CATH Classification

Domain Context

CATH Clusters

Superfamily Phosphorylase Kinase; domain 1
Functional Family Mitogen-activated protein kinase kinase kinase 5

Enzyme Information

2.7.11.25
Mitogen-activated protein kinase kinase kinase.
based on mapping to UniProt Q99683
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)

Q99683
M3K5_HUMAN
Homo sapiens
Mitogen-activated protein kinase kinase kinase 5

PDB Structure

PDB 5UOR
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure.
Lanier, M., Pickens, J., Bigi, S.V., Bradshaw-Pierce, E.L., Chambers, A., Cheruvallath, Z.S., Cole, D., Dougan, D.R., Ermolieff, J., Gibson, T., Halkowycz, P., Hirokawa, A., Ivetac, A., Miura, J., Nunez, E., Sabat, M., Tyhonas, J., Wang, H., Wang, X., Swann, S.
ACS Med Chem Lett