phosphatase and tensin homolog
Target id: 2497
Nomenclature: phosphatase and tensin homolog
Abbreviated Name: PTEN
Family: Lipid phosphate phosphatases
Contents:
Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | - | 403 | 10q23.31 | PTEN | phosphatase and tensin homolog | |
| Mouse | - | 403 | 19 28.14 cM | Pten | phosphatase and tensin homolog | |
| Rat | - | 403 | 1q41-q43 | Pten | phosphatase and tensin homolog | |
| Previous and Unofficial Names |
| BZS | MMAC1 | mutated in multiple advanced cancers 1 | TEP1 |
| Database Links |
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| Alphafold | P60484 (Hs), O08586 (Mm) |
| BRENDA | 3.1.3.16, 3.1.3.48, 3.1.3.67 |
| CATH/Gene3D | 3.90.190.10 |
| ChEMBL Target | CHEMBL2052032 (Hs) |
| Ensembl Gene | ENSG00000171862 (Hs), ENSMUSG00000013663 (Mm), ENSRNOG00000020723 (Rn) |
| Entrez Gene | 5728 (Hs), 19211 (Mm), 50557 (Rn) |
| Human Protein Atlas | ENSG00000171862 (Hs) |
| KEGG Enzyme | 3.1.3.16, 3.1.3.48, 3.1.3.67 |
| KEGG Gene | hsa:5728 (Hs), mmu:19211 (Mm), rno:50557 (Rn) |
| OMIM | 601728 (Hs) |
| Pharos | P60484 (Hs) |
| RefSeq Nucleotide | NM_000314 (Hs), NM_008960 (Mm), NM_031606 (Rn) |
| RefSeq Protein | NP_000305 (Hs), NP_032986 (Mm), NP_113794 (Rn) |
| UniProtKB | P60484 (Hs), O08586 (Mm) |
| Wikipedia | PTEN (Hs) |
| Enzyme Reaction |
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| Substrates and Reaction Kinetics |
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Download all structure-activity data for this target as a CSV file 
| Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||
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| Immunopharmacology Comments |
| Accumulating evidence suggests that loss-of-function mutations or deletion of PTEN is an immune evasion mechanism exploited by tumour cells [5], and that disrupted PTEN activity may have implications for resistance to T cell-mediated immunotherapy (checkpoint blockade) [2,4]. |
| Immuno Process Associations | ||
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| Phenotypes, Alleles and Disease Models
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Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||
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| General Comments |
| PTEN's phosphatase activity dephosphorylates phosphatidylinositol (3,4,5)-trisphosphate (PtdIns (3,4,5)P3 or PIP3) to PIP2 (which leads to inhibition of the AKT signaling pathway), and it also appears to have some protein phosphatase activity. PTEN acts as a tumour suppressor. Inactivation of PTEN expression (by mutation or deletion) is one of the most common oncogenic pathways identified in human cancers. PTEN mutations have also been identified in non-cancerous neoplasia (e.g. hamartomas) [3,6-7]. |
References
1. Mak LH, Knott J, Scott KA, Scott C, Whyte GF, Ye Y, Mann DJ, Ces O, Stivers J, Woscholski R. (2012) Arylstibonic acids are potent and isoform-selective inhibitors of Cdc25a and Cdc25b phosphatases. Bioorg Med Chem, 20 (14): 4371-6. [PMID:22705189]
2. Peng W, Chen JQ, Liu C, Malu S, Creasy C, Tetzlaff MT, Xu C, McKenzie JA, Zhang C, Liang X et al.. (2016) Loss of PTEN Promotes Resistance to T Cell-Mediated Immunotherapy. Cancer Discov, 6 (2): 202-16. [PMID:26645196]
3. Pilarski R, Eng C. (2004) Will the real Cowden syndrome please stand up (again)? Expanding mutational and clinical spectra of the PTEN hamartoma tumour syndrome. J Med Genet, 41 (5): 323-6. [PMID:15121767]
4. Roh W, Chen PL, Reuben A, Spencer CN, Prieto PA, Miller JP, Gopalakrishnan V, Wang F, Cooper ZA, Reddy SM et al.. (2017) Integrated molecular analysis of tumor biopsies on sequential CTLA-4 and PD-1 blockade reveals markers of response and resistance. Sci Transl Med, 9 (379). [PMID:28251903]
5. Spranger S, Gajewski TF. (2018) Impact of oncogenic pathways on evasion of antitumour immune responses. Nat Rev Cancer, 18 (3): 139-147. [PMID:29326431]
6. Uemura S, Matsubayashi H, Kiyozumi Y, Uesaka K, Yamamoto Y, Sasaki K, Abe M, Urakami K, Kusuhara M, Yamaguchi K. (2018) Pancreatic adenocarcinoma with a germline PTEN p.Arg234Gln mutation. Fam Cancer, 17 (2): 255-259. [PMID:28755079]
7. Yakubov E, Ghoochani A, Buslei R, Buchfelder M, Eyüpoglu IY, Savaskan N. (2016) Hidden association of Cowden syndrome, PTEN mutation and meningioma frequency. Oncoscience, 3 (5-6): 149-55. [PMID:27489861]
How to cite this page
Lipid phosphate phosphatases: phosphatase and tensin homolog. Last modified on 10/07/2018. Accessed on 11/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2497.
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