Details of the Target

General Information of Target

Target ID LDTP11228
Target Name MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1)
Gene Name MKNK1
Gene ID 8569
Synonyms
MNK1; MAP kinase-interacting serine/threonine-protein kinase 1; EC 2.7.11.1; MAP kinase signal-integrating kinase 1; MAPK signal-integrating kinase 1; Mnk1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MWTADEIAQLCYEHYGIRLPKKGKPEPNHEWTLLAAVVKIQSPADKACDTPDKPVQVTKE
VVSMGTGTKCIGQSKMRKNGDILNDSHAEVIARRSFQRYLLHQLQLAATLKEDSIFVPGT
QKGVWKLRRDLIFVFFSSHTPCGDASIIPMLEFEDQPCCPVFRNWAHNSSVEASSNLEAP
GNERKCEDPDSPVTKKMRLEPGTAAREVTNGAAHHQSFGKQKSGPISPGIHSCDLTVEGL
ATVTRIAPGSAKVIDVYRTGAKCVPGEAGDSGKPGAAFHQVGLLRVKPGRGDRTRSMSCS
DKMARWNVLGCQGALLMHLLEEPIYLSAVVIGKCPYSQEAMQRALIGRCQNVSALPKGFG
VQELKILQSDLLFEQSRSAVQAKRADSPGRLVPCGAAISWSAVPEQPLDVTANGFPQGTT
KKTIGSLQARSQISKVELFRSFQKLLSRIARDKWPHSLRVQKLDTYQEYKEAASSYQEAW
STLRKQVFGSWIRNPPDYHQFK
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CAMK Ser/Thr protein kinase family
Subcellular location
Cytoplasm
Function
May play a role in the response to environmental stress and cytokines. Appears to regulate translation by phosphorylating EIF4E, thus increasing the affinity of this protein for the 7-methylguanosine-containing mRNA cap.
TTD ID
T97136
Uniprot ID
Q9BUB5
DrugMap ID
TTEZAUX
Ensemble ID
ENST00000649800.1
HGNC ID
HGNC:7110
ChEMBL ID
CHEMBL4718

