Navigation Links
Image of new antibiotic in action opens up new opportunities to combat antibacterial resistance
Date:8/4/2010

Detailed pictures published today reveal how a new type of experimental antibiotic can kill bacteria that are already resistant to existing treatments [1]. The findings could ultimately help scientists to develop new antibiotics to tackle the bacteria responsible for many hospital and community-acquired infections.

Using an imaging technique called x-ray crystallography, a team of researchers from GlaxoSmithKline (GSK) captured a snapshot of the new compound latched on to the enzyme topoisomerase. This enzyme is part of the bacteria's internal machinery and helps the bacteria produce proteins and replicate. Stopping this enzyme prevents the bacteria from reproducing. Medicines, known as the quinolones, that target the enzyme have been used successfully as antibiotics since 1962, however bacteria are increasingly developing resistance to this class of drugs.

By looking at x-ray images, the team have demonstrated that the new investigational medicine attaches to the enzyme in a different place to the quinolones, enabling it to stop the same bacteria that are resistant to these older treatments. The research is published today in the journal Nature, and is the result of two unique collaborations between GSK and the Wellcome Trust's Seeding Drug Discovery initiative and the U.S. Defense Threat Reduction Agency (DTRA).

"We already knew that targeting this enzyme was clinically proven to stop bacteria in their tracks, we just needed to be a bit more inventive in how we attacked it," said Michael Gwynn, from GSK's Infectious Diseases research group. "These images and the data showing the efficacy of this compound against a range of bacteria validate our approach, demonstrating that the enzyme can still be blocked even in bacteria already resistant to other antibiotics that work against this same enzyme."

The study also reports the potency of the new compound, called GSK 299423, against antibiotic-resistant strains of bacteria such as Staphylococus aureus, including methicillin resistance S. aureus (MRSA), and against gram negative bacteria like E. coli, Pseudomonas, Klebsiella and Acinetobacter. Gram-negative bacteria are particularly difficult to attack as they have an outer membrane surrounding the bacterial cell wall which interferes with drug penetration. New medicines must not only be toxic to the pathogen, but must first overcome the barriers to entry into the cell.

Commenting on the importance of the findings, Ted Bianco of the Wellcome Trust said: "This is an important step forward in the race against antibiotic resistance. By solving the new structure of this important bacterial enzyme, and understanding how these drugs work, the team has opened the door for targeted drug design of new antibiotics, which are urgently needed."

The particular compound from this study is one of a group that is currently being worked on in order to develop the best compounds in terms of efficacy and safety. This should help identify drug candidates that could be taken forward into early stage trials in humans.

Development of the new drug class to tackle gram-negative infections is supported as part of the Trust's Seeding Drug Discovery initiative. The collaboration provides GSK with a 4 million award from the Trust with GSK matching the contribution in staff, equipment, and other programme costs. The research collaborations with the Trust and with DTRA are aimed at developing an entirely new class of antibacterials to tackle hospital-acquired infections and potential bio-threat outbreaks.

"The Wellcome Trust has recently announced a five-year extension to the Seeding Drug Discovery initiative, enabling us to continue to support drug development in areas of unmet medical need," added Rick Davis, Business Development Manager at the Wellcome Trust.


'/>"/>

Contact: Jen Middleton
j.middleton@wellcome.ac.uk
44-207-611-7262
Wellcome Trust
Source:Eurekalert

Related biology technology :

1. Repligen Announces FDA and EMA Approval of Re-analysis of Images from Phase 3 Trial of RG1068 for Pancreatic Imaging
2. Physicists capture first images of atomic spin
3. Caliper Life Sciences Launches Living Image(R) 4.0 Software
4. Imagenetix to Present at 2nd Annual LD MICRO Conference at the Luxe Sunset Bel Air
5. Imagenetix, Inc. to Present at the 2009 RedChip New York Equities Conference
6. First Spaceborne Hyperspectral Imager Will Use QImaging Rolera-MGi EMCCD Camera
7. Imagenetix, Inc. Announces Interview With Bloomberg Radio
8. Boston University Periodontal Study on Imagenetix Compound Published in The Journal of Periodontology
9. Imagenetix, Inc. Reports First Quarter 2010 Results
10. Powerful Image Registration and Recognition Software Unveiled for Medical, Satellite, and Defense Imaging Industries
11. ChemImage Works to Improve Existing Methods of Imaging Untreated Fingerprints on Paper Substrates
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:7/18/2017)... , ... July 18, 2017 , ... Blood centers traditionally ... across the region. Nationally, summer is a struggle for community blood centers as high ... San Antonio Chamber of Commerce is teaming up with the South ...
(Date:7/17/2017)... ... ... The Academy of Model Aeronautics (AMA) will host Aviation Adventure Day on ... from 9 a.m. to 2 p.m. at the International Aeromodeling Center in Muncie, Indiana. ... Day will be packed with entertaining activities for the entire family. Attendees will learn ...
(Date:7/17/2017)... ... July 17, 2017 , ... Panitch Schwarze Belisario ... in the BiG (Biomedical Innovation Group) annual meeting in China. , This year’s ... antigen receptor T-cell) therapy, a rapidly developing highly personalized anti-cancer technology that involves ...
(Date:7/16/2017)... ... July 16, 2017 , ... OHAUS Corporation, a ... launch of its new line of Extreme Environment Shakers today. , Extreme Environment ... and humidity for optimal cell growth such as cell cultures, solubility studies and ...
Breaking Biology Technology:
(Date:4/24/2017)... -- Janice Kephart , former 9/11 Commission ... LLP (IdSP) , today issues the following statement: ... 6, 2017 Executive Order: Protecting the Nation ... instilled with greater confidence, enabling the reactivation of ... are suspended by until at least July 2017). ...
(Date:4/17/2017)... , April 17, 2017 NXT-ID, Inc. ... company, announces the filing of its 2016 Annual Report on Form ... Exchange Commission. ... Form 10-K is available in the Investor Relations section of the ... on the SEC,s website at http://www.sec.gov . 2016 ...
(Date:4/11/2017)... BEACH GARDENS, Fla. , April 11, 2017 ... identity management and secure authentication solutions, today announced ... contract by Intelligence Advanced Research Projects Activity (IARPA) ... for IARPA,s Thor program. "Innovation has ... onset and IARPA,s Thor program will allow us ...
Breaking Biology News(10 mins):