KDM1A


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KDM1A

A gene on chromosome 1p36.12 that encodes a demethylase which acts on histone H3 as a coactivator or a co-repressor, depending on the context.
References in periodicals archive ?
IMG-7289 is a small molecule developed by Imago BioSciences that inhibits lysine-specific demethylase 1 (LSD1 or KDM1A), an enzyme regulating cytokine expression and shown to be vital in sustaining self-renewal in cancer stem/progenitor cells, particularly neoplastic bone marrow cells.
According to the company, IMG-7289 is a small molecule developed by inhibits lysine-specific demethylase 1 (LSD1 or KDM1A), an enzyme regulating gene expression in hematopoietic cells.
In addition, KDM1A, a flavin adenine dinucleotide- (FAD-) dependent lysine-specific demethylase specifically with monomethyl- and dimethylhistone H3 lysine-4 (H3K4) and lysine-9 (H3K9) substrate, is an important regulator of MLL-AF9 leukemia stem cell (LSC) oncogenic potential by blocking differentiation [134].
Roche and Oryzon Genomics SA today announced they have entered into a worldwide collaboration to research, develop and commercialize inhibitors of Lysine Specific Demethylase-1 (LSD1; KDM1A), an epigenetic modulator that regulates gene expression.
IMG-7289 is a small molecule that inhibits lysine-specific demethylase 1 (LSD1 or KDM1A), an enzyme regulating gene expression in hematopoietic cells.
The company said its clinical programe is focused on three druggable intervention points with potential to improve safety and efficacy of current AML combination therapies, around which it has robust IP and substantial freedom to operate: RASP-101, an established anticancer therapeutic for treating nucleophosmin (NPM1) mutated acute myeloid leukemia (AML); RASP-201, an inhibitor of lysine specific histone demethylase 1 (LSD1 or KDM1A), which is overexpressed in several human cancers including AML plays an important role in epigenetic modification that contributes to cellular proliferation; and, RASP-301, high affinity, NPM1 binding molecules exhibiting selective cytotoxic activity on AML cells.