# Molecular basis for ligand and cell type specific regulation of opioid receptors

> **NIH NIH R00** · OREGON HEALTH & SCIENCE UNIVERSITY · 2021 · $249,000

## Abstract

Abstract/Project Summary.
Opioid abuse and addiction are major public health concerns. Opioids are highly useful analgesics, yet an
estimated two million people in the United States suffer disorders related to abuse of prescription opioids. The
social and economic costs of these disorders are devastating and on the rise: an average of 44 people die every
day from prescription opioid overdoses. Opioids are structurally diverse molecules that include oxycodone,
heroin and endorphins, and the physiological effects of these molecules are mediated by G protein-coupled
receptors (GPCRs). Recently developed `biased' opioid agonists demonstrate that this diversity can be mined to
identify drugs with less harmful side effects, but the mechanism of action of these `biased' agonists remains
incompletely resolved. New technical advances now make it possible to biochemically capture the protein
interaction networks mediating GPCR activity from inside of living cells with sub-minute temporal resolution.
The ability to capture, quantify, and characterize the endogenous proteins which mediate and regulate opioid
activity opens new doors for determining how biased agonists differ from endogenous ligands or drugs of abuse.
This K99/R00 award combines critical new training in cutting-edge proteomics with traditional cell biological
techniques to examine the mechanism of biased opioid agonism: Aim 1-Define the kinetics by which different
classes of opioids alter mu opioid receptor (µOR) location and coupling to its transducer and regulatory
proteins; Aim 2-Identify new protein regulators of µOR stimulated by standard or biased opioids. Aim 3-
Define µOR signaling targets and determine if these proteins differ between opioids. Future studies based on
these results will help to define how opioid receptors operate under normal, pharmacologically activated, or
disease states resulting from drug abuse and addiction.

## Key facts

- **NIH application ID:** 10246474
- **Project number:** 5R00DA043607-05
- **Recipient organization:** OREGON HEALTH & SCIENCE UNIVERSITY
- **Principal Investigator:** Braden Lobingier
- **Activity code:** R00 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $249,000
- **Award type:** 5
- **Project period:** 2019-09-01 → 2023-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10246474

## Citation

> US National Institutes of Health, RePORTER application 10246474, Molecular basis for ligand and cell type specific regulation of opioid receptors (5R00DA043607-05). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10246474. Licensed CC0.

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