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A team of scientists based in Oncology and Discovery Sciences iMeds at AstraZeneca, Alderley Park have published their latest findings in the Journal of Medicinal Chemistry.
The paper, entitled "Structure-guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2", repors the identification of multiple series of highly selective covalent ERK1/2 inhibitors informated by structure based drug design (SBDD).
In oncology clinical development, the RAS/RAF/MEK/ERK signaling pathway has been targeted with a number of small molecule inhibitors across multiple disease indications. Cell lines with acquired resistance to B-RAF and MEK inhibitors have been shown to maintain sensitivity to ERK1/2 inhibition by small molecule inhibitors. A number of selective non-colvalent ERK1/2 inhibitors act via a colvalent mechanism of action. This paper highlights the use of high throughput screening to identify selective covalent tool compounds for potential in vitro and in vivo studies.
The full paper is available online: DOI: 10.1021/acs.jmedchem.5b00466.
If you are interest in this article and want to know more, take a look at our information about X-ray crystallography experiments or our work with the pharmaceutical industry. Alternatively, please contact us on industry@diamond.ac.uk.
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