Date published: 2025-9-19

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RGS7 (regulator of G protein signaling) Inhibitors

RGS7 inhibitors are a class of chemical compounds that specifically target and inhibit the function of regulator of G protein signaling 7 (RGS7), a member of the RGS protein family involved in the modulation of G protein-coupled receptor (GPCR) signaling pathways. RGS7 acts as a GTPase-activating protein (GAP), accelerating the hydrolysis of GTP to GDP on the α subunit of G proteins, thereby terminating the signal transduction initiated by GPCR activation. By shortening the active state of G proteins, RGS7 plays a crucial role in regulating the intensity and duration of cellular responses to various extracellular stimuli, such as hormones, neurotransmitters, and sensory signals. Inhibitors of RGS7 disrupt this regulatory function, allowing G proteins to remain active for longer periods, which can alter downstream signaling events within the cell.

Inhibiting RGS7 provides a valuable tool for studying GPCR signaling dynamics and the mechanisms that control signal termination in cells. By blocking RGS7 activity, researchers can observe the effects of prolonged G protein activation, revealing insights into how cells respond to sustained signals and the role of RGS proteins in maintaining signal fidelity. Additionally, RGS7 is involved in specific cellular processes, such as neuronal signaling and sensory perception, making its inhibition particularly useful for understanding how G protein regulation impacts these specialized functions. The study of RGS7 inhibitors allows for a deeper exploration of the fine-tuned balance between signal activation and deactivation within GPCR pathways, highlighting the importance of precise regulation in maintaining cellular communication and overall physiological function.

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