EVENT SPONSOR

Welcome to ELRIG’s Discovery Technologies 2021: Early Drug Discovery Strategies 

With the rapid advancement of new technologies the potential for developing life changing therapeutic interventions has never been so promising.  With these possibilities new challenges arise, not least how to prosecute drug discovery campaigns against new and novel targets and those previously deemed intractable. This conference will explore evolving early drug discovery technologies to overcome these obstacles by focusing on three core themes:

• Emerging Discovery Strategies:Historically drug discovery efforts largely focused on traditional target classes such as enzymes, GPCRs and nuclear receptors and aimed to modulate them via binding of small molecules or monoclonal antibodies. Whilst largely successful and still extremely relevant, it’s believed a large proportion of the human proteome, whilst may present valid targets, may be undruggable by these traditional approaches. Other valid targets are difficult to prosecute discovery campaigns against with the current technologies available. To continue to address unmet medical need, the discovery process needs to unremittingly evolve and innovate. Emerging Discovery Strategies will focus on these developing areas showcasing examples of identifying and utilising new target classes, drug modalities and the parallel development of novel screening strategies. We’ll also consider how exploitation of big data integrated with machine learning can help drive discovery efforts to new heights.
• Mass Spectrometry & Biophysical Approaches in Early Drug Discovery:Recent years have seen increasing use of mass spectrometry (MS) and other biophysical methods alongside more traditional high throughput screening technologies in the search for target modulators and binders. They provide a direct assay readout, often with no labels or other reporters, and are therefore less susceptible to artefacts that can adversely affect other technologies. These methods can detect formation of covalent and non-covalent protein-ligand complexes and are not necessarily reliant on enzyme activity. As such they offer a route to screen targets that are catalytically inert, and are also able to detect ligand binding to regions of a protein other than the active site. They are therefore applicable to screen for novel therapeutic modalities such as PROTACs and RNA binding, as well as providing a means to directly screen covalent libraries. There are an increasing number of proteins emerging from genomics initiatives with strong rationale as drug targets for which biophysical screening approaches are desirable, so the demand for them is likely to grow. In this session application of various MS and biophysical methods for biochemical screening including covalent and non-covalent binding strategies will be discussed.
• Hit Triage:Small molecule screening has been a mainstay of hit identification and lead generation efforts for decades. Success is ultimately driven by a triumvirate of factors: reagents, chemistry and technology. Whether a cellular or biochemical approach is applied all reagents utilised need to be of high calibre and relevant for the disease target. The compound collection needs to be suitably diverse and of high quality. Finally the assay technology needs to be fit for purpose. Different technologies are impacted by varying assay artefacts that can result in false positive or negative results. If any of these three broad factors is suboptimal the potential success of the endeavour is diminished. This track will concentrate on the pitfalls that may arise due to the compounds tested and the assay technologies used. Many undesirable mechanisms exist to deleteriously enrich hit outputs and obscure the chemistry that projects should be focusing on. The content will include novel approaches for identifying metal contaminated and redox cycling compounds, the behaviour of nuisance compounds in cell painting studies and working examples of effective triage strategies.

This year’s Discovery Technologies is planned to  take place face-to-face at Alderley Park, Alderley Edge, Cheshire SK10 4TG.  In addition to learning about the latest and most cutting-edge, science on early drug discovery strategies, there will be ample networking opportunities as well as an exhibition show-casing the technologies and their applications.