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New class of compounds found to block coronavirus reproduction
In cell cultures, a compound named STM2457 was shown to interfere with coronavirus replication, making it a potential treatment for SARS-CoV-2.
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Small Molecules
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Novel algorithm uses mass spec data to predict identity of molecules
A new algorithm called MolDiscovery uses mass spectrometry data from molecules to predict their identity and whether they are unknown substances.
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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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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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New approach for treating cystic fibrosis shows success in mice
Researchers have developed a potential strategy to treat cystic fibrosis, using oligonucleotides to correct certain gene defects.
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High-throughput screening platform detects henipavirus antivirals
A new high-throughput screening platform has been used to identify two compounds with antiviral activity against the Nipah and Hendra viruses.
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High-throughput screening assay developed to discover antimalarials
A new assay has been developed to screen for small molecule inhibitors of the Rh5 protein, which is essential for malaria parasite survival.
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Small molecule screens reveal new class of anticancer compounds
Two screening techniques were used by researchers to find anticancer compounds that target the aryl hydrocarbon receptor.
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Small-molecule cocktail could improve use of stem cells in treatments
Researchers have shown that Chroman 1, Emricasan and trans-ISRIB, in combination with polyamines, are effective at protecting induced pluripotent stem cells from stress.
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Inhibiting METTL3 enzyme combats acute myeloid leukaemia in mice
Scientists have developed a drug called STM2457 which inhibits a key enzyme involved in acute myeloid leukaemia.
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Novel PF74-like small molecules developed to target HIV capsid protein
Scientists have developed PF74-like small molecules able to target the HIV-1 capsid protein, identifying four potent compounds.
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Tumour cell vaccine strategy developed for neuroblastoma and melanoma
A combination of checkpoint and small molecule inhibitors showed success at targeting Myc oncogenes in mouse neuroblastoma and melanoma models.