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

ENPP1 (P22413) - Overview - Molecular Target Synopsis

Protein


ENPP1, Ectonucleotide pyrophosphatase/phosphodiesterase family member 1
Enzyme Classification 3.1.4.1
UniProt P22413

Also Known as ENPP1_HUMAN, ENPP1, M6S1, NPPS, PC1, PDNP1

By generating PPi, plays a role in regulating pyrophosphate levels, and functions in bone mineralization and soft tissue calcification. PPi inhibits mineralization by binding to nascent hydroxyapatite (HA) crystals, thereby preventing further growth of these crystals. Preferentially hydrolyzes ATP, but can also hydrolyze other nucleoside 5' triphosphates such as GTP, CTP, TTP and UTP to their corresponding monophosphates with release of pyrophosphate and diadenosine polyphosphates, and also 3',5'-cAMP to AMP. May also be involved in the regulation of the availability of nucleotide sugars in the endoplasmic reticulum and Golgi, and the regulation of purinergic signaling. Appears to modulate insulin sensitivity and function. The secreted form is monomeric (By similarity). Homodimer. Interacts with INSR.

2YS0
SOLUTION STRUCTURE OF THE SOMATOMEDIN B DOMAIN OF HUMAN ECTONUCLEOTIDE PYROPHOSPHATASE/PHOSPHODIESTERASE FAMILY MEMBER
RCSB/PDB
Inspect Structure
See all 3D Structures for ENPP1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
925ENSG00000197594ENST00000360971ENSP00000354238P22413-1
378ENSG00000197594ENST00000513998ENSP00000422424

Sub-cellular localization


UniProt: ENPP1 is active in the following subcellular-locations: basolateral cell membrane, cell membrane, secreted.
GO terms: ENPP1 is active in the following subcellular-locations: basolateral plasma membrane, cell surface, extracellular space, integral component of membrane, integral component of plasma membrane, lysosomal membrane, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ENPP1 has gain in 0 cell-lines, loss in 3 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MDA_MB_231, SF_539, SK_MEL_28

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hep G2, Hs 839.T, RERF-LC-OK

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: NHLF, HSMM, AG445

(see details)

3D Structures


For ENPP1 there are:
1 structures (1 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ENPP1 has been screened with 150 compounds (330 bioactivities), 19 compounds have bioactivities that show binding affinity of <= 500nM (33 bioactivities). (see details)