General Information of Drug Therapeutic Target (DTT) (ID: TT3DCYJ)

DTT Name Microtubule affinity regulating kinase 3 (MARK3)
Synonyms
cTAK1; Serine/threonine-protein kinase p78; Ser/Thr protein kinase PAR-1; Protein kinase STK10); Protein kinase STK10; Par-1a; MAP/microtubule affinity-regulating kinase 3; EMK2; EMK-2; ELKL motif kinase 2; Cdc25C-associated protein kinase 1; C-TAK1
Gene Name MARK3
DTT Type
Clinical trial target
[1]
BioChemical Class
Kinase
UniProt ID
MARK3_HUMAN
TTD ID
T90553
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
EC Number
EC 2.7.11.1
Sequence
MSTRTPLPTVNERDTENHTSHGDGRQEVTSRTSRSGARCRNSIASCADEQPHIGNYRLLK
TIGKGNFAKVKLARHILTGREVAIKIIDKTQLNPTSLQKLFREVRIMKILNHPNIVKLFE
VIETEKTLYLIMEYASGGEVFDYLVAHGRMKEKEARSKFRQIVSAVQYCHQKRIVHRDLK
AENLLLDADMNIKIADFGFSNEFTVGGKLDTFCGSPPYAAPELFQGKKYDGPEVDVWSLG
VILYTLVSGSLPFDGQNLKELRERVLRGKYRIPFYMSTDCENLLKRFLVLNPIKRGTLEQ
IMKDRWINAGHEEDELKPFVEPELDISDQKRIDIMVGMGYSQEEIQESLSKMKYDEITAT
YLLLGRKSSELDASDSSSSSNLSLAKVRPSSDLNNSTGQSPHHKVQRSVSSSQKQRRYSD
HAGPAIPSVVAYPKRSQTSTADSDLKEDGISSRKSSGSAVGGKGIAPASPMLGNASNPNK
ADIPERKKSSTVPSSNTASGGMTRRNTYVCSERTTADRHSVIQNGKENSTIPDQRTPVAS
THSISSAATPDRIRFPRGTASRSTFHGQPRERRTATYNGPPASPSLSHEATPLSQTRSRG
STNLFSKLTSKLTRRNMSFRFIKRLPTEYERNGRYEGSSRNVSAEQKDENKEAKPRSLRF
TWSMKTTSSMDPGDMMREIRKVLDANNCDYEQRERFLLFCVHGDGHAENLVQWEMEVCKL
PRLSLNGVRFKRISGTSIAFKNIASKIANELKL
Function
Involved in the specific phosphorylation of microtubule-associated proteins for MAP2 and MAP4. Phosphorylates the microtubule-associated protein MAPT/TAU. Phosphorylates CDC25C on 'Ser-216'. Regulates localization and activity of some histone deacetylases by mediating phosphorylation of HDAC7, promoting subsequent interaction between HDAC7 and 14-3-3 and export from the nucleus. Negatively regulates the Hippo signaling pathway and antagonizes the phosphorylation of LATS1. Cooperates with DLG5 to inhibit the kinase activity of STK3/MST2 toward LATS1. Serine/threonine-protein kinase.
Reactome Pathway
MAP2K and MAPK activation (R-HSA-5674135 )
Negative regulation of MAPK pathway (R-HSA-5675221 )
RAF activation (R-HSA-5673000 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CBP-501 DMCWVPU Mesothelioma 2C51.2 Phase 1/2 [1]
------------------------------------------------------------------------------------
1 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID23099093C17d DMWS7O9 Discovery agent N.A. Investigative [2]
------------------------------------------------------------------------------------

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Lung cancer 2C82 Lung tissue 2.18E-06 0.13 0.48
------------------------------------------------------------------------------------

References

1 National Cancer Institute Drug Dictionary (drug id 577812).
2 Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKepsilon kinases. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7169-73.