Details of the Target

General Information of Target

Target ID LDTP02168
Target Name Lipoprotein lipase (LPL)
Gene Name LPL
Gene ID 4023
Synonyms
LIPD; Lipoprotein lipase; LPL; EC 3.1.1.34; 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
MESKALLVLTLAVWLQSLTASRGGVAAADQRRDFIDIESKFALRTPEDTAEDTCHLIPGV
AESVATCHFNHSSKTFMVIHGWTVTGMYESWVPKLVAALYKREPDSNVIVVDWLSRAQEH
YPVSAGYTKLVGQDVARFINWMEEEFNYPLDNVHLLGYSLGAHAAGIAGSLTNKKVNRIT
GLDPAGPNFEYAEAPSRLSPDDADFVDVLHTFTRGSPGRSIGIQKPVGHVDIYPNGGTFQ
PGCNIGEAIRVIAERGLGDVDQLVKCSHERSIHLFIDSLLNEENPSKAYRCSSKEAFEKG
LCLSCRKNRCNNLGYEINKVRAKRSSKMYLKTRSQMPYKVFHYQVKIHFSGTESETHTNQ
AFEISLYGTVAESENIPFTLPEVSTNKTYSFLIYTEVDIGELLMLKLKWKSDSYFSWSDW
WSSPGFAIQKIRVKAGETQKKVIFCSREKVSHLQKGKAPAVFVKCHDKSLNKKSG
Target Type
Successful
Target Bioclass
Enzyme
Family
AB hydrolase superfamily, Lipase family
Subcellular location
Cell membrane
Function
Key enzyme in triglyceride metabolism. 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. Although it has both phospholipase and triglyceride lipase activities it is primarily a triglyceride lipase with low but detectable phospholipase activity. 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.
TTD ID
T28692
Uniprot ID
P06858
DrugMap ID
TTOF3WZ
Ensemble ID
ENST00000650287.1
HGNC ID
HGNC:6677
ChEMBL ID
CHEMBL2060

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
OPA-S-S-alkyne
 Probe Info  		K129(1.65); K265(1.86)  LDD3494  [1]
TFBX
 Probe Info  		N.A.  LDD0027  [2]
DBIA
 Probe Info  		C243(0.44); C310(0.39)  LDD2236  [3]
Acrolein
 Probe Info  		N.A.  LDD0217  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [4]
 LDCM0107  IAA HeLa N.A.  LDD0221  [4]
 LDCM0022  KB02 MGG123 C310(1.90)  LDD2469  [5]
 LDCM0023  KB03 MGG123 C310(2.00)  LDD2886  [5]
 LDCM0024  KB05 MGG123 C310(2.23)  LDD3303  [5]
 LDCM0109  NEM HeLa H210(0.00); H120(0.00)  LDD0223  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein arginine N-methyltransferase 5 (PRMT5) Protein arginine N-methyltransferase family O14744
Nucleoside diphosphate kinase, mitochondrial (NME4) NDK family O00746
26S proteasome non-ATPase regulatory subunit 9 (PSMD9) Proteasome subunit p27 family O00233
Ribonuclease SLFN12 (SLFN12) Schlafen family Q8IYM2
Vitamin K epoxide reductase complex subunit 1-like protein 1 (VKORC1L1) VKOR family Q8N0U8
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Sorting nexin-12 (SNX12) Sorting nexin family Q9UMY4
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Translation initiation factor eIF2B subunit delta (EIF2B4) EIF-2B alpha/beta/delta subunits family Q9UI10
Transmembrane protein 185A (TMEM185A) TMEM185 family Q8NFB2
Glycosylphosphatidylinositol-anchored high density lipoprotein-binding protein 1 (GPIHBP1) . Q8IV16

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Clofibrate Small molecular drug D0J5DC
Gemfibrozil Small molecular drug D05VIX
Semaglutide Small molecular drug DB13928
Tyloxapol Small molecular drug DB06439
Glycyrrhizic Acid . DB13751
Omega-3-carboxylic Acids . DB09568
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amt-011 . D01RNV
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ibrolipim Small molecular drug D0SA3J
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ws-070117 . D0OH9B

References

1 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
2 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
3 Global profiling of phosphorylation-dependent changes in cysteine reactivity. Nat Methods. 2022 Mar;19(3):341-352. doi: 10.1038/s41592-022-01398-2. Epub 2022 Feb 28.
Mass spectrometry data entry: PXD026730
4 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
5 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