Chemical biology, kinases, mass spectrometry, X-ray crystallography, assay development, cell signalling, proteomics
https://orcid.org/0000-0003-3414-8348Benns, H. J., Storch, M., Falco, J. A., Fisher, F. R., Tamaki, F., Alves, E., Wincott, C. J., Milne, R., Wiedemar, N., Craven, G. B., Baragaña, B., Wyllie, S., Baum, J., Baldwin, G. S., Weerapana, E., Tate, E. W., & Child, M. A. CRISPR-based oligo recombineering prioritizes apicomplexan cysteines for drug discovery. Nature Microbiology, 7, 1891–1905 (2022)
https://doi.org/10.1038/s41564-022-01249-y
Liu, Y., De Castro Ribeiro, O., Haapanen, O., Craven, G. B., Sharma, V., Muench, S. P. & Goldman, A. Unexpected structures formed by the kinase RET C634R mutant extracellular domain suggest potential oncogenic mechanisms in MEN2A. J. Biol. Chem. 298, 102380 (2022).
https://doi.org/10.1016/j.jbc.2022.102380
Yang, T., Cuesta, A., Wan, X., Craven, G. B., Hirakawa, B., Khamphavong, P., May, J. R., Kath, J. C., Lapek, J. D., Niessen, S., Burlingame, A. L., Carelli, J. D. & Taunton, J. Reversible lysine-targeted probes reveal residence time-based kinase selectivity. Nat. Chem. Biol. 18, 934–941 (2022).
https://doi.org/10.1038/s41589-022-01019-1
Qin, B.,* Craven, G. B.,* Hou, P.,* Chesti, J., Lu, X., Child, E. S., Morgan, R. M. L., Niu, W., Zhao, L., Armstrong, A., Mann, D. J. & Cui, S. Acrylamide fragment inhibitors that induce unprecedented conformational distortions in enterovirus 71 3C and SARS-CoV-2 main protease. Acta Pharmaceutica Sinica B, 12, 3924–3933 (2022). *Shared first authorship
https://doi.org/10.1016/j.apsb.2022.06.002
Jamshidiha, M., Hogg, T. L., Sutherell, C. L., Craven, G. B., Tersa, M., De Vita, E., Brustur, D., Hassan, S., Petracca, R., Morgan, R. M. L., Sanz-hernández, M., Norman, J. C., Armstrong, A., Mann, D. J. & Tate, E. W. Identification of the first structurally validated covalent ligands of the small GTPase RAB27A. RSC Med. Chem. 13, 150–155 (2022).
https://doi.org/10.1039/D1MD00225B
Craven, G. B., Briggs, E. L., Zammit, C. M., McDermott, A., Greed, S., Affron, D. P., Leinfellner, C., Cudmore, H. R., Tweedy, R. R., Luisi, R., Bull, J. A. & Armstrong, A. Synthesis and Configurational Assignment of Vinyl Sulfoximines and Sulfonimidamides. J. Org. Chem. 86, 7403–7424 (2021).
https://doi.org/10.1021/acs.joc.1c00373
Craven, G. B.; Affron, D. P.; Kösel, T.; Wong, T. L. M.; Jukes, Z. H.; Liu, C. T.; Morgan, R. M. L.; Armstrong, A.; Mann, D. J. Multiparameter Kinetic Analysis for Covalent Fragment Optimization by Using Quantitative Irreversible Tethering (qIT). ChemBioChem 21, 3417–3422 (2020).
https://doi.org/10.1002/cbic.202000457
Craven, G.B., Mann, D.J. & Armstrong, A. Quantitative Irreversible Tethering (qIT) for Target-directed Covalent Fragment Screening. BIO-PROTOCOL 10, (2020).
https://doi.org/10.21769/BioProtoc.3855
Craven, G. B.,* Affron, D. P.,* Raymond, P. N., Mann, D. J. & Armstrong, A. Vinyl sulfonamide synthesis for irreversible tethering via a novel α-selenoether protection strategy. Medchemcomm 10, 158–163 (2019). *Shared first authorship
https://doi.org/10.1039/C8MD00566D
Craven, G. B., Affron, D. P., Allen, C. E., Matthies, S., Greener, J. G., Morgan, R. M. L., Tate, E. W., Armstrong, A. & Mann, D. J. High-Throughput Kinetic Analysis for Target-Directed Covalent Ligand Discovery. Angew. Chem. Int. Ed. 57, 5257–5261 (2018).
https://doi.org/10.1002/anie.201711825
Idiris, F. I. M., Majesté, C. E., Craven, G. B. & Jones, C. R. Intramolecular hydride transfer onto arynes: redox-neutral and transition metal-free C(sp3)–H functionalization of amines. Chem. Sci. 9, 2873–2878 (2018).
https://doi.org/10.1039/C8SC00181B
Alguel, Y., Amilis, S., Leung, J., Lambrinidis, G., Capaldi, S., Scull, N. J., Craven, G. B., Iwata, S., Armstrong, A., Mikros, E., Diallinas, G., Cameron, A. D. & Byrne, B. Structure of eukaryotic purine/H+ symporter UapA suggests a role for homodimerization in transport activity. Nat. Commun. 7, 11336 (2016).
https://doi.org/10.1038/ncomms11336