Controlling a Fat-Regulating Protein Dramatically Increases Insulin Sensitivity

The research findings could lead to the development of drugs that reduce the risk of developing type 2 diabetes and cardiovascular problems.

| Aug 22, 2010

PPARy is a protein that regulates the body's production of fat cells. However, obesity can modify how PPARy works, leading to decreased insulin sensitivity and the development of metabolic syndrome. (Metabolic syndrome is the cluster of factors, including insulin resistance, overweight, high blood pressure, and abnormal blood sugar levels, that is a precursor to type 2 diabetes.)

But now a joint team of researchers from The Scripps Research Institute in San Diego and the Dana-Farber Cancer Institute at Harvard University in Cambridge has found a way to control the adverse changes in PPARy brought on by obesity.

One of those changes is phosphorylation, when an enzyme called cdk5 kinase adds a phosphate group to PPARy. That addition causes PPARy to alter the expression of several genes, including one that regulates production of adiponectin, a protein essential to insulin sensitivity. 

The challenge for the scientists was to find a way to change PPARy back to its normal state without inducing it to overproduce fat cells. They knew from a previous study that an agonist, a compound that makes cells respond in certain ways, interacted with the region of PPARy known to regulate fat generation. The agonist in that case was a full agonist, meaning that it was able to easily combine with a receptor in that region of PPARy and activate it to do a certain thing-in this case, not generate fat cells.

The researchers wondered if partial agonists-chemical agents that have only partial effects on certain cell receptors-could be used to counteract the insulin-suppressing effects of phosphorylation on PPARy without the side effect of ramping up fat cell production.

They found that while partial agonists did not interact with the PPARy receptor that governs fat cell production, one, called MRL24, worked  extremely well in the exact region of PPARy where phosphorylation takes place. By altering and diminishing that region's receptiveness to  phosphorylation, MRL24 allowed PPARy to increase the production of adiponectin.

Those findings, which open the door to learning how to fully manipulate PPARy, could lead to drugs that reduce the risk of developing type 2 diabetes and cardiovascular problems. If PPARy can be prevented in obese people from losing its ability to direct the production of adiponectin, it could become a significant therapy in treating the effects of extreme overweight.

* * *


Click Here To View Or Post Comments

Categories: Blood Sugar, Diabetes, Diabetes, Health Research, Insulin, Pre-Diabetes, Research, Type 2 Issues

Take the Diabetes Health Pump Survey
See What's Inside
Read this FREE issue now
For healthcare professionals only
  • 12th Annual Product Reference Guide
  • Insulin Syringe Chart
  • Insulin Pen Needles Chart
  • Fast-Acting Glucose
  • Sharps Disposal
  • Blood Glucose Meters Chart
  • Insulin Pumps Chart
See the entire table of contents here!

You can view the current or previous issues of Diabetes Health online, in their entirety, anytime you want.
Click Here To View

See if you qualify for our free healthcare professional magazines. Click here to start your application for Pre-Diabetes Health, Diabetes Health Pharmacist and Diabetes Health Professional.

Learn More About the Professional Subscription

Free Diabetes Health e-Newsletter

Top Rated
Print | Email | Share | Comments (0)

You May Also Be Interested In...


Add your comments about this article below. You can add comments as a registered user or anonymously. If you choose to post anonymously your comments will be sent to our moderator for approval before they appear on this page. If you choose to post as a registered user your comments will appear instantly.

When voicing your views via the comment feature, please respect the Diabetes Health community by refraining from comments that could be considered offensive to other people. Diabetes Health reserves the right to remove comments when necessary to maintain the cordial voice of the diabetes community.

For your privacy and protection, we ask that you do not include personal details such as address or telephone number in any comments posted.

Don't have your Diabetes Health Username? Register now and add your comments to all our content.

Have Your Say...

Username: Password:
©1991-2015 Diabetes Health | Home | Privacy | Press | Advertising | Help | Contact Us | Donate | Sitemap

Diabetes Health Medical Disclaimer

The information on this site is not intended or implied to be a substitute for professional medical advice, diagnosis or treatment. All content, including text, graphics, images, and information, contained on or available through this website is for general information purposes only. Opinions expressed here are the opinions of writers, contributors, and commentators, and are not necessarily those of Diabetes Health. Never disregard professional medical advice or delay seeking medical treatment because of something you have read on or accessed through this website.