PublIcatIons
2024
25. Characterising the Protein-Protein Interaction Between MDM2 and 14-3-3σ; Proof of Concept for Small Molecule Stabilisation, J. A. Ward, B. Romartinez-Alonso, D. F Kay, J. Bellamy-Carter, B. Thurairajah, J. Basran, H. Kwon, A. C. Leney, S. Macip, P. Roversi, F. W. Muskett, R. G. Doveston, J. Biol. Chem. 2024, https://doi.org/10.1016/j.jbc.2024.105651
2023
24. Tracking the mechanism of covalent molecular glue stabilization using native mass spectrometry, C. J. A. Verhoef, D. F. Kay, L. van Dijck, R.G. Doveston, L. Brunsveld, A.C. Leney, P. J. Cossar, Chem. Sci. 2023, DOI: 10.1039/D3SC01732J
2022
23. Contemporary biophysical approaches for studying 14-3-3 protein-protein interactions, B. Thurairajah, A. J. Husdon, R. G. Doveston, Front Mol Biosci, 2022 Nov 8, 9:1043673.
2021
22. Cooperative Stabilisation of 14-3-3 Protein-Protein Interactions via Covalent Protein Modification, M. Falcicchio, J. A. Ward, S. Y. Chothia, J. Basran, A. Mohindra, S. Macip, P. Roversi, R. G. Doveston, Chem. Sci. 2021, 12, 12985-12992.
21. Discovering Protein-Protein Interaction Stabilisers by Native Mass Spectrometry, J. Bellamy-Carter, M. Mohata, M. Falcicchio, J. Basran, Y. Higuchi, R.G. Doveston, A. C. Leney, Chem. Sci. 2021, 12, 10724-20731.
20. Structure–Activity Relationship Studies of Trisubstituted Isoxazoles as Selective Allosteric Ligands for the Retinoic-Acid-Receptor-Related Orphan Receptor γt, F. A. Meijer, A. O. W. M. Saris, R. G. Doveston, G. J. M. Oerlemans, R. J. M. de Vries, B. A. Somsen, A. Unger, B. Klebl, C. Ottmann, P. J. Cossar, L. Brunsveld, J. Med. Chem. 2021, 64, 9238-9258.
19. Covalent Occlusion of the RORγt Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site, F. A. Meijer, M. C. M. van den Oetelaar, R. G. Doveston, E. N. R. Sampers, L. Brunsveld, ACS Med. Chem. Lett. 2021, 12, 631-639.
18. Cooperativity in Ligand Binding between the Orthosteric and Allosteric Binding Sites of RORγt, R. M. J. M. de Vries, F. A. Meijer, R. G. Doveston, I. A. Leijten-van de Gevel, L. Brunsveld, Proc. Nat. Acad. Sci. 2021, 118, e2021287118.
2020
17. Regulation of p53 by the 14-3-3 Protein Interaction Network: New Opportunities for Drug Discovery in Cancer, M. Falcicchio, J. A. Ward, S. Macip, R. G. Doveston – Cell Death Discovery 2020, 6, 126.
16. Fragment-based Differential Targeting of PPI Stabilizer Interfaces, X. Guillory, M. Wolter, S. Leysen, J. F. Neves, A. Kuusk, S. Genet, B. Somsen, J. K. Morrow, E. Rivers, L. van Beek, J. Patel, R. Goodnow, H. Schoenherr, N. Fuller, Q. Cao, R. G. Doveston, L. Brunsveld, M. R. Arkin, P. Castaldi, H. Boyd, I. Landrieu, H. Chen, C. Ottmann - J. Med. Chem. 2020, 63, 13, 6694–6707.
15. Elucidation of an Allosteric Mode-of-Action for a Thienopyrazole RORgt Inverse Agonist, R. M. J. M. de Vries, R. G. Doveston, F. A. Meijer, L. Brunsveld – ChemMedChem 2020, 561-565.
14. Ligand-based Design of Allosteric RORγt Inverse Agonists, R.G. Doveston, F. A. Meijer, R. M. J. M. de Vries, G. Vos, A. Vos, M. Scheepstra, S. Leysen, C. Ottmann, L.-G. Milroy and L. Brunsveld – J. Med. Chem. 2020, 241-259.
