{"meta":{"totalResults":1,"from":0},"results":[{"aliases":[{"type":"CodeName","name":"RO7051790"},{"type":"CodeName","name":"ORY 1001"},{"type":"CodeName","name":"RG6016"},{"type":"CodeName","name":"RG 6016"},{"type":"CodeName","name":"RO 7051790"},{"type":"Synonym","name":"trans-N1-((1R,2S)-2-phenylcyclopropyl)-1,4-cyclohexanediamine"},{"type":"CodeName","name":"ORY-1001"},{"type":"ChemicalStructureName","name":"1,4-cyclohexanediamine, N1-((1R,2S)-2-phenylcyclopropyl)-, trans-"},{"type":"CASRegistryName","name":"1431304-21-0"}],"definition":{"html":"An orally available inhibitor of lysine specific histone demethylase 1 (KDM1A; LSD1), with potential antineoplastic activity. Upon administration, iadademstat 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 H3 (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, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family, is overexpressed in certain tumor cells and plays a key role in in the regulation of gene expression, tumor cell growth and survival.","text":"An orally available inhibitor of lysine specific histone demethylase 1 (KDM1A; LSD1), with potential antineoplastic activity. Upon administration, iadademstat 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 H3 (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, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family, is overexpressed in certain tumor cells and plays a key role in in the regulation of gene expression, tumor cell growth and survival."},"drugInfoSummaryLink":null,"nciConceptId":"C131908","nciConceptName":"Iadademstat","termId":786364,"name":"iadademstat","firstLetter":"i","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"iadademstat"}],"links":null}