Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTGZ91P)

• DTT Name: Lecithin-cholesterol acyltransferase (LCAT)
• Synonyms: Phospholipidcholesterolacyltransferase; Phospholipid-cholesterol acyltransferase; Phosphatidylcholinesterol acyltransferase; Phosphatidylcholine-sterol acyltransferase
• Gene Name: LCAT
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Acyltransferase
• UniProt ID: LCAT_HUMAN
• TTD ID: T05661
• EC Number: EC 2.3.1.43
• Sequence:
  MGPPGSPWQWVTLLLGLLLPPAAPFWLLNVLFPPHTTPKAELSNHTRPVILVPGCLGNQL
  EAKLDKPDVVNWMCYRKTEDFFTIWLDLNMFLPLGVDCWIDNTRVVYNRSSGLVSNAPGV
  QIRVPGFGKTYSVEYLDSSKLAGYLHTLVQNLVNNGYVRDETVRAAPYDWRLEPGQQEEY
  YRKLAGLVEEMHAAYGKPVFLIGHSLGCLHLLYFLLRQPQAWKDRFIDGFISLGAPWGGS
  IKPMLVLASGDNQGIPIMSSIKLKEEQRITTTSPWMFPSRMAWPEDHVFISTPSFNYTGR
  DFQRFFADLHFEEGWYMWLQSRDLLAGLPAPGVEVYCLYGVGLPTPRTYIYDHGFPYTDP
  VGVLYEDGDDTVATRSTELCGLWQGRQPQPVHLLPLHGIQHLNMVFSNLTLEHINAILLG
  AYRQGPPASPTASPEPPPPE
• Function: Synthesized mainly in the liver and secreted into plasma where it converts cholesterol and phosphatidylcholines (lecithins) to cholesteryl esters and lysophosphatidylcholines on the surface of high and low density lipoproteins (HDLs and LDLs). The cholesterol ester is then transported back to the liver. Has a preference for plasma 16:0-18:2 or 18:O-18:2 phosphatidylcholines. Also produced in the brain by primary astrocytes, and esterifies free cholesterol on nascent APOE-containing lipoproteins secreted from glia and influences cerebral spinal fluid (CSF) APOE- and APOA1 levels. Together with APOE and the cholesterol transporter ABCA1, plays a key role in the maturation of glial-derived, nascent lipoproteins. Required for remodeling high-density lipoprotein particles into their spherical forms. Central enzyme in the extracellular metabolism of plasma lipoproteins.
• KEGG Pathway: Glycerophospholipid metabolism (hsa00564)
• Reactome Pathway: HDL-mediated lipid transport (R-HSA-194223)

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
MEDI6012	DMU4CS8	Coronary artery disease	BA80	Phase 2	[1]

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

• DTT DME Name: Lecithin-cholesterol acyltransferase (LCAT) DME Info
• Gene Name: LCAT

1 Investigative Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Phosphatidylcholine	DMY2RVX	N. A.	N. A.	Investigative	[2]

References

• [1] Familial lecithin-cholesterol acyltransferase (LCAT) deficiency; a differential of proteinuria. J Nephropathol. 2015 January; 4(1): 25-28.
• [2] Characterization of lecithin:cholesterol acyltransferase expressed in a human lung cell line. Protein Expr Purif. 2004 Aug;36(2):157-64.