General Information of Target

Target ID LDTP05986
Target Name Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 (ENPP2)
Gene Name ENPP2
Gene ID 5168
Synonyms
ATX; PDNP2; Ectonucleotide pyrophosphatase/phosphodiesterase family member 2; E-NPP 2; EC 3.1.4.39; Autotaxin; Extracellular lysophospholipase D; LysoPLD
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MARRSSFQSCQIISLFTFAVGVNICLGFTAHRIKRAEGWEEGPPTVLSDSPWTNISGSCK
GRCFELQEAGPPDCRCDNLCKSYTSCCHDFDELCLKTARGWECTKDRCGEVRNEENACHC
SEDCLARGDCCTNYQVVCKGESHWVDDDCEEIKAAECPAGFVRPPLIIFSVDGFRASYMK
KGSKVMPNIEKLRSCGTHSPYMRPVYPTKTFPNLYTLATGLYPESHGIVGNSMYDPVFDA
TFHLRGREKFNHRWWGGQPLWITATKQGVKAGTFFWSVVIPHERRILTILQWLTLPDHER
PSVYAFYSEQPDFSGHKYGPFGPEMTNPLREIDKIVGQLMDGLKQLKLHRCVNVIFVGDH
GMEDVTCDRTEFLSNYLTNVDDITLVPGTLGRIRSKFSNNAKYDPKAIIANLTCKKPDQH
FKPYLKQHLPKRLHYANNRRIEDIHLLVERRWHVARKPLDVYKKPSGKCFFQGDHGFDNK
VNSMQTVFVGYGSTFKYKTKVPPFENIELYNVMCDLLGLKPAPNNGTHGSLNHLLRTNTF
RPTMPEEVTRPNYPGIMYLQSDFDLGCTCDDKVEPKNKLDELNKRLHTKGSTEERHLLYG
RPAVLYRTRYDILYHTDFESGYSEIFLMPLWTSYTVSKQAEVSSVPDHLTSCVRPDVRVS
PSFSQNCLAYKNDKQMSYGFLFPPYLSSSPEAKYDAFLVTNMVPMYPAFKRVWNYFQRVL
VKKYASERNGVNVISGPIFDYDYDGLHDTEDKIKQYVEGSSIPVPTHYYSIITSCLDFTQ
PADKCDGPLSVSSFILPHRPDNEESCNSSEDESKWVEELMKMHTARVRDIEHLTSLDFFR
KTSRSYPEILTLKTYLHTYESEI
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Nucleotide pyrophosphatase/phosphodiesterase family
Subcellular location
Secreted
Function
Hydrolyzes lysophospholipids to produce the signaling molecule lysophosphatidic acid (LPA) in extracellular fluids. Major substrate is lysophosphatidylcholine. Can also act on sphingosylphosphorylcholine producing sphingosine-1-phosphate, a modulator of cell motility. Can hydrolyze, in vitro, bis-pNPP, to some extent pNP-TMP, and barely ATP. Involved in several motility-related processes such as angiogenesis and neurite outgrowth. Acts as an angiogenic factor by stimulating migration of smooth muscle cells and microtubule formation. Stimulates migration of melanoma cells, probably via a pertussis toxin-sensitive G protein. May have a role in induction of parturition. Possible involvement in cell proliferation and adipose tissue development (Probable). Tumor cell motility-stimulating factor. Required for LPA production in activated platelets, cleaves the sn-1 lysophospholipids to generate sn-1 lysophosphatidic acids containing predominantly 18:2 and 20:4 fatty acids. Shows a preference for the sn-1 to the sn-2 isomer of 1-O-alkyl-sn-glycero-3-phosphocholine (lyso-PAF).
TTD ID
T63512
Uniprot ID
Q13822
DrugMap ID
TTSCIM2
Ensemble ID
ENST00000075322.11
HGNC ID
HGNC:3357
ChEMBL ID
CHEMBL3691

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.G182S DBIA    Probe Info 
ABC1 SNV: p.Q310L DBIA    Probe Info 
HCT15 SNV: p.R369G DBIA    Probe Info 
HT115 SNV: p.E110K DBIA    Probe Info 
KYM1 SNV: p.M820I DBIA    Probe Info 
KYSE410 SNV: p.F16L DBIA    Probe Info 
LS180 SNV: p.W713Ter DBIA    Probe Info 
NCIH2286 SNV: p.D474E DBIA    Probe Info 
NCIH2291 SNV: p.Q11Ter .
SW403 SNV: p.P763H DBIA    Probe Info 
TE8 SNV: p.D404Y DBIA    Probe Info 
VMRCRCW SNV: p.T208I DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C466(1.52)  LDD3314  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 22RV1 C466(1.38)  LDD2243  [1]
 LDCM0023  KB03 22RV1 C466(1.95)  LDD2660  [1]
 LDCM0024  KB05 IGR37 C466(1.52)  LDD3314  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840