Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTV3O87)

• DTT Name: ERK activator kinase 5 (MAP2K5)
• Synonyms: PRKMK5; Mitogen-activatedprotein kinase kinase 5; MKK5; MEK5; MEK 5; MAPKK 5; MAPK/ERK kinase 5; MAP kinase kinase5; MAP kinase kinase 5; Dual specificity mitogen-activated protein kinase kinase 5
• Gene Name: MAP2K5
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Kinase
• UniProt ID: MP2K5_HUMAN
• TTD ID: T17143
• EC Number: EC 2.7.12.2
• Sequence:
  MLWLALGPFPAMENQVLVIRIKIPNSGAVDWTVHSGPQLLFRDVLDVIGQVLPEATTTAF
  EYEDEDGDRITVRSDEEMKAMLSYYYSTVMEQQVNGQLIEPLQIFPRACKPPGERNIHGL
  KVNTRAGPSQHSSPAVSDSLPSNSLKKSSAELKKILANGQMNEQDIRYRDTLGHGNGGTV
  YKAYHVPSGKILAVKVILLDITLELQKQIMSELEILYKCDSSYIIGFYGAFFVENRISIC
  TEFMDGGSLDVYRKMPEHVLGRIAVAVVKGLTYLWSLKILHRDVKPSNMLVNTRGQVKLC
  DFGVSTQLVNSIAKTYVGTNAYMAPERISGEQYGIHSDVWSLGISFMELALGRFPYPQIQ
  KNQGSLMPLQLLQCIVDEDSPVLPVGEFSEPFVHFITQCMRKQPKERPAPEELMGHPFIV
  QFNDGNAAVVSMWVCRALEERRSQQGPP
• Function: Activation of this pathway appears to play a critical role in protecting cells from stress-induced apoptosis, neuronal survival and cardiac development and angiogenesis. Acts as a scaffold for the formation of a ternary MAP3K2/MAP3K3-MAP3K5-MAPK7 signaling complex.
• KEGG Pathway:
  MAPK signaling pathway (hsa04010)
  Gap junction (hsa04540)
  Neurotrophin signaling pathway (hsa04722)
  Oxytocin signaling pathway (hsa04921)
  Fluid shear stress and atherosclerosis (hsa05418)
• Reactome Pathway: Signalling to ERK5 (R-HSA-198765)

Molecular Interaction Atlas (MIA) of This DTT

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BIX 02188	DMFHY04	Discovery agent	N.A.	Investigative	[1]

References

• [1] Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5.