95. Antibody-based imaging of bioreductive prodrug release in hypoxia Ç. Tosun, M. Mallerman, A. L. D. Wallabregue, S. Phillips, C. M. Edwards, S. J. Conway, E. M. Hammond. ChemRxiv, 2023, DOI: 10.26434/chemrxiv-2023-9n5s0
93. Identification of histone peptide binding specificity and small molecule ligands for the bromodomains of TRIM33α and TRIM33β A. R. Sekirnik, J. K. Reynolds, L. See, J. P. Bluck, A. R. Scorah, C. Tallant, B. Lee, K. B. Leszczynska, R. L. Grimley, R. I. Storer, M. Malattia, S. Crespillo, S. Caria, S. Duclos, E. M. Hammond, S. Knapp, G. M. Morris, F. Duarte, P. C. Biggin, S. J. Conway. ACS Chem.Biol., 2022, 17, 2753
88. Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain. M. Brand, J. Clayton, M. Moroglu, M. Schiedel, S. Picaud, J. P. Bluck, A. Skwarska, A. K. N. Chan, C. M. C. Laurin, A. R. Scorah, K. F. L. See, T. P. C. Rooney, O. Fedorov, G. Perell, W. A. Cortopassi, K. E. Christensen, R. I. Cooper, R. S. Paton, W. C. K. Pomerantz, P. C. Biggin, E. M. Hammond, P. Filippakopoulos, S. J. Conway. J. Med. Chem., 2021, 64, 10102
86. Bioactivation of isoxazole-containing bromodomain and extra terminal domain (BET) inhibitors. N. R. Flynn, M. D. Ward, M. A. Schleiff, C. M. C. Laurin, S. J. Conway, G. Boysen, S. J. Swamidass, G. P. Miller. Metabolites, 2021, 11, 390
85. Development and pre-clinical testing of a novel hypoxia-activated KDAC inhibitor. A. Skwarska, E. D. D. Calder, I. N. Mistry, D. Sneddon, S. J. Conway, E. M. Hammond. Cell Chem Biol., 2021, 28, 1258.
84. Stereo- and regiodefined DNA-encoded chemical libraries enable efficient tumour-targeting applications N. Favalli, G. Bassi, C. Pellegrino, J. Millul, R. De Luca, S. Cazzamalli, S. Yang, A. Trenner, N. Mozzafari, R. Myburgh, M. Moroglu, S. J. Conway, A. Sartori, M. M. Manz, R. A. Lerner, P. Vogt, J. Scheuermann, D. Neri. Nature Chem., 2021, 13, 540
83. Novel bioactivation of isoxazole-containing bromodomain and extra terminal domain (BET) inhibitors. G. P. Miller, M. Schleiff, N. Flynn, M. Ward, C. Laurin, S. J. Conway, S. Swamidass. FASEB J., 2021, 35, DOI: 10.1096/fasebj.2021.35.S1.04681.
82. Development of isotope-enriched phosphatidylinositol-4- and 5-phosphate cellular mass spectrometry probes A. M. Joffrin, A. M. Saunders, D. Barneda, V. Flemington, A. L. Thompson, H. J. Sanganee, S. J. Conway. Chemical Science, 2021, 12, 2549.
81. Fragment-based identification of ligands for bromodomain-containing factor 3 of Trypanosoma cruzi. C. M. C. Laurin, J. P. Bluck, A. K. Chan, M. Keller, A. Boczek, L. E. Jennings, A. R. Scorah, K. F. L. See, D. S. Hewings, F. Woodhouse, J. K. Reynolds, M. Schiedel, P. G.Humphreys, P. C. Biggin, S. J. Conway. ACS Infect. Diseases, 2020, 7, 2238.
80. Epigenetics 2.0: Special Issue on Epigenetics – Call for Papers. S. J. Conway, P. Arimondo, C. Arrowsmith, J. Jin, C. Luo, N. Meanwell, W. Young, G. Georg, S. Wang. J. Med. Chem., 2020, 63, 12129-12130.
79. Pharmacological inhibition of ATR can block autophagy through an ATR-independent mechanism E. Bowler, A. Skwarska, J. D. Wilson, S. Ramachandran, H. Bolland, A. Easton, M-S.Hwang, K. B. Leszczynska, S. J. Conway, E. M. Hammond. iScience, 2020, 101668
78. A single-stranded DNA-encoded chemical library based on a stereoisomeric scaffold enables ligand discovery by modular assembly of building blocks. G. Bassi, N. Favalli, M. Vuk, M. Catalano, A. Martinelli, A. Trenner, A. Porro, S. Yang, C L. Tham, M. Moroglu, W. W. Yue, S. J. Conway, P. K. Vogt, A. A. Sartori, J. Scheuermann, D. Neri. Advanced Science, 2020, 2001970
77. Selective fragments for the CREBBP bromodomain identified from an Encoded Self‑Assembly Chemical Library. M. Catalano, M. Moroglu, P. Balbi, F. Mazzieri, J. Clayton, K.H. Andrews, M. Bigatti, J. Scheuermann, S. J. Conway, D. Neri. ChemMedChem, 2020, 15, 1752-1756
76. Hypoxia-activated pro-drugs of the KDAC inhibitor vorinostat (SAHA). E. D. D. Calder, A. Skwarska, I. N. Mistry, D. Sneddon, S. J. Conway, E. M. Hammond. Tetrahedron, 2020, 76, 131170 (Invited submission in honour of Prof. Steve Davis)
74. PPIs as therapeutic targets for anticancer drug discovery: the case study of MDM2 and BET bromodomain inhibitors. M. Espadinha, S. J. Conway, M. M. M. Santos. Small Molecule Drug Discovery; A. Trabocchi, E. Lenci Eds.; 2020, 267–288.
73. Engineering transkingdom signalling in plants to control gene expression in rhizosphere bacteria. B. A. Geddes, P. Paramasivan, A. M. Joffrin, K. Grant, A. L. Thompson, K. E. Christensen, S. J. Conway, G. E. D. Oldroyd, P. S. Poole. Nature Communications, 2019, 10, 3430.
72. Interaction of the mechanosensitive channel, MscS, with the membrane bilayer through lipid intercalation into grooves and pockets. T. Rasmussen, A. Rasmussen, L. Yang, C. Kaul, S. Black, H. Galbiati, S. J. Conway, S. Miller, P. Blount, I. R. Booth. J. Mol. Biol., 2019, 431, 3339.
71. Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation. M. Schiedel, M. Moroglu, D. M. H. Ascough, A. E. R. Chamberlain, J. J. A. G. Kamps, A. R. Sekirnik, S. J. Conway. Angew. Chem. Int. Ed., 2019, 58, 8353-8357.
68. BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability. L. E. Jennings, M. Schiedel, D. S. Hewings, S. Picaud, C. M. C. Laurin, P. A. Bruno, J. P. Bluck, A. R. Scorah, L. See, J. K. Reynolds, M. Moroglu, I. N. Mistry, A. Hicks, P. Guzanov, J. Clayton, C. N. G. Evans, G. Stazi, P. C. Biggin, A. K. Mapp, E. M. Hammond, P. G. Humphreys, P. Filippakopoulos, S. J. Conway. Bioorg. Med. Chem., 2018, 26, 2937.
67. High-density functional-RNA arrays as a versatile platform for studying RNA-based interactions J. O. Phillips, L. E. Butt, C. A. Henderson, M. Devonshire, J. Healy, S. J. Conway, N. Locker, A. R. Pickford, H. A. Vincent, A. J. Callaghan. Nucleic Acids Res., 2018, 46, e86
66. Adenosine Monophosphate binding stabilