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Target intelligence / Profile preview
Lysine demethylase 6B (KDM6B)
- Target
- KDM6B
- Molecular classification
- Enzyme, Histone modification enzyme (Histone demethylase), Epigenetic regulator
01
Overview
Lysine demethylase 6B (KDM6B, also known as JMJD3) is an epigenetic enzyme that removes repressive trimethyl marks from lysine 27 of histone H3 (H3K27me3), thereby activating transcription. KDM6B plays critical roles in embryonic development, cell differentiation, immune cell maturation, and epithelial-mesenchymal transition (EMT). Aberrant expression or mutation of KDM6B is associated with cancer metastasis, neurodevelopmental syndromes, and inflammatory diseases. Selective small molecule inhibitors such as GSK-J1 and GSK-J4 are used to study its function and therapeutic potential, particularly for inflammation and cancer.
- Other names
- JMJD3JmjC domain-containing protein 3
02
Mechanism of action
Inhibition leads to retention of H3K27 methylation, repression of target gene expression, modulation of inflammatory and differentiation pathways.
03
Biological functions
Gene expression regulation (via demethylation of H3K27me3)Chromatin remodelingCell differentiation (including neuronal and immune cell maturation)Epithelial-mesenchymal transition (EMT)Immune response modulationCell proliferationNeuronal development and diversification
04
Disease associations
Cancer (breast cancer metastasis, prostate cancer, general carcinogenesis)Neurodevelopmental disordersInflammationCerebral folate deficiencyAutism spectrum disorder and intellectual disability (via gene mutations)
05
Safety considerations
Inhibition or loss of function impairs normal cell differentiation and immune function, potentially leading to developmental defects, compromised tissue repair, and immune dysfunctionPossible broad effects due to role in global gene expression regulation.
06
Interacting drugs
GSK-J1 (selective KDM6 family inhibitor; in vitro and research use)
1 more in the full profile.
07
Biomarkers
Overexpression in invasive cancersMutational screening (for neurodevelopmental disorders and cerebral folate deficiency)
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