Details of the Target

General Information of Target

Target ID LDTP10526
Target Name MAP/microtubule affinity-regulating kinase 4 (MARK4)
Gene Name MARK4
Gene ID 57787
Synonyms
KIAA1860; MARKL1; MAP/microtubule affinity-regulating kinase 4; EC 2.7.11.1; MAP/microtubule affinity-regulating kinase-like 1
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MGRRPARCYRYCKNKPYPKSRFCRGVPDAKIRIFDLGRKKAKVDEFPLGGHMVSDEYEQL
SSEALEAARICANKYMVKSCGRDGFHMRVRLHPFHVIRINKMLSCAGADRLQTGMRGAFG
KPQGTVARVHIGQVIMSIRTKLQNEEHVIEALRRAKFKFPGRQKIHISKKWGFTKFNADE
FEDMVAKKCLIPDGCGVKYVPSHGPLDKWRVLHS
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CAMK Ser/Thr protein kinase family, SNF1 subfamily
Subcellular location
Cytoplasm, cytoskeleton, microtubule organizing center, centrosome
Function
Serine/threonine-protein kinase. Phosphorylates the microtubule-associated protein MAPT/TAU. Also phosphorylates the microtubule-associated proteins MAP2 and MAP4. Involved in regulation of the microtubule network, causing reorganization of microtubules into bundles. Required for the initiation of axoneme extension during cilium assembly. Regulates the centrosomal location of ODF2 and phosphorylates ODF2 in vitro. Plays a role in cell cycle progression, specifically in the G1/S checkpoint. Reduces neuronal cell survival. Plays a role in energy homeostasis by regulating satiety and metabolic rate. Promotes adipogenesis by activating JNK1 and inhibiting the p38MAPK pathway, and triggers apoptosis by activating the JNK1 pathway. Phosphorylates mTORC1 complex member RPTOR and acts as a negative regulator of the mTORC1 complex, probably due to disruption of the interaction between phosphorylated RPTOR and the RRAGA/RRAGC heterodimer which is required for mTORC1 activation. Involved in NLRP3 positioning along microtubules by mediating NLRP3 recruitment to microtubule organizing center (MTOC) upon inflammasome activation.
Uniprot ID
Q96L34
Ensemble ID
ENST00000262891.9
HGNC ID
HGNC:13538
ChEMBL ID
CHEMBL5754

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.R265Q DBIA    Probe Info 
AN3CA SNV: p.E192G DBIA    Probe Info 
CCK81 SNV: p.R556W DBIA    Probe Info 
CHL1 SNV: p.D328N DBIA    Probe Info 
ETK1 SNV: p.P9Q .
HEC1 SNV: p.R418C DBIA    Probe Info 
HUH1 SNV: p.Q573H DBIA    Probe Info 
JURKAT Deletion: p.A520LfsTer100 .
KMRC1 SNV: p.G30V DBIA    Probe Info 
MOLT4 SNV: p.R721Q .
NCIH1666 SNV: p.Q174P DBIA    Probe Info 
NCIH1993 SNV: p.S406G .
NCIH2172 Deletion: p.K67RfsTer29 DBIA    Probe Info 
OE33 SNV: p.K448Q DBIA    Probe Info 
REH SNV: p.A138T DBIA    Probe Info 
TOV21G SNV: p.P544H DBIA    Probe Info 

