Target intelligence / Profile preview

G kinase-anchoring protein 1 (GKAP1)

Target
GKAP1
Molecular classification
Scaffold protein (anchoring protein), Signal organizing protein, Other (not an enzyme, receptor, ion channel, transporter, or transcription factor)
01

Overview

G kinase-anchoring protein 1 is a scaffold protein that organizes and anchors cGMP-dependent protein kinase I alpha (cGK-Iα) and possibly other signaling molecules to specific subcellular sites, thus facilitating spatially constrained signal transduction. In humans, it regulates insulin-dependent IRS1 tyrosine phosphorylation, modulating IRS1 availability to the insulin receptor and is required for insulin-induced translocation of glucose transporter SLC2A4 to the membrane in adipocytes. GKAP1 appears important in germ cell development, particularly its mouse homolog. Broadly, GKAP1’s scaffold functions anchor kinases and phosphatases, enabling precise and efficient intracellular signaling within pathways such as those mediated by G-protein-coupled receptors, though it is not itself a receptor or enzyme.

Other names
GKAP1GKAP42cGMP-dependent protein kinase anchoring protein 42kDa
02

Mechanism of action

Not directly targeted by drugs; may modulate drug actions that involve insulin signaling (e.g., antidiabetic agents) by scaffolding IRS1 and insulin receptor interactions.

03

Biological functions

Anchors cGMP-dependent protein kinase I (cGK-Iα) to subcellular compartmentsRegulates insulin-dependent IRS1 tyrosine phosphorylation in adipocytesModulates cellular availability and localization of signaling proteins (e.g., IRS1)Involved in germ cell development (via cGK-Iα recruitment to Golgi)Contributes to precision of intracellular signaling, organizing kinases/phosphatases
04

Disease associations

Implicated in metabolic disorders (e.g., insulin signaling dysfunction)May play a role in TNF-induced impairment of insulin-dependent IRS1 phosphorylation, relevant to inflammation and insulin resistancePotential roles in germ cell development abnormalitiesOther (possible but less directly substantiated; additional disease associations unclear)
05

Safety considerations

No notable safety concerns or therapeutic challenges directly associated with targeting GKAP1, as it is not a current drug target
06

Interacting drugs

No established direct therapeutic drugs known to specifically target GKAP1. May indirectly influence drug response via insulin signaling pathways.
07

Biomarkers

At present, GKAP1 is not routinely used as a direct biomarker for patient selection or efficacy monitoring

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