Protein tyrosine phosphatases non-receptor type (PTPN)

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Class I classical (Cys-based) phosphatases
Protein tyrosine phosphatases non-receptor type (PTPN)

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Protein tyrosine phosphatases (PTPs) catalyse the hydrolysis of phosphate monoesters on tyrosine residues, in opposition to tyrosine kinase-catalysed phosphorylation.
The HGNC lists 17 members in the 'Protein tyrosine phosphatases, non-receptor type (PTPN)' family (ID 812).

Enzymes

Targets of relevance to immunopharmacology are highlighted in blue

PTP1B (protein tyrosine phosphatase non-receptor type 1) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2976

Nomenclature

protein tyrosine phosphatase non-receptor type 1

Common abbreviation

PTP1B

Previous and unofficial names

protein tyrosine phosphatase | protein tyrosine phosphatase, non-receptor type 1 | PTP1B

Genes

PTPN1 (Hs), Ptpn1 (Mm), Ptpn1 (Rn)

Ensembl ID

ENSG00000196396 (Hs), ENSMUSG00000027540 (Mm), ENSRNOG00000010574 (Rn)

UniProtKB AC

P18031 (Hs), P35821 (Mm), P20417 (Rn)

EC number

3.1.3.48
Dephosphorylates O-phosphotyrosine groups in phosphoproteins. Protein tyrosine phosphate + H₂O <=> protein tyrosine + phosphate

Inhibitors

compound 182 [PMID: 37500611] pK_i 9.5 [3]

compound 182 [PMID: 37500611] pIC₅₀ 9.2 [3]

Comment

Participates in regulating the JAK-Stat pathway, and T cell receptor and cytokine signalling. Inhibition of PTPN1/2 promotes anti-tumour immunity [1,3,7].

protein tyrosine phosphatase non-receptor type 2 Show summary »« Hide summary

Target Id

3255

Nomenclature

protein tyrosine phosphatase non-receptor type 2

Previous and unofficial names

PTPT | TC-PTP | TCPTP | T-cell protein-tyrosine phosphatase

Genes

PTPN2 (Hs), Ptpn2 (Mm), Ptpn2 (Rn)

Ensembl ID

ENSG00000175354 (Hs), ENSMUSG00000024539 (Mm)

UniProtKB AC

P17706 (Hs), Q06180 (Mm)

EC number

3.1.3.48

Inhibitors

compound 182 [PMID: 37500611] pK_i 9.6 [3]

compound 182 [PMID: 37500611] pIC₅₀ 9.2 [3]

Comment

Participates in regulating the JAK-Stat pathway, and T cell receptor and cytokine signalling. Inhibition of PTPN1/2 promotes anti-tumour immunity [1,3,7].

SHP2 (protein tyrosine phosphatase non-receptor type 11) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

3203

Nomenclature

protein tyrosine phosphatase non-receptor type 11

Common abbreviation

SHP2

Previous and unofficial names

Noonan syndrome 1 (NS1) | SH2 domain-containing protein tyrosine phosphatase 2 | SHP-2 | src homology region 2 domain phosphatase | Src homology-2 domain-containing phosphatase Shp2

Genes

PTPN11 (Hs)

Ensembl ID

ENSG00000179295 (Hs)

UniProtKB AC

Q06124 (Hs)

EC number

3.1.3.48

Comment

PTPN11 (also known as SHP2) is a cytosolic protein-tyrosine phosphatase. It is an important convergent node that activates multiple RAS signalling pathways in human diseases, and it is an active molecular target for cancer therapy development [4-5].

LYP (protein tyrosine phosphatase non-receptor type 22 / PTPN22) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

3084

Nomenclature

protein tyrosine phosphatase non-receptor type 22

Systematic nomenclature

PTPN22

Common abbreviation

LYP

Previous and unofficial names

Genes

PTPN22 (Hs), Ptpn22 (Mm), Ptpn22 (Rn)

Ensembl ID

ENSG00000134242 (Hs), ENSMUSG00000027843 (Mm), ENSRNOG00000019614 (Rn)

UniProtKB AC

Q9Y2R2 (Hs), P29352 (Mm)

EC number

3.1.3.48
H2O + O-phospho-L-tyrosyl-[protein] = L-tyrosyl-[protein] + phosphate [6]

References

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1. Baumgartner CK, Ebrahimi-Nik H, Iracheta-Vellve A, Hamel KM, Olander KE, Davis TGR, McGuire KA, Halvorsen GT, Avila OI, Patel CH et al.. (2023) The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity. Nature, 622 (7984): 850-862. [PMID:37794185]

2. Cohen S, Dadi H, Shaoul E, Sharfe N, Roifman CM. (1999) Cloning and characterization of a lymphoid-specific, inducible human protein tyrosine phosphatase, Lyp. Blood, 93 (6): 2013-24. [PMID:10068674]

3. Liang S, Tran E, Du X, Dong J, Sudholz H, Chen H, Qu Z, Huntington ND, Babon JJ, Kershaw NJ et al.. (2023) A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity. Nat Commun, 14 (1): 4524. [PMID:37500611]

4. Nagasaka M, Azmi AS. (2022) Clinical progress of KRAS-targeted therapies: what next?. Future Med Chem, 14 (15): 1107-1110. [PMID:35758004]

5. Song Z, Wang M, Ge Y, Chen XP, Xu Z, Sun Y, Xiong XF. (2021) Tyrosine phosphatase SHP2 inhibitors in tumor-targeted therapies. Acta Pharm Sin B, 11 (1): 13-29. [PMID:33532178]

6. Yu X, Chen M, Zhang S, Yu ZH, Sun JP, Wang L, Liu S, Imasaki T, Takagi Y, Zhang ZY. (2011) Substrate specificity of lymphoid-specific tyrosine phosphatase (Lyp) and identification of Src kinase-associated protein of 55 kDa homolog (SKAP-HOM) as a Lyp substrate. J Biol Chem, 286 (35): 30526-34. [PMID:21719704]

7. (2023) A Dual PTPN2/PTPN1 Active-Site Inhibitor Promotes Antitumor Immunity. Cancer Discov,: OF1 [Epub ahead of print]. [PMID:37861299]

How to cite this family page

Database page citation:

Protein tyrosine phosphatases non-receptor type (PTPN). Accessed on 27/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=980.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.