General Information of Target

Target ID LDTP02581
Target Name Cholesteryl ester transfer protein (CETP)
Gene Name CETP
Gene ID 1071
Synonyms
Cholesteryl ester transfer protein; Lipid transfer protein I
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLAATVLTLALLGNAHACSKGTSHEAGIVCRITKPALLVLNHETAKVIQTAFQRASYPDI
TGEKAMMLLGQVKYGLHNIQISHLSIASSQVELVEAKSIDVSIQNVSVVFKGTLKYGYTT
AWWLGIDQSIDFEIDSAIDLQINTQLTCDSGRVRTDAPDCYLSFHKLLLHLQGEREPGWI
KQLFTNFISFTLKLVLKGQICKEINVISNIMADFVQTRAASILSDGDIGVDISLTGDPVI
TASYLESHHKGHFIYKNVSEDLPLPTFSPTLLGDSRMLYFWFSERVFHSLAKVAFQDGRL
MLSLMGDEFKAVLETWGFNTNQEIFQEVVGGFPSQAQVTVHCLKMPKISCQNKGVVVNSS
VMVKFLFPRPDQQHSVAYTFEEDIVTTVQASYSKKKLFLSLLDFQITPKTVSNLTESSSE
SVQSFLQSMITAVGIPEVMSRLEVVFTALMNSKGVSLFDIINPEIITRDGFLLLQMDFGF
PEHLLVDFLQSLS
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
BPI/LBP/Plunc superfamily, BPI/LBP family
Subcellular location
Secreted
Function
Involved in the transfer of neutral lipids, including cholesteryl ester and triglyceride, among lipoprotein particles. Allows the net movement of cholesteryl ester from high density lipoproteins/HDL to triglyceride-rich very low density lipoproteins/VLDL, and the equimolar transport of triglyceride from VLDL to HDL. Regulates the reverse cholesterol transport, by which excess cholesterol is removed from peripheral tissues and returned to the liver for elimination.
TTD ID
T15334
Uniprot ID
P11597
DrugMap ID
TTFQAYR
Ensemble ID
ENST00000200676.8
HGNC ID
HGNC:1869
ChEMBL ID
CHEMBL3572

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO792 SNV: p.S440F .
MCC13 SNV: p.G173E; p.L401F .
MFE319 SNV: p.L302F .
NCIH1944 SNV: p.V361A .
TOV21G Deletion: p.F488SfsTer5 .

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
BTD
 Probe Info 
C350(5.48)  LDD1699  [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
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C350(1.21)  LDD2126  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Anacetrapib Small molecular drug D07HLS
Dalcetrapib Small molecular drug D05SSC
Evacetrapib Small molecular drug D02XXN
Phase 2
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Drl-17822 . D07UJA
Jtt-302 . D04ZBU
Ta-8995 . D0G7MM
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bay-60-5521 . D00JQE
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bay-38-1315 Small molecular drug D05QXT
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nsc-40331 Small molecular drug D0M1TF
Nsc-89508 Small molecular drug D05TQP
Sc-795 Small molecular drug D04WPM
Tetrahydroquinoline A Small molecular drug D04VCE
Tetrahydroquinoline B Small molecular drug D0C9FK
Discontinued
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cp-800569 Small molecular drug D03MAD
Torcetrapib Small molecular drug D07GDN
Ceti-1 Vaccine D0J4KC
Ds-1442 . D0F8XI
Pf-3185043 . D0K3GU
R7232 . D0B0UN

References

1 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
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