Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTLUQ8E)

• DTT Name: Hormone sensitive lipase (LIPE)
• Synonyms: Hormone-sensitive lipase; HSL
• Gene Name: LIPE
• DTT Type: Successful target; [1]
• BioChemical Class: Carboxylic ester hydrolase
• UniProt ID: LIPS_HUMAN
• TTD ID: T55689
• EC Number: EC 3.1.1.79
• Sequence:
  MEPGSKSVSRSDWQPEPHQRPITPLEPGPEKTPIAQPESKTLQGSNTQQKPASNQRPLTQ
  QETPAQHDAESQKEPRAQQKSASQEEFLAPQKPAPQQSPYIQRVLLTQQEAASQQGPGLG
  KESITQQEPALRQRHVAQPGPGPGEPPPAQQEAESTPAAQAKPGAKREPSAPTESTSQET
  PEQSDKQTTPVQGAKSKQGSLTELGFLTKLQELSIQRSALEWKALSEWVTDSESESDVGS
  SSDTDSPATMGGMVAQGVKLGFKGKSGYKVMSGYSGTSPHEKTSARNHRHYQDTASRLIH
  NMDLRTMTQSLVTLAEDNIAFFSSQGPGETAQRLSGVFAGVREQALGLEPALGRLLGVAH
  LFDLDPETPANGYRSLVHTARCCLAHLLHKSRYVASNRRSIFFRTSHNLAELEAYLAALT
  QLRALVYYAQRLLVTNRPGVLFFEGDEGLTADFLREYVTLHKGCFYGRCLGFQFTPAIRP
  FLQTISIGLVSFGEHYKRNETGLSVAASSLFTSGRFAIDPELRGAEFERITQNLDVHFWK
  AFWNITEMEVLSSLANMASATVRVSRLLSLPPEAFEMPLTADPTLTVTISPPLAHTGPGP
  VLVRLISYDLREGQDSEELSSLIKSNGQRSLELWPRPQQAPRSRSLIVHFHGGGFVAQTS
  RSHEPYLKSWAQELGAPIISIDYSLAPEAPFPRALEECFFAYCWAIKHCALLGSTGERIC
  LAGDSAGGNLCFTVALRAAAYGVRVPDGIMAAYPATMLQPAASPSRLLSLMDPLLPLSVL
  SKCVSAYAGAKTEDHSNSDQKALGMMGLVRRDTALLLRDFRLGASSWLNSFLELSGRKSQ
  KMSEPIAEPMRRSVSEAALAQPQGPLGTDSLKNLTLRDLSLRGNSETSSDTPEMSLSAET
  LSPSTPSDVNFLLPPEDAGEEAEAKNELSPMDRGLGVRAAFPEGFHPRRSSQGATQMPLY
  SSPIVKNPFMSPLLAPDSMLKSLPPVHIVACALDPMLDDSVMLARRLRNLGQPVTLRVVE
  DLPHGFLTLAALCRETRQAAELCVERIRLVLTPPAGAGPSGETGAAGVDGGCGGRH
• Function: In adipose tissue and heart, it primarily hydrolyzes stored triglycerides to free fatty acids, while in steroidogenic tissues, it principally converts cholesteryl esters to free cholesterol for steroid hormone production.
• KEGG Pathway:
  cAMP signaling pathway (hsa04024)
  AMPK signaling pathway (hsa04152)
  Insulin signaling pathway (hsa04910)
• Reactome Pathway: Hormone-sensitive lipase (HSL)-mediated triacylglycerol hydrolysis (R-HSA-163560)
• BioCyc Pathway: MetaCyc:HS01328-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BENZYL BENZOATE	DMDPYI5	Infestations of lice and scabies	1G00.Z	Approved	[1]

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID15026062C41	DMJGFLD	Pancreatitis	DC31-DC34	Clinical trial	[2]

7 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-(3-methoxybenzylthio)-2-phenylacetic acid	DM21MAU	Discovery agent	N.A.	Investigative	[3]
BIFENOX	DM4MUXT	Discovery agent	N.A.	Investigative	[3]
ETHIOFENCARB	DMQTEDP	Discovery agent	N.A.	Investigative	[3]
NCI-159878	DMTCBLS	Discovery agent	N.A.	Investigative	[3]
NCI-58425	DM9C7GP	Discovery agent	N.A.	Investigative	[3]
OXYBENZONE	DMMZYX6	Discovery agent	N.A.	Investigative	[3]
PMI-008	DMHX704	Obesity	5B81	Investigative	[4]

References

• [1] The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
• [2] Carbazates as potent inhibitors of hormone-sensitive lipase. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1741-4.
• [3] Combining ligand-based pharmacophore modeling, quantitative structure-activity relationship analysis and in silico screening for the discovery of n... J Med Chem. 2008 Oct 23;51(20):6478-94.
• [4] 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: 2593).