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Regulator of G protein signaling 10 (RGS10)

Target
RGS10
Molecular classification
Enzyme (specifically, GTPase-activating protein), Other (signal transduction regulator)
01

Overview

Regulator of G protein signaling 10 (RGS10) is a member of the RGS protein family, which functions as a GTPase-activating protein (GAP) specific for Gα subunits of heterotrimeric G proteins, particularly in the Gi/o/z class[1][3][5]. RGS10 accelerates the conversion of active GTP-bound Gα subunits to their inactive GDP-bound form, thereby terminating GPCR signaling. It is a small cytosolic protein highly expressed in the brain, immune cells, platelets, and cells involved in bone remodeling. Distinct isoforms (RGS10A and RGS10B) exist due to alternative splicing. RGS10 regulates critical biological processes including signal transduction, immune response, osteoclast and chondrocyte differentiation, platelet activation, and cardiac remodeling. Dysregulation of RGS10 has been implicated in a range of pathologies, such as neurodegenerative diseases, cancer, cardiovascular disease, osteopetrosis, thrombosis, and inflammatory disorders. Currently, there are no approved drugs targeting RGS10, but its pivotal regulatory roles make it a promising therapeutic target for multiple conditions[2][3][4][5].

Other names
RGS10Regulator of G-protein signaling 10Regulator of G protein signalling 10RGS10A (isoform)RGS10B (isoform)
02

Mechanism of action

GTPase-activating protein; acts by accelerating GTP hydrolysis on Gα subunits to terminate signaling downstream of G protein-coupled receptors (GPCRs)[1][5]. Negative regulation of Gi/o/z signaling pathways[1][5].

03

Biological functions

Signal transductionTermination of GPCR signalingRegulation of immune responseCell differentiation (osteoclasts, chondrocytes)Platelet functionRegulation of cardiac remodeling
04

Disease associations

Neurodegenerative disease (e.g., Parkinson’s disease, multiple sclerosis)Cancer (e.g., ovarian cancer)Cardiovascular disease (e.g., pathological cardiac remodeling)Hematological/platelet disorders (thrombosis)Metabolic bone disease (osteopetrosis)Inflammation
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Safety considerations

As an intracellular regulatory protein without current direct therapeutic agents, major safety concerns have not been well defined for RGS10 inhibition or activation. However, dysregulation is associated with increased thrombosis, altered immune function, osteopetrosis, and various disease risks[5].
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Interacting drugs

No specific approved drugs directly targeting RGS10 are clearly documented in the current literature[5].
07

Biomarkers

Elevated or suppressed RGS10 expression can indicate involvement in diseases such as cardiac remodeling, neurodegenerative disorders, osteopetrosis, chemoresistant ovarian cancer, and inflammatory conditions[2][3][5].Increased RGS10 in platelets may correlate with aspirin resistance and metabolic syndrome[5].

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