GRK2 tagged posts

GRK2 interaction with DOR, not kinase activity, desensitizes the receptor at the plasma membrane in
peripheral pain-sensing neurons. Priming by inflammatory mediator BK induces PKC-dependent RKIP sequestration of
GRK2 to the cytosol, enhancing DOR responsiveness. Knock down of GRK2 enhances peripheral DOR-mediated
analgesia in vivo.

Opioid abuse is a growing public health crisis, affecting up to 36 million people worldwide. Many of these individuals first get hooked on prescription painkillers that target mu opioid receptors in the brain. A study in rats published August 25 in Cell Reports suggests that a different approach that targets delta opioid receptors on sensory neurons in peripheral tissues might avoid side effects and high abuse potential of currently available pain relievers.