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A team of researchers from the University of Liverpool and AstraZeneca has made an important contribution to our understanding of cancer cell regulation, holding promise for improved future cancer treatment.
The ATR protein has been imaged at ‘near-atomic resolution’, providing greater insight into its activation in DNA repair.
Are selective, brain-penetrant inhibitors of LRRK2 an answer?
Changes leading to the hyperactivation of the protein kinase Akt are observed in 50% of all tumours. Understanding Akt’s regulatory mechanisms is therefore essential for developing and improving cancer therapies....
28 March 2017 | By Charles River
Discover how their multidisciplinary approach to hit ID, design and synthesis of novel chemical templates and development of targeted in vitro and in vivo assays resulted in the nomination of the first development candidate in just over two years...
Monitoring cellular drug permeability and target engagement enables assessment of compound efficacy and confirmation of mode of action. InCELL Pulse target engagement assays provide the ability to confirm compound cell entry and target engagement while overcoming limitations of current target engagement assays...
21 October 2016 | By DiscoverX Corporation
Monitoring cellular drug penetration and drug-target interaction enables assessment of compound efficacy and confirmation of mode of action...
4 October 2016 | By Cisbio
Cisbio Bioassays has developed several assays for covering all the needs for monitoring kinase targets...
16 September 2016 | By Niamh Louise Marriott, Digital Content Producer
Inhibition of the protein kinase CK2 results in a blockade of exactly those signal pathways required by TH17 cells in order to evolve...
In the pre-imatinib (Glivec®) era, two out of three patients died within five years from chronic myeloid leukemia and there was no hope for a curative treatment. Imatinib’s introduction in 2001 marked a breakthrough – as the first approved kinase inhibitor, it was a game-changer in cancer therapy and revolutionised…
13 May 2016 | By Wojciech Czardybon, PhD, Project Manager, Discovery Laboratory Manager, Selvita S.A.
In this article, Wojciech Czardybon of Selvita discusses the potential of PIM/FLT3 dual inhibition in treating acute myeloid leukaemia and other cancers...
In the past two decades, several alternative, non-radiometric assay formats have been developed for the high-throughput screening (HTS) of target classes such as protein kinases, which were previously screened using radiometric assays. Radiometric screening (and the expertise to perform such HTS) has thus declined in recent years...
Cells, organs and organisms are complex biological systems consisting of inter-related components that co-operatively work to maintain function and respond to change. Malfunction of any component can lead to pathologies and disease, leading to system-wide changes and subsequent adaptation. Hence, the ability to study and predict system behaviour will considerably…
History has demonstrated that the use of companion in vitro diagnostic tests to select cancer patients positive for a drug target significantly improves response to targeted anti-cancer therapies...
22 September 2015 | By Victoria White
The companies are validating the druggability of two kinase targets in a specific genetic context and have generated multiple novel chemical series against these targets...
