Target intelligence / Profile preview

Arrestin beta-1 (ARRB1)

Target
ARRB1
Molecular classification
Adaptor protein, Signal transducer, Regulatory protein, Other
01

Overview

Arrestin beta-1 (ARRB1) is a multifunctional adaptor protein that regulates G protein-coupled receptor (GPCR) signaling by promoting receptor desensitization and internalization following ligand activation[1][2][3][4][5]. Beyond this canonical role, ARRB1 acts as a scaffold for a variety of intracellular signaling pathways, mediating both G protein-dependent and independent signaling, and is involved in diverse cellular functions including cell proliferation, metabolism, cytoskeletal organization, gene transcription, and epigenetic regulation[2][3]. ARRB1 is widely expressed in the central nervous system and immune cells and is implicated in the pathogenesis of diseases such as cancer, neurodegenerative disorders, and cardiovascular disease; its activity modulates key pathways through interactions with enzymes, kinases, transcription factors, and epigenetic regulators[3][1][2][4][5].

Other names
Beta-arrestin-1ARRB1ARR1Arrestin beta-1Non-visual arrestin-2Arrestin 2ARB1Beta-arrestin 1Non-visual arrestin 2
02

Mechanism of action

Modulation of signaling pathways via GPCR desensitization, Scaffold for MAPK/ERK activation, Regulation of receptor endocytosis and ubiquitination, Modulation of metabolic enzymes (PKM2), Recruitment of transcription co-activators (histone acetyltransferases)

03

Biological functions

Signal transductionDesensitization of G protein-coupled receptorsScaffolding and modulation of intracellular signalingEndocytosis of receptorsRegulation of gene transcriptionRegulation of cell metabolismCytoskeletal reorganization
04

Disease associations

CancerNeurodegenerative diseaseCardiovascular diseaseInflammationOther
05

Safety considerations

Complexity and ubiquity in signaling pathways create therapeutic challenges such as off-target effects and potential impact on multiple physiological systemsdisruption may affect immune response and cell homeostasis
06

Interacting drugs

DASA-58 (PKM2 activator)

1 more in the full profile.

07

Biomarkers

ARRB1 expression in cancer tissue (prognostic biomarker, e.g., in gastric cancer)

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