Researchers switch focus to different brown fat receptors

19 October 2020

Receptor activation could lead to new treatments for diabetes and obesity.

Researchers have found a method by which to activate brown fat in humans, this could pave the way in new treatments for Type-2 diabetes and obesity.

Brown fat burns energy and generates heat, a process known as thermogenesis, after being activated by cold or chemical signals. Humans have small deposits of brown fat and, for a number of years, scientists have believed that finding a drug that would activate the fat could improve metabolism. However it is now believed that research has been focused on the wrong set of receptors in brown fat cells.  

Researchers say that thermogenesis occurs via beta 2 adrenergic receptors (β2-AR) signalling in humans not β3-AR as previously thought. In a recent paper, the researchers showed that oral doses of the drug mirabegron (a β3-AR agonist) only elicited increases in brown fat thermogenesis when given at the maximum allowable dose.  However, they used other drugs to stimulate and inhibit the activity of β2-AR receptors in brown fat cells which did result in thermogenesis.

The research team said most clinical trials that have attempted to induce brown fat to burn energy performed poorly as they targeted β3-AR. This is the receptor found to cause thermogenesis when tests were carried out on animals.

‘Activation of brown fat burns calories, improves insulin sensitivity and even affects appetite regulation. Our data reveals a previously unknown key to locking these functions in humans,’ the researchers said.  Work will continue with attempts to validate the findings by activating brown fat with drugs that target β2-AR.

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