Target intelligence / Profile preview

Regulator of G-protein signaling 1 (RGS1)

Target
RGS1
Molecular classification
Enzyme (GTPase-activating protein), Signal transduction regulator, Regulatory protein
01

Overview

Regulator of G-protein signaling 1 (RGS1) is a cytosolic protein that functions as a GTPase-activating protein (GAP) for G protein alpha subunits, terminating GPCR signaling by accelerating GTP hydrolysis. RGS1 plays essential roles in immune cell migration, tissue residency, and trafficking by selectively deactivating chemokine signaling in B and T lymphocytes. It is involved in the regulation of the cell cycle and proliferation, acting as an oncogene in several cancers, including ovarian, lung, gastric, and hematological malignancies. RGS1 is associated with autoimmune diseases and chronic inflammation by modulating lymphocyte behavior. Due to its central regulatory role, RGS1 is under intensive study as a potential therapeutic target and biomarker in oncology and immunology, though clinical drug interactions have not yet been fully established.

Other names
BL34IER1IR20B-cell activation protein BL34Early response protein 1R20Immediate-early response 1Epididymis secretory protein Li 87HEL-S-87
02

Mechanism of action

Inhibition of RGS1 activity may suppress GPCR-mediated cell signaling by blocking GTPase acceleration on G protein alpha subunits, leading to altered chemotactic, proliferative, and inflammatory responses. RGS1 involvement in NF-kB pathway activation in cancer cells; inhibition of this pathway halts cancer cell proliferation. Modulation of immune cell trafficking via impact on chemokine receptor signaling.

03

Biological functions

Signal transduction (especially regulation of GPCR pathways)Immune response (regulation of lymphocyte migration and trafficking; inhibition of B cell chemotaxis, modulation of T cell tissue residency)Cell cycle regulation and cell proliferation (impact in cancer growth)Chemokine receptor signaling regulationInflammatory response (implicated in chronic inflammation)
04

Disease associations

Cancer (oncogene function in ovarian, lung, gastric, and hematological cancers)Inflammation (autoimmune diseases, chronic intestinal inflammation, colitis)Infection (role in immune surveillance against pathogens)LymphomaCeliac Disease
05

Safety considerations

Targeting RGS1 may impact essential immune cell trafficking and tissue-resident T cell maintenance, potentially affecting infection control and autoimmune responsesTherapeutic modulation of RGS1 could alter B and T lymphocyte migration, impacting both protective immunity and risk of immune dysregulationRGS1 is widely expressed and involved in fundamental regulatory pathways, so off-target effects and immune suppression must be considered
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Interacting drugs

JSH-23
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Biomarkers

Elevated RGS1 expression is a biomarker of poor prognosis in ovarian cancer, multiple myeloma, non-Hodgkin lymphoma, and other malignanciesRGS1 expression in tissue-resident memory T cells may serve as a marker of immune surveillance capacity

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