Target Information

Target General Infomation
Target ID
T90553
Former ID
TTDC00281
Target Name
MARK3
Gene Name
MARK3
Synonyms
C-TAK1; Cdc25C-associated protein kinase 1; MAP/microtubule affinity-regulating kinase 3; Protein kinase STK10); Ser/Thr protein kinase PAR-1; Serine/threonine-protein kinase p78; cTAK1; MARK3
Target Type
Clinical Trial
Disease Mesothelioma [ICD9: 163; ICD10: C45]
Function
Involved in the specific phosphorylation of microtubule- associated proteins for tau, MAP2 and MAP4. 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.
BioChemical Class
Kinase
Target Validation
T90553
UniProt ID
P27448
EC Number
EC 2.7.11.1
Sequence
MSTRTPLPTVNERDTENHTSHGDGRQEVTSRTSRSGARCRNSIASCADEQPHIGNYRLLK
TIGKGNFAKVKLARHILTGREVAIKIIDKTQLNPTSLQKLFREVRIMKILNHPNIVKLFE
VIETEKTLYLIMEYASGGEVFDYLVAHGRMKEKEARSKFRQIVSAVQYCHQKRIVHRDLK
AENLLLDADMNIKIADFGFSNEFTVGGKLDTFCGSPPYAAPELFQGKKYDGPEVDVWSLG
VILYTLVSGSLPFDGQNLKELRERVLRGKYRIPFYMSTDCENLLKRFLVLNPIKRGTLEQ
IMKDRWINAGHEEDELKPFVEPELDISDQKRIDIMVGMGYSQEEIQESLSKMKYDEITAT
YLLLGRKSSELDASDSSSSSNLSLAKVRPSSDLNNSTGQSPHHKVQRSVFSSQKQRRYSD
HAGPAIPSVVAYPKRSQTSTADSDLKEDGISSRKSSGSAVGGKGIAPASPMLGNASNPNK
ADIPERKKSSTVPSSNTASGGMTRRNTYVCSERTTADRHSVIQNGKENSTIPDQRTPVAS
THSISSAATPDRIRFPRGTASRSTFHGQPRERRTATYNGPPASPSLSHEATPLSQTRSRG
STNLFSKLTSKLTRRNMSFRFIKRLPTEYERNGRYEGSSRNVSAEQKDENKEAKPRSLRF
TWSMKTTSSMDPGDMMREIRKVLDANNCDYEQRERFLLFCVHGDGHAENLVQWEMEVCKL
PRLSLNGVRFKRISGTSIAFKNIASKIANELKL
Drugs and Mode of Action
Drug(s) CBP-501 Drug Info Phase 1/2 Mesothelioma [522352]
Inhibitor CBP-501 Drug Info [550418]
compound 17d Drug Info [532095]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Reactome RAF activation
MAP2K and MAPK activation
Negative regulation of MAPK pathway
References
Ref 522352ClinicalTrials.gov (NCT00700336) Study of CBP501 + Pemetrexed + Cisplatin on MPM (Phase I/II). U.S. National Institutes of Health.
Ref 532095Synthesis 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.
Ref 550418National Cancer Institute Drug Dictionary (drug id 577812).

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