Contact information
+44 (0) 1865 617586
Centre for Medicines Discovery, NDM Research Building, Roosevelt Drive, Oxford, OX3 7FZ
Websites
Jon Elkins
Principal Investigator, Cellular Signalling and Biotechnology
We are a research group working at the interface between chemistry, 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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Discovery of MDI-114215: A Potent and Selective LIMK Inhibitor To Treat Fragile X Syndrome.
Baldwin AG. et al, (2024), Journal of medicinal chemistry
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Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist
Balıkçı E. et al, (2024), Journal of Medicinal Chemistry, 67, 7245 - 7259
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Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.
de Souza Gama FH. et al, (2024), Journal of medicinal chemistry
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Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases.
Henderson SH. et al, (2024), European journal of medicinal chemistry, 269
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Recent advances in the structural biology of tyrosine kinases.
Rygiel KA. and Elkins JM., (2023), Current opinion in structural biology, 82
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Updated protein domain annotation of the PARP protein family sheds new light on biological function.
Suskiewicz MJ. et al, (2023), Nucleic acids research