Hit-to-Lead In-Depth Focus 2018
This In-Depth Focus examines our understanding of the comprehensive and complex innate immune system, to develop novel treatments and an open source model to eliminate nuisance compounds
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Screening In-Depth Focus 2018
This In-Depth Focus looks at a high-throughput approach for measuring intracellular ATP levels to access compound-mediated cellular toxicity, the role of drug transporters in phenotypic screening, and how to leverage the power of HTS in the new and rapidly evolving collaborative drug discovery landscape.
Targets In-Depth Focus 2018
In this supplement: Omics-informed drug target discovery in combating emerging infectious diseases, and self-delivering RNAi: paving the way for a new class of cancer immunotherapies.
Targeting innate immunity to treat disease: potential therapeutic applications
Despite being one of the more ancient aspects of immunity, therapeutic modulation of the innate immune system has rarely been attempted. Innate immunity is intrinsically linked to the generation of inflammation – necessary for signalling to the adaptive immune system but often self-perpetuating and over-exaggerated, leading to deleterious effects, including…
Leveraging the power of HTS in the new and rapidly evolving collaborative drug discovery landscape
Over the last five years drug discovery has undergone a rapid evolution from a closed and proprietary endeavour to an open and collaborative process. Large and small pharma now openly collaborate with each other and the wider academic world to leverage their collective depth of knowledge to increase the chances…
A high-throughput approach for measuring intracellular ATP levels to access compound-mediated cellular toxicity
Many drugs fail in clinical trials due to toxicity-related issues; therefore, drug-mediated cellular toxicity should be determined at an early stage in the drug discovery value chain. There are many assay systems that can be utilised to measure cellular toxicity. In this article we demonstrate that intracellular ATP concentrations are…
The role of drug transporters in phenotypic screening
The relative failure of molecular target-based drug discovery has led to a return to phenotypic screening. Targets that are intracellular necessitate their drug ligands to pass through plasma membranes, where the protein:lipid ratio is often 3:1 by mass and at least 1:1 by area. The widespread view that most of…
Drug Target Review – Issue 4 2018
In this issue: Omics-informed drug target discovery in combating emerging infectious diseases, measuring intracellular ATP levels to access compound-mediated cellular toxicity, and turning organoids into physiologically relevant high-content assays for drug discovery.
Exploring quality of life for stoma patients
There are many people with a stoma living in the community in the UK. A commonly reported problem with living with a stoma is a poor quality of life because of uncertainty and doubts in the mind of the person with a stoma. The focus of this article is reviewing…
Expert view: Creating metabolic liabilities to target cancer
As the pace of genetic approaches to combating cancer slows, researchers are focusing on novel approaches to identify and create metabolic liabilities in cells. Cancer cells rewire their metabolism to survive and proliferate rapidly; however, there is no single metabolic phenotype that enables this rewired state.
Metabolomics in drug and biomarker discovery
Metabolomics is the state-of-the-art qualitative or quantitative analysis of metabolites present in biological samples. Since the majority of diseases are associated with metabolic alterations – either as a cause or result of the disease process – metabolomics is increasingly being used in drug and biomarker discovery.
Mass spectrometry and drug development – how the two come together
Since the development of the so-called soft ionisation techniques: electrospray ionisation and matrix-assisted laser desorption and ionisation in the 1980s and early 1990s and the development of high-resolution mass spectrometers, mass spectrometry (MS) has come to the fore in studying complex biological systems...
Pharmacological targeting of mitochondrial dysfunction in Parkinson’s disease: approaches and perspectives
Mitochondrial dysfunction has been widely implicated in the neuronal degeneration in Parkinson’s disease (PD). Mitochondria-targeted protective compounds that prevent or minimise a wide range of mitochondrial defects constitute potential therapeutic strategies in the prevention and treatment of neuronal degeneration in PD.
Synthetic biology in drug discovery
Synthetic biology is broadly defined as the design and construction of novel artificial biological pathways, organisms or devices; or the redesign of existing natural biological systems.1 It brings together a range of disciplines and skills, from biology and chemistry to computing, bioinformatics and engineering.
Improved screening of therapeutic candidates using integrated fragment-based approaches
An integrated fragment-based approach, which reveals enzymatic inhibitors with potential therapeutic application, is the subject of this webinar.Taking place on 25 October 2018 at 3:00pm, the webinar is supported by NanoTemper Technologies.
