Target intelligence / Profile preview

PRKCA-binding protein (PICK1)

Target
PICK1
Molecular classification
Adapter protein, PDZ domain-containing protein, BAR domain-containing protein, Peripheral membrane protein
01

Overview

PRKCA-binding protein, commonly known as Protein Interacting with C Kinase 1 (PICK1), is a peripheral membrane adapter protein essential for the trafficking and organization of various membrane-bound receptors and transporters. It is characterized by a PDZ domain that mediates protein-protein interactions and a BAR domain that facilitates binding to curved lipid membranes. In the central nervous system, PICK1 is a critical regulator of synaptic plasticity, particularly through its role in the internalization and recycling of AMPA-type glutamate receptors (specifically the GluR2 subunit) during long-term depression. Beyond its neuronal roles, PICK1 is involved in the biogenesis of insulin granules in pancreatic beta cells and the formation of the acrosome in developing sperm. Due to its involvement in neuropathic pain, drug addiction, and metabolic regulation, PICK1 has become a target of interest for drug development. Therapeutic strategies focus on inhibiting its PDZ domain using small molecules like FSC231 or peptide-based inhibitors to disrupt pathological protein interactions and restore normal receptor trafficking.

Other names
Protein interacting with C kinase 1Protein kinase C-alpha-binding proteinPRKCABPPICK
02

Mechanism of action

Inhibition of the PDZ domain to disrupt protein-protein interactions and modulate receptor trafficking

03

Biological functions

Synaptic plasticityReceptor traffickingAMPA receptor internalizationInsulin secretion regulationAcrosome formationActin polymerization regulationIon channel regulation
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Disease associations

Chronic painNeuropathic painObesityMale infertilitySchizophreniaDrug addictionCancer
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Safety considerations

Potential for male infertilityRisk of impaired insulin secretionPotential cognitive side effects due to altered synaptic plasticity
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Interacting drugs

FSC231

1 more in the full profile.

07

Biomarkers

PICK1 mRNA expression levelsPICK1 genetic polymorphisms

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