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

Innovative Technology Enables First Crystal Structure of mGlu5 Transmembrane Domain to be Determined

Published: Saturday, July 19, 2014
Last Updated: Saturday, July 19, 2014
Bookmark and Share
Several novel drug candidates have been identified to help treat specific neuropsychiatric disorders.

The first high-resolution X-ray crystal structure of the metabotropic glutamate receptor 5 (mGlu5) transmembrane domain was reported in Nature this week. The work was performed at Heptares Therapeutics, a leading drug discovery and development company using TTP Labtech’s innovative liquid handling technology for lipidic cubic phase crystallography (mosquito LCP).

Dr Andy Doré, Head of Crystallography at Heptares Therapeutics and joint first author of the recent article in Nature, stated, "the mosquito LCP was used for all crystallization setups of the mGlu5-StaR resulting in us obtaining high resolution diffraction quality crystals for this receptor. The ability to reliably dispense low volume boli in 96 well LCP experiments using mosquito LCP is ideal for screening initial conditions and optimizing this and other difficult targets."

mGlu5 is a member of the GPCR family of proteins and plays an essential part in neuronal signalling making it an important drug target for modulating cell function and influencing neuropsychiatric disorders.

Metabotropic glutamate receptors are Class C GPCRs, which respond to the neurotransmitter glutamate and therefore are of considerable interest as drug targets for the treatment of a range of diseases, including fragile X syndrome, autism, depression, anxiety, addiction and movement disorders.

Structural studies to date have been restricted to the extracellular domain of mGlu5, providing little understanding of the membrane-spanning signal transduction domain, and hindering drug discovery efforts.

In this scientific publication the scientists at Heptares describe the crystal structure of the transmembrane domain of mGlu5 in complex with the negative allosteric modulator (NAM), mavoglurant. Heptares has used these new findings to identify several novel differentiated mGlu5 NAM drug candidates with improved potency and pharmacokinetic properties compared to previous candidate molecules.

To help increase the accuracy, speed and throughput of crystallography screening, optimization and crystal production, TTP Labtech has engineered innovative automated liquid handling solutions, including the mosquito crystal and mosquito LCP, to significantly improve this process.

TTP Labtech's mosquito LCP is used by most of the world class institutions and leading pharmaceutical and biotechnology companies for protein crystallization screening. It overcomes the common problems encountered with accurately dispensing the highly viscous LCP mixture used in membrane protein crystallization. It allows users to fully automate LCP set-ups accurately and repeatedly and the technology has played an important role in the determination of many protein structures, including some key GPCRs.

"As early adopters of the mosquito LCP, we have had a close collaborative relationship with Dr Doré's team since 2010," commented Joby Jenkins, global director of automation at TTP Labtech.

Jenkins continued, “The huge success of Heptares in determining ground breaking GPCR structures has resulted in increased productivity and the need for additional mosquito LCP instruments. We are delighted that our liquid handlers have been, and will be, an integral part of their ongoing success.”


Further Information

Join For Free

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 3,500+ scientific posters on ePosters
  • More than 5,000+ 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 TechnologyNetworks.com 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.

