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Lysine methyltransferase 5A (SETD8)
- Target
- SETD8
- Molecular classification
- Enzyme, Protein lysine methyltransferase, Histone modification enzyme, Epigenetic regulator
01
Overview
Lysine methyltransferase 5A (SETD8, also known as SET8, Pr-SET7, KMT5A) is a protein lysine methyltransferase enzyme that specifically catalyzes the monomethylation of lysine 20 on histone H4 (H4K20me1) as well as select non-histone proteins such as p53 and PCNA. Its enzymatic activity plays a crucial role in the regulation of chromatin structure, cell cycle progression, DNA replication, and the response to DNA damage. SETD8 activity is tightly controlled and essential for normal cell proliferation, differentiation, and survival. In pathology, overexpression or dysregulation of SETD8 is implicated in cancer progression, poor prognosis, and metastasis, making it an attractive target for therapeutic intervention. Selective pharmacological inhibitors of SETD8 are under preclinical investigation for cancer and potentially other diseases characterized by aberrant epigenetic regulation.
- Other names
- SET8Pr-SET7KMT5A
02
Mechanism of action
Inhibition of SETD8 enzymatic activity, leading to decreased H4K20 monomethylation; Induction of cell cycle arrest; Disruption of DNA repair and chromatin structure; Inhibition of angiogenesis and proliferation (antitumor effects)
03
Biological functions
Histone H4 lysine 20 monomethylation (H4K20me1)DNA replication regulationDNA damage response and repairCell cycle regulationTranscription modulation (both activation and repression; context-dependent)Regulation of chromatin compactionRegulation of cell proliferation and differentiation
04
Disease associations
Cancer (associated with tumorigenesis, progression, and prognosis in multiple cancers)Potential roles in cardiovascular disease (by regulating angiogenesis)Neurological and developmental disorders (implicated via dysregulation of epigenetic functions)
05
Safety considerations
Potential for genomic instability if SETD8 is over-inhibited, due to impaired DNA damage responseRisk of off-target effects with insufficiently selective inhibitorsEffects on normal cell proliferation and unintended toxicity in proliferating tissues
06
Interacting drugs
BVT-948 (selective SETD8 inhibitor)
1 more in the full profile.
07
Biomarkers
H4K20me1 levels (used as a biomarker for SETD8 activity)SETD8 protein or mRNA expression (prognostic marker in various cancers)
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