13. Adoption of a Turn Conformation Drives the Binding Affinity of p53 C-Terminal Domain Peptides to 14-3-3σ, A. Kuusk, J. F. Neves, K. B. Rodriguez, A. Gunnarsson., Y. B. Ruiz-Blanco, M. Ehrmann, H. Chen, I. Landrieu, E.Sanchez-Garcia, H. Boyd, C. Ottmann, R. G. Doveston – ACS Chem. Bio. 2020, 262-271.
12. Substituted Heterocyclic Compounds and Their Use as Retinoid-Related Orphan Receptor (ROR) Gamma-t Inhibitors, L. Brunsveld, R. G. Doveston, S. Leysen, L-G. Milroy, F. A. Meijer, M. Scheepstra, C. Ottmann – International Patent Application PCT/NL2020/050020, filed 15th January 2019, revised 15th January 2020.
2012-2018
11. Small Molecule Modulators of 14-3-3 Protein-Protein Interactions, L. M. Stevers, E. Sijbesma, M. Botta, C. MacKintosh, T. Obsil, I. Landrieu, A. J. Wilson, A.Karawajczyk, J. Eickhoff, J. Davis, M. Hann, G. O’Mahony, M. Perry, R. G. Doveston, L. Brunsveld, C. Ottmann – J. Med. Chem., 2018, 3755-3778.
10. Synthesis and Demonstration of the Biological Relevance of sp(3)-rich Scaffolds Distantly Related to Natural Product Frameworks, D. J. Foley, P. G. E. Craven, P. M. Collins, R. G. Doveston, A. Aimon, R. Talon, I. Churcher, F. von Delft, S. P. Marsden, A. Nelson – Chem. Eur. J., 2017, 23, 15227-15232.
9. Stabilzation of the p53-14-3-3 Protein-Protein Interaction: Proof-of-Concept for Small-Molecule Modulation, R. G. Doveston, A. Kuusk, S. Andrei, S. Leysen, Q. Cao, P. Castaldi, A. Hendricks, H. Boyd, C. Ottmann – FEBS Letts., 2017, 591, 2449-2457.
8. Stabilization of Protein-Protein Interactions in Drug Discovery, S. Andrei, E. Sijbesma, M. Hann, J. Davis, G. O’Mahony, M. Perry, A. Karawajczyk, J. Eickhoff, R. G. Doveston, L.-G. Milroy, L. Brunsveld, C. Ottmann – Exp. Op. Drug Discov., 2017, 12, 925-940.
7. Structural Interface Between LRRK2 and 14-3-3 Protein, L. M. Stevers, R. M. J. M. de Vries, R. G. Doveston, L.-G. Milroy, L. Brunsveld, C. Ottmann – Biochemical Journal 2017, 474, 1273-1287.
6. A Divergent Synthetic Approach to Diverse Molecular Scaffolds: Assessment of Lead-Likeness using LLAMA, an Open-Access Computational Tool, I. Colomer, C. J. Empson, P. Craven, Z. Owen, R. G. Doveston, I. Churcher, S. P. Marsden and A. Nelson - Chem. Commun. 2016, 52, 7209-7212.
5. A Systematic Approach to Diverse, Lead-like Scaffolds From α,α-Disubstituted Amino Acids, D. J. Foley, R. G. Doveston, I. Churcher, A. Nelson and S. P. Marsden – Chem. Commun., 2015, 51, 11174-11177.
The above article was highlighted in Chemistry World, July 2015, Volume 12, Issue 7, Page 24.
4. A Unified Lead-Oriented Synthesis of Over 50 Molecular Scaffolds, R. G. Doveston, P. Tosatti, M. Dow, D. J. Foley, H. Y. Li, A. J. Campbell, D. House, I. Churcher, S. P. Marsden and A. Nelson – Org. Biomol. Chem., 2015, 13, 859-865.
3. Towards the Realisation of Lead-Oriented Synthesis, R. G. Doveston, S. P. Marsden and A. Nelson – Drug Discov. Today, 2014, 813-819.
2. Total Synthesis of an Oxepine Natural Product, (±)-Janoxepin, R. G. Doveston, R. Steendam, S. Jones and R. J. K. Taylor – Org. Lett., 2012, 14, 1122-1125.
The above article was summarised in Synfacts, 2012, 8, 477 (Contributors: S. V. Ley and C. F. Carter).
1. An Expedient Synthesis of the Proposed Biosynthetic Precursor of the Oxepine Natural Product, Janoxepin, R. G. Doveston and R. J. K. Taylor – Tetrahedron Lett., 2012, 53, 2533-2536.