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Researchers discover class of drugs that could treat mantle cell lymphoma
A screening campaign has revealed that small molecule inhibitors of the SOX 11 oncogene are toxic to mantle cell lymphoma in vitro.
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Screening
Medical screening is a strategy used to identify the possible presence of an as-yet-undiagnosed disease in individuals without signs or symptoms.
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Transcriptional reprogramming rescues vascular fate of misidentified pluripotent cell‑derived epithelial cells
A team of scientists has found that a type of cell derived from human stem cells and widely used for brain research and drug development may have been leading researchers astray for years. Here, Dr Raphaël Lis from Weill Cornell Medicine explains how forcing the activity of three known endothelial cell transcription…
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Drug development in stem cell-derived liver organoid models
To ensure that new drugs are effective and have as little toxicity as possible, they first need to be tested in model systems before entering clinical trials. In this Q&A, Dr Takanori Takebe outlines his research into liver organoids derived from stem cells that can be used to test new…
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Making cell culture models more physiologically relevant
A major limitation in drug development is the occurrence of drug-candidate toxicity during clinical research. This may occur because tumour-derived cell lines are limited as a pre-clinical model – in part because of an altered metabolic poise. A recent study has revealed a profound plasticity in gene expression and metabolic poise that can…
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Small molecule to potentially treat diabetes discovered in screening study
A small molecule found in a cell-based ultra-high-throughput screening campaign was shown to treat diabetes in cells and mice.
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Covalent fragment screening in cell-based phenotypic models of disease: a collaborative approach
The application of chemical perturbation approaches in phenotypic models is often used to identify protein targets for therapeutic discovery. Increasingly, small molecule fragments which covalently bind to their protein targets are being used to explore the druggable proteome and the resulting fragment‑protein interactions are characterised by chemoproteomic techniques. In this…
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Targeting phosphodiesterase 3A: discovery of a promising cancer therapy
A new promising sarcoma target, phosphodiesterase 3A (PDE3A), and drugs targeting it have been identified by researchers at the University of Helsinki. Dr Katja Ivanitskiy, Dr Harri Sihto and Professor Olli Kallioniemi outline emerging evidence that indicates PDE3A protein-targeting compounds may induce sarcoma cell death by acting as a molecular…
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Screening for COVID-19 drugs
With the COVID-19 pandemic ongoing, new therapeutic drugs to combat SARS-CoV-2 are still required. In this article, Professor Arvind Patel from the Medical Research Council (MRC) – Centre for Virus Research (CVR) at the University of Glasgow spoke with Drug Target Review’s Victoria Rees to discuss the work being done…
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Assessing compound activity to accelerate drug discovery
In this article, Drug Target Review’s Victoria Rees explores a new screening platform that assesses the biological activity of molecules to identify potential drugs. Using their new technique, researchers from the US National Institutes of Health (NIH) identified potential COVID-19 therapeutics.
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Why some screening hits are a PAIN
A major challenge during high-throughput and fragment screening is the potential for identifying ‘frequent hitters’ – compounds that affect unrelated targets. Matthew Lloyd from the University of Bath explains why these hits can arise during drug discovery and how machine learning could be the answer to identifying these compounds.
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Application note: Effectiveness of CRISPR‑Cas9 using pools of synthetic crRNAs in high-content analysis screening experiments
Chemical synthesis of guide RNAs for CRISPR-Cas9 gene editing enables accurate and rapid production of CRISPR libraries and screening in an arrayed, one-gene-per-well fashion.
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Mass spec method developed to identify drugs to fight resistant bacteria
Researchers have developed a native state mass spectrometry technique to identify inhibitors of the bacterial protein metallo-beta-lactamase.
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Drug Target Review Screening ebook 2021
This ebook has articles on the use of screening to identify COVID-19 drugs and how assessing compound activity could accelerate drug discovery.
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High-throughput screening protocol created to discover SHP2 inhibitors
Researchers have developed a cross-validation high-throughput screening method to accelerate the identification of SHP2 inhibitors.
whitepaper
ebook: Why you need to digitally transform your R&D organisation
Despite many companies considering digital transformation a top priority, research shows that 70% of digital transformation initiatives fail. In this ebook, we explore why and how the right approach can see your organisation succeed.