Featured Research

from universities, journals, and other organizations

Discovery brings hope of new tailor-made anti-cancer agents

Date:
April 21, 2013
Source:
Walter and Eliza Hall Institute
Summary:
Scientists have tailor-made a new chemical compound that blocks a protein that has been linked to poor responses to treatment in cancer patients. The development of the compound, called WEHI-539, is an important step towards the design of a potential new anti-cancer agent.

Dr Guillaume Lessene and his collaborators have tailor-made a new chemical compound that blocks a protein that has been linked to poor responses to treatment in cancer patients.
Credit: Image courtesy of Walter and Eliza Hall Institute

Scientists at the Walter and Eliza Hall Institute and their collaborators have tailor-made a new chemical compound that blocks a protein that has been linked to poor responses to treatment in cancer patients.

Related Articles


The development of the compound, called WEHI-539, is an important step towards the design of a potential new anti-cancer agent.

WEHI-539 has been designed to bind and block the function of a protein called BCL-XL that normally prevents cells from dying. The death and elimination of abnormal cells in the body is an important safeguard against cancer development. But cancer cells often acquire genetic changes that allow them to bypass cell death, which also reduces the effectiveness of anti-cancer treatments such as chemotherapy.

Cancer cells can become long-lived by producing high levels of BCL-XL protein, and high levels of BCL-XL are also associated with poorer outcomes for patients with lung, stomach, colon and pancreatic cancer.

Dr Guillaume Lessene, Professor Keith Watson and Professor David Huang from the institute's ACRF Chemical Biology division, and Dr Peter Czabotar and Professor Peter Colman from the institute's Structural Biology division led the development of WEHI-539 in collaboration with colleagues at Genentech, a member of the Roche group. The research is published online today in the journal Nature Chemical Biology.

Dr Lessene said the development of WEHI-539 was an important milestone on the way to creating potential anti-cancer agents that act to restore cell death by inhibiting BCL-XL. "Although WEHI-539 is not optimised for use in patients, it will be a very valuable tool for researchers to use to dissect how BCL-XL controls cancer cell survival," he said.

WEHI-539 belongs to a class of chemicals called 'BH3-mimetics', which all bind to the same region of BCL-XL or related proteins. Two BH3-mimetics, called navitoclax (ABT-263) and ABT-199/GDC-0199 are currently in clinical trials for the treatment of cancer, particularly those of the blood and lymph glands (leukemia and lymphoma).

Dr Lessene said WEHI-539 was the product of a sustained research program. "We were very excited to see the team's work culminate in a compound that specifically inhibits BCL-XL," he said. "WEHI-539 is the first compound that our chemists have developed from scratch, using the three-dimensional structure of BCL-XL to build and refine its design."


Story Source:

The above story is based on materials provided by Walter and Eliza Hall Institute. Note: Materials may be edited for content and length.


Journal Reference:

  1. Guillaume Lessene, Peter E Czabotar, Brad E Sleebs, Kerry Zobel, Kym N Lowes, Jerry M Adams, Jonathan B Baell, Peter M Colman, Kurt Deshayes, Wayne J Fairbrother, John A Flygare, Paul Gibbons, Wilhelmus J A Kersten, Sanji Kulasegaram, Rebecca M Moss, John P Parisot, Brian J Smith, Ian P Street, Hong Yang, David C S Huang, Keith G Watson. Structure-guided design of a selective BCL-XL inhibitor. Nature Chemical Biology, 2013; DOI: 10.1038/nchembio.1246

Cite This Page:

Walter and Eliza Hall Institute. "Discovery brings hope of new tailor-made anti-cancer agents." ScienceDaily. ScienceDaily, 21 April 2013. <www.sciencedaily.com/releases/2013/04/130421153846.htm>.
Walter and Eliza Hall Institute. (2013, April 21). Discovery brings hope of new tailor-made anti-cancer agents. ScienceDaily. Retrieved November 23, 2014 from www.sciencedaily.com/releases/2013/04/130421153846.htm
Walter and Eliza Hall Institute. "Discovery brings hope of new tailor-made anti-cancer agents." ScienceDaily. www.sciencedaily.com/releases/2013/04/130421153846.htm (accessed November 23, 2014).

Share This


More From ScienceDaily



More Health & Medicine News

Sunday, November 23, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Ebola-Hit Sierra Leone's Late Cocoa Leaves Bitter Taste

Ebola-Hit Sierra Leone's Late Cocoa Leaves Bitter Taste

AFP (Nov. 23, 2014) The arable district of Kenema in Sierra Leone -- at the centre of the Ebola outbreak in May -- has been under quarantine for three months as the cocoa harvest comes in. Duration: 01:32 Video provided by AFP
Powered by NewsLook.com
Don't Fall For Flu Shot Myths

Don't Fall For Flu Shot Myths

Newsy (Nov. 23, 2014) Misconceptions abound when it comes to your annual flu shot. Medical experts say most people older than 6 months should get the shot. Video provided by Newsy
Powered by NewsLook.com
WFP: Ebola Risks Heightened Among Women Throughout Africa

WFP: Ebola Risks Heightened Among Women Throughout Africa

AFP (Nov. 21, 2014) Having children has always been a frightening prospect in Sierra Leone, the world's most dangerous place to give birth, but Ebola has presented an alarming new threat for expectant mothers. Duration: 00:37 Video provided by AFP
Powered by NewsLook.com
Could Your Genes Be The Reason You're Single?

Could Your Genes Be The Reason You're Single?

Newsy (Nov. 21, 2014) Researchers in Beijing discovered a gene called 5-HTA1, and carriers are reportedly 20 percent more likely to be single. Video provided by Newsy
Powered by NewsLook.com

Search ScienceDaily

Number of stories in archives: 140,361

Find with keyword(s):
Enter a keyword or phrase to search ScienceDaily for related topics and research stories.

Save/Print:
Share:

Breaking News:

Strange & Offbeat Stories


Health & Medicine

Mind & Brain

Living & Well

In Other News

... from NewsDaily.com

Science News

Health News

Environment News

Technology News



Save/Print:
Share:

Free Subscriptions


Get the latest science news with ScienceDaily's free email newsletters, updated daily and weekly. Or view hourly updated newsfeeds in your RSS reader:

Get Social & Mobile


Keep up to date with the latest news from ScienceDaily via social networks and mobile apps:

Have Feedback?


Tell us what you think of ScienceDaily -- we welcome both positive and negative comments. Have any problems using the site? Questions?
Mobile: iPhone Android Web
Follow: Facebook Twitter Google+
Subscribe: RSS Feeds Email Newsletters
Latest Headlines Health & Medicine Mind & Brain Space & Time Matter & Energy Computers & Math Plants & Animals Earth & Climate Fossils & Ruins