MLchartDataset catalogue

LSD1 inhibitor SYHA1807

Term · Oncology and biomedicine · MLC-T-ONC-014892

An orally available inhibitor of lysine-specific demethylase 1 (LSD1; KDM1A), with potential antineoplastic activity. Upon oral administration, LSD1 inhibitor SYHA1807 targets, binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. LSD1 is overexpressed in a number of tumor cell types. LSD1 acts on histone H3 as a transcription co-repressor through demethylation of lysine 4 (H3K4) or as a transcription co-activator through demethylation of lysine 9 (H3K9).

Table 1. Record
IdentifierMLC-T-ONC-014892
FieldOncology and biomedicine
Synonymslysine-specific demethylase 1 inhibitor SYHA1807
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-014892",
  "term": "LSD1 inhibitor SYHA1807",
  "field": "Oncology and biomedicine",
  "definition": "An orally available inhibitor of lysine-specific demethylase 1 (LSD1; KDM1A), with potential antineoplastic activity. Upon oral administration, LSD1 inhibitor SYHA1807 targets, binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. LSD1 is overexpressed in a number of tumor cell types. LSD1 acts on histone H3 as a transcription co-repressor through demethylation of lysine 4 (H3K4) or as a transcription co-activator through demethylation of lysine 9 (H3K9).",
  "synonyms": [
    "lysine-specific demethylase 1 inhibitor SYHA1807"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/lsd1-inhibitor-syha1807/"
}

Record 10,342 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.