Details of the Target

General Information of Target

Target ID LDTP03552
Target Name Pyruvate kinase PKLR (PKLR)
Gene Name PKLR
Gene ID 5313
Synonyms
PK1; PKL; Pyruvate kinase PKLR; EC 2.7.1.40; Pyruvate kinase 1; Pyruvate kinase isozymes L/R; R-type/L-type pyruvate kinase; Red cell/liver pyruvate kinase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSIQENISSLQLRSWVSKSQRDLAKSILIGAPGGPAGYLRRASVAQLTQELGTAFFQQQQ
LPAAMADTFLEHLCLLDIDSEPVAARSTSIIATIGPASRSVERLKEMIKAGMNIARLNFS
HGSHEYHAESIANVREAVESFAGSPLSYRPVAIALDTKGPEIRTGILQGGPESEVELVKG
SQVLVTVDPAFRTRGNANTVWVDYPNIVRVVPVGGRIYIDDGLISLVVQKIGPEGLVTQV
ENGGVLGSRKGVNLPGAQVDLPGLSEQDVRDLRFGVEHGVDIVFASFVRKASDVAAVRAA
LGPEGHGIKIISKIENHEGVKRFDEILEVSDGIMVARGDLGIEIPAEKVFLAQKMMIGRC
NLAGKPVVCATQMLESMITKPRPTRAETSDVANAVLDGADCIMLSGETAKGNFPVEAVKM
QHAIAREAEAAVYHRQLFEELRRAAPLSRDPTEVTAIGAVEAAFKCCAAAIIVLTTTGRS
AQLLSRYRPRAAVIAVTRSAQAARQVHLCRGVFPLLYREPPEAIWADDVDRRVQFGIESG
KLRGFLRVGDLVIVVTGWRPGSGYTNIMRVLSIS
Target Type
Successful
Target Bioclass
Enzyme
Family
Pyruvate kinase family
Function Pyruvate kinase that catalyzes the conversion of phosphoenolpyruvate to pyruvate with the synthesis of ATP, and which plays a key role in glycolysis.
TTD ID
T63155
Uniprot ID
P30613
DrugMap ID
TT31N4S
Ensemble ID
ENST00000342741.6
HGNC ID
HGNC:9020
ChEMBL ID
CHEMBL1075126

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AU565 Substitution: p.E106K .
CHL1 SNV: p.G232S .
HT29 SNV: p.K179N .
JURKAT SNV: p.V187M .
KYM1 SNV: p.G95W .
SW1783 SNV: p.V228I .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-EBA
 Probe Info  		3.40  LDD0215  [1]
STPyne
 Probe Info  		K354(15.73)  LDD2217  [2]
DBIA
 Probe Info  		C509(1.24)  LDD3443  [3]
HPAP
 Probe Info  		3.38  LDD0063  [4]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [5]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [5]
IPM
 Probe Info  		N.A.  LDD2156  [6]
NAIA_5
 Probe Info  		N.A.  LDD2223  [7]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe11
 Probe Info  		8.41  LDD0472  [8]
FFF probe13
 Probe Info  		18.06  LDD0476  [8]
FFF probe3
 Probe Info  		12.23  LDD0465  [8]
STS-1
 Probe Info  		N.A.  LDD0068  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 Hep 3B2.1-7 C509(1.65)  LDD2353  [3]
 LDCM0023  KB03 Hep 3B2.1-7 C509(3.83)  LDD2770  [3]
 LDCM0024  KB05 SNU-449 C509(1.24)  LDD3443  [3]
 LDCM0014  Panhematin K562 3.38  LDD0063  [4]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acyclovir Small molecular drug DB00787
Pyruvic Acid Small molecular drug DB00119
Mitapivat . DB16236
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2-phosphoglycolic Acid Small molecular drug DB02726
Beta-d-fructofuranose 16-bisphosphate . DB04551

References

1 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
2 Global profiling of lysine reactivity and ligandability in the human proteome. Nat Chem. 2017 Dec;9(12):1181-1190. doi: 10.1038/nchem.2826. Epub 2017 Jul 31.
3 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
4 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
5 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
6 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
7 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
8 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
9 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.