Details of the Target

General Information of Target

Target ID LDTP06625
Target Name Guanylate kinase (GUK1)
Gene Name GUK1
Gene ID 2987
Synonyms
GMK; GMPK; Guanylate kinase; EC 2.7.4.8; GMP kinase; Guanylate kinase 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSGPRPVVLSGPSGAGKSTLLKRLLQEHSGIFGFSVSHTTRNPRPGEENGKDYYFVTREV
MQRDIAAGDFIEHAEFSGNLYGTSKVAVQAVQAMNRICVLDVDLQGVRNIKATDLRPIYI
SVQPPSLHVLEQRLRQRNTETEESLVKRLAAAQADMESSKEPGLFDVVIINDSLDQAYAE
LKEALSEEIKKAQRTGA
Target Bioclass
Enzyme
Family
Guanylate kinase family
Subcellular location
Photoreceptor inner segment
Function
Catalyzes the phosphorylation of GMP to GDP. Essential enzyme for recycling GMP and indirectly, cyclic GMP (cGMP). Involved in the cGMP metabolism in photoreceptors. It may also have a role in the survival and growth progression of some tumors. In addition to its physiological role, GUK1 is essential for convert prodrugs used for the treatment of cancers and viral infections into their pharmacologically active metabolites, most notably acyclovir, ganciclovir, and 6-thioguanine and its closely related analog 6-mercaptopurine.
Uniprot ID
Q16774
Ensemble ID
ENST00000366728.6
HGNC ID
HGNC:4693
ChEMBL ID
CHEMBL4989

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 17 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
TH211
 Probe Info  		Y53(12.91)  LDD0260  [1]
Probe 1
 Probe Info  		Y81(12.21)  LDD3495  [2]
DBIA
 Probe Info  		C98(2.52)  LDD3312  [3]
HHS-475
 Probe Info  		Y81(1.52)  LDD0264  [4]
HHS-465
 Probe Info  		Y81(10.00)  LDD2237  [5]
Acrolein
 Probe Info  		N.A.  LDD0227  [6]
5E-2FA
 Probe Info  		H128(0.00); H28(0.00)  LDD2235  [7]
m-APA
 Probe Info  		H128(0.00); H28(0.00)  LDD2231  [7]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [8]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [9]
IPIAA_H
 Probe Info  		N.A.  LDD0030  [10]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [10]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [8]
IPM
 Probe Info  		N.A.  LDD0025  [11]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [11]
TFBX
 Probe Info  		N.A.  LDD0027  [11]
SF
 Probe Info  		N.A.  LDD0028  [12]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C98(0.90)  LDD1508  [13]
 LDCM0277  AC18 HEK-293T C98(0.99)  LDD1516  [13]
 LDCM0279  AC2 HEK-293T C98(1.00)  LDD1518  [13]
 LDCM0286  AC26 HEK-293T C98(1.04)  LDD1525  [13]
 LDCM0295  AC34 HEK-293T C98(0.90)  LDD1534  [13]
 LDCM0304  AC42 HEK-293T C98(0.96)  LDD1543  [13]
 LDCM0313  AC50 HEK-293T C98(0.96)  LDD1552  [13]
 LDCM0321  AC58 HEK-293T C98(1.00)  LDD1560  [13]
 LDCM0371  CL102 HEK-293T C98(0.87)  LDD1575  [13]
 LDCM0375  CL106 HEK-293T C98(0.91)  LDD1579  [13]
 LDCM0380  CL110 HEK-293T C98(0.87)  LDD1584  [13]
 LDCM0384  CL114 HEK-293T C98(0.79)  LDD1588  [13]
 LDCM0388  CL118 HEK-293T C98(1.11)  LDD1592  [13]
 LDCM0393  CL122 HEK-293T C98(0.99)  LDD1597  [13]
 LDCM0397  CL126 HEK-293T C98(0.89)  LDD1601  [13]
 LDCM0401  CL14 HEK-293T C98(0.86)  LDD1605  [13]
 LDCM0405  CL18 HEK-293T C98(0.89)  LDD1609  [13]
 LDCM0407  CL2 HEK-293T C98(0.85)  LDD1611  [13]
 LDCM0414  CL26 HEK-293T C98(1.11)  LDD1618  [13]
 LDCM0419  CL30 HEK-293T C98(0.94)  LDD1623  [13]
 LDCM0432  CL42 HEK-293T C98(1.06)  LDD1636  [13]
 LDCM0441  CL50 HEK-293T C98(0.75)  LDD1645  [13]
 LDCM0445  CL54 HEK-293T C98(1.07)  LDD1648  [13]
 LDCM0451  CL6 HEK-293T C98(0.97)  LDD1654  [13]
 LDCM0454  CL62 HEK-293T C98(1.02)  LDD1657  [13]
 LDCM0458  CL66 HEK-293T C98(1.08)  LDD1661  [13]
 LDCM0467  CL74 HEK-293T C98(0.92)  LDD1670  [13]
 LDCM0471  CL78 HEK-293T C98(1.11)  LDD1674  [13]
 LDCM0480  CL86 HEK-293T C98(0.95)  LDD1683  [13]
 LDCM0485  CL90 HEK-293T C98(1.03)  LDD1688  [13]
 LDCM0493  CL98 HEK-293T C98(0.95)  LDD1696  [13]
 LDCM0427  Fragment51 HEK-293T C98(0.88)  LDD1631  [13]
 LDCM0116  HHS-0101 DM93 Y81(1.52)  LDD0264  [4]
 LDCM0117  HHS-0201 DM93 Y81(1.43)  LDD0265  [4]
 LDCM0118  HHS-0301 DM93 Y81(0.46)  LDD0266  [4]
 LDCM0119  HHS-0401 DM93 Y81(1.92)  LDD0267  [4]
 LDCM0120  HHS-0701 DM93 Y81(4.56)  LDD0268  [4]
 LDCM0022  KB02 HEK-293T C98(0.95)  LDD1492  [13]
 LDCM0023  KB03 HEK-293T C98(0.91)  LDD1497  [13]
 LDCM0024  KB05 HMCB C98(2.52)  LDD3312  [3]
 LDCM0109  NEM HeLa N.A.  LDD0227  [6]

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
Acyclovir Small molecular drug DB00787
Valaciclovir Small molecular drug DB00577
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Guanosine-5'-monophosphate Small molecular drug DB01972

References

1 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
2 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
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 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
5 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
6 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.
7 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
8 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
9 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
10 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
11 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
12 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
13 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