Target intelligence / Profile preview

Histone H2A.Z (H2A.Z) (H2A.Z)

Target
H2A.Z
Molecular classification
Histone variant, Chromatin-associated protein, Epigenetic regulator
01

Overview

Histone H2A.Z is a highly conserved H2A histone variant that plays a critical role in regulating chromatin structure and gene expression. Unlike canonical histones, H2A.Z is deposited into specific genomic regions, such as promoters and enhancers, by specialized remodeling complexes like SRCAP and p400/TIP60 (UniProt P0C0S8). Its presence can either facilitate or repress transcription depending on the cellular context and its post-translational modifications, such as acetylation or ubiquitination (PubMed: 28611434). In many cancers, H2A.Z is significantly overexpressed and is associated with increased cell proliferation, epithelial-mesenchymal transition, and poor clinical outcomes (PubMed: 31515460). Consequently, it has emerged as a potential therapeutic target and diagnostic biomarker in oncology. Current pharmacological strategies often focus on inhibiting the enzymes responsible for its deposition or modification, as well as using nucleic acid-based therapies to reduce its expression (PubMed: 33806134). Because H2A.Z is essential for normal development, therapeutic interventions must carefully balance efficacy against potential systemic toxicity.

Other names
H2AFZH2AZH2A.Z-1H2A/zH2A histone family member Z
02

Mechanism of action

Modulation of chromatin accessibility through the inhibition of H2A.Z deposition by the SRCAP complex or the reduction of H2A.Z protein levels via nucleic acid-based therapies.

03

Biological functions

Chromatin remodelingGene expression regulationDNA damage repairCell cycle regulationChromosome segregation
04

Disease associations

CancerNeurodevelopmental disorder
05

Safety considerations

Potential for systemic transcriptional dysregulationEssentiality in early embryonic developmentRisk of genomic instability
06

Interacting drugs

Experimental antisense oligonucleotides

3 more in the full profile.

07

Biomarkers

H2A.Z protein expression levelsH2AFZ mRNA levelsH2A.Z acetylation status

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