How a New Discovery Could be a Breakthrough for the Opioid Crisis

The opioid epidemic in the United States is nothing short of a crisis. Over 50,000 people died from opiate-related drug overdoses in 2016 alone, and rates are on a precipitous rise. Opiate abuse among demographic groups typically insulated from the risk for drug addiction is skyrocketing.

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Opioids and Pain Receptors: An Addictive Combination

It’s long been hypothesized that the solution to the opioid crisis lies within the creation of an analgesic opioid that blocks pain without the addictive, brain-damaging side effects. It’s a tall order, and one that has been hampered by scientists’ inability to map the actual crystalline structure of the pain receptors that opioids latch onto within the body. Without knowing a pain receptor’s shape, researchers can’t build a drug to match it.

There are four known pain receptors that bond with opioids: kappa, mu, delta, and nociceptin. The mu receptor is what causes issues – and also seems to be the most attractive to particularly deadly opioids such as fentanyl – because it produces a litany of side effects when metabolizing a drug. The kappa receptor is the most likely candidate for a better opioid drug as it is known to offer pain relief with only minor side effects.

 

How Scientists Have Cracked the Kappa Code

The kappa receptor has been notoriously difficult to map. In 2012, X-ray crystallography of the protein finally revealed the inactive receptor’s shape; active kappa structures, on the other hand, have been elusive. In early 2018, pharmacologist Bryan Roth and his team at the University of North Carolina School of Medicine may have finally cracked the code.

Using a complicated “propping” technique, Roth and his team were able to effectively stabilize the protein in its active state, resulting in a mere 21 diffracted proteins after crystallization. Thankfully, those proteins provided enough measurable data for labs around the world to get to work on virtual simulations of millions of compounds pairing with the receptors.

 

The Solution to the Opioid Epidemic?

Could the solution to the opioid crisis possibly be as a simple as better opioids? Most experts agree the solution will come in a myriad of forms: bespoke opioid drugs aimed at specific pain receptors; drugs that eliminate the need for opioids altogether; better drug testing technology for opioid abuse.

IMCS is deeply invested in the science of proteomics. Our flagship product, IMCSTips, uses dispersive pipette extraction  technology to achieve incredibly high binding capacities and consistent, reproducible results. IMCSzyme, our pure beta glucuronidase enzyme, is used to quickly and efficiently hydrolyze over a million samples a month for drug testing efforts in labs across the U.S. and the world.


Would you like to speak to a member of our team about how IMCSTips could help advance your research in proteomics? Our chemists are standing by and happy to speak with you about the qualities that make IMCSTips so unique.

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