Featured Research

from universities, journals, and other organizations

Technological breakthrough paves the way for better drugs

Date:
July 5, 2013
Source:
Karolinska Institutet
Summary:
Researchers have developed the first method for directly measuring the extent to which drugs reach their targets in the cell. The method could make a significant contribution to the development of new, improved drug substances.

This illustration shows the path of a drug from a pill to a drug target.
Credit: Daniel Martinez Molina

Researchers at Karolinska Institutet in Sweden have developed the first method for directly measuring the extent to which drugs reach their targets in the cell. The method, which is described in the scientific journal Science, could make a significant contribution to the development of new, improved drug substances.

Most drugs operate by binding to one or more proteins and affecting their function, which creates two common bottlenecks in the development of drugs; identifying the right target proteins and designing drug molecules able to efficiently seek out and bind to them. No method has been available for directly measuring the efficiency of the drug molecules to locate and bind to its target protein. Now researchers from Karolinska Institutet have developed a new tool called CETSA (Cellular Thermal Shift Assay), which utilise the concept that target proteins usually get stabilised when drug molecules bind.

"We have shown that the method works on a wide variety of target proteins and allows us to directly measure whether the drug molecules reach their targets in cells and animal models," says lead investigator Professor Pär Nordlund of the Department of Medical Biochemistry and Biophysics. "We believe that CETSA will eventually help to improve the efficiency of many drugs and contribute to better drug molecules and more successful treatments."

The lack of methods to directly measure the binding of a drug to its target protein has caused a degree of uncertainty in many phases of drug development. In some cases, where drug candidates have not lived up to expectations in clinical trials on humans, it has transpired that the drug molecules have failed to bind to the right protein. The group behind the study believes that CETSA will be an important control stage and a complement to other methods.

In the present study, the researchers also examined processes that can lead to drug resistance in cells. The team believes that by virtue of its ability to determine whether existing drugs are suitable for individual patients, the method is of potential value to the practice of individualised treatment.

"We believe that the method can provide an important diagnostic tool in the treatment of cancer, for example, as CETSA can, in principle, enable us to determine which drug is most effective at targeting the proteins in the tumour," says Daniel Martinez Molina at the Department of Medical Biochemistry and Biophysics, who leads a team in the project aiming at establishing CETSA for patient studies. "This also makes it possible for clinicians to ascertain at an early stage of treatment whether the tumour has developed a certain kind of resistance and which type of therapy could then be more suitable for the patient."

The evaluation of CETSA has been conducted in collaboration with Yihai Cao's research group at the Department of Microbiology, Tumor and Cell Biology at Karolinska Institutet, Pelago Bioscience AB and Nanyang Technological University in Singapore. Professor Pär Nordlund and Dr Daniel Martinez Molina are two of the founders of the company, which was also involved in the study. The project was financed by external grants from the Swedish Research Council, the Swedish Cancer Society and the European Research Council.


Story Source:

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


Journal Reference:

  1. D. M. Molina, R. Jafari, M. Ignatushchenko, T. Seki, E. A. Larsson, C. Dan, L. Sreekumar, Y. Cao, P. Nordlund. Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay. Science, 2013; 341 (6141): 84 DOI: 10.1126/science.1233606

Cite This Page:

Karolinska Institutet. "Technological breakthrough paves the way for better drugs." ScienceDaily. ScienceDaily, 5 July 2013. <www.sciencedaily.com/releases/2013/07/130705101541.htm>.
Karolinska Institutet. (2013, July 5). Technological breakthrough paves the way for better drugs. ScienceDaily. Retrieved July 22, 2014 from www.sciencedaily.com/releases/2013/07/130705101541.htm
Karolinska Institutet. "Technological breakthrough paves the way for better drugs." ScienceDaily. www.sciencedaily.com/releases/2013/07/130705101541.htm (accessed July 22, 2014).

Share This




More Health & Medicine News

Tuesday, July 22, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Courts Conflicted Over Healthcare Law

Courts Conflicted Over Healthcare Law

AP (July 22, 2014) — Two federal appeals courts issued conflicting rulings Tuesday on the legality of the federally-run healthcare exchange that operates in 36 states. (July 22) Video provided by AP
Powered by NewsLook.com
Why Do People Believe We Only Use 10 Percent Of Our Brains?

Why Do People Believe We Only Use 10 Percent Of Our Brains?

Newsy (July 22, 2014) — The new sci-fi thriller "Lucy" is making people question whether we really use all our brainpower. But, as scientists have insisted for years, we do. Video provided by Newsy
Powered by NewsLook.com
Scientists Find New Way To Make Human Platelets

Scientists Find New Way To Make Human Platelets

Newsy (July 22, 2014) — Boston scientists have discovered a new way to create fully functioning human platelets using a bioreactor and human stem cells. Video provided by Newsy
Powered by NewsLook.com
Gilead's $1000-a-Pill Drug Could Cure Hep C in HIV-Positive People

Gilead's $1000-a-Pill Drug Could Cure Hep C in HIV-Positive People

TheStreet (July 21, 2014) — New research shows Gilead Science's drug Sovaldi helps in curing hepatitis C in those who suffer from HIV. In a medical study, the combination of Gilead's Hep C drug with anti-viral drug Ribavirin cured 76% of HIV-positive patients suffering from the most common hepatitis C strain. Hepatitis C and related complications have been a top cause of death in HIV-positive patients. Typical medication used to treat the disease, including interferon proteins, tended to react badly with HIV drugs. However, Sovaldi's %1,000-a-pill price tag could limit the number of patients able to access the treatment. TheStreet's Keris Lahiff reports from New York. Video provided by TheStreet
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