Anti-cancer, G-1 agonist drug may reduce the severity of diabetes and obesity

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As part of a new study, researchers at the University of New Mexico probed the effects of the GPER-selective agonist G-1 and found that the cancer fighting drug may also be efficient for reducing complications associated with obesity. The findings were published in the journal Science Translational Medicine.

According to statistics by the International Diabetes Federation, nearly 460 million adults suffered from diabetes on a global scale last year. Additionally, statistics also showed that approximately 39 percent of adults in the U.S. currently suffer from obesity.

To understand the cause of those high number of cases, researchers turned their attention to the G protein–coupled estrogen receptor (GPER), which is activated by G-1. In the study, various models of diabetes and obesity were utilized on rodents to identify how selective GPER agonism affects multiple aspects of metabolism associated with both conditions.

“We and others have shown that GPER deficiency results in phenotypic abnormalities similar to those observed in mice lacking ERα with regard to metabolism, including obesity, dyslipidemia, insulin resistance, glucose intolerance, and inflammation,” the study reads.

“These observations suggest a potential overlap or synergy in the metabolic functions carried out by both receptors.”

Based on their conclusion, researchers uncovered a new unrecognized role for the potential treatment of obesity and diabetes with the GPER agonist G-1.

“This is the first study to demonstrate the beneficial metabolic effects of a GPER-selective agonist in vivo in both female and male mice. We show that G-1 exerts potent antiobesity and antidiabetic effects specifically through the stimulation of energy expenditure in the absence of effects on food intake or locomotor activity,” researchers concluded.

“Our results could lead to therapeutic approaches against obesity and its associated metabolic consequences such as diabetes, not only in postmenopausal women but also in men.”