Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTOF3WZ)

• DTT Name: Lipoprotein lipase (LPL)
• Synonyms: LIPD
• Gene Name: LPL
• DTT Type: Successful target; [1]
• BioChemical Class: Carboxylic ester hydrolase
• UniProt ID: LIPL_HUMAN
• TTD ID: T28692
• EC Number: EC 3.1.1.34
• Sequence:
  MESKALLVLTLAVWLQSLTASRGGVAAADQRRDFIDIESKFALRTPEDTAEDTCHLIPGV
  AESVATCHFNHSSKTFMVIHGWTVTGMYESWVPKLVAALYKREPDSNVIVVDWLSRAQEH
  YPVSAGYTKLVGQDVARFINWMEEEFNYPLDNVHLLGYSLGAHAAGIAGSLTNKKVNRIT
  GLDPAGPNFEYAEAPSRLSPDDADFVDVLHTFTRGSPGRSIGIQKPVGHVDIYPNGGTFQ
  PGCNIGEAIRVIAERGLGDVDQLVKCSHERSIHLFIDSLLNEENPSKAYRCSSKEAFEKG
  LCLSCRKNRCNNLGYEINKVRAKRSSKMYLKTRSQMPYKVFHYQVKIHFSGTESETHTNQ
  AFEISLYGTVAESENIPFTLPEVSTNKTYSFLIYTEVDIGELLMLKLKWKSDSYFSWSDW
  WSSPGFAIQKIRVKAGETQKKVIFCSREKVSHLQKGKAPAVFVKCHDKSLNKKSG
• Function: Catalyzes the hydrolysis of triglycerides from circulating chylomicrons and very low density lipoproteins (VLDL), and thereby plays an important role in lipid clearance from the blood stream, lipid utilization and storage. Mediates margination of triglyceride-rich lipoprotein particles in capillaries. Recruited to its site of action on the luminal surface of vascular endothelium by binding to GPIHBP1 and cell surface heparan sulfate proteoglycans. Key enzyme in triglyceride metabolism.
• KEGG Pathway:
  Glycerolipid metabolism (hsa00561)
  PPAR signaling pathway (hsa03320)
  Alzheimer's disease (hsa05010)
• Reactome Pathway:
  Transcriptional regulation of white adipocyte differentiation (R-HSA-381340)
  Retinoid metabolism and transport (R-HSA-975634)
  Chylomicron-mediated lipid transport (R-HSA-174800)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Clofibrate	DMPC1J7	Dysbetalipoproteinemia	5C80.2	Approved	[1]
Gemfibrozil	DMD8Q3J	Hyperlipidaemia	5C80	Approved	[2]

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AMT-011	DM8QIRN	Blood forming organ disorder	JB64.1	Phase 3	[3]
Ibrolipim	DMOPWSX	Hyperlipidaemia	5C80	Phase 2	[4]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
WS-070117	DMYNIG5	Hyperlipidaemia	5C80	Investigative	[3]

References

• [1] Effects of clofibrate treatment in laying hens. Poult Sci. 2007 Jun;86(6):1187-95.
• [2] Mode of action of fibrates in the regulation of triglyceride and HDL-cholesterol metabolism. Drugs Today (Barc). 2006 Jan;42(1):39-64.
• [3] Alipogene tiparvovec for the treatment of lipoprotein lipase deficiency. Drugs Today (Barc). 2013 Mar;49(3):161-70.
• [4] NO-1886 (ibrolipim), a lipoprotein lipase activator, increases the expression of uncoupling protein 3 in skeletal muscle and suppresses fat accumulation in high-fat diet-induced obesity in rats. Metabolism. 2005 Dec;54(12):1587-92.