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Streamlining drug discovery assays for cancer and cardiovascular disease

Posted: 19 March 2018 | | No comments yet

Declining R&D productivity is a key challenge in the pharmaceutical industry. To increase the success rate of candidate drugs entering the clinical phase, companies must address the early stages of drug discovery.

Streamlining Drug Discovery Assays for Cancer and Cardiovascular Disease

In this webinar, Dr Philip Gribbon discusses the quantification of cell migration phenotypes in cardiovascular-related target validation and drug discovery, and Dr Eric Chevet discusses the role of the endoplasmic reticulum in cancer development.

In lead optimisation, target-based assays are still the most affordable means of rapidly performing fast iterations and remain core to screening. However, the desire for biological-relevance is driving ongoing growth in cell-based assays.

Meanwhile, screeners are continuing to streamline processes by eliminating time-consuming steps such as washing, by generating multiple readouts simultaneously from a single well, or by using automation.

Dr Eric Chevet, Research Director, Institut National de la Santé et de la Recherche Médicale (INSERM), discusses how the endoplasmic reticulum (ER), plays a critical role in cancer development, particularly glioblastoma multiform (GBM). The ER stress sensor IRE1 contributes to GBM progression, impacting tissue invasion and tumour vascularisation. Dr Chevet describes an AlphaScreen-based assay that recapitulates the IRE1 activation process and has been used to identify new peptide-derived modulators of IRE1 activity that are active in vitro and in vivo.

Dr Philip Gribbon, Chief Scientific Officer at the Fraunhofer IME, discusses the quantification of cell migration phenotypes in cardiovascular-related target validation and drug discovery. He describes a label-free, automated and reproducible investigation of cellular motility with instant data assessment, using image-based cytometry. This method overcomes the time-consuming task of manual quantification, which is also limited by subjectivity and the lack of quantifiable metrics.

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