Target intelligence / Profile preview

Lysine-specific demethylase 1A (LSD1)

Target: LSD1
Molecular classification: Enzyme, Histone modification, Amine Oxidase, Transcription factor

Overview

Lysine-specific demethylase 1A (KDM1A), also known as LSD1, is a flavin-dependent amine oxidase that catalyzes the removal of mono- and di-methyl groups from lysine residues on histone proteins, specifically histone H3 at lysines 4 (H3K4me1/2) and, under certain conditions, lysine 9 (H3K9me1/2). This activity regulates chromatin structure and thereby controls gene transcription. Overexpression or dysregulation of KDM1A has been implicated in various cancers.

Other names: AOF2BHC110KDM1A

Mechanism of action

Inhibition of histone demethylation

Biological functions

Epigenetic regulationDevelopmentHematopoiesisTranscriptional repressionTranscriptional activationOocyte growthEmbryogenesisTissue-specific differentiation

Disease associations

Cancer progressionCancer maintenanceAcute myeloid leukemia (AML)Solid tumorsBreast cancerCervical cancer

Safety considerations

Overexpression or dysregulation implicated in various cancersPromotes proliferation, impairs differentiation, enhances cell motility/invasivenessContributes to poor prognosis by maintaining stemness features or blocking cellular maturation programsShapes immune responses within tumor microenvironments by influencing macrophage polarization and T cell exhaustion states

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