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BioFocus e-update autumn 09
Celebrating 10 years, 100 libraries, and 100 patents
In September of 2009 we launched our 100th SoftFocus® library - 2009 also marks the 10 year anniversary of this cutting edge product. The SoftFocus libraries are designed to give higher hit-rates against appropriate targets than diverse screening can achieve. In addition, the design of the libraries yields immediate structure-activity relationships which can shorten hit-to-lead timelines thus accelerating drug discovery. The success of our libraries can be measured in many ways, but the fact we are most proud of at BioFocus is that the screening of our SoftFocus libraries has led to more than 100 patents and several clinical candidates.
In the past 10 years we have expanded our range of available libraries from kinase and GPCR focused libraries to ion channels (ligand and voltage dependent), nucleosides and proteases. Most recently we have launched a helix mimetic library, the first in what we plan to be a series of new libraries targeting protein-protein interactions.
To learn more about our library design, view structures and check on availability please visit our newly developed secure library website.
Thought leaders gather for successful GPCR conference
On September 22nd-23rd 2009, BioFocus, in collaboration with MDS Analytical Technologies and DiscoveRx Inc., hosted a panel of thought leaders from the pharmaceutical and academic sectors to explore novel applications and cutting edge technologies for GPCR screening and profiling. The latest research and the evolution of our understanding of GPCR biology and chemistry were discussed. Topics included the use of structural biology analysis, label free methodologies, novel fluorescent ligands and state of the art instrumentation. Speakers and delegates enjoyed the two-day event as part of a new series of scientific meetings devised, part-sponsored and hosted by BioFocus.
The conference included a keynote address by Fiona Marshall (Heptares Therapeutics) describing the use of mutagenesis and structural biology techniques to generate stable isolated GPCR proteins for use in drug discovery, followed by David Fischer (BioFocus) who discussed how GPR3 was identified as a novel Alzheimer's drug target in human cells using BioFocus target discovery expertise (see Science, 2009, 323(5916), 946-951).
Speakers from within the academic sector included Anthony Davenport (University of Cambridge) presenting his research into orphan and deorphanised GPCRs in drug discovery; David Greaves (University of Oxford) who is investigating GPCRs as targets for inflammation, and Thierry Durroux (CNRS) who is using time resolved fluorescence resonance transfer to study GPCR/GPCR and GPCR/ ligand interactions. Pharmaceutical industry speakers included Steve Charlton (Novartis) who reviewed the use of new assay technologies study β2 adrenoceptor signalling kinetics; Kalpana Patel (GlaxoSmithKline) and Graham Rickett (Pfizer) who both presented their individual approaches to configuring clinically-predicative assay readouts; Richard Fosbeary (Takeda Cambridge) who reviewed use of CellKey™ cell impedance technology for configuring Gαi coupled receptor activity; and Xavier Leroy (Actelion Pharmaceuticals) who reviewed multiplexed and real time assay formats for the study of GPCRs. The second day of the conference included presentations regarding the latest technological innovations from MDS Analytical Technologies and DiscoveRx, alongside presentations focused upon the use of cutting edge technologies for GPCR research from GlaxoSmithKline (Angela Dunne, Andrew Green and Leonarda Di Candia) and Novo Nordisk (Lone Pridal).
This was the second in a new series of scientific conferences organised by BioFocus, hosted at the Nucleus Conference Centre, Saffron Walden. The GPCR conference follows the highly successful Ion Channels in Drug Discovery and Development meeting which took place in October 2008, co-hosted with MDS Analytical Technologies. The aim of the series of conferences is to provide a forum for industry and academic researchers to exchange scientific ideas and experiences in key areas of drug discovery. The co-organisers subsidise each conference making attendance free to delegates. Details regarding the theme for the next conference will be released early in 2010.
The changing world of drug discovery
Richard Gordon, Senior Director Sales and Marketing
The world around us is changing at an ever increasing pace as companies seek new ways to survive the current economic environment. The biopharmaceutical industry is not immune and the changes in the 'top 20' companies in the last 12 months highlight this with mergers, acquisitions and site closures dominating the news. In addition, the biotechnology industry is under severe pressure as venture capital organizations become more critical in their investment patterns, whilst the big pharmaceutical companies wait to pick up "closing down" bargains. Charities and not-for-profit organizations sponsoring drug discovery have also had constraints placed on spending, as investment income falls and in some cases, street donations have reduced!
