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Lysine methyltransferase 5C (KMT5C)
- Target
- KMT5C
- Molecular classification
- Enzyme, Histone methyltransferase, Epigenetic modifier
01
Overview
Lysine methyltransferase 5C (KMT5C, also known as SUV420H2) is an enzyme that catalyzes the trimethylation of lysine 20 on histone H4 (H4K20me3), a key repressive chromatin mark. It plays critical roles in chromatin compaction, DNA damage response, cell cycle control, and transcriptional repression. KMT5C is essential for maintaining genome integrity, and its loss or dysregulation is associated with tumor progression, metastasis, and poor prognosis in multiple cancer types. Additionally, KMT5C has a regulatory function in adipocyte thermogenesis and energy metabolism, implicating it in metabolic diseases such as obesity and diabetes. The enzyme is considered a therapeutic prospect for epigenetic cancer and metabolic disease intervention, but direct clinical inhibitors have not yet reached advanced development stages.
- Other names
- SUV420H2Histone-lysine N-methyltransferase KMT5C
02
Mechanism of action
Inhibition of H4K20 trimethylation; Epigenetic modulation leading to reactivation of tumor suppressor genes or inhibition of oncogenic programs
03
Biological functions
Histone methylation (specifically trimethylation of lysine 20 on histone H4, i.e., H4K20me3)Chromatin structure regulationGenome integrity maintenance (DNA damage repair, DNA replication)Cell cycle controlTranscriptional repressionRegulation of adipocyte thermogenesis
04
Disease associations
Cancer (notably breast, pancreatic, renal cell, and leukemia)Metabolic disease (obesity, type 2 diabetes)Other (potential role in chromatin-related disorders)
05
Safety considerations
Off-target epigenetic effects (risk of affecting genome stability, DNA repair, or unwanted cell cycle arrest due to broad action on histone methylation)Potential impact on stem/progenitor cell states and heterochromatin integrity
06
Interacting drugs
No specific approved drugs directly targeting KMT5C were identified in the current sources; however, KMT5C is being studied as a potential epigenetic drug target in cancer and metabolic disease.
07
Biomarkers
H4K20me3 levels (epigenetic biomarker in cancer prognosis, e.g., breast cancer, leukemia)KMT5C expression levels (indicator in several cancer types and metabolic disorders)
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