL209 QGITSWGSDP219 CGRSDKPGVY 228 TNICRYLDWI238 KKIIGSKG
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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 Similarity Proteins
Human Tissue Distribution
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There is no similarity protein (E value < 0.005) for this target
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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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| Chemical Structure based Activity Landscape of Target | Top |
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| References | Top | |||||
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| REF 1 | The human KLK8 (neuropsin/ovasin) gene: identification of two novel splice variants and its prognostic value in ovarian cancer. Clin Cancer Res. 2001 Apr;7(4):806-11. | |||||
| REF 2 | Structural determinants of specificity and regulation of activity in the allosteric loop network of human KLK8/neuropsin. Sci Rep. 2018 Jul 16;8(1):10705. | |||||
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