Navigation Links
Lengthening time a drug remains bound to a target may lead to improving diagnostics, therapy
Date:4/25/2010

ANAHEIM, CA Studies led by Stony Brook University professor of chemistry Peter J. Tonge indicate that modifications that enhance the time a drug remains bound to its target, or residence time, may lead to better diagnostic and therapeutic agents.

Tonge will present these results at the American Society for Biochemistry and Molecular Biology's annual meeting in a talk titled "Slow Onset Inhibitors of Bacterial Fatty Acid Biosynthesis: Residence Time, In Vivo Activity and In Vivo Imaging." The talk will be held in Anaheim Convention Center Room 304C, on Sunday April 25 at 9:55 am PST.

"Our research team believes that many drugs are effective because they have long residence times on their target," says Tonge, Director of Infectious Disease Research at the Institute for Chemical Biology & Drug Discovery. "This concept has largely been ignored by investigators, and residence time is not usually incorporated into the drug discovery process."

Tonge explains that most drug discovery efforts obtain only data on the thermodynamic affinity of the drug for its target, measurements that are made at constant drug concentration. However, the Stony Brook University-led research factors in residence time, which he emphasizes is critical for activity in vivo where drug concentrations fluctuate with time.

"The central component of our work is that the length of time a drug remains bound to a target is very important for the activity of the compound in vivo," he adds.

Tonge, together with collaborators at Colorado State University and the University of Wrzburg in Germany, have developed a series of compounds that inhibit an enzyme target from Francisella tularensis, where the in vivo antibacterial activity of the compounds correlates with their residence time on the target and not with their thermodynamic affinity for the target. This resulted in a direct correlation between residence time and in vivo activity against an infectious agent.

The research team has also developed a long residence time inhibitor of an enzyme drug target in Mycobacterium tuberculosis and demonstrated that this compound has antibacterial activity in an animal model of tuberculosis.

Because compounds with long residence times should accumulate in bacteria, Tonge explains that the research may lead to the development of agents to image bacterial populations in vivo using positron emission tomography. He says that researchers could then further the concept and develop a method for non-invasive imaging of bacterial populations in humans for both diagnostic purposes and also to monitor bacterial load during drug therapy, thereby helping to chart a drug's effectiveness against bacterial infection.


'/>"/>

Contact: Nicole Kresge
nkresge@asbmb.org
202-316-5447
Federation of American Societies for Experimental Biology
Source:Eurekalert

Related biology news :

1. Northern forests do not benefit from lengthening growing season
2. Ancient remains put teeth into Barker hypothesis
3. A year after discovery, Congos mother lode of gorillas remains vulnerable
4. Lead-based consumer paint remains a global public health threat
5. Analysis of Copernicus putative remains support identity
6. Laughter remains good medicine
7. Laughter remains good medicine
8. Accelerated bone turnover remains after weight loss
9. New technique determines the number of fat cells remains constant in all body types
10. Chesapeake Bay ecosystem health remains poor, but slightly improved in 2007
11. Fear of being laughed at crosses cultural boundaries
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:4/11/2017)... 11, 2017 NXT-ID, Inc. (NASDAQ:   ... announces the appointment of independent Directors Mr. Robin D. ... Board of Directors, furthering the company,s corporate governance and expertise. ... Gino Pereira , ... forward to their guidance and benefiting from their considerable expertise ...
(Date:4/5/2017)... Today HYPR Corp. , leading innovator ... of the HYPR platform is officially FIDO® Certified ... architecture that empowers biometric authentication across Fortune 500 enterprises ... over 15 million users across the financial services industry, ... product suites and physical access represent a growing portion ...
(Date:4/3/2017)... , April 3, 2017  Data ... precision engineering platform, detected a statistically significant ... product prior to treatment and objective response ... the potential to predict whether cancer patients ... to treatment, as well as to improve ...
Breaking Biology News(10 mins):
(Date:10/10/2017)... (PRWEB) , ... October 10, 2017 , ... San Diego-based ... of its corporate rebranding initiative announced today. The bold new look is part ... as the company moves into a significant growth period. , It will also expand ...
(Date:10/10/2017)... ... October 10, 2017 , ... For the ... won a US2020 STEM Mentoring Award. Representatives of the FirstHand program travelled to ... Experience from US2020. , US2020’s mission is to change the trajectory of STEM ...
(Date:10/10/2017)... research firm Parks Associates announced today that Tom Kerber ... Annual Meeting , October 11 in Scottsdale, Arizona . ... how smart safety and security products impact the competitive landscape. ... Parks Associates: Smart Home Devices: Main Purchase Driver ... "The residential security market has experienced continued growth, and the ...
(Date:10/10/2017)... ... October 10, 2017 , ... ... business process optimization firm for the life sciences and healthcare industries, announces a ... in San Francisco. , The presentation, “Automating GxP Validation for Agile Cloud Platforms,” ...
Breaking Biology Technology: