Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTU6FSC)

• DTT Name: Extracellular signal-regulated kinase 5 (ERK5)
• Synonyms: PRKM7; Mitogen-activated protein kinase 7; MAPK 7; MAP kinase 7; ERK-5; Big MAP kinase 1; BMK1; BMK-1
• Gene Name: MAPK7
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: Kinase
• UniProt ID: MK07_HUMAN
• TTD ID: T70851
• EC Number: EC 2.7.11.24
• Sequence:
  MAEPLKEEDGEDGSAEPPGPVKAEPAHTAASVAAKNLALLKARSFDVTFDVGDEYEIIET
  IGNGAYGVVSSARRRLTGQQVAIKKIPNAFDVVTNAKRTLRELKILKHFKHDNIIAIKDI
  LRPTVPYGEFKSVYVVLDLMESDLHQIIHSSQPLTLEHVRYFLYQLLRGLKYMHSAQVIH
  RDLKPSNLLVNENCELKIGDFGMARGLCTSPAEHQYFMTEYVATRWYRAPELMLSLHEYT
  QAIDLWSVGCIFGEMLARRQLFPGKNYVHQLQLIMMVLGTPSPAVIQAVGAERVRAYIQS
  LPPRQPVPWETVYPGADRQALSLLGRMLRFEPSARISAAAALRHPFLAKYHDPDDEPDCA
  PPFDFAFDREALTRERIKEAIVAEIEDFHARREGIRQQIRFQPSLQPVASEPGCPDVEMP
  SPWAPSGDCAMESPPPAPPPCPGPAPDTIDLTLQPPPPVSEPAPPKKDGAISDNTKAALK
  AALLKSLRSRLRDGPSAPLEAPEPRKPVTAQERQREREEKRRRRQERAKEREKRRQERER
  KERGAGASGGPSTDPLAGLVLSDNDRSLLERWTRMARPAAPALTSVPAPAPAPTPTPTPV
  QPTSPPPGPVAQPTGPQPQSAGSTSGPVPQPACPPPGPAPHPTGPPGPIPVPAPPQIATS
  TSLLAAQSLVPPPGLPGSSTPGVLPYFPPGLPPPDAGGAPQSSMSESPDVNLVTQQLSKS
  QVEDPLPPVFSGTPKGSGAGYGVGFDLEEFLNQSFDMGVADGPQDGQADSASLSASLLAD
  WLEGHGMNPADIESLQREIQMDSPMLLADLPDLQDP
• Function: The upstream activator of MAPK7 is the MAPK kinase MAP2K5. Upon activation, it translocates to the nucleus and phosphorylates various downstream targets including MEF2C. EGF activates MAPK7 through a Ras-independent and MAP2K5-dependent pathway. May have a role in muscle cell differentiation. May be important for endothelial function and maintenance of blood vessel integrity. MAP2K5 and MAPK7 interact specifically with one another and not with MEK1/ERK1 or MEK2/ERK2 pathways. Phosphorylates SGK1 at Ser-78 and this is required for growth factor-induced cell cycle progression. Involved in the regulation of p53/TP53 by disrupting the PML-MDM2 interaction. Plays a role in various cellular processes such as proliferation, differentiation and cell survival.
• KEGG Pathway:
  MAPK signaling pathway (hsa04010)
  Gap junction (hsa04540)
  IL-17 signaling pathway (hsa04657)
  Neurotrophin signaling pathway (hsa04722)
  GnRH signaling pathway (hsa04912)
  Oxytocin signaling pathway (hsa04921)
  MicroRNAs in cancer (hsa05206)
  Fluid shear stress and atherosclerosis (hsa05418)
• Reactome Pathway:
  Signalling to ERK5 (R-HSA-198765)
  ERKs are inactivated (R-HSA-202670)
  Senescence-Associated Secretory Phenotype (SASP) (R-HSA-2559582)
  Gastrin-CREB signalling pathway via PKC and MAPK (R-HSA-881907)
  RET signaling (R-HSA-8853659)
  ERK/MAPK targets (R-HSA-198753)

Molecular Interaction Atlas (MIA) of This DTT

3 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID26924192-Compound-30	DMWXNIJ	N. A.	N. A.	Patented	[1]
PMID26924192-Compound-32	DM0JSOZ	N. A.	N. A.	Patented	[1]
PMID26924192-Compound-33	DM9NWXM	N. A.	N. A.	Patented	[1]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
XMD8-92	DMZIHKY	Discovery agent	N.A.	Investigative	[2]

References

• [1] BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.
• [2] Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell. 2010 Sep 14;18(3):258-67.