Target intelligence / Profile preview

Cadherin EGF LAG seven-pass G-type receptor 3 (CELSR3)

Target
CELSR3
Molecular classification
Adhesion G protein-coupled receptor (GPCR), Cadherin superfamily, Transmembrane receptor
01

Overview

Cadherin EGF LAG seven-pass G-type receptor 3 (CELSR3) is a large transmembrane protein of the flamingo subgroup in the cadherin superfamily, characterized by nine cadherin repeats, seven epidermal growth factor-like (EGF) domains, two laminin G repeats, and a seven-helix transmembrane domain[1][2][5]. It functions primarily in cell adhesion and planar cell polarity signaling, coordinating directional growth, migration, and connectivity of neurons during development[2][3][1]. CELSR3 interacts with Frizzled3 to modulate neural circuit formation and is implicated in the formation of central nervous system architecture, neuronal migration, and cilia organization[2][3]. Its dysregulation has been associated with neurodevelopmental disorders, cancer, and aberrant tissue organization[2][3][4][7]. No FDA- or EMA-approved drugs currently target CELSR3 directly, and its mechanisms of pharmacological modulation are not established; it is, however, a candidate biomarker and target in oncology and neurology research[2][4][7].

Other names
ADGRC3HFMI1CDHF11EGFL1FMI1RESDA1MEGF2flamingo homolog 1multiple EGF-like domains protein 2Cadherin family member 11Epidermal growth factor-like protein 1hFmi1
02

Mechanism of action

Not established for any approved drugs; receptor participates in cell adhesion, PCP signaling, calcium signaling, and possibly non-canonical Wnt signaling via Frizzled3; experimental modulation affects intracellular calcium via PLC

03

Biological functions

Cell adhesion and cell-cell contactPlanar cell polarity (PCP) signalingNeural development: axon guidance, neuronal migration, synaptic formation, establishment of neural wiringRegulation of neuronal polarity and cilia organizationVessel valve formation and tissue morphogenesis
04

Disease associations

Neurodevelopmental disorders (including Tourette disorder)Cancer (ovarian cancer stem-like subgroups, head and neck squamous cell carcinoma)Other developmental defects and central nervous system malformations
05

Safety considerations

No specific safety concerns for therapeutic targeting reported; challenges may include neural/developmental toxicity due to its essential role in neurodevelopment
06

Biomarkers

Prognostic marker for head and neck squamous cell carcinoma (HNSCC)Risk gene in Tourette disorder

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