Related Content

David Newble Joins TTP Labtech as New Managing Director
Recent appointment promises to drive innovation strategy and further strengthen R&D pipeline
Thursday, June 18, 2015
TTP Labtech and Almac Group’s Form Strategic Alliance
Alliance consolidates fluorescence lifetime technology to form a one-stop shop for compound screening.
Thursday, February 05, 2015
TTP Labtech Revenues up 43%
The company has reported an impressive 43% increase in revenues and an associated increase in profits over 2013.
Monday, June 23, 2014
TTP Labtech Acquires Assets from AssayMetrics
Significant improvements in assay reagents and availability of HTS-compatible readers has propelled fluorescence lifetime technology to the vanguard of cost-effective screening technologies.
Thursday, January 09, 2014
Major Protein Structure Discovery Achieved Using TTP Labtech’s Mosquito LCP
Researchers have successfully reported the structure of a Class B G-Protein Coupled Receptor (GPCR) using lipidic cubic phase (LCP) protein crystallisation.
Friday, July 26, 2013
TTP Labtech Announces On-Going Growth
An investment of £3.8M in global R&D sees product sales grow over 20%.
Thursday, July 11, 2013
TTP Labtech Announces Company Growth
New product offering demonstrates strong commitment to product development.
Friday, May 11, 2012
Driving the Science of the Future
TTP LabTech announce that they are founding sponsors of the inaugural European Lab Automation (ELA) conference and exhibition, to be held at the Conference Centre Hamburg (CCH), Hamburg, Germany, from the 30th June-1st July.
Friday, May 20, 2011
Increased Demand Drives Queensland Compound Library Expansion
QCL capacity is increased by the acquisition of a fourth additional comPOUND® storage module.
Thursday, June 10, 2010
Improve your screening know-how with TTP LabTech at Screening Europe 2010
This year at Screening Europe 2010, TTP LabTech will be sharing its in-house expertise and technical advice with exhibition delegates in order to further improve current high content screening techniques and workflows.
Thursday, January 28, 2010
TTP LabTech Delivers Automated Chemistry System for Salt and Polymorph Screening to AstraZeneca
The three year laboratory automation project involved the design and build of a fully automated system for salt and polymorph screening of novel compounds.
Wednesday, January 28, 2009
TTP LabTech's European Roadshow
The roadshow offers the opportunity to try out the latest in low-volume liquid handling and high content screening systems, as well as learning more about compound management, instrumentation development and custom automation.
Thursday, September 13, 2007
TTP LabTech Announce US Expansion to Meet Growing Customer Demand
TTP LabTech further expands its US facilities with the recruitment of sales and customer service personnel for its East Coast office in Cambridge, MA.
Monday, July 30, 2007
TTP Extends Global Reach
After building up a strong base of customers in the USA and Europe over the past three years, TTP LabTech have now appointed distributors for Japan, India and Australia/New Zealand.
Wednesday, April 04, 2007
Scientific News
Mass Spec Technology Drives Innovation Across the Biopharma Workflow
With greater resolving power, analytical speed, and accuracy, new mass spectrometry technology and techniques are infiltrating the biopharmaceuticals workflow.
One Step Closer to Precision Medicine for Chronic Lung Disease Sufferers
A study led by University of North Carolina at Chapel Hill, and National Jewish Health, has provided evidence of links between SNPs and known COPD blood protein biomarkers.
CES Score May Predict Response to Cancer Treatment
Researchers identify new type of biomarker that helps predict prognosis and response to several types of cancer treatment.
Treating Sepsis with Marine Mitochondria
Mitochondrial alternative oxidase from a marine animal combats bacterial sepsis.
New Therapeutic Target for Crohn’s Disease
A promising new target for drugs that treat IBD has been identified along with a possible biomarker for IBD severity.
Researchers Find Fungus-Fighting Compound
A compound has been identifed that blocks growth of a fungus responsible for lung infections and allergic reactions.
Analysing 10,000 Cells Simultaneously
New techniquethat traps 10,000 cells on a single chip has potential for cancer screening for individuals.
Peer Reviewed Study Demonstrates Mass Spec Technique
The peer reviewed study demonstrates MS workflow, TMTCalibrator workflow, which dramatically enhances detection of key early stage Alzheimer’s biomarkers.
Small Molecules Lead to a Big Change in Reaction Outcomes
Scientists have changed the behaviour of a group of molecules involved in carbon-oxygen bond synthesis.
Enhancing Antibiotics to Defeat Resistant Bacteria
Scientists enhance ability of antibiotics to defeat resistant types of bacteria using molecules called PPMOs
SELECTBIO

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
3,500+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
5,000+ scientific videos
Close
Premium CrownJOIN TECHNOLOGY NETWORKS PREMIUM FOR FREE!