Date published: 2025-10-11

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ART2B Inhibitors

ART2B inhibitors are chemical compounds that specifically block the activity of ADP-ribosyltransferase 2B (ART2B), an enzyme that facilitates the transfer of ADP-ribose molecules from NAD⁺ to specific protein substrates, primarily modifying arginine residues. This process, known as ADP-ribosylation, plays a significant role in regulating the function of proteins by altering their activity, interactions, and stability. ART2B, as a member of the broader ADP-ribosyltransferase family, is involved in modulating key protein functions within various biological pathways. ART2B inhibitors are designed to prevent this modification by directly binding to the enzyme's active site or another regulatory domain, blocking its enzymatic function and thereby halting the transfer of ADP-ribose units to target proteins.

The inhibition of ART2B affects a variety of cellular mechanisms that depend on ADP-ribosylation, influencing processes such as protein signaling, cell communication, and protein-protein interactions. By disrupting ART2B's ability to modify proteins, ART2B inhibitors can induce changes in protein conformations, affect their binding affinities, or modulate their cellular localization. These inhibitors are essential tools in biochemical and cellular studies, helping researchers investigate the specific functions of ADP-ribosylation and the role of ART2B in controlling protein dynamics. Through selective inhibition of ART2B, researchers can explore the enzyme's contribution to a range of molecular pathways, shedding light on the regulatory effects that ADP-ribosylation has on cellular homeostasis, signaling cascades, and protein networks. The specificity of ART2B inhibitors provides a critical approach to studying enzyme function in complex biological systems.

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