Science and Technology
publicado em 28/05/2013 às 10h08:00
   Dê o seu voto:

Compound derived from poisonous toxin anemone combat obesity

Results show that ShK-186 blocks the activity of a protein that promotes inflammation by potassium channel Kv1.3

 
font size
A-
A+

Scientists at UC Irvine reported this week that a synthetic compound ShK-186, originally derived from a sea anemone toxin, has been found to enhance metabolic activity and shows potential as a treatment for obesity and insulin resistance.

The findings published the week of May 27 in the Proceedings of the National Academy of Sciences reveal that ShK-186 selectively blocks the activity of a protein that promotes inflammation through the Kv1.3 potassium channel. The study presents the first evidence that the drug candidate which in March showed positive results in a Phase 1 safety clinical trial may also work in an anti-obesity capacity.

UC Irvine licensed ShK-186 to Kineta Inc., a Seattle based biotechnology company in 2009; it is the company's lead drug candidate. Kineta is developing this compound to treat autoimmune diseases, such as multiple sclerosis, psoriatic arthritis and lupus. It has also licensed the use of ShK-186 for the treatment of metabolic syndrome and obesity.

Potassium channels regulate cell membrane potential and control a variety of cellular processes. Earlier studies using mice that lack Kv1.3, a potassium channel gene, suggested that Kv1.3 regulated body weight and the basal metabolic rate.

In the present study, Dr. George Chandy and his colleagues evaluated ShK-186 because it has high selectivity for the Kv1.3 target, a favorable pharmacokinetic profile, and meets the qualities of an industry-standard drug. In tests on obese mice that ate a high-fat, high-sugar diet, ShK-186 therapy reduced weight gain, white fat deposits, fatty liver, blood cholesterol and blood sugar by activating calorie-burning brown fat, suppressing inflammation of white fat and augmenting liver function. The compound had no effect on mice that ate a standard chow diet, suggesting that the obesity-causing diet triggers the expression of the Kv1.3 target.

"This is a new twist in a sustained journey of discovery made over the 30 years that charts the course for expeditious translation to humans who suffer from potentially lethal consequences of metabolic syndrome and autoimmune diseases," said Chandy, professor of physiology & biophysics at UC Irvine and a Kineta scientific advisor. "We evaluated ShK-186 in an obesity model because it has high selectivity for the Kv1.3 target, a favorable pharmacokinetic profile, and meets the qualities of an industry-standard drug."

"These data are quite exciting and strongly support the notion that inhibition of the Kv1.3 channel provides a highly effective method for managing obesity and its associated metabolic abnormalities. The results obtained with ShK-186 are consistent with what one would expect to see with a potent inhibitor of this channel. While additional studies are needed, the potential clinical relevance of this work is enormous, since a significant number of people are afflicted with obesity and its associated complications, and no Kv1.3 inhibitor, as a drug candidate for obesity, has reached the clinic until now," said Dr. Gary V. Desir, professor of medicine at Yale University, and an expert on the Kv1.3 channel's role in renal potassium secretion and glucose metabolism. Dr. Desir was not involved with the study.

"Knowing that ShK-186's unique mechanism of action may have broad utilization across multiple therapeutic disciplines, such as autoimmune diseases and now obesity, further adds to the potential of this compound. This study also shows how medical progress can be made through academic and private sector partnerships," added Charles Magness, Ph.D., President and CEO of Kineta.

Source: UNIVERSIDADE DA CALIFÓRNIA
  • Share this pageShare this page
  • Share this pageCorrect
  • ShareShare
  • AlertAlert
Reduced link: 
  • You are recommending this story: Compound derived from poisonous toxin anemone combat obesity
  • Fill in the following form to send your recommendation to your friend:

  • You are suggesting a correction for this story: Compound derived from poisonous toxin anemone combat obesity


Receba notícias do iSaúde no seu e-mail de acordo com os assuntos de seu interesse.
Seu nome:
Seu email:
Desejo receber um alerta com estes assuntos:
Obesity    poisonous anemone toxin    ShK-186    potassium channel    University of California at Irvine    George Chandy   
Comments:
Comment
Leave your comment
Close
(Required fields are marked with an *)

(Your email address will never be published or shared.)

Enter the letters and numbers below and click in the button "send"

  • Twitter iSaúde
advertising
Informe Saúde printed version

Recommend the portal
Close [X]
  • You are recommending this story: http://www.isaude.net
  • Fill in the following form to send your recommendation to your friend:

RSS news from the portal  iSaúde.net
Get the newsletter of the portal  iSaúde.net
Recommend the portal iSaúde.net
News from  iSaúde.net in your blog or website.
Get news on the subject of your interest.
© 2000-2011 www.isaude.net Todos os direitos reservados.