The length of time that drug molecules attach to their target protein varies greatly and impacts the protein’s behaviour and drug efficacy. In a new study, scientists in Finland have identified some causal factors for this variance, with the hope it will bring clarity for drug developers.
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Automating functional cell-based bioassays: assay reproducibility and performance for potency testing programmes
28 May 2021 | By Eurofins DiscoverX* and Tecan
In this on-demand webinar, we discuss how Eurofins DiscoverX’s off-the-shelf, MOA-based functional, cellular assays address these challenges, enabling drug discovery programmes up to late-stage development and market release.
Novel small molecule inhibitors of oncogenic SHP2 variants characterised by cellular target engagement
28 January 2021 | By Eurofins DiscoverX & Sanford Burnham Prebys Discovery
In this on-demand webinar industry experts discuss how the InCELL Pulse technology provides a valuable tool for the discovery and characterisation of novel SHP2 inhibitors.
Researchers have found the small molecules Apilimod and Vacuolin-1 inhibited the PIKfyve kinase in cells, preventing infection from Zaire ebolavirus and SARS-CoV-2.
Modulating the TCR signaling pathway using biologics, small molecules or genetic engineering is highly relevant to many therapeutic areas including cancer immunotherapy, adoptive cell therapy, vaccine development and autoimmune disease.
Using cyro-electron microscopy, researchers have imaged the binding site between a molecule and the tumour suppressor protein PP2A, enabling optimisation of the drug compound.
Using the ubiquitin-proteasome system to fight inflammatory conditions could provide more treatment options for patients. Dr Jared Gollob from Kymera Therapeutics explains why targeted protein degradation is the way forward for autoinflammatory and autoimmune disease therapies.
Scientists in the US have applied a novel technique to finally unravel a particular kinase enzyme that is associated with familial Parkinson’s disease; providing a clearer potential therapeutic target.
A study has shown that type II kinase inhibitors targeting CDK8 alone are ineffective because mutations leave them inactive, suggesting future therapies should target CDK8 in complex.
Kinase-mediated phosphorylation is a control point for nearly all activity within a cell, making kinases important in many diseases.
A new study has shown that restoring the amount of the kinase, HIPK2, in a kinase-depleted mouse model rescued it from heart failure and identifies HIPK2 as a novel regulator of heart failure progression.
A research team has found that blocking a particular kinase in a mouse model of arrhythmogenic cardiomyopathy led to improved survival rates.