news
MSK1 protein keeps metastatic breast cancer cells dormant
A study has identified the genes involved in the latent asymptomatic state of breast cancer metastases...
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Kinases
news
Blocking 20-HETE chemical counters the siren call of aggressive cancers
Scientists have successfully blocked the powerful call of two types of aggressive cancer – glioblastoma and breast cancer – in laboratory models; with evidence that inhibiting the chemical 20-HETE halts tumour growth.
news
Industry-academic collaboration results in improved understanding of cancer cell regulation
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.
news
Scientists visualise structure of key DNA repair component
The ATR protein has been imaged at ‘near-atomic resolution’, providing greater insight into its activation in DNA repair.
whitepaper
Whitepaper: In search of a disease-modifying agent for Parkinson’s disease: a discovery story
Are selective, brain-penetrant inhibitors of LRRK2 an answer?
news
Shedding light on the brakes of Akt activity
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....
webinar
Designing a Novel Cancer Drug: From Hit ID to Candidate
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...
whitepaper
Booklet: InCELL Pulse™ Target Engagement Kinase Reference Set
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...
product
DiscoverX In Vitro Pharmacology Services – Simplify Your Drug Discovery Workflow
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...
product
Cisbio Bioassays Kinases – A comprehensive platform of assays and reagents for evaluating kinase activity
4 October 2016 | By Cisbio
Cisbio Bioassays has developed several assays for covering all the needs for monitoring kinase targets...
news
Inhibiting protein kinase CK2 prevents T cell development, could lead to innovative MS treatment
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...
article
New horizons in next-generation small molecule kinase inhibitors
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…
article
PIM/FLT3 dual inhibition
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...
article
The relevance of homogeneous radiometric assays in modern drug discovery
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...
article
Mass spectrometry and systems biology approaches in drug target discovery
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…
