Target intelligence / Profile preview

Glypican-4 (GPC4)

Target
GPC4
Molecular classification
Heparan sulfate proteoglycan, Cell surface protein, Glycosyl-phosphatidylinositol (GPI)-anchored protein, Adipokine
01

Overview

Glypican-4 is a cell surface heparan sulfate proteoglycan encoded by the GPC4 gene in humans. It is attached to the cell membrane via a glycosyl-phosphatidylinositol (GPI) anchor and is part of the glypican family, which modulates signaling by growth factors involved in development, metabolism, and disease. Glypican-4 acts as a co-receptor, especially for insulin and Wnt signaling pathways, regulating cell growth, differentiation, and morphogenetic movements during embryogenesis. It is notably released from adipose tissue as a soluble factor (adipokine), with circulating levels correlated with body mass index and insulin resistance. Glypican-4 plays roles in metabolic disorders, developmental syndromes, and cancer, making it a candidate target for biomarkers and, potentially, therapeutic intervention.

Other names
GPC4K-glypicanGlypican 4
02

Mechanism of action

Modulation of cell surface receptor signaling (acts as a co-receptor for insulin and growth factor receptors, influencing downstream signaling cascades); Regulation of non-canonical Wnt/PCP pathways (facilitates convergent extension movements and morphogenesis)

03

Biological functions

Cell signalingRegulation of cell proliferation and differentiationModulator of insulin receptor signalingRegulation of embryonic development and morphogenesisAdipocyte differentiationControl of convergent extension movements during gastrulation
04

Disease associations

Metabolic syndromeType 2 diabetesCancerCongenital malformation syndromesBone and facial developmental abnormalitiesOther (potential involvement in cardiovascular and developmental disorders)
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Safety considerations

Blockade of glypican-4 may impair essential developmental processesPotential off-target effects on growth factor signaling, embryogenesis, and glucose metabolism
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Interacting drugs

None currently approved as direct therapeutics targeting Glypican-4
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Biomarkers

Serum glypican-4 (GPC4) as a biomarker for insulin resistance, obesity, and metabolic syndrome

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