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Fraunhofer IME integrates European ScreeningPort to enhance its expertise and capabilities in drug discovery

Industry news / 9 July 2014 / Fraunhofer

The operative business of European ScreeningPort GmbH has been integrated into the Fraunhofer Institute for Molecular Biology and Applied Ecology IME located in Aachen…

Screening: In-depth focus 2013

Issue 3 2013, Screening, Supplements / 30 July 2013 / Anthony Mitchell Davies, Alice Vajda, Sarah Louise, Laure Marignol, Sheraz Gul, Emma J. Shanks

New approaches to cell based assays for high content screening and analysis.
Reduce, reuse, recycle: how drug repositioning is finding its niche in drug discovery.
Workshop Review: Biochemical assays for screening.
Screening roundtable.

Sheraz Gul

The evolution of the Contract Research Organisation and the future of the pharmaceutical industry

Contract Research, Issue 1 2013 / 20 February 2013 / Kevin Lustig and Maria Thompson, Assay Depot, Sheraz Gul, European ScreeningPort GmbH,

This article discusses how the pharmaceutical industry can leverage its competencies in outsourcing to accelerate time to market, improve quality and increase innovation at all stages of the drug discovery and development process. The pharmaceutical industry is being battered by a perfect storm of not just one but three major issues, any of which on its own would prove a tough nut to crack…

Drug discovery assays for the histone deacetylase class of enzymes

Drug discovery assays for the histone deacetylase class of enzymes

Issue 6 2012, Screening / 18 December 2012 / Sheraz Gul and Gesa Witt, European ScreeningPort GmbH

The histone deacetylase (HDAC) class of enzyme are a group of conserved enzymes known for their ability to remove acetyl groups from lysine residues on histone tails. Since aberrant HDAC enzyme expression is observed in various diseases, there is increasing interest in finding small molecules which function as HDAC enzyme inhibitors. This article reviews the various biochemical assays available for monitoring HDAC enzyme activity that have been validated for use in High Throughput Screening. The assays referred to are compatible with standard microtitre plates (96 and 384 well format) and make use of absorbance, luminescence and fluorescence detection methods.

The histone deacetylase class of enzymes: The histone deacetylase (HDAC) class of enzymes are involved in many biological pathways and one of their best known properties is their ability to remove acetyl groups from lysine residues on amino-terminal histone tails. Thus far, 18 HDAC enzymes have been identified which are divided into zinc dependent and NAD dependent enzymes. The Class I HDAC enzymes include the zinc dependent HDACs 1, 2, 3, and 8 and consist of 350-500 amino acid residues. The Class II HDAC enzymes are also zinc dependent but are larger, consist of about 1,000 amino acid residues and are subdivided into Class IIa (HDAC4, 5, 7, and 9) and Class IIb (HDAC6 and HDAC10) enzymes. The Class I and Class II HDAC enzymes can be inhibited by trichostatin A (TSA) and this inhibitor is often used as a reference to bench-mark their assays. The Class III HDAC enzymes are the sirtuin enzymes (SIRT1-7) and are NAD-dependent. This class of enzymes is not sensitive to TSA but can be inhibited for example by nicotinamide.

RedHill Biopharma has last patient visit in phase IIa study with RHB-104 for multiple sclerosis

Discovery and validation of biomarkers for multiple sclerosis

Issue 6 2011, Screening / 13 December 2011 / Ole Pless and Sheraz Gul, European ScreeningPort GmbH

Multiple Sclerosis (MS) is an autoimmune disease leading to a chronic inflammation and degeneration of the central nervous system. It is one of the major neurological diseases with approximately 2.5 million suffering patients worldwide. Until now, the underlying mechanisms have not been fully elucidated, but the cause of the disease can be modulated to limit progression and severity. Currently, there are no validated biomarkers available to predict the progression of MS or response to a clinical intervention apart from MRI. In order to identify protein biomarkers for MS as well as other diseases, significant infrastructure is required and this is discussed.

The term ‘biomarker’ has been defined as a “characteristic that is objectively measured and evaluated as an indicator of normal biological processes, pathogenic processes, or pharmacologic responses to a therapeutic intervention”. The measurement of normal and dysfunctional biological processes and their changes in response to therapeutic intervention forms the basis of biomarkers. The advances in genetics and molecular biology leading to the sequencing of the human genome has resulted in the identification of a variety of novel targets implicated in different disease states. Further technological developments including high throughput profiling of various samples using genomics, transcriptomics and proteomics has led to the identification of gene and protein based markers that characterise disease states for a number of indications including breast cancer, colorectal cancer and cardiovascular diseases. Additional initiatives that have led to the identification of biomarkers with minimal invasive methods such as proteomics technologies and systems biology have proven extremely effective for discovering potential biomarkers and drug targets. These technologies tend to provide large data sets that can be difficult to deconvolute for biomarker discovery. This bottleneck can be reduced by using several strategies. The first is to constrict the number of potential biomarkers and drug targets by dividing the proteome into smaller, more biologically significant segments. The second is to widen the bottleneck with higheroutput and higher-throughput screening technologies. The third is to incorporate more preliminary validation into the discovery process. New and emerging technologies provide promise for each of these strategies.

