Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTS8T1M)

DTT Name	Lysosomal acid lipase (LIPA)
Synonyms	Sterol esterase; Lysosomal acid lipase/cholesteryl ester hydrolase; Lipase A; LIPA; LAL; Cholesteryl esterase; Acid cholesteryl ester hydrolase
Gene Name	LIPA
DTT Type	Successful target	[1]
BioChemical Class	Carboxylic ester hydrolase
UniProt ID	LICH_HUMAN
TTD ID	T24373
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
EC Number	EC 3.1.1.13
Sequence	MKMRFLGLVVCLVLWTLHSEGSGGKLTAVDPETNMNVSEIISYWGFPSEEYLVETEDGYI LCLNRIPHGRKNHSDKGPKPVVFLQHGLLADSSNWVTNLANSSLGFILADAGFDVWMGNS RGNTWSRKHKTLSVSQDEFWAFSYDEMAKYDLPASINFILNKTGQEQVYYVGHSQGTTIG FIAFSQIPELAKRIKMFFALGPVASVAFCTSPMAKLGRLPDHLIKDLFGDKEFLPQSAFL KWLGTHVCTHVILKELCGNLCFLLCGFNERNLNMSRVDVYTTHSPAGTSVQNMLHWSQAV KFQKFQAFDWGSSAKNYFHYNQSYPPTYNVKDMLVPTAVWSGGHDWLADVYDVNILLTQI TNLVFHESIPEWEHLDFIWGLDAPWRLYNKIINLMRKYQ
Function	Crucial for the intracellular hydrolysis of cholesteryl esters and triglycerides that have been internalized via receptor- mediated endocytosis of lipoprotein particles. Important in mediating the effect of LDL (low density lipoprotein) uptake on suppression of hydroxymethylglutaryl-CoA reductase and activation of endogenous cellular cholesteryl ester formation.
KEGG Pathway	Steroid biosynthesis (hsa00100 ) Lysosome (hsa04142 )
Reactome Pathway	LDL clearance (R-HSA-8964038 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

Jump to Detail Molecular Interaction Atlas of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SBC-102	DMDK7T9	Enzyme deficiency	5C51-5C57	Approved	[1]
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The Drug-Metabolizing Enzyme (DME) Role of This DTT

DTT DME Name

Acid cholesteryl ester hydrolase (LIPA) DME Info

Gene Name

LIPA

1 Clinical Trial Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Carfentanil	DM7ADGX	N. A.	N. A.	Phase 2	[2]
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References

1	A Phase 3 Trial of Sebelipase Alfa in Lysosomal Acid Lipase Deficiency. N Engl J Med. 2015 Sep 10;373(11):1010-20.
2	Metabolism of carfentanil, an ultra-potent opioid, in human liver microsomes and human hepatocytes by high-resolution mass spectrometry. AAPS J. 2016 Nov;18(6):1489-1499.