Veterans Affairs

Obesity treatment through purinergic receptors

Selective blocking the activity of the P2Y2 purinergic receptor results in a resistance to diet-induced obesity, an increased metabolic rate, and a better glucose tolerance

Medical & Biotechnology

The most common cause of obesity is the consumption of more calories than a person can metabolize.

Current drugs used for the prevention or treatment of obesity fall into three categories: drugs that suppress appetite by acting on the brain (sibutramine, Reductil® and/or Meridia®); drugs that boost body’s metabolic rate (cannabinoid receptor antagonists and Metformin); and drugs that interfere with the body’s ability to absorb specific nutrients in food, such as fat (Orlistat®, Xenical®, and Alli®).

Pharmaceuticals in this $3.5 billion market have significant limitations in terms of safety, efficacy, or both.

Drugs that suppress the appetite by acting on the brain have severe side effects that are neurological, psychological, or both. These drugs carry a risk of high blood pressure, faster heart rate, palpitation, restlessness, agitation, and insomnia.

Due to these limitations, drugs that suppress appetite have been withdrawn from the market by the FDA and approval of newer drugs has been made more stringent. Drugs that increase the body’s metabolic rate have their own limitations, such as lack of consistent effect. Drugs that block absorption of dietary fat, cause gastrointestinal problems.

Based on research showing that genetic deletion of the P2Y2 purinergic receptor results in resistance to the development of high-fat-induced obesity in mice, researchers at the Department of Veterans Affairs have proposed treating diet-induced obesity by administering an oligonucleotide (antisense oligo, ribozyme, siRNA or other agents) that blunts the expression of the P2Y2 receptor. Mechanistically, blunting of the expression of the P2Y2 receptor increases the energy metabolism in an adipocyte cell. This work has led to the proposal of fusion proteins, oligonucleotides, siRNA, or selective antagonists as therapeutics.

This research is protected by US patent 10,107,795, which is related to US patent 10,024,846, and international patent filing WO 2014066830.

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