Target intelligence / Profile preview

Non-histone protein acetylation modulation

Molecular classification
Histone modification, Post-translational modification, Other
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Overview

Non-histone protein acetylation modulation refers to the dynamic regulation of acetylation (primarily lysine acetylation) on proteins other than histones, mediated by acetyltransferases and deacetylases. This post-translational modification can regulate protein stability, enzymatic activity, protein-protein interactions, subcellular localization, and cross-talk with other modifications. Non-histone protein acetylation is involved in a broad range of cellular processes, including gene transcription, DNA repair, cell division, metabolism, and cell signaling, and dysregulation is implicated in diseases such as cancer and neurodegeneration. Instead of designating a single molecular target, this term encompasses a set of regulatory enzymes (like lysine acetyltransferases and deacetylases) and their non-histone substrates. Drugs that influence non-histone acetylation, such as HDAC inhibitors, have therapeutic relevance but act on the modifying enzymes rather than on a single substrate.

Other names
Non-histone acetylation regulationNon-histone protein acetylationNon-histone lysine acetylationNon-histone protein acetylome modulation
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Mechanism of action

Inhibition of deacetylase activity (increases acetylation levels); Inhibition of acetyltransferase activity (decreases acetylation levels)

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Biological functions

Gene transcriptionDNA damage repairCell divisionProtein foldingAutophagyCell signalingMetabolismEnzyme regulationProtein stabilitySubcellular localization
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Disease associations

CancerNeurodegenerative diseaseInflammationMetabolic disordersOther
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Safety considerations

Off-target effects due to broad impact on many cellular proteinsToxicity from global modulation of protein acetylationPotential effects on normal cellular and physiological processes
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Interacting drugs

Histone deacetylase (HDAC) inhibitors (e.g., vorinostat, panobinostat)

1 more in the full profile.

07

Biomarkers

Levels of acetylated non-histone proteins (context dependent)Specific modification sites on proteins (context dependent)Acetylation of α-tubulin, p53, and others are sometimes investigated

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