Epigenetics
Bioscience 4 4 4 4 4 4 4
Cayman Chemical Diagenode EMD Millipore 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4
Epigentek 4 4 4 4 4
Invitrogen PerkinElmer Promega 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4
Reaction Biology 4 4 4 4 4 4 4
or label-free methods permitting the detection of multiple modification events across a single native substrate. Although some of the first reported assays for HDACs were mainly fluorimetric (based on flu- orescent intensity), epigenetic targets are increasing- ly being assayed by a broad range of different screening technologies. While many perceive radio- metric approaches as the ‘gold standard’, the jury is out as to which technology will prove most predic- tive and suited to routine primary screening. As the survey pointed out, there are important challenges, such as assay specificity and the retention of activity in purified proteins, which must be addressed. However, there does appear to be advantages asso- ciated with some of the more generic approaches currently being validated, for example suitability to all types of histone substrates and application across a diverse range of histone modifications. These approaches now need to be translated in a set of robust ready-to-use assay kits or tool-box reagents to really open up the field to HTS. Table 1 also high- lights the increasing number of vendors that now offer fee-for-service screening and profiling against epigenetic targets. It is premature to describe this activity as comparable to kinase outsourcing, but
Drug Discovery World Spring 2011
clearly the industry is gearing up in the expectation that many companies will choose to outsource com- pound testing against a panel of epigenetic assays. The survey showed that one of the main drivers for this was to access an assay/screening technology respondents do not have or use in-house. In conclu- sion, the tools required to support epigenetic screen- ing are fast emerging as our knowledge of these tar- gets increases, such that we can expect to see greater adoption or external use of these assays by Pharma and Biotech lead discovery programmes over the coming years.
DDW
Dr John Comley is Managing Director of HTStec Limited, an independent market research consultan- cy whose focus is on assisting clients delivering novel enabling platform technologies (liquid handling, lab- oratory automation, detection instrumentation and assay reagent technologies) to drug discovery and the life sciences. Since its formation seven years ago, HTStec has published more than 50 market reports on enabling technologies and Dr Comley has authored more than 30 review articles in Drug Discovery World. Please contact
info@htstec.com for more information about HTStec reports.
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References 1The NIH Roadmap Epigenomics Program.
http://nihroadmap.nih.gov/epige nomics/. 2 Epigenetics – An Emerging Target Class For Drug Discovery, At the SBS 16th Annual Conference & Exhibition, Phoenix, Arizona, April 11-15, 2010. 3 Epigenetic Screening Trends 2010 Report, published by HTStec Limited, Cambridge, UK, June 2010.
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