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
DBIA
 Probe Info  		C101(1.58)  LDD3384  [1]
IA-alkyne
 Probe Info  		N.A.  LDD0165  [2]
IPM
 Probe Info  		C432(0.00); C101(0.00)  LDD2156  [3]
TFBX
 Probe Info  		N.A.  LDD0148  [4]
AOyne
 Probe Info  		14.60  LDD0443  [5]
NAIA_5
 Probe Info  		C219(0.00); C320(0.00)  LDD2223  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C231(1.09)  LDD1508  [7]
 LDCM0226  AC11 HEK-293T C231(1.03)  LDD1509  [7]
 LDCM0277  AC18 HEK-293T C231(1.03)  LDD1516  [7]
 LDCM0278  AC19 HEK-293T C231(1.05)  LDD1517  [7]
 LDCM0279  AC2 HEK-293T C231(1.01)  LDD1518  [7]
 LDCM0281  AC21 HEK-293T C231(1.27)  LDD1520  [7]
 LDCM0284  AC24 HEK-293T C101(1.05)  LDD1523  [7]
 LDCM0286  AC26 HEK-293T C231(1.15)  LDD1525  [7]
 LDCM0287  AC27 HEK-293T C231(0.82)  LDD1526  [7]
 LDCM0289  AC29 HEK-293T C231(1.00)  LDD1528  [7]
 LDCM0290  AC3 HEK-293T C231(0.96)  LDD1529  [7]
 LDCM0293  AC32 HEK-293T C101(1.25)  LDD1532  [7]
 LDCM0295  AC34 HEK-293T C231(1.14)  LDD1534  [7]
 LDCM0296  AC35 HEK-293T C231(0.99)  LDD1535  [7]
 LDCM0298  AC37 HEK-293T C231(1.13)  LDD1537  [7]
 LDCM0302  AC40 HEK-293T C101(1.15)  LDD1541  [7]
 LDCM0304  AC42 HEK-293T C231(1.02)  LDD1543  [7]
 LDCM0305  AC43 HEK-293T C231(0.99)  LDD1544  [7]
 LDCM0307  AC45 HEK-293T C231(1.10)  LDD1546  [7]
 LDCM0310  AC48 HEK-293T C101(0.81)  LDD1549  [7]
 LDCM0312  AC5 HEK-293T C231(1.00)  LDD1551  [7]
 LDCM0313  AC50 HEK-293T C231(1.07)  LDD1552  [7]
 LDCM0314  AC51 HEK-293T C231(0.89)  LDD1553  [7]
 LDCM0316  AC53 HEK-293T C231(1.07)  LDD1555  [7]
 LDCM0319  AC56 HEK-293T C101(1.04)  LDD1558  [7]
 LDCM0321  AC58 HEK-293T C231(1.07)  LDD1560  [7]
 LDCM0322  AC59 HEK-293T C231(1.01)  LDD1561  [7]
 LDCM0325  AC61 HEK-293T C231(1.11)  LDD1564  [7]
 LDCM0328  AC64 HEK-293T C101(0.80)  LDD1567  [7]
 LDCM0345  AC8 HEK-293T C101(0.75)  LDD1569  [7]
 LDCM0248  AKOS034007472 HEK-293T C231(1.09)  LDD1511  [7]
 LDCM0275  AKOS034007705 HEK-293T C101(0.71)  LDD1514  [7]
 LDCM0372  CL103 HEK-293T C101(1.09)  LDD1576  [7]
 LDCM0376  CL107 HEK-293T C101(1.04)  LDD1580  [7]
 LDCM0381  CL111 HEK-293T C101(0.93)  LDD1585  [7]
 LDCM0385  CL115 HEK-293T C101(0.86)  LDD1589  [7]
 LDCM0389  CL119 HEK-293T C101(0.80)  LDD1593  [7]
 LDCM0390  CL12 HEK-293T C101(1.25)  LDD1594  [7]
 LDCM0394  CL123 HEK-293T C101(0.99)  LDD1598  [7]
 LDCM0398  CL127 HEK-293T C101(1.02)  LDD1602  [7]
 LDCM0402  CL15 HEK-293T C101(0.92)  LDD1606  [7]
 LDCM0405  CL18 HEK-293T C231(1.06)  LDD1609  [7]
 LDCM0406  CL19 HEK-293T C231(1.04)  LDD1610  [7]
 LDCM0409  CL21 HEK-293T C231(1.16)  LDD1613  [7]
 LDCM0412  CL24 HEK-293T C101(1.47)  LDD1616  [7]
 LDCM0415  CL27 HEK-293T C101(1.08)  LDD1619  [7]
 LDCM0418  CL3 HEK-293T C101(1.04)  LDD1622  [7]
 LDCM0419  CL30 HEK-293T C231(1.05)  LDD1623  [7]
 LDCM0420  CL31 HEK-293T C231(0.92)  LDD1624  [7]
 LDCM0422  CL33 HEK-293T C231(1.06)  LDD1626  [7]
 LDCM0425  CL36 HEK-293T C101(0.98)  LDD1629  [7]
 LDCM0428  CL39 HEK-293T C101(0.96)  LDD1632  [7]
 LDCM0432  CL42 HEK-293T C231(1.14)  LDD1636  [7]
 LDCM0433  CL43 HEK-293T C231(1.01)  LDD1637  [7]
 LDCM0435  CL45 HEK-293T C231(1.07)  LDD1639  [7]
 LDCM0438  CL48 HEK-293T C101(0.88)  LDD1642  [7]
 LDCM0445  CL54 HEK-293T C231(1.00)  LDD1648  [7]
 LDCM0446  CL55 HEK-293T C231(0.89)  LDD1649  [7]
 LDCM0448  CL57 HEK-293T C231(1.01)  LDD1651  [7]
 LDCM0451  CL6 HEK-293T C231(1.04)  LDD1654  [7]
 LDCM0452  CL60 HEK-293T C101(1.00)  LDD1655  [7]
 LDCM0455  CL63 HEK-293T C101(0.99)  LDD1658  [7]
 LDCM0458  CL66 HEK-293T C231(1.00)  LDD1661  [7]
 LDCM0459  CL67 HEK-293T C231(1.05)  LDD1662  [7]
 LDCM0461  CL69 HEK-293T C231(1.12)  LDD1664  [7]
 LDCM0462  CL7 HEK-293T C231(1.00)  LDD1665  [7]
 LDCM0465  CL72 HEK-293T C101(0.93)  LDD1668  [7]
 LDCM0471  CL78 HEK-293T C231(1.28)  LDD1674  [7]
 LDCM0472  CL79 HEK-293T C231(0.93)  LDD1675  [7]
 LDCM0475  CL81 HEK-293T C231(1.20)  LDD1678  [7]
 LDCM0478  CL84 HEK-293T C101(1.29)  LDD1681  [7]
 LDCM0481  CL87 HEK-293T C101(1.10)  LDD1684  [7]
 LDCM0484  CL9 HEK-293T C231(1.13)  LDD1687  [7]
 LDCM0485  CL90 HEK-293T C231(0.88)  LDD1688  [7]
 LDCM0486  CL91 HEK-293T C231(1.09)  LDD1689  [7]
 LDCM0488  CL93 HEK-293T C231(1.00)  LDD1691  [7]
 LDCM0491  CL96 HEK-293T C101(0.95)  LDD1694  [7]
 LDCM0494  CL99 HEK-293T C101(1.01)  LDD1697  [7]
 LDCM0495  E2913 HEK-293T C101(0.97)  LDD1698  [7]
 LDCM0468  Fragment33 HEK-293T C101(0.84)  LDD1671  [7]
 LDCM0022  KB02 CAL-33 C101(1.83)  LDD2287  [1]
 LDCM0023  KB03 CAL-33 C101(2.68)  LDD2704  [1]
 LDCM0024  KB05 OVCAR-8 C101(1.58)  LDD3384  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Mitogen-activated protein kinase 1 (MAPK1) CMGC Ser/Thr protein kinase family P28482
Mitogen-activated protein kinase 14 (MAPK14) CMGC Ser/Thr protein kinase family Q16539
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Optineurin (OPTN) . Q96CV9
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ataxin-1 (ATXN1) ATXN1 family P54253

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Eft508 . D07XOV

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 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
3 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
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 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
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
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