Kappa Opioid Receptor Structure Revealed, A Potential Milestone in Medication Development

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New research funded by the National Institute on Drug Abuse illuminates the crystal structure of the activated kappa opioid receptor (KOR). The breakthrough could facilitate the development of new medications to treat pain and addiction.

Image by Bryan L. Roth MD, PhD
The structure of MP1104 in complex with the active state of the kappa opioid receptor as solved by x-ray crystallography.

The KOR is activated by one of the body’s natural opioid molecules, called dynorphin. When activated, the receptor produces analgesia. It also suppresses the rewarding effects of addictive drugs, reducing the motivation to use them, but also contributes to withdrawal and stress responses that motivate addictive behavior.

Researchers can use the newly revealed, fine-grained KOR structure to tease apart how the receptor’s interaction with dynorphin produces its diverse effects, and how its interactions with other molecules modulate those effects. Medicinal chemists may use this knowledge to design new medications that preserve or enhance dynorphin’s analgesic efficacy while improving treatments for addiction.

For a copy of the abstract, go to "Structure of a nanobody-stabilized active state of the kappa opioid receptor," published in Cell.

For more information about opioids, go to www.nida.nih.gov/drugs-abuse/opioids.

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