Date published: 2025-11-5

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ART2A Inhibitors

ART2A inhibitors are a class of chemical compounds that specifically target and inhibit the enzymatic activity of ADP-ribosyltransferase 2A (ART2A), an enzyme involved in the post-translational modification process known as ADP-ribosylation. ART2A, like other members of the ADP-ribosyltransferase family, catalyzes the transfer of ADP-ribose from nicotinamide adenine dinucleotide (NAD⁺) to specific target proteins, often modifying arginine residues. This modification can regulate the function of proteins, including their stability, activity, and interactions with other cellular components. ART2A inhibitors interfere with this process by blocking the enzyme's ability to catalyze ADP-ribosylation, thereby preventing the modification of target proteins.

Inhibition of ART2A can have widespread effects on cellular signaling and protein function. By inhibiting the activity of ART2A, these compounds disrupt the addition of ADP-ribose units to specific protein substrates, potentially altering their structure, localization, or interactions within the cell. This can impact numerous cellular pathways, as ADP-ribosylation is a key regulator of processes such as signal transduction, protein-protein interactions, and cellular communication. ART2A inhibitors are valuable in research settings, where they are used to dissect the role of ADP-ribosylation in various biological processes. By selectively targeting ART2A, these inhibitors help to clarify the enzyme's role in modulating protein functions and provide a means to study the intricate regulatory mechanisms underlying ADP-ribosylation.

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