Target intelligence / Profile preview

Regulator of G protein signaling 11 (RGS11)

Target
RGS11
Molecular classification
Other (GTPase-activating protein, member of the R7 subfamily of RGS proteins), Signal transduction regulator
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Overview

Regulator of G protein signaling 11 (RGS11) is a member of the R7 subfamily of regulators of G protein signaling (RGS) proteins, characterized by their ability to accelerate the GTPase activity of Gα subunits, terminating signal transduction through G protein-coupled receptors (GPCRs)[2][7]. RGS11 contains a Dishevelled/EGL-10/Pleckstrin (DEP) domain, an RGS domain, and a G protein γ subunit-like (GGL) domain, enabling it to form heterodimers with the Gβ5 protein and function specifically in certain neuronal and retinal signaling pathways[2][3]. In the nervous system, particularly the retina, RGS11 (often paired with RGS7) is critical for the rapid deactivation of G protein signaling, thus shaping the sensitivity and timing of visual response in rod ON-bipolar cells[3]. In context of disease, RGS11 has been implicated in cancer, where its overexpression is associated with increased metastatic potential and poorer prognosis in lung adenocarcinoma through modulation of Rac1-dependent cell migration and ERK signaling[1][6]. No drugs are clinically established to specifically target RGS11 as of the current knowledge, and altering its activity may pose challenges due to its physiological signaling roles in the CNS and retina[1][3].

Other names
RGS11RS11regulator of G-protein signaling 11regulator of G protein signaling 11
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Mechanism of action

Accelerates GTPase activity of Gα subunits, inactivating G-protein coupled receptor signaling[1][7]

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Biological functions

Signal transductionRegulation of G protein-coupled receptor signalingCell migrationModulation of neuronal signaling
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Disease associations

Cancer (metastasis, especially in lung adenocarcinoma)Neurobiology (functions in visual signaling in retina)
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Safety considerations

Possible challenge: modulating RGS11 may affect not only cancer progression (metastasis) but also normal neuronal and retinal function[1][3]
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Biomarkers

Overexpression associated with poor prognosis and metastasis in certain cancers, e.g., lung adenocarcinoma[1][6]

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