Navigation Links
Lengthening time a drug remains bound to a target may lead to improving diagnostics, therapy

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
Federation of American Societies for Experimental Biology

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:
(Date:8/15/2017)... LLC , a medical device company focused on improving the safety ... ISO 13485 Certification, the global standard for medical device quality management ... ... for the early detection of IV infiltrations. ... "This is an important milestone for ivWatch, as it validates our ...
(Date:6/23/2017)... ITHACA, N.Y. , June 23, 2017 ... a leader in dairy research, today announced a new ... help reduce the chances that the global milk supply ... this dairy project, Cornell University has become the newest ... Food Supply Chain, a food safety initiative that includes ...
(Date:5/16/2017)... TEANECK, N.J. , May 16, 2017  Veratad ... leading provider of online age and identity verification solutions, ... the K(NO)W Identity Conference 2017, May 15 thru May ... Ronald Regan Building and International Trade Center. ... across the globe and in today,s quickly evolving digital ...
Breaking Biology News(10 mins):
(Date:10/11/2017)... N.C. (PRWEB) , ... October 11, 2017 , ... ... ARCS® Foundation President Andi Purple announced Dr. Suneel I. Sheikh, the co-founder, ... ( ASTER Labs ), Inc. has been selected for membership in ARCS ...
(Date:10/11/2017)... ... ... is a basic first aid supply for any work environment, but most personal eye wash ... if a dangerous substance enters both eyes? It’s one less decision, and likely quicker response ... piece. , “Whether its dirt and debris, or an acid or alkali, getting anything in ...
(Date:10/11/2017)... ... October 11, 2017 , ... Proscia Inc ., ... a Webinar titled, “Pathology is going digital. Is your lab ready?” with Dr. ... best practices and how Proscia improves lab economics and realizes an increase in ...
(Date:10/11/2017)... and LAGUNA HILLS, Calif. , Oct. ... Cancer Research, London (ICR) and University ... SKY92, SkylineDx,s prognostic tool to risk-stratify patients with multiple myeloma ... MUK nine . The University of Leeds ... partly funded by Myeloma UK, and ICR will perform the ...
Breaking Biology Technology: