Target intelligence / Profile preview

Lysine-utilizing enzymes and transporters

Molecular classification
Enzyme, Transporter
01

Overview

Lysine-utilizing enzymes and transporters constitute a diverse functional group of proteins involved in the cellular uptake, catabolic processing, and post-translational modification of the essential amino acid lysine. This category includes key epigenetic regulators such as lysine-specific demethylase 1 (LSD1/KDM1A) and various lysine acetyltransferases (KATs), which modulate gene expression by modifying histone tails (UniProt O60341). It also encompasses metabolic enzymes like aminoadipate-semialdehyde synthase (AASS), which is central to the primary lysine degradation pathway in mitochondria (UniProt Q9UDR5). Furthermore, solute carrier transporters such as SLC7A1 (CAT-1) and SLC7A2 (CAT-2) are responsible for the high-affinity transport of lysine across the plasma membrane (UniProt P11370). Dysregulation of these proteins is linked to several pathologies, including various cancers where LSD1 promotes oncogenic gene expression, and metabolic disorders like hyperlysinemia. Therapeutic interventions targeting this group include small-molecule inhibitors of LSD1, such as iadademstat and bomedemstat, which are currently being evaluated in clinical trials for myeloid malignancies (NCT03514407, NCT03136185).

Other names
Lysine metabolic enzymesLysine transportersBasic amino acid transportersLysine-modifying enzymesCationic amino acid transporters
02

Mechanism of action

Inhibition of lysine-specific demethylase 1 (LSD1), inhibition of lysine acetyltransferases (KATs), or modulation of lysine transport via solute carrier proteins.

03

Biological functions

Amino acid metabolismEpigenetic regulationProtein synthesisTransportSignal transduction
04

Disease associations

CancerMetabolic diseaseInfectionNeurodegenerative disease
05

Safety considerations

Hematological toxicity (e.g., thrombocytopenia)Off-target epigenetic modificationsDisruption of systemic amino acid homeostasis
06

Interacting drugs

Iadademstat

4 more in the full profile.

07

Biomarkers

Plasma lysine levelsHistone H3 lysine 4 (H3K4) methylation statusAminoadipate-semialdehyde synthase (AASS) activitySaccharopine levels

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