Details of the Target

General Information of Target

Target ID LDTP00190
Target Name Thymidine kinase 2, mitochondrial (TK2)
Gene Name TK2
Gene ID 7084
Synonyms
Thymidine kinase 2, mitochondrial; EC 2.7.1.21; 2'-deoxyuridine kinase TK2; EC 2.7.1.74; Deoxycytidine kinase TK2; EC 2.7.1.-; Mt-TK
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLLWPLRGWAARALRCFGPGSRGSPASGPGPRRVQRRAWPPDKEQEKEKKSVICVEGNIA
SGKTTCLEFFSNATDVEVLTEPVSKWRNVRGHNPLGLMYHDASRWGLTLQTYVQLTMLDR
HTRPQVSSVRLMERSIHSARYIFVENLYRSGKMPEVDYVVLSEWFDWILRNMDVSVDLIV
YLRTNPETCYQRLKKRCREEEKVIPLEYLEAIHHLHEEWLIKGSLFPMAAPVLVIEADHH
MERMLELFEQNRDRILTPENRKHCP
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
DCK/DGK family
Subcellular location
Mitochondrion
Function
Phosphorylates thymidine, deoxycytidine, and deoxyuridine in the mitochondrial matrix. In non-replicating cells, where cytosolic dNTP synthesis is down-regulated, mtDNA synthesis depends solely on TK2 and DGUOK. Widely used as target of antiviral and chemotherapeutic agents.
TTD ID
T22976
Uniprot ID
O00142
DrugMap ID
TT7KNZQ
Ensemble ID
ENST00000417693.8
HGNC ID
HGNC:11831
ChEMBL ID
CHEMBL4580

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 SNV: p.L2P DBIA    Probe Info 
KYSE410 SNV: p.P31A .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		N.A.  LDD0241  [1]
DBIA
 Probe Info  		C92(1.63)  LDD3313  [2]
BTD
 Probe Info  		C189(0.79)  LDD2137  [3]
IA-alkyne
 Probe Info  		C54(0.00); C189(0.00)  LDD0036  [4]
TFBX
 Probe Info  		N.A.  LDD0027  [5]
OSF
 Probe Info  		N.A.  LDD0029  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0226  AC11 HEK-293T C189(1.05)  LDD1509  [7]
 LDCM0278  AC19 HEK-293T C189(0.79)  LDD1517  [7]
 LDCM0287  AC27 HEK-293T C189(0.81)  LDD1526  [7]
 LDCM0290  AC3 HEK-293T C189(0.96)  LDD1529  [7]
 LDCM0296  AC35 HEK-293T C189(0.87)  LDD1535  [7]
 LDCM0305  AC43 HEK-293T C189(0.98)  LDD1544  [7]
 LDCM0314  AC51 HEK-293T C189(0.67)  LDD1553  [7]
 LDCM0322  AC59 HEK-293T C189(1.30)  LDD1561  [7]
 LDCM0369  CL100 HEK-293T C16(0.78)  LDD1573  [7]
 LDCM0373  CL104 HEK-293T C16(0.96)  LDD1577  [7]
 LDCM0377  CL108 HEK-293T C16(0.98)  LDD1581  [7]
 LDCM0382  CL112 HEK-293T C16(0.98)  LDD1586  [7]
 LDCM0386  CL116 HEK-293T C16(0.91)  LDD1590  [7]
 LDCM0391  CL120 HEK-293T C16(0.90)  LDD1595  [7]
 LDCM0395  CL124 HEK-293T C16(0.95)  LDD1599  [7]
 LDCM0399  CL128 HEK-293T C16(0.83)  LDD1603  [7]
 LDCM0403  CL16 HEK-293T C16(1.03)  LDD1607  [7]
 LDCM0406  CL19 HEK-293T C189(0.87)  LDD1610  [7]
 LDCM0416  CL28 HEK-293T C16(1.08)  LDD1620  [7]
 LDCM0420  CL31 HEK-293T C189(1.03)  LDD1624  [7]
 LDCM0429  CL4 HEK-293T C16(0.91)  LDD1633  [7]
 LDCM0430  CL40 HEK-293T C16(1.05)  LDD1634  [7]
 LDCM0433  CL43 HEK-293T C189(0.93)  LDD1637  [7]
 LDCM0443  CL52 HEK-293T C16(1.04)  LDD1646  [7]
 LDCM0446  CL55 HEK-293T C189(0.92)  LDD1649  [7]
 LDCM0456  CL64 HEK-293T C16(1.08)  LDD1659  [7]
 LDCM0459  CL67 HEK-293T C189(1.39)  LDD1662  [7]
 LDCM0462  CL7 HEK-293T C189(0.69)  LDD1665  [7]
 LDCM0469  CL76 HEK-293T C16(1.00)  LDD1672  [7]
 LDCM0472  CL79 HEK-293T C189(1.53)  LDD1675  [7]
 LDCM0482  CL88 HEK-293T C16(0.84)  LDD1685  [7]
 LDCM0486  CL91 HEK-293T C189(1.01)  LDD1689  [7]
 LDCM0022  KB02 8305C C92(1.95)  LDD2248  [2]
 LDCM0023  KB03 8305C C92(2.26)  LDD2665  [2]
 LDCM0024  KB05 Hs 936.T C92(1.63)  LDD3313  [2]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C189(0.79)  LDD2137  [3]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Brivudine Small molecular drug DB03312
Gemcitabine Small molecular drug DB00441
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mt-1621 Deoxynucleoside DI4SM3
Investigative
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1-[(Z)-4-(Triphenylmethoxy)-2-butenyl]Thymine Small molecular drug D0I6UV
1-[5-(Triphenylmethoxy)Pentyl]Thymine Small molecular drug D00KWL
1-[6-(Triphenylmethoxy)Hexyl]Thymine Small molecular drug D02CCD
2'-deoxycytidine Small molecular drug DB02594
Thymidine Small molecular drug DB04485
Thymidine 5'-triphosphate Small molecular drug DB02452

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
2 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
3 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
4 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
5 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
6 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
7 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402