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

PTPN6 (P29350) - Overview - Molecular Target Synopsis

Protein


PTPN6, Tyrosine-protein phosphatase non-receptor type 6
Enzyme Classification 3.1.3.48
UniProt P29350

Also Known as PTN6_HUMAN, PTPN6, HCP, PTP1C

Modulates signaling by tyrosine phosphorylated cell surface receptors such as KIT and the EGF receptor/EGFR. The SH2 regions may interact with other cellular components to modulate its own phosphatase activity against interacting substrates. Together with MTUS1, induces UBE2V2 expression upon angiotensin II stimulation. Plays a key role in hematopoiesis. Monomer. Interacts with MTUS1 (By similarity). Interacts with MILR1 (tyrosine-phosphorylated) (By similarity). Interacts with KIT (By similarity). Interacts with SIRPA/PTPNS1 (PubMed:9712903). Interacts with LILRB1 and LILRB2 (PubMed:9285411, PubMed:9842885). Interacts with FCRL2 and FCRL4 (PubMed:11162587, PubMed:14597715). Interacts with FCRL3 and FCRL6 (tyrosine phosphorylated form) (PubMed:20933011, PubMed:11162587, PubMed:19843936). Interacts with CD84 (PubMed:11414741). Interacts with CD300LF (PubMed:15184070). Interacts with CDK2 (PubMed:21262353). Interacts with KIR2DL1; the interaction is enhanced by ARRB2 (PubMed:18604210). Interacts (via SH2 1 domain) with ROS1; the interaction is direct and promotes ROS1 dephosphorylation (PubMed:11266449). Interacts with EGFR; inhibits EGFR-dependent activation of MAPK/ERK (PubMed:21258366). Interacts with LYN (PubMed:10574931). Interacts with the tyrosine phosphorylated form of PDPK1 (PubMed:19591923). Interacts with CEACAM1 (via cytoplasmic domain); this interaction depends on the monomer/dimer equilibrium and is phosphorylation-dependent (By similarity). Interacts with MPIG6B (via ITIM motif) (PubMed:23112346).

4HJQ
SHP-1 CATALYTIC DOMAIN WPD LOOP CLOSED
RCSB/PDB
Inspect Structure
See all 3D Structures for PTPN6

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PTPN6 is active in the following subcellular-locations: cytoplasm, nucleus.
GO terms: PTPN6 is active in the following subcellular-locations: alpha-beta T cell receptor complex, cell-cell junction, cytoplasm, cytosol, extracellular exosome, extracellular region, membrane, nucleolus, nucleoplasm, nucleus, protein-containing complex, specific granule lumen, tertiary granule lumen.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PTPN6 has gain in 4 cell-lines, loss in 1 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, CCRF_CEM, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HEL, CCRF-SB, MV-4-11

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: CD20-positive B cell, CD14-positive monocyte, GM12878

(see details)

3D Structures


For PTPN6 there are:
12 structures (14 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PTPN6 has been screened with 456 compounds (552 bioactivities), 13 compounds have bioactivities that show binding affinity of <= 500nM (14 bioactivities). (see details)