Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

PTPN1 (P18031) - Overview - Molecular Target Synopsis

Protein


PTPN1, Tyrosine-protein phosphatase non-receptor type 1
Enzyme Classification 3.1.3.48
UniProt P18031

Also Known as PTN1_HUMAN, PTPN1, PTP1B

Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response. Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion. May also regulate the hepatocyte growth factor receptor signaling pathway through dephosphorylation of MET. Interacts with EPHA3 (phosphorylated); dephosphorylates EPHA3 and may regulate its trafficking and function. Interacts with MET.

1OEO
PTP1B WITH THE CATALYTIC CYSTEINE OXIDIZED TO SULFONIC ACID
RCSB/PDB
Inspect Structure
See all 3D Structures for PTPN1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
435ENSG00000196396ENST00000371621ENSP00000360683P18031-1
362ENSG00000196396ENST00000541713ENSP00000437732

Sub-cellular localization


UniProt: PTPN1 is active in the following subcellular-locations: endoplasmic reticulum membrane.
GO terms: PTPN1 is active in the following subcellular-locations: cytoplasmic side of endoplasmic reticulum membrane, cytosol, early endosome, endoplasmic reticulum, protein-containing complex, sorting endosome.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PTPN1 has gain in 19 cell-lines, loss in 0 cell-lines and no signal in 986 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H226, UACC_62, UACC_257

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC2911, MKN-74, TMD8

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HMEC, SK-N-SH, HSMM

(see details)

3D Structures


For PTPN1 there are:
273 structures (289 chains) solved
229 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PTPN1 has been screened with 4611 compounds (6920 bioactivities), 510 compounds have bioactivities that show binding affinity of <= 500nM (668 bioactivities). (see details)