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
AHL-Pu-1
 Probe Info  		C49(3.88)  LDD0169  [1]
DBIA
 Probe Info  		C459(17.84)  LDD0209  [2]
ATP probe
 Probe Info  		N.A.  LDD0199  [3]
IA-alkyne
 Probe Info  		C49(0.00); C459(0.00)  LDD0165  [4]
NAIA_4
 Probe Info  		C49(0.00); C459(0.00); C642(0.00)  LDD2226  [5]
IPM
 Probe Info  		C459(0.00); C49(0.00); C642(0.00); C299(0.00)  LDD2156  [6]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [7]
AOyne
 Probe Info  		10.10  LDD0443  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA HEK-293T C49(3.88)  LDD0169  [1]
 LDCM0214  AC1 HEK-293T C459(0.96)  LDD1507  [9]
 LDCM0215  AC10 HEK-293T C459(0.91)  LDD1508  [9]
 LDCM0226  AC11 HEK-293T C459(1.10)  LDD1509  [9]
 LDCM0237  AC12 HEK-293T C459(0.98)  LDD1510  [9]
 LDCM0270  AC15 HEK-293T C459(0.95)  LDD1513  [9]
 LDCM0276  AC17 HEK-293T C459(1.06)  LDD1515  [9]
 LDCM0277  AC18 HEK-293T C459(0.96)  LDD1516  [9]
 LDCM0278  AC19 HEK-293T C459(1.44)  LDD1517  [9]
 LDCM0279  AC2 HEK-293T C459(0.95)  LDD1518  [9]
 LDCM0280  AC20 HEK-293T C459(1.00)  LDD1519  [9]
 LDCM0281  AC21 HEK-293T C459(0.92)  LDD1520  [9]
 LDCM0283  AC23 HEK-293T C459(1.27)  LDD1522  [9]
 LDCM0285  AC25 HEK-293T C459(1.07)  LDD1524  [9]
 LDCM0286  AC26 HEK-293T C459(1.12)  LDD1525  [9]
 LDCM0287  AC27 HEK-293T C459(0.97)  LDD1526  [9]
 LDCM0288  AC28 HEK-293T C459(0.93)  LDD1527  [9]
 LDCM0289  AC29 HEK-293T C459(0.87)  LDD1528  [9]
 LDCM0290  AC3 HEK-293T C459(0.97)  LDD1529  [9]
 LDCM0292  AC31 HEK-293T C459(1.22)  LDD1531  [9]
 LDCM0294  AC33 HEK-293T C459(1.14)  LDD1533  [9]
 LDCM0295  AC34 HEK-293T C459(0.92)  LDD1534  [9]
 LDCM0296  AC35 HEK-293T C459(1.05)  LDD1535  [9]
 LDCM0297  AC36 HEK-293T C459(1.15)  LDD1536  [9]
 LDCM0298  AC37 HEK-293T C459(0.99)  LDD1537  [9]
 LDCM0300  AC39 HEK-293T C459(0.96)  LDD1539  [9]
 LDCM0301  AC4 HEK-293T C459(1.02)  LDD1540  [9]
 LDCM0303  AC41 HEK-293T C459(1.06)  LDD1542  [9]
 LDCM0304  AC42 HEK-293T C459(1.24)  LDD1543  [9]
 LDCM0305  AC43 HEK-293T C459(1.14)  LDD1544  [9]
 LDCM0306  AC44 HEK-293T C459(1.15)  LDD1545  [9]
 LDCM0307  AC45 HEK-293T C459(1.17)  LDD1546  [9]
 LDCM0309  AC47 HEK-293T C459(0.91)  LDD1548  [9]
 LDCM0311  AC49 HEK-293T C459(1.09)  LDD1550  [9]
 LDCM0312  AC5 HEK-293T C459(0.93)  LDD1551  [9]
 LDCM0313  AC50 HEK-293T C459(1.08)  LDD1552  [9]
 LDCM0314  AC51 HEK-293T C459(1.00)  LDD1553  [9]
 LDCM0315  AC52 HEK-293T C459(0.96)  LDD1554  [9]
 LDCM0316  AC53 HEK-293T C459(0.90)  LDD1555  [9]
 LDCM0318  AC55 HEK-293T C459(1.11)  LDD1557  [9]
 LDCM0320  AC57 HEK-293T C459(1.07)  LDD1559  [9]
 LDCM0321  AC58 HEK-293T C459(0.94)  LDD1560  [9]
 LDCM0322  AC59 HEK-293T C459(1.04)  LDD1561  [9]
 LDCM0324  AC60 HEK-293T C459(0.95)  LDD1563  [9]
 LDCM0325  AC61 HEK-293T C459(0.93)  LDD1564  [9]
 LDCM0327  AC63 HEK-293T C459(1.00)  LDD1566  [9]
