Target Information
| Target General Information | Top | |||||
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| Target ID |
T85328
(Former ID: TTDI00240)
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| Target Name |
Protein tyrosine phosphatase IVA 1 (PRL-1)
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| Synonyms |
Protein-tyrosine phosphatase of regenerating liver 1; Protein-tyrosine phosphatase 4a1; Protein tyrosine phosphatase type IVA 1; PTPCAAX1; PTP(CAAXI); PRL1
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| Gene Name |
PTP4A1
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
May play a role in the development and maintenance of differentiating epithelial tissues. Enhances cell proliferation, cell motility and invasive activity, and promotes cancer metastasis. Protein tyrosine phosphatase which stimulates progression from G1 into S phase during mitosis.
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| BioChemical Class |
Phosphoric monoester hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.1.3.48
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| Sequence |
MARMNRPAPVEVTYKNMRFLITHNPTNATLNKFIEELKKYGVTTIVRVCEATYDTTLVEK
EGIHVLDWPFDDGAPPSNQIVDDWLSLVKIKFREEPGCCIAVHCVAGLGRAPVLVALALI EGGMKYEDAVQFIRQKRRGAFNSKQLLYLEKYRPKMRLRFKDSNGHRNNCCIQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T03XRZ | |||||
| 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: 3-(5,6-dimethylisoindol-2-yl)-N-[(E)-furan-2-ylmethylideneamino]benzamide | Ligand Info | |||||
| Structure Description | Crystal Structure of PRL-1 complex with compound analogy 3 | PDB:5BX1 | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [2] |
| PDB Sequence |
APVEVTYKNM
17 RFLITHNPTN27 ATLNKFIEEL37 KKYGVTTIVR47 VCEATYDTTL57 VEKEGIHVLD 67 WPFDDGAPPS77 NQIVDDWLSL87 VKIKFREEPG97 CCIAVHCVAG107 LGRAPVLVAL 117 ALIEGGMKYE127 DAVQFIRQKR137 RGAFNSKQLL147 YLEKYRPKMR157 LRF |
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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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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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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| References | Top | |||||
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| REF 1 | Protein tyrosine phosphatase PTP4A1 promotes proliferation and epithelial-mesenchymal transition in intrahepatic cholangiocarcinoma via the PI3K/AK... Oncotarget. 2016 Nov 15;7(46):75210-75220. | |||||
| REF 2 | Crystal Structure of PRL-1 complex with compound analogy 3 | |||||
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