General Information of Target

Target ID LDTP14177
Target Name Endothelial lipase (LIPG)
Gene Name LIPG
Gene ID 9388
Synonyms
Endothelial lipase; EC 3.1.1.3; Endothelial cell-derived lipase; EDL; EL; Phospholipase A1; EC 3.1.1.32
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNSFFGTPAASWCLLESDVSSAPDKEAGRERRALSVQQRGGPAWSGSLEWSRQSAGDRRR
LGLSRQTAKSSWSRSRDRTCCCRRAWWILVPAADRARRERFIMNEKWDTNSSENWHPIWN
VNDTKHHLYSDINITYVNYYLHQPQVAAIFIISYFLIFFLCMMGNTVVCFIVMRNKHMHT
VTNLFILNLAISDLLVGIFCMPITLLDNIIAGWPFGNTMCKISGLVQGISVAASVFTLVA
IAVDRFQCVVYPFKPKLTIKTAFVIIMIIWVLAITIMSPSAVMLHVQEEKYYRVRLNSQN
KTSPVYWCREDWPNQEMRKIYTTVLFANIYLAPLSLIVIMYGRIGISLFRAAVPHTGRKN
QEQWHVVSRKKQKIIKMLLIVALLFILSWLPLWTLMMLSDYADLSPNELQIINIYIYPFA
HWLAFGNSSVNPIIYGFFNENFRRGFQEAFQLQLCQKRAKPMEAYALKAKSHVLINTSNQ
LVQESTFQNPHGETLLYRKSAEKPQQELVMEELKETTNSSEI
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
AB hydrolase superfamily, Lipase family
Subcellular location
Secreted
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.
TTD ID
T19368
Uniprot ID
Q9Y5X9
DrugMap ID
TTHSZXO
Ensemble ID
ENST00000261292.9
HGNC ID
HGNC:6623
ChEMBL ID
CHEMBL5080

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 Insertion: p.I307DfsTer11 .
HCT15 SNV: p.D211Y .
HDMYZ SNV: p.M1? .
KP4 SNV: p.V182M .
MFE319 Deletion: p.L126WfsTer40 .
SUPT1 SNV: p.R448H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C316(2.48)  LDD3493  [1]
NAIA_4
 Probe Info 
N.A.  LDD2226  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 CAL-51 C316(2.91); C463(2.27)  LDD2288  [1]
 LDCM0023  KB03 CAL-51 C316(4.75); C463(2.92)  LDD2705  [1]
 LDCM0024  KB05 ZR-75-1 C316(2.48)  LDD3493  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264