Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTK1N5G)

• DTT Name: MAPK/ERK kinase kinase 2 (MAP3K2)
• Synonyms: Mitogen-activated protein kinase kinase kinase 2; MEKK2; MEKK 2; MEK kinase 2; MAPKKK2
• Gene Name: MAP3K2
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Kinase
• UniProt ID: M3K2_HUMAN
• TTD ID: T76508
• EC Number: EC 2.7.11.25
• Sequence:
  MDDQQALNSIMQDLAVLHKASRPALSLQETRKAKSSSPKKQNDVRVKFEHRGEKRILQFP
  RPVKLEDLRSKAKIAFGQSMDLHYTNNELVIPLTTQDDLDKAVELLDRSIHMKSLKILLV
  INGSTQATNLEPLPSLEDLDNTVFGAERKKRLSIIGPTSRDRSSPPPGYIPDELHQVARN
  GSFTSINSEGEFIPESMDQMLDPLSLSSPENSGSGSCPSLDSPLDGESYPKSRMPRAQSY
  PDNHQEFSDYDNPIFEKFGKGGTYPRRYHVSYHHQEYNDGRKTFPRARRTQGTSLRSPVS
  FSPTDHSLSTSSGSSIFTPEYDDSRIRRRGSDIDNPTLTVMDISPPSRSPRAPTNWRLGK
  LLGQGAFGRVYLCYDVDTGRELAVKQVQFDPDSPETSKEVNALECEIQLLKNLLHERIVQ
  YYGCLRDPQEKTLSIFMEYMPGGSIKDQLKAYGALTENVTRKYTRQILEGVHYLHSNMIV
  HRDIKGANILRDSTGNVKLGDFGASKRLQTICLSGTGMKSVTGTPYWMSPEVISGEGYGR
  KADIWSVACTVVEMLTEKPPWAEFEAMAAIFKIATQPTNPKLPPHVSDYTRDFLKRIFVE
  AKLRPSADELLRHMFVHYH
• Function: Regulates the JNK and ERK5 pathways by phosphorylating and activating MAP2K5 and MAP2K7. Plays a role in caveolae kiss-and-run dynamics. Component of a protein kinase signal transduction cascade.
• KEGG Pathway:
  MAPK signaling pathway (hsa04010)
  Gap junction (hsa04540)
  GnRH signaling pathway (hsa04912)

Molecular Interaction Atlas (MIA) of This DTT

5 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CI-1040	DMF3DZX	Discovery agent	N.A.	Investigative	[1]
LLZ16407	DM783BP	Discovery agent	N.A.	Investigative	[1]
Ro092210	DM2DXHO	Discovery agent	N.A.	Investigative	[1]
U0126	DM31OGF	Discovery agent	N.A.	Investigative	[1]
URMC-099	DMCJXWK	Discovery agent	N.A.	Investigative	[2]

References

• [1] Pharmacological inhibitors of MAPK pathways. Trends Pharmacol Sci. 2002 Jan;23(1):40-5.
• [2] Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 Oct 24;56(20):8032-48.