Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTHEE942)

• DOT Name: Endothelial lipase (LIPG)
• Synonyms: EC 3.1.1.3; Endothelial cell-derived lipase; EDL; EL; Phospholipase A1; EC 3.1.1.32
• Gene Name: LIPG
• UniProt ID: LIPG_HUMAN
• EC Number: 3.1.1.3; 3.1.1.32
• Pfam ID: PF00151 ; PF01477
• Sequence:
  MSNSVPLLCFWSLCYCFAAGSPVPFGPEGRLEDKLHKPKATQTEVKPSVRFNLRTSKDPE
  HEGCYLSVGHSQPLEDCSFNMTAKTFFIIHGWTMSGIFENWLHKLVSALHTREKDANVVV
  VDWLPLAHQLYTDAVNNTRVVGHSIARMLDWLQEKDDFSLGNVHLIGYSLGAHVAGYAGN
  FVKGTVGRITGLDPAGPMFEGADIHKRLSPDDADFVDVLHTYTRSFGLSIGIQMPVGHID
  IYPNGGDFQPGCGLNDVLGSIAYGTITEVVKCEHERAVHLFVDSLVNQDKPSFAFQCTDS
  NRFKKGICLSCRKNRCNSIGYNAKKMRNKRNSKMYLKTRAGMPFRVYHYQMKIHVFSYKN
  MGEIEPTFYVTLYGTNADSQTLPLEIVERIEQNATNTFLVYTEEDLGDLLKIQLTWEGAS
  QSWYNLWKEFRSYLSQPRNPGRELNIRRIRVKSGETQRKLTFCTEDPENTSISPGRELWF
  RKCRDGWRMKNETSPTVELP
• Function: Exerts both phospholipase and triglyceride lipase activities. More active as a phospholipase than a triglyceride lipase. Hydrolyzes triglycerides, both with short-chain fatty acyl groups (tributyrin) and long-chain fatty acyl groups (triolein) with similar levels of activity toward both types of substrates. Hydrolyzes high density lipoproteins (HDL) more efficiently than other lipoproteins.
• Tissue Specificity: High level of expression in the liver, placenta, lung, thyroid, kidney, testis and in the corpus luteum of the ovary. Expressed also in coronary artery endothelial cells, umbilical vein endothelial cells and in hepatocytes and osteosarcoma cell lines. Not detected in heart, brain and muscle.
• KEGG Pathway:
  Glycerolipid metabolism (hsa00561)
  Metabolic pathways (hsa01100)
  Cholesterol metabolism (hsa04979)
• Reactome Pathway: HDL remodeling (R-HSA-8964058)

Molecular Interaction Atlas (MIA) of This DOT

This DOT Affected the Drug Response of 1 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Mitoxantrone	DMM39BF	Approved	Endothelial lipase (LIPG) affects the response to substance of Mitoxantrone.	[25]

25 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the expression of Endothelial lipase (LIPG).	[1]
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Endothelial lipase (LIPG).	[2]
Acetaminophen	DMUIE76	Approved	Acetaminophen decreases the expression of Endothelial lipase (LIPG).	[3]
Doxorubicin	DMVP5YE	Approved	Doxorubicin affects the expression of Endothelial lipase (LIPG).	[4]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate increases the expression of Endothelial lipase (LIPG).	[5]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Endothelial lipase (LIPG).	[2]
Quercetin	DM3NC4M	Approved	Quercetin decreases the expression of Endothelial lipase (LIPG).	[6]
Calcitriol	DM8ZVJ7	Approved	Calcitriol increases the expression of Endothelial lipase (LIPG).	[7]
Vorinostat	DMWMPD4	Approved	Vorinostat decreases the expression of Endothelial lipase (LIPG).	[8]
Zoledronate	DMIXC7G	Approved	Zoledronate increases the expression of Endothelial lipase (LIPG).	[9]
Progesterone	DMUY35B	Approved	Progesterone increases the expression of Endothelial lipase (LIPG).	[10]
Niclosamide	DMJAGXQ	Approved	Niclosamide decreases the expression of Endothelial lipase (LIPG).	[11]
Hydroquinone	DM6AVR4	Approved	Hydroquinone increases the expression of Endothelial lipase (LIPG).	[12]
Rosiglitazone	DMILWZR	Approved	Rosiglitazone decreases the expression of Endothelial lipase (LIPG).	[13]
Ethanol	DMDRQZU	Approved	Ethanol increases the expression of Endothelial lipase (LIPG).	[14]
Urethane	DM7NSI0	Phase 4	Urethane increases the expression of Endothelial lipase (LIPG).	[15]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of Endothelial lipase (LIPG).	[17]
Leflunomide	DMR8ONJ	Phase 1 Trial	Leflunomide increases the expression of Endothelial lipase (LIPG).	[18]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 increases the expression of Endothelial lipase (LIPG).	[19]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Endothelial lipase (LIPG).	[20]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde increases the expression of Endothelial lipase (LIPG).	[21]
Milchsaure	DM462BT	Investigative	Milchsaure increases the expression of Endothelial lipase (LIPG).	[22]
OXYQUINOLINE	DMZVS9Y	Investigative	OXYQUINOLINE decreases the expression of Endothelial lipase (LIPG).	[6]
Resorcinol	DMM37C0	Investigative	Resorcinol increases the expression of Endothelial lipase (LIPG).	[23]
T0901317	DMZQVDI	Investigative	T0901317 increases the expression of Endothelial lipase (LIPG).	[24]

1 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the methylation of Endothelial lipase (LIPG).	[16]

References

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