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Masitinib found to be an effective COVID-19 treatment in mouse model
Scientists from the University of Chicago discovered that the drug masitinib inhibits the replication of SARS-CoV-2 in mice.
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Crystallography
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Microcrystal electron diffraction could advance drug development
UK researchers have shown how microcrystal electron diffraction (MicroED) could obtain the structures of potential pharmaceuticals.
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The use of biophysical methods in the hit-to-lead process
Optimisation of a hit towards a lead happens in a variety of ways, as a lead needs to meet various criteria such as activity, affinity to the target, selectivity, solubility, permeability or metabolic stability to become a promising candidate. A balance between in vitro profiles and pharmacokinetic attributes has to…
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X-ray screening reveals two promising SARS-CoV-2 drug candidates
Using a high-brilliance X-ray lightsource and protein crystallography, researchers have identified two drugs that inhibit the main protease of SARS-CoV-2.
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Researchers reveal how key enzyme APT2 works in cells
Using X-ray crystallography and simulations, researchers have shown that APT2 is a hybrid between a lipid carrier protein and a hydrolase.
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Structure of protein that triggers neurodegeneration isolated and analysed
Using X-ray crystallography and cryo-electron microscopy, researchers have elucidated the structure of the SARM1 protein, a target for neurodegeneration.
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Acquiring structural data on membrane proteins – a spotlight on GPCRs
Lan Zhu from Arizona State University explains how cryo-EM methods can be used to obtain structural information on membrane proteins such as GPCRs.
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VP3 protein: revealing the structure of a potential rotavirus drug target
Researchers hope that by revealing the rotavirus VP3 protein structure and mRNA capping functions, novel antivirals could be designed to prevent or combat rotavirus infections.
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Structure of lipin enzyme responsible for triglycerides revealed for first time
Researchers have obtained the crystal structure of the lipin enzyme, the regulator of triglyceride production, which they say could inform research into heart disease, obesity and diabetes.
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Advances in mass spectrometry: unlocking the potential of chemical crosslinking as a structural biology tool
Chemical crosslinking coupled with mass spectrometry (XL-MS) has been used for many years to study protein structure and function. However, recent advances in MS technology, as well as crosslinking reagents and data analysis tools, mean the technique has truly come of age. Here, Albert JR Heck, Alexander Makarov, Henning Urlaub…
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Cancer immunotherapies may be improved with early immune response
A new mechanism has been reported for detecting foreign material during early immune responses which may help detect elusive cancers.
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The promise and pitfalls of serial femtosecond X-ray crystallography
A report from scientists at the Moscow Institute of Physics and Technology highlights the advantages and disadvantages of serial femtosecond X-ray crystallography. This article investigates the review, focusing on its role in drug development.
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In-depth research maps virulence factor of the influenza A virus in real time
Findings from a recent study could lead to the development of therapeutic approaches against influenza A viruses.
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Scientists develop novel method for membrane protein crystallisation
Scientists in Switzerland have developed a new means of crystallising membrane proteins – a hitherto elusive feat – in order to study their structure and aid understanding of their processes.
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Scientists develop green fluorescent protein to aid intracellular research
Researchers at Osaka University in Japan have developed a superior acid-tolerant green fluorescent protein to enhance the study of intracellular molecular dynamics.
