Target intelligence / Profile preview

Lysine-specific demethylase 1A mRNA (KDM1A mRNA)

Target
KDM1A mRNA
Molecular classification
Messenger RNA, Nucleic acid
01

Overview

Lysine-specific demethylase 1A (LSD1) mRNA is the messenger RNA transcript that encodes the KDM1A enzyme, a pivotal epigenetic regulator. The resulting LSD1 protein is a flavin-adenine dinucleotide (FAD)-dependent amine oxidase that specifically demethylates mono- and dimethylated histone H3 lysine 4 (H3K4) and lysine 9 (H3K9), thereby modulating gene transcription (Shi et al., 2004 [2]). In various malignancies, including acute myeloid leukemia (AML) and small cell lung cancer (SCLC), LSD1 mRNA is frequently overexpressed, which leads to high protein levels that suppress cellular differentiation and promote oncogenic growth (Mohammad et al., 2015 [3]). While clinical-stage drugs are primarily small molecules targeting the protein's catalytic site, targeting the LSD1 mRNA via antisense oligonucleotides (ASOs) or small interfering RNAs (siRNAs) offers a strategy to deplete the entire protein pool, including its non-enzymatic scaffolding functions (Wang et al., 2015 [4]). This transcript-level intervention is a significant area of research for its potential to provide more comprehensive inhibition of LSD1-mediated signaling compared to enzymatic inhibitors alone. Furthermore, reducing mRNA levels can prevent the formation of the LSD1-CoREST complex, which is essential for its stability and function in many cancer types (UniProt Consortium, 2023 [1]).

Other names
LSD1 mRNAAOF2 mRNABHC110 mRNAKDM1 mRNA transcript
02

Mechanism of action

RNA interference (RNAi) or RNase H-mediated degradation of the mRNA transcript, preventing the translation of the LSD1 protein.

03

Biological functions

Protein codingEpigenetic regulation (via protein product)Gene expression regulation
04

Disease associations

Acute myeloid leukemiaSmall cell lung cancerProstate cancerBreast cancer
05

Safety considerations

Off-target hybridizationDelivery to target tissuesInnate immune response to exogenous nucleic acids
06

Interacting drugs

Antisense oligonucleotides (experimental)

1 more in the full profile.

07

Biomarkers

LSD1 mRNA expression levelsLSD1 protein levelsH3K4me1/2 methylation status

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