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Expert view: Conquering late stage failures with advanced hit-to-lead techniques
Failing early in drug discovery is the primary driving force for new techniques in the hit-to-lead phase.
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Hit-to-Lead
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Identification of hits and leads for human African trypanosomiasis
Neglected tropical diseases (NTD) affect more than one billion people and new targets and drugs are needed to tackle these infections. The multi-disciplinary NMTrypI consortium has identified a number of different compound classes which could be effective against these diseases. This article reviews some of these compounds...
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Expert view: Optimising the hit-to-lead workflow
Hits identified in high-throughput screens are evaluated within the hit-to-lead phase of drug discovery, where they undergo an iterative optimisation process employing a variety of techniques to identify promising lead compounds to move forward to the lead optimisation phase.
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A pragmatic approach to hit validation following biochemical high-throughput screening
Progressing actives from a high-throughput screen (HTS) of a target protein into suitable starting points for lead identification is fraught with pitfalls. The volume and quality of the HTS output is a function of the quality of the screening library, as well as specific properties of both the target and…
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IONIS-HTTRx lowers deadly Huntington’s disease protein
The first drug targeting the cause of Huntington’s disease was safe and well-tolerated in its first human trial…
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Meeting access challenges with adaptive trial designs
With access challenges even after successful but costly development programmes, the industry is under pressure to speed up the clinical development process and produce more for less. Adaptive trial designs, more collaborative working and data sharing could provide a solution in the area of cancer immunotherapy, says Jacqueline Karmel, principal…
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Expert view: Improving hit-to-lead results
Declining R&D productivity is a key challenge in the pharmaceutical industry today.
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Novel compound restores immune response in patients with melanoma
A novel compound may restore immune response in patients with melanoma, according to a study presented at the ESMO Immuno Oncology Congress 2017.1
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Hit To Lead In-Depth Focus 2017
In this In-Depth Focus we look at a pragmatic approach to hit validation following biochemical high-throughput screening as well as identification of hits and leads for human African trypanosomiasis.
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Drug Target Review – Issue #4 2017
Issue 4 of Drug Target Review looks at artificial intelligence in drug discovery and features In-Depth Focuses on Screening, Hit to Lead and Informatics.
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CXCL5 protein found to stimulate tumour growth in prostate cancer
Researchers identify a pathway that causes tumour acceleration in metastatic prostate cancer cells...
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RT-QuIC testing detects prion protein in the skin of CJD patients
Scientists have detected abnormal prion protein in the skin of patients that have died from Creutzfeldt-Jakob disease...
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Tumour environment found to trigger cells to metastasize
The environment surrounding a tumour can trigger metastatic behaviour in cancer cells...
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Alzheimer’s Tau protein forms toxic complexes with cell membranes
Researchers identify the sequence and structural factors that drive Tau interaction with membranes...
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Pre-diabetes discovery marks step towards precision medicine
Researchers have identified three specific molecules that accurately indicate insulin resistance - a major predictor of diabetes...
