Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTSCIM2)

• DTT Name: Extracellular lysophospholipase D (E-NPP2)
• Synonyms: LysoPLD; Ectonucleotide pyrophosphatase/phosphodiesterase family member 2; E-NPP 2; Autotaxin; ATX
• Gene Name: ENPP2
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: Phosphoric diester hydrolase
• UniProt ID: ENPP2_HUMAN
• TTD ID: T63512
• EC Number: EC 3.1.4.39
• Sequence:
  MARRSSFQSCQIISLFTFAVGVNICLGFTAHRIKRAEGWEEGPPTVLSDSPWTNISGSCK
  GRCFELQEAGPPDCRCDNLCKSYTSCCHDFDELCLKTARGWECTKDRCGEVRNEENACHC
  SEDCLARGDCCTNYQVVCKGESHWVDDDCEEIKAAECPAGFVRPPLIIFSVDGFRASYMK
  KGSKVMPNIEKLRSCGTHSPYMRPVYPTKTFPNLYTLATGLYPESHGIVGNSMYDPVFDA
  TFHLRGREKFNHRWWGGQPLWITATKQGVKAGTFFWSVVIPHERRILTILQWLTLPDHER
  PSVYAFYSEQPDFSGHKYGPFGPEMTNPLREIDKIVGQLMDGLKQLKLHRCVNVIFVGDH
  GMEDVTCDRTEFLSNYLTNVDDITLVPGTLGRIRSKFSNNAKYDPKAIIANLTCKKPDQH
  FKPYLKQHLPKRLHYANNRRIEDIHLLVERRWHVARKPLDVYKKPSGKCFFQGDHGFDNK
  VNSMQTVFVGYGSTFKYKTKVPPFENIELYNVMCDLLGLKPAPNNGTHGSLNHLLRTNTF
  RPTMPEEVTRPNYPGIMYLQSDFDLGCTCDDKVEPKNKLDELNKRLHTKGSTEERHLLYG
  RPAVLYRTRYDILYHTDFESGYSEIFLMPLWTSYTVSKQAEVSSVPDHLTSCVRPDVRVS
  PSFSQNCLAYKNDKQMSYGFLFPPYLSSSPEAKYDAFLVTNMVPMYPAFKRVWNYFQRVL
  VKKYASERNGVNVISGPIFDYDYDGLHDTEDKIKQYVEGSSIPVPTHYYSIITSCLDFTQ
  PADKCDGPLSVSSFILPHRPDNEESCNSSEDESKWVEELMKMHTARVRDIEHLTSLDFFR
  KTSRSYPEILTLKTYLHTYESEI
• Function: Hydrolyzes lysophospholipids to produce the signaling molecule lysophosphatidic acid (LPA) in extracellular fluids. Major substrate is lysophosphatidylcholine. Also can 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.
• KEGG Pathway: Ether lipid metabolism (hsa00565)
• Reactome Pathway: Vitamin B5 (pantothenate) metabolism (R-HSA-199220)
• BioCyc Pathway: MetaCyc:HS06258-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cudetaxestat	DMYLDN9	Idiopathic pulmonary fibrosis	CB03.4	Phase 2	[2]

26 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Complex heterocyclic compound 1	DMWYJF6	Inflammation	1A00-CA43.1	Patented	[1]
Dihydropyrido pyrimidine derivative 1	DMSTC9Z	N. A.	N. A.	Patented	[1]
Heteroaromatic ring derivative 1	DMI732U	N. A.	N. A.	Patented	[1]
Heteroaromatic ring derivative 2	DM5YD4W	N. A.	N. A.	Patented	[1]
Heteroaromatic ring derivative 3	DMKJL5T	N. A.	N. A.	Patented	[1]
Heteroaromatic ring derivative 4	DM9IL5Q	N. A.	N. A.	Patented	[1]
Imidazopyrimidinone derivative 1	DMWN17V	N. A.	N. A.	Patented	[1]
Octahydro-pyrrolo[3,4-c]-pyrrole derivative 1	DM0ECWR	N. A.	N. A.	Patented	[1]
Piperazine derivative 8	DM1XUVB	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-10	DMA7OEF	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-11	DMOYMWZ	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-14	DMA91X2	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-20	DMWSL5G	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-21	DM8PET6	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-22	DMRCM1O	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-23	DMM0BVE	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-24	DMDOVIZ	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-26	DMJZSWF	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-27	DMVZPIO	N. A.	N. A.	Patented	[1]
PMID28447479-Compound-4	DMUBM1Y	N. A.	N. A.	Patented	[1]
Pyrazole derivative 87	DMGZUAY	N. A.	N. A.	Patented	[1]
Pyrazolo[3,4-c]pyridine derivative 1	DMQHCDZ	N. A.	N. A.	Patented	[1]
Pyridine and pyrimidine derivative 1	DMGEYJW	Fibrosis	GA14-GC01	Patented	[1]
Pyrimidinone derivative 5	DMLFY57	N. A.	N. A.	Patented	[1]
Tetra-hydro-carboline derivative 1	DM5MVLG	N. A.	N. A.	Patented	[1]
Tetra-hydro-carboline derivative 2	DMXTL7V	N. A.	N. A.	Patented	[1]

References

• [1] Autotaxin inhibitors: a patent review (2012-2016).Expert Opin Ther Pat. 2017 Jul;27(7):815-829.
• [2] An updated patent review of autotaxin inhibitors (2017-present). Expert Opin Ther Pat. 2021 May;31(5):421-434.