Details of the Target

General Information of Target

Target ID LDTP04340
Target Name Ketohexokinase (KHK)
Gene Name KHK
Gene ID 3795
Synonyms
Ketohexokinase; EC 2.7.1.3; Hepatic fructokinase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEEKQILCVGLVVLDVISLVDKYPKEDSEIRCLSQRWQRGGNASNSCTVLSLLGAPCAFM
GSMAPGHVADFLVADFRRRGVDVSQVAWQSKGDTPSSCCIINNSNGNRTIVLHDTSLPDV
SATDFEKVDLTQFKWIHIEGRNASEQVKMLQRIDAHNTRQPPEQKIRVSVEVEKPREELF
QLFGYGDVVFVSKDVAKHLGFQSAEEALRGLYGRVRKGAVLVCAWAEEGADALGPDGKLL
HSDAFPPPRVVDTLGAGDTFNASVIFSLSQGRSVQEALRFGCQVAGKKCGLQGFDGIV
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Carbohydrate kinase PfkB family
Function Catalyzes the phosphorylation of the ketose sugar fructose to fructose-1-phosphate.
TTD ID
T79326
Uniprot ID
P50053
DrugMap ID
TTPAFR9
Ensemble ID
ENST00000260598.10
HGNC ID
HGNC:6315
ChEMBL ID
CHEMBL1275212

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.G290C .
NCIH2286 SNV: p.V170L .
NCIH716 SNV: p.L254M .
TKKK SNV: p.Q275R .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C282(2.87)  LDD2268  [1]
BTD
 Probe Info  		C282(1.03)  LDD2090  [2]
IPM
 Probe Info  		C282(2.11)  LDD1701  [2]
ATP probe
 Probe Info  		N.A.  LDD0199  [3]
TFBX
 Probe Info  		N.A.  LDD0027  [4]
WYneN
 Probe Info  		N.A.  LDD0021  [5]
NAIA_5
 Probe Info  		N.A.  LDD2223  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C282(0.43)  LDD2142  [2]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C282(0.53)  LDD2112  [2]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C282(1.38)  LDD1702  [2]
 LDCM0022  KB02 BRX211 C282(2.87)  LDD2268  [1]
 LDCM0023  KB03 MDA-MB-231 C282(2.11)  LDD1701  [2]
 LDCM0024  KB05 BRX211 C282(5.17)  LDD3102  [1]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C282(1.03)  LDD2090  [2]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C282(0.92)  LDD2097  [2]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C282(0.39)  LDD2100  [2]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C282(1.20)  LDD2105  [2]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C282(0.60)  LDD2108  [2]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C282(0.35)  LDD2114  [2]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C282(0.32)  LDD2115  [2]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C282(0.45)  LDD2118  [2]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C282(0.23)  LDD2122  [2]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C282(0.28)  LDD2124  [2]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C282(0.16)  LDD2126  [2]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C282(0.55)  LDD2133  [2]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C282(0.60)  LDD2141  [2]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C282(0.22)  LDD2145  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
LIM/homeobox protein Lhx2 (LHX2) . P50458
LIM/homeobox protein Lhx9 (LHX9) . Q9NQ69
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid protein-binding protein 2 (APPBP2) . Q92624

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 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
3 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
4 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
5 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
6 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