Corporate Banner
Satellite Banner
Scientific Community
Become a Member | Sign in
Home>News>This Article

Chemists Devise New Way to Prepare Molecules for Drug Testing

Published: Monday, August 19, 2013
Last Updated: Monday, August 19, 2013
Bookmark and Share
Metal-catalyzed cross-couplings of carbon bonds could enable creation of libraries of drug candidates to accelerate drug discovery.

James Bond had his reasons for ordering his martinis “shaken, not stirred.” Similarly, drug manufacturers need to make sure the molecules in a new drug are arranged in an exact manner, lest there be dire consequences. Specifically, they need to be wary of enantiomers, mirror-image molecules composed of the same atoms, but arranged differently.

“One mirror image could be therapeutic while another could be poisonous,” said Dr. Mark R. Biscoe, assistant professor of chemistry at The City College of New York. The classic case is thalidomide, a drug marketed in the 1950s and 1960s to treat morning sickness, which resulted in serious birth defects.

Professor Biscoe led a team of researchers at CCNY that developed a new method for preparing libraries of single-enantiomer molecules for therapeutic and toxicity studies that is faster and potentially less costly than methods now used in the pharmaceutical industry. Their findings were reported in Nature Chemistry.

Currently, drug developers typically rely on a chiral resolution process whereby compounds with roughly equal parts of the two enantiomers are separated into the individual enantiomers. Bioenzymatic processes can also be employed to generate single-enantiomer molecules. These strategies are wasteful and costly, Professor Biscoe explained.

He and colleagues found that a metal such as palladium could be employed to achieve a cross-coupling reaction with a single-enantiomer molecule without impacting the integrity of the mirror image formed in the product. By doing so, they could isolate one mirror image for evaluation as a drug candidate.

“By using a single-enantiomer partner in a cross-coupling reaction, we can rapidly generate a diverse library of biologically active molecules for use in drug screening,” he said.

The research was funded by the National Institutes of Health, City College, the Alfred P. Sloan Foundation and PSC-CUNY, with additional support from the National Science Foundation and the American Chemical Society Petroleum Research Fund.

Further Information
Access to this exclusive content is for Technology Networks Premium members only.

Join Technology Networks Premium for free access to:

  • Exclusive articles
  • Presentations from international conferences
  • Over 2,600+ scientific posters on ePosters
  • More than 3,800+ scientific videos on LabTube
  • 35 community eNewsletters

Sign In

Forgotten your details? Click Here
If you are not a member you can join here

*Please note: By logging into you agree to accept the use of cookies. To find out more about the cookies we use and how to delete them, see our privacy policy.

Scientific News
Enzyme Malfunction May be Why Binge Drinking Can Lead to Alcoholism
A new study in mice shows that restoring the synthesis of a key brain chemical tied to inhibiting addictive behavior may help prevent alcohol cravings following binge drinking.
Developing a Gel that Mimics Human Breast for Cancer Research
Scientists at the Universities of Manchester and Nottingham have been funded to develop a gel that will match many of the biological structures of human breast tissue, to advance cancer research and reduce animal testing.
Lung Repair and Regeneration Gene Discovered
New role for hedgehog gene offers better understanding of lung disease.
New Gene Therapy for Vision Loss From a Mitochondrial Disease
NIH-funded study shows success in targeting mitochondrial DNA in mice.
Self-Propelled Powder to Stop Bleeding
UBC researchers have created the first self-propelled particles capable of delivering coagulants against the flow of blood to treat severe bleeding, a potentially huge advancement in trauma care.
Tension Helps Heart Cells Develop Normally in the Lab
Stanford engineers have uncovered the important role tension plays in growing heart cells out of the body.
Controlling Body Temperature in Response to 'Fight or Flight'
New research in The FASEB Journal suggests that blocking TRPV1 protein causes an increased release of noradrenaline, leading to an increase in core body temperatures.
Inroads Against Leukaemia
Potential for halting disease in molecule isolated from sea sponges.
Researchers Disguise Drugs As Platelets to Target Cancer
Researchers have for the first time developed a technique that coats anticancer drugs in membranes made from a patient’s own platelets.
A Fundamental Protection Mechanism Against Formalin In Mammals is Revealed
Formaldehyde, or formalin, is well known to all of us as a common chemical used in many industrial processes and also as a preservative, remarkably we also produce formaldehyde in our bodies.

Skyscraper Banner
Go to LabTube
Go to eposters
Access to the latest scientific news
Exclusive articles
Upload and share your posters on ePosters
Latest presentations and webinars
View a library of 1,800+ scientific and medical posters
2,600+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
3,800+ scientific videos