 LDCM0334  AC7 HEK-293T C459(1.16)  LDD1568  [9]
 LDCM0248  AKOS034007472 HEK-293T C459(0.85)  LDD1511  [9]
 LDCM0356  AKOS034007680 HEK-293T C459(1.20)  LDD1570  [9]
 LDCM0367  CL1 HEK-293T C459(1.06)  LDD1571  [9]
 LDCM0370  CL101 HEK-293T C459(1.03)  LDD1574  [9]
 LDCM0371  CL102 HEK-293T C459(0.98)  LDD1575  [9]
 LDCM0374  CL105 HEK-293T C459(0.98)  LDD1578  [9]
 LDCM0375  CL106 HEK-293T C459(0.96)  LDD1579  [9]
 LDCM0378  CL109 HEK-293T C459(1.08)  LDD1582  [9]
 LDCM0379  CL11 HEK-293T C459(1.34)  LDD1583  [9]
 LDCM0380  CL110 HEK-293T C459(0.85)  LDD1584  [9]
 LDCM0383  CL113 HEK-293T C459(1.10)  LDD1587  [9]
 LDCM0384  CL114 HEK-293T C459(1.11)  LDD1588  [9]
 LDCM0387  CL117 HEK-293T C459(1.19)  LDD1591  [9]
 LDCM0388  CL118 HEK-293T C459(0.85)  LDD1592  [9]
 LDCM0392  CL121 HEK-293T C459(1.11)  LDD1596  [9]
 LDCM0393  CL122 HEK-293T C459(0.89)  LDD1597  [9]
 LDCM0396  CL125 HEK-293T C459(1.02)  LDD1600  [9]
 LDCM0397  CL126 HEK-293T C459(1.15)  LDD1601  [9]
 LDCM0400  CL13 HEK-293T C459(1.18)  LDD1604  [9]
 LDCM0401  CL14 HEK-293T C459(1.05)  LDD1605  [9]
 LDCM0404  CL17 HEK-293T C459(1.28)  LDD1608  [9]
 LDCM0405  CL18 HEK-293T C459(1.01)  LDD1609  [9]
 LDCM0406  CL19 HEK-293T C459(1.01)  LDD1610  [9]
 LDCM0407  CL2 HEK-293T C459(0.95)  LDD1611  [9]
 LDCM0408  CL20 HEK-293T C459(1.04)  LDD1612  [9]
 LDCM0409  CL21 HEK-293T C459(0.82)  LDD1613  [9]
 LDCM0411  CL23 HEK-293T C459(1.11)  LDD1615  [9]
 LDCM0413  CL25 HEK-293T C459(0.99)  LDD1617  [9]
 LDCM0414  CL26 HEK-293T C459(0.92)  LDD1618  [9]
 LDCM0417  CL29 HEK-293T C459(1.09)  LDD1621  [9]
 LDCM0419  CL30 HEK-293T C459(0.91)  LDD1623  [9]
 LDCM0420  CL31 HEK-293T C459(1.13)  LDD1624  [9]
 LDCM0421  CL32 HEK-293T C459(1.01)  LDD1625  [9]
 LDCM0422  CL33 HEK-293T C459(0.84)  LDD1626  [9]
 LDCM0424  CL35 HEK-293T C459(1.09)  LDD1628  [9]
 LDCM0426  CL37 HEK-293T C459(0.90)  LDD1630  [9]
 LDCM0431  CL41 HEK-293T C459(1.08)  LDD1635  [9]
 LDCM0432  CL42 HEK-293T C459(0.96)  LDD1636  [9]
 LDCM0433  CL43 HEK-293T C459(1.02)  LDD1637  [9]
 LDCM0434  CL44 HEK-293T C459(1.11)  LDD1638  [9]
 LDCM0435  CL45 HEK-293T C459(1.11)  LDD1639  [9]
 LDCM0437  CL47 HEK-293T C459(0.98)  LDD1641  [9]
 LDCM0439  CL49 HEK-293T C459(1.10)  LDD1643  [9]
 LDCM0440  CL5 HEK-293T C459(1.10)  LDD1644  [9]
 LDCM0441  CL50 HEK-293T C459(1.06)  LDD1645  [9]
 LDCM0444  CL53 HEK-293T C459(1.15)  LDD1647  [9]
 LDCM0445  CL54 HEK-293T C459(0.96)  LDD1648  [9]
 LDCM0446  CL55 HEK-293T C459(1.12)  LDD1649  [9]
 LDCM0447  CL56 HEK-293T C459(1.12)  LDD1650  [9]
 LDCM0448  CL57 HEK-293T C459(1.08)  LDD1651  [9]
 LDCM0450  CL59 HEK-293T C459(1.11)  LDD1653  [9]
 LDCM0451  CL6 HEK-293T C459(0.87)  LDD1654  [9]
 LDCM0453  CL61 HEK-293T C459(0.94)  LDD1656  [9]
 LDCM0454  CL62 HEK-293T C459(1.09)  LDD1657  [9]
 LDCM0457  CL65 HEK-293T C459(1.19)  LDD1660  [9]
