{"entity":{"id":"lsd1","kind":"target","name":"LSD1 (KDM1A)","aka":["LSD1","lysine-specific demethylase 1","lysine demethylase 1A","AOF2"],"tldr":"LSD1 is an enzyme that removes small chemical tags from the proteins DNA is wound around, switching genes off or on. Many cancers carry a lot of it and it helps keep leukaemia cells immature; several LSD1 inhibitors have been tested in blood cancers and solid tumours.","summary":"KDM1A, usually called LSD1 (chromosome 1p36.12), is a FAD-dependent histone demethylase that removes methyl groups from lysine 4 and lysine 9 of histone H3, acting as a corepressor or coactivator depending on its partners; on nucleosomes it needs the CoREST complex (UniProt O60341). A 2023 review in Frontiers in Pharmacology states that LSD1 is overexpressed in many cancers, including breast, gastric, prostate, hepatocellular and oesophageal cancer and acute myeloid leukaemia, where it blocks differentiation and increases proliferation, migration and invasiveness, and that nine LSD1 inhibitors had entered clinical trials, among them iadademstat and bomedemstat (doi:10.3389/fphar.2023.1120911). In OnCo, REC-4539 is described by its developer as a reversible, brain-penetrant LSD1 inhibitor; the technology record lsd1-inhibitors covers the class.","asOf":"2026-11-03","links":[{"label":"HGNC HGNC:29079","url":"https://www.genenames.org/data/gene-symbol-report/#!/hgnc_id/HGNC:29079"},{"label":"UniProt O60341","url":"https://www.uniprot.org/uniprotkb/O60341/entry"},{"label":"NCBI Gene 23028","url":"https://www.ncbi.nlm.nih.gov/gene/23028"},{"label":"LSD1 inhibitors for cancer treatment (Front Pharmacol 2023)","url":"https://doi.org/10.3389/fphar.2023.1120911"}],"tags":["pipeline-gap-target"],"related":[],"cancers":["aml","sclc"],"sections":[],"technologies":["lsd1-inhibitors"],"targets":[],"drugs":["rec-4539"],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["Prevalence not recorded: HGNC, UniProt and the paper cited give no positivity rate."],"provenance":{"editedBy":"OnCo gap audit, class 5 targets (HGNC REST, UniProt REST, Europe PMC, corpus drug records)","editedOn":"2026-11-03"},"symbol":"KDM1A","role":["drug-target"],"sources":[],"specificitySources":[],"hgnc":"HGNC:29079","ensembl":"ENSG00000004487","uniprot":"O60341","entrez":"23028","biology":"Flavin-dependent amine oxidase that demethylates mono- and dimethylated H3K4 (a mark of active genes) and, with partners, H3K9; it also acts on non-histone proteins (UniProt O60341).","whereFound":["Acute myeloid leukaemia and several solid tumours (overexpression, doi:10.3389/fphar.2023.1120911)","Small cell lung cancer and AML (REC-4539 trial)"],"targetClass":"enzyme","prevalence":[]},"route":"/targets/lsd1/","neighbours":{"cancer":[{"id":"aml","kind":"cancer","name":"Acute myeloid leukaemia","route":"/cancers/aml/"},{"id":"sclc","kind":"cancer","name":"Small-cell lung cancer","route":"/cancers/sclc/"}],"technology":[{"id":"lsd1-inhibitors","kind":"technology","name":"LSD1 inhibitors","route":"/technologies/lsd1-inhibitors/"}],"drug":[{"id":"rec-4539","kind":"drug","name":"REC-4539","route":"/drugs/rec-4539/"}]}}