Contact information
+44 (0) 1865 617586
Centre for Medicines Discovery, Biochemistry Building, South Parks Road, Oxford, OX1 3QU
Websites
Jon Elkins
Principal Investigator, Cellular Signalling
We are a research group working in the areas of chemical biology and drug discovery.
We are interested in understanding the molecular mechanisms of proteins involved in cellular signalling, especially those involved in signalling via post-translational modifications such as phosphorylation or ADP-ribosylation. Phosphorylation is catalysed by protein kinases; there are over 500 protein kinases in the human genome and most of them remain poorly characterized despite their importance regulating physiology. Our approach is to use high resolution structural information for the generation of selective inhibitors (chemical probes) which we use to gain understanding of the functions of these largely uncharacterized proteins. Our lab generated a large repository of efficient expression systems, recombinant proteins and crystal structures that now enables family wide structural comparison and screening. ADP-ribosylation is important in numerous cellular processes; as well as a well-established role in DNA damage detection and repair it is also important for host-virus interactions, epigenetic regulation and metabolism. We also have interests in lipid kinases and sphingolipid biosynthesis, which both have strong links to inflammation and cancer, and where mutations in the various proteins involved are associated with a variety of rare diseases.
Recent publications
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Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
Journal article
Collins R. et al, (2022), J Med Chem
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Chemical Probes for Understudied Kinases: Challenges and Opportunities.
Journal article
Serafim RAM. et al, (2021), Journal of medicinal chemistry
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Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold.
Journal article
Serafim RAM. et al, (2021), Journal of medicinal chemistry
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Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.
Journal article
Henderson SH. et al, (2021), Journal of medicinal chemistry, 64, 11709 - 11728
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Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Journal article
Berger B-T. et al, (2021), Cell chemical biology, 28, 686 - 698.e7
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Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family.
Journal article
Quevedo CE. et al, (2020), Bioorganic & medicinal chemistry, 28