Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Bile-salt-activated lipase (CEL)
• Synonyms: Pancreatic lysophospholipase; Pancreatic cholesterol esterase; Cholesterol esterase; Carboxyl ester lipase; CEL; Bile-salt-stimulated lipase; BSSL; BAL
• Gene Name: CEL
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Carboxylic ester hydrolase
• UniProt ID: CEL_HUMAN
• TTD ID: T39677
• EC Number: EC 3.1.1.13
• Sequence:
  MGRLQLVVLGLTCCWAVASAAKLGAVYTEGGFVEGVNKKLGLLGDSVDIFKGIPFAAPTK
  ALENPQPHPGWQGTLKAKNFKKRCLQATITQDSTYGDEDCLYLNIWVPQGRKQVSRDLPV
  MIWIYGGAFLMGSGHGANFLNNYLYDGEEIATRGNVIVVTFNYRVGPLGFLSTGDANLPG
  NYGLRDQHMAIAWVKRNIAAFGGDPNNITLFGESAGGASVSLQTLSPYNKGLIRRAISQS
  GVALSPWVIQKNPLFWAKKVAEKVGCPVGDAARMAQCLKVTDPRALTLAYKVPLAGLEYP
  MLHYVGFVPVIDGDFIPADPINLYANAADIDYIAGTNNMDGHIFASIDMPAINKGNKKVT
  EEDFYKLVSEFTITKGLRGAKTTFDVYTESWAQDPSQENKKKTVVDFETDVLFLVPTEIA
  LAQHRANAKSAKTYAYLFSHPSRMPVYPKWVGADHADDIQYVFGKPFATPTGYRPQDRTV
  SKAMIAYWTNFAKTGDPNMGDSAVPTHWEPYTTENSGYLEITKKMGSSSMKRSLRTNFLR
  YWTLTYLALPTVTDQEATPVPPTGDSEATPVPPTGDSETAPVPPTGDSGAPPVPPTGDSG
  APPVPPTGDSGAPPVPPTGDSGAPPVPPTGDSGAPPVPPTGDSGAPPVPPTGDSGAPPVP
  PTGDSGAPPVPPTGDAGPPPVPPTGDSGAPPVPPTGDSGAPPVTPTGDSETAPVPPTGDS
  GAPPVPPTGDSEAAPVPPTDDSKEAQMPAVIRF
• Function: Catalyzes fat and vitamin absorption. Acts in concert with pancreatic lipase and colipase for the complete digestion of dietary triglycerides.
• Reactome Pathway: Digestion of dietary lipid (R-HSA-192456)

Molecular Interaction Atlas (MIA) of This DTT

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bucelipase alfa	DM50SNX	Exocrine pancreatic insufficiency	DC35.1	Phase 3	[1]
Taurocholic Acid	DM2LZ8F	Type-2 diabetes	5A11	Phase 1/2	[2]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CVT-1	DMPWZCI	Hypercholesterolaemia	5C80.0	Terminated	[3]

3 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID24556381C10f	DMK6GAU	Discovery agent	N.A.	Investigative	[4]
PMID24556381C10l	DMOH45T	Discovery agent	N.A.	Investigative	[4]
TgBSSL	DMBFX7S	Pancreatic malfunction	DC30-DC3Z	Investigative	[5]

The Drug-Metabolizing Enzyme (DME) Role of This DTT

• DTT DME Name: Carboxyl ester lipase (CEL) DME Info
• Gene Name: CEL

1 Approved Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Triacetin	DM0AEPG	Onychomycosis	EE12.1	Approved	[6]

References

• [1] ClinicalTrials.gov (NCT00743483) Efficacy of Bucelipase Alfa (BSSL) in Patients With Cystic Fibrosis and Pancreatic Insufficiency. U.S. National Institutes of Health.
• [2] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [3] Lack of effect of cholesterol esterase inhibitor CVT-1 on cholesterol absorption and LDL cholesterol in humans. Cardiovasc Drugs Ther. 1999 Sep;13(5):449-54.
• [4] Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1545-9.
• [5] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2872).
• [6] Lipoamidase activity in normal and mutagenized pancreatic cholesterol esterase (bile salt-stimulated lipase). Biochem J. 1993 Apr 1;291 ( Pt 1):65-9.