 LDCM0458  CL66 HEK-293T C459(0.96)  LDD1661  [9]
 LDCM0459  CL67 HEK-293T C459(1.12)  LDD1662  [9]
 LDCM0460  CL68 HEK-293T C459(1.02)  LDD1663  [9]
 LDCM0461  CL69 HEK-293T C459(0.92)  LDD1664  [9]
 LDCM0462  CL7 HEK-293T C459(1.10)  LDD1665  [9]
 LDCM0464  CL71 HEK-293T C459(1.19)  LDD1667  [9]
 LDCM0466  CL73 HEK-293T C459(1.10)  LDD1669  [9]
 LDCM0467  CL74 HEK-293T C459(1.15)  LDD1670  [9]
 LDCM0470  CL77 HEK-293T C459(1.38)  LDD1673  [9]
 LDCM0471  CL78 HEK-293T C459(1.10)  LDD1674  [9]
 LDCM0472  CL79 HEK-293T C459(1.01)  LDD1675  [9]
 LDCM0473  CL8 HEK-293T C459(0.96)  LDD1676  [9]
 LDCM0474  CL80 HEK-293T C459(1.10)  LDD1677  [9]
 LDCM0475  CL81 HEK-293T C459(0.99)  LDD1678  [9]
 LDCM0477  CL83 HEK-293T C459(1.28)  LDD1680  [9]
 LDCM0479  CL85 HEK-293T C459(1.02)  LDD1682  [9]
 LDCM0480  CL86 HEK-293T C459(1.33)  LDD1683  [9]
 LDCM0483  CL89 HEK-293T C459(1.03)  LDD1686  [9]
 LDCM0484  CL9 HEK-293T C459(0.97)  LDD1687  [9]
 LDCM0485  CL90 HEK-293T C459(1.01)  LDD1688  [9]
 LDCM0486  CL91 HEK-293T C459(1.03)  LDD1689  [9]
 LDCM0487  CL92 HEK-293T C459(1.02)  LDD1690  [9]
 LDCM0488  CL93 HEK-293T C459(0.98)  LDD1691  [9]
 LDCM0490  CL95 HEK-293T C459(0.99)  LDD1693  [9]
 LDCM0492  CL97 HEK-293T C459(1.02)  LDD1695  [9]
 LDCM0493  CL98 HEK-293T C459(0.93)  LDD1696  [9]
 LDCM0427  Fragment51 HEK-293T C459(0.96)  LDD1631  [9]
 LDCM0022  KB02 HEK-293T C459(0.96)  LDD1492  [9]
 LDCM0023  KB03 Jurkat C459(17.84)  LDD0209  [2]
 LDCM0024  KB05 G361 C459(2.37)  LDD3311  [10]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein kinase C iota type (PRKCI) AGC Ser/Thr protein kinase family P41743
Serine/threonine-protein kinase STK11 (STK11) CAMK Ser/Thr protein kinase family Q15831
Tyrosine-protein kinase Lyn (LYN) Tyr protein kinase family P07948
Cell division control protein 42 homolog (CDC42) Rho family P60953
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein eta (YWHAH) 14-3-3 family Q04917
Keratin, type I cuticular Ha1 (KRT31) Intermediate filament family Q15323
Partitioning defective 6 homolog gamma (PARD6G) PAR6 family Q9BYG4
Paraneoplastic antigen Ma1 (PNMA1) PNMA family Q8ND90
Tubulin gamma-1 chain (TUBG1) Tubulin family P23258

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

References

1 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
2 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
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 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
5 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
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 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
8 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.
9 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
10 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