Featured Research

from universities, journals, and other organizations

For drug makers, new 3-D control opens wealth of options

Date:
February 7, 2013
Source:
Yale University
Summary:
Scientists have demonstrated a new, highly versatile approach for quickly assembling drug-like compounds, establishing a broad new route to drug discovery and medical treatment.

A team of scientists anchored at Yale University has demonstrated a new, highly versatile approach for quickly assembling drug-like compounds, establishing a broad new route to drug discovery and medical treatment. They report their results in the journal Science on Feb 8.

Drug molecules interact with their targets, such as proteins or enzymes, by attaching to them in a way that neutralizes the target's undesirable effects in the body. This is sometimes called the "lock-and-key" method. The new approach offers scientists far greater control over the three-dimensional structure of a key class of molecular compounds, making it easier to fashion drug molecules that fit their targets in the right way.

"Now we've got a lot more control over the shape and orientation of this class of drug compounds, and this essentially gives us greater flexibility in creating effective drugs," said Jonathan Ellman, the Yale chemist who led the experiment.

The research reported in Science revolves around piperidines, a class of organic compounds widely used in pharmaceuticals, including the familiar drugs quinine, morphine, oxycodone, Plavix, Cialis, and Aricept. Piperidines are core structures, or scaffolds, upon which molecular fragments -- parts of the drug molecule -- can be displayed for binding to a drug's targets. The scientists have shown a way to generate different piperidine derivatives by varying acid strength.

"Our research allows us to make new piperidines easily," Ellman said. "The approach has biomedical relevance because the scaffold upon which the fragments are displayed is present in many of the most important drugs."

The research is being published without patent constraints and could be used by drug developers immediately, said Ellman, who is the Eugene Higgins Professor of Chemistry and professor of pharmacology. "I believe that this is the most effective approach for rapidly translating this work into new drugs," he said.


Story Source:

The above story is based on materials provided by Yale University. Note: Materials may be edited for content and length.


Journal Reference:

  1. S. Duttwyler, S. Chen, M. K. Takase, K. B. Wiberg, R. G. Bergman, J. A. Ellman. Proton Donor Acidity Controls Selectivity in Nonaromatic Nitrogen Heterocycle Synthesis. Science, 2013; 339 (6120): 678 DOI: 10.1126/science.1230704

Cite This Page:

Yale University. "For drug makers, new 3-D control opens wealth of options." ScienceDaily. ScienceDaily, 7 February 2013. <www.sciencedaily.com/releases/2013/02/130207141500.htm>.
Yale University. (2013, February 7). For drug makers, new 3-D control opens wealth of options. ScienceDaily. Retrieved September 17, 2014 from www.sciencedaily.com/releases/2013/02/130207141500.htm
Yale University. "For drug makers, new 3-D control opens wealth of options." ScienceDaily. www.sciencedaily.com/releases/2013/02/130207141500.htm (accessed September 17, 2014).

Share This



More Health & Medicine News

Wednesday, September 17, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

President To Send 3,000 Military Personnel To Fight Ebola

President To Send 3,000 Military Personnel To Fight Ebola

Newsy (Sep. 16, 2014) President Obama is expected to send 3,000 troops to West Africa as part of the effort to contain Ebola's spread. Video provided by Newsy
Powered by NewsLook.com
Man Floats for 31 Hours in Gulf Waters

Man Floats for 31 Hours in Gulf Waters

AP (Sep. 16, 2014) A Texas man is lucky to be alive after he and three others floated for more than a day in the Gulf of Mexico when their boat sank during a fishing trip. (Sept. 16) Video provided by AP
Powered by NewsLook.com
Ivorians Abandon Monkey Pets in Fear Over Ebola Virus

Ivorians Abandon Monkey Pets in Fear Over Ebola Virus

AFP (Sep. 16, 2014) Since the arrival of Ebola in Ivory Coast, Ivorians have been abandoning their pets, particularly monkeys, in the fear that they may transmit the virus. Duration: 00:47 Video provided by AFP
Powered by NewsLook.com
Study Links Male-Pattern Baldness To Prostate Cancer

Study Links Male-Pattern Baldness To Prostate Cancer

Newsy (Sep. 16, 2014) New findings suggest men with a certain type of baldness at age 45 are 39 percent more likely to develop aggressive prostate cancer. 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:
from the past week

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