Target intelligence / Profile preview

Mitogen-activated protein kinase kinase kinase kinase 5 (MAP4K5)

Target
MAP4K5
Molecular classification
Enzyme, Serine/threonine protein kinase, Mitogen-activated protein kinase family
01

Overview

Mitogen-activated protein kinase kinase kinase kinase 5 (MAP4K5) is a cytoplasmic serine/threonine kinase and member of the MAPK signaling cascade, particularly upstream of JNK activation involved in cellular stress responses. It acts by transferring phosphate groups to specific substrate proteins and has homologs among yeast kinases functioning at the initiation of MAP kinase pathways. MAP4K5 participates in the regulation of immune responses, cell differentiation, and may have roles in disease states such as cancer and metabolic disorders. Its expression is cytoplasmic and tissue-specific, especially in smooth muscle and lymphoid organs, but its full physiological and pathological roles remain under investigation.

Other names
MAP4K5GCKRKHSKHS1MAPKKKK5Kinase homologous to SPS1/STE20Germinal center kinase-related
02

Mechanism of action

Drugs hypothetically targeting MAP4K5 would likely act as kinase inhibitors, blocking its phosphorylation activity and downstream activation of the JNK pathway.

03

Biological functions

Signal transductionStress responseActivation of Jun N-terminal kinase (JNK)Regulation of immune cell signaling and development (e.g., B and T lymphocytes)Possible role in Wnt-induced Rac-JNK signaling
04

Disease associations

Cancer (e.g., acute myeloid leukemia)Autoimmune inflammationObesityType 2 diabetes
05

Safety considerations

Inhibition may dysregulate immune function, stress responses, and potentially disrupt normal cell cycle and differentiation, warranting caution in therapeutic development for autoimmune, metabolic, or oncological indications.
06

Interacting drugs

No approved or investigational drugs directly targeting MAP4K5 are listed in major databases as of now. Some ligands and molecules used in screening may exist, as indicated by structure-activity data in pharmacology resources, but no clinical drug is specified.
07

Biomarkers

No validated biomarkers for patient selection or efficacy monitoring specific to MAP4K5 status are reported as of current knowledge.

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