Conversely, the mood in the pharmaceutical CRO industry has remained quite buoyant as organizations requiring access to research capabilities and technologies are clearly moving from outsourcing parts of projects to employing organizations capable of taking on integrated projects, with the CRO handing back the finished product at the end. This is a clear trend and is widely tipped to be the next generation of outsourcing model.
If you wish to see how BioFocus can help you with outsourcing integrated projects, please contact us.
A subtle name change, new faces and new partners
Chris Newton, SVP BioFocus
What is in a name? Company names usually convey a message – the names of its owners, what the company does, or (with combination names) reflecting two organizations that came together. In July 2006, BioFocus and Discovery Partners International (DPI) merged their operations. In the intervening three years, the trading organization BioFocus DPI has built a great reputation for focusing chemistry on biological endpoints and being a preferred partner for the discovery of new drugs. However, today the DPI part of the trading name has rather lost its association with “partnership”, indeed some think the DPI suffix is akin to the German AG, or US Inc., suggesting incorporation in some unrevealed country. Hence we deem it right to change our trading name now back to simply “BioFocus”. Our literature and materials will begin to reflect this change from October 2009.
Good organizations employ the best people. Our ADME/PK division that supports our integrated drug discovery service unit in the UK will be directed by Dr. John Nash from October 2009. John joins us from the Charles River organization in North America, where in the past few years he has built a very successful ADME/PK service business.
Our network of technology partners continues to expand, with DiscoveRx Inc. being the subject of our latest announcement. BioFocus now has preferential access to GPCR screening technologies from US-based DiscoveRx, which we think our screening partners with interest in drug discovery against GPCRs will find extremely useful.
Can stem cells help us generate better disease-relevant in vitro assays?
Kate Hilyard, VP Biological Sciences
Drug discovery for many important human diseases is hampered by the fact that disease relevant in vitro assays are not readily available. For example, being able to access human motor neurons for preclinical assays is very challenging, and having a supply that enables a screen of, e.g., 30,000 data points for either target discovery or drug discovery has previously been impossible. The advent of stem cell biology is changing this as more is learnt about how to culture stem cells in large quantities and differentiate them consistently into the target cell of interest.
Many biotechnology companies are betting on the clinical application of stem cell therapy to generate a good return on their investment. We are applying stem cells to open new areas of in vitro research. Disease relevant assays can be used for target discovery and for hit finding and compound profiling. The target discovery platform at BioFocus uses an adenoviral library of short hairpin RNAs (SilenceSelect®) to knockdown the druggable genome in a disease relevant phenotypic assay in order to identify novel disease targets. We are currently applying this to the orphan disease amyotrophic lateral sclerosis or ALS, using a disease relevant assay that utilizes motor neurons produced from human stem cells, supplied by California Stem Cells Inc. The ion channel team of BioFocus has validated the motor neuron phenotype using electrophysiology. This program would not be possible without this source of human motor neurons.
Other applications of stem cell derived cells are in the area of ADME. Key cell types that are being generated are hepatocytes and cardiomyocytes for the study of drug metabolism and toxicology.
The biology of the differentiation process is complex and the factors required to differentiate the cells are kept as secret recipes. But as more types of cells are differentiated and the processes are validated for reproducibility, for example growth of the differentiated cells in 96 well plates is one significant challenge that has been overcome in the ALS project, we hope this approach will help to de-orphanise some of our most challenging degenerative diseases and give patients hope.
Hot topics in drug discovery: finding the next lead
Aimed at both medicinal chemists and biologists, this meeting on November 11th at the SCI in Belgrave Square, London, UK will focus on the highlights of drug discovery and some industry best practices. Speakers from BioFocus and some of the world’s top pharma companies will cover a wide range of hot topics through actual experiences and case studies. Register now to guarantee your place at this impressive event.
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