Target intelligence / Profile preview

Adhesion G protein-coupled receptor B3 (ADGRB3)

Target
ADGRB3
Molecular classification
G protein-coupled receptor, Adhesion GPCR, Receptor, Transmembrane protein
01

Overview

Adhesion G protein-coupled receptor B3 (ADGRB3), also known as BAI3, is a member of the adhesion GPCR family with a large extracellular domain responsible for cell–cell adhesion and signaling[1][3][4][5]. Highly expressed in the brain, ADGRB3 is crucial for synaptic development, dendritic morphogenesis, and the elimination of redundant synapses, impacting circuit refinement essential for motor learning and cognition[1][2]. It interacts with secreted C1q-like proteins to regulate synaptic density, and its disruption is implicated in neurodevelopmental disorders[1][2]. Beyond the nervous system, ADGRB3 mediates myoblast fusion in muscle and modulates metabolic and angiogenic pathways[1][3][5]. Aberrant ADGRB3 expression or genomic alteration is linked to certain malignancies (lung, breast, ovarian, gastric, prostate) and vascular or metabolic diseases including insulin regulation and venous thromboembolism[1][3][5]. No drugs currently target ADGRB3 directly, but its roles in diverse physiological and pathological processes are under investigation as potential therapeutic opportunities.

Other names
BAI3Brain-specific angiogenesis inhibitor 3KIAA0550dJ91B17.1BAI-3
02

Mechanism of action

Not established—ADGRB3 is considered an orphan receptor (no approved drugs directly targeting it); Signal regulation via tethered agonist after autoproteolytic cleavage within the GAIN domain; Binds secreted C1q-like proteins; modulates synaptic density and insulin secretion through downstream signaling.

03

Biological functions

Signal transductionCell–cell adhesionRegulation of synapse formation and remodelingDendritic arborization and morphogenesisMotor learning (via synapse elimination)Myoblast fusion (muscle development)Angiogenesis regulationModulation of metabolic homeostasis
04

Disease associations

Cancer (including lung, gastric, breast, ovarian, prostate)Neurodevelopmental disorders (intellectual disability, ataxia, behavioral abnormalities)Metabolic disease (association with insulin secretion and body mass index)Vascular disease (e.g., venous thromboembolism)
05

Safety considerations

Not established due to lack of clinical drugsDisruption or copy number variation associated with neurodevelopmental, cranial, and connective tissue anomalies
06

Biomarkers

Diagnostic marker in small-cell lung carcinoma (aberrant expression/localization)Genetic variation used for population-level associations (e.g., metabolic traits)

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