Drug discovery assays for the histone deacetylase class of enzymes

Implementing electronic laboratory notebooks to improve the efficiency of pre-clinical drug discovery

Informatics, Issue 6 2011 / 13 December 2011 / Sheraz Gul, Vice President and Head of Biology, European ScreeningPort GmbH

The pre-clinical phase of drug discovery spans a period in the region of five years and requires contributions from multi-disciplinary teams often working at different sites. These teams can generate significant amounts of data which are processed using standard as well as specialist software. The recording of a substantial amount of project related experimental work has historically been performed using paper-based laboratory notebooks completed manually with all files usually being stored locally.

This scenario poses a variety of issues such as delayed access to important information to the project team members which could ultimately reduce its efficiency and thus increase the time taken to complete the project. These paper-based notebooks are now being replaced by an electronic laboratory notebook (eLNB) within research laboratories in industry and academia. Such software allows the documentation of experimental data and its sharing within the multi-disciplinary research team and would be expected to improve data integrity, reduce the time to complete the project and improve communication. This article discusses some of the advantages that would be expected to be achieved upon implementing an eLNB in pre-clinical drug discovery.

Sheraz Gul

Reducing attrition in drug discovery: The role of biomarkers

Cancer Biology, Issue 3 2011 / 20 June 2011 / Sheraz Gul, Vice President & Head of Biology, European ScreeningPort GmbH

The development of most diseases is often attributed to the dysfunction of the activities of key proteins involved in biological processes and their modulation by a therapeutic agent is considered to offer the potential to alleviate the disease state.

Figure 1 Typical critical path for small molecule Drug Discovery programs. Drug Discovery involves identification of a Target of interest for which an assay is developed. This assay is then adapted for screening purposes and utilised in a High Throughput Screening campaign against small molecule libraries. The High Throughput Screening campaign will usually yield many Hit molecules. Confirmation, Counter and Selectivity Screening will provide a final list of Validated Hits.

Establishing assays and small molecule screening facilities for Drug discovery programs

Issue 1 2011, Screening / 16 February 2011 / Sheraz Gul, Vice President & Head of Biology, European ScreeningPort GmbH

Although many of the marketed small molecule drugs have been discovered by research and development efforts within the pharmaceutical industry, there has been a paradigm shift with external sources increasingly being relied upon to fill their pipelines. This trend is likely to increase and the key pre-clinical activities carried out by organisations outside the pharmaceutical industry include target validation, assay development and their use in High Throughput Screening campaigns, validation of the Hit molecules, Hit-to-Lead and Lead-to-Candidate screening/chemistry. In order to perform these activities, adequate know-how and technical expertise is essential so that the processes meet appropriate industry standards. This article discusses some of the challenges associated with assay development and the automation of High Throughput Screening.

drug discovery & drug development

Implementation of appropriate assays and HTS technologies in drug discovery

Issue 2 2010, Screening / 9 May 2010 / Sheraz Gul, Vice President, European ScreeningPort GmbH

In this article, an overview regarding advances in assay formats for specific target classes and options that should be considered when considering hardware will be given. There has been a significant growth in the assay and automation technologies that are available for compound screening activities and it is essential to evaluate a variety of these before beginning a drug discovery program, the aims of these being to ensure the most relevant assay formats that are available are adopted.

The changing landscape of automation in pre-clinical drug discovery

Industry Focus 2010, Past issues / 22 February 2010 /

Over the past decade we have seen a significant realignment of activities associated with drug discovery and this will continue for a multitude of reasons. Within the pharmaceutical industry we have seen significant changes e.g. a decrease in the numbers of drugs that are being approved by the regulatory authorities and the looming expiration of patented drugs, both of which have an immediate and direct consequence on revenue streams. In light of these issues, the pharmaceutical industry is responding appropriately. These changes have included a re-assessment of the strategies being employed in the pre-clinical phase of drug discovery, some of which are discussed in relation to automation solutions.

Lab Automation Roundtable

Issue 6 2009, Past issues / 12 December 2009 /

Participants: Dr Gordon R Alton, President and CEO, Altonyx Consulting / Dr Scott Bowes
Scientist, Novartis / Dr Sheraz Gul, Vice President and Head of Biology, European ScreeningPort /
Chris Molloy, Vice President of Corporate Development, IDBS

Development and implementation of an automated compound screening activities facility

Issue 2 2009, Past issues / 20 March 2009 /

There has been a continuous move by the large commercially orientated players involved in Drug Discovery to initiate novel methods to increase income streams and productivity. An example of the former has been the acquisition of companies and their drug pipelines and in the case of the latter, rationalisation of internal Research & Development activities. This is well illustrated by GlaxoSmithKline Pharmaceuticals which have formed small focused research units called the Centres for Excellence in Drug Discovery (CEDD) and the Discovery Performance Units (DPU) each of which having increased accountability1.

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