Developing Photoaffinity Probes for Dopamine Receptor D₂ to Determine Targets of Parkinson's Disease Drugs.

ABSTRACT: Dopaminergic pathways control highly consequential aspects of physiology and behavior. One of the most therapeutically important and best-studied receptors in these pathways is dopamine receptor D₂ (DRD2). Unfortunately, DRD2 is challenging to study with traditional molecular biological techniques, and most drugs designed to target DRD2 are ligands for many other receptors. Here, we developed probes able to both covalently bind to DRD2 using photoaffinity labeling and provide a chemical handle for detection or affinity purification. These probes behaved like good DRD2 agonists in traditional biochemical assays and were able to perform in chemical-biological assays of cell and receptor labeling. Rat whole brain labeling and affinity enrichment using the probes permitted proteomic

SUBMITTER: Kim ST 

PROVIDER: S-EPMC9585581 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature