CATH Classification

Domain Context

CATH Clusters

Superfamily Phosphorylase Kinase; domain 1
Functional Family Mitogen-activated protein kinase kinase kinase

Enzyme Information

2.7.11.25
Mitogen-activated protein kinase kinase kinase.
based on mapping to UniProt P80192
ATP + a protein = ADP + a phosphoprotein.
-!- This enzyme phosphorylates and activates its downstream protein kinase, EC 2.7.12.2, but requires MAPKKKK for activation. -!- Some members of this family can be activated by p21-activated kinases (PAK/STE20) or Ras. -!- While c-Raf and c-Mos activate the classical MAPK/ERK pathway, MEKK1 and MEKK2 preferentially activate the c-Jun N-terminal protein kinase(JNK)/stress-activated protein kinase (SAPK) pathway. -!- Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. -!- Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e.g. insulin and growth hormone), mitogens (e.g. epidermal growth factor and platelet-derived growth factor), vasoactive peptides (e.g. angiotensin-II and endothelin), inflammatory cytokines of the tumor necrosis factor (TNF) family and environmental stresses such as osmotic shock, ionizing radiation and ischemeic injury. -!- Formerly EC 2.7.1.37.

UniProtKB Entries (1)

P80192
M3K9_HUMAN
Homo sapiens
Mitogen-activated protein kinase kinase kinase 9

PDB Structure

PDB 3DTC
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Hudkins, R.L., Diebold, J.L., Tao, M., Josef, K.A., Park, C.H., Angeles, T.S., Aimone, L.D., Husten, J., Ator, M.A., Meyer, S.L., Holskin, B.P., Durkin, J.T., Fedorov, A.A., Fedorov, E.V., Almo, S.C., Mathiasen, J.R., Bozyczko-Coyne, D., Saporito, M.S., Scott, R.W., Mallamo, J.P.
J.Med.Chem.