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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.
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.
In plain words · 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.
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.
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).
1 product aims at LSD1 (KDM1A): small molecules. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
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).
REC-4539 is an experimental small molecule LSD1 inhibitor from Recursion Pharmaceuticals, in phase 1 trials for small-cell lung cancer, acute myeloid leukaemia and solid tumours.
Query for this target: (TITLE:"LSD1" OR ABSTRACT:"LSD1" OR TITLE:"KDM1A" OR ABSTRACT:"KDM1A" OR TITLE:"lysine-specific demethylase 1" OR ABSTRACT:"lysine-specific demethylase 1" OR TITLE:"lysine demethylase 1A" OR ABSTRACT:"lysine demethylase 1A" OR TITLE:"AOF2" OR ABSTRACT:"AOF2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about LSD1 (KDM1A), not a curated reading list.
Shares Acute myeloid leukaemia and the tag pipeline-gap-target.
Shares Acute myeloid leukaemia and the tag pipeline-gap-target.
Shares Acute myeloid leukaemia and the tag pipeline-gap-target.
Shares REC-4539, Small-cell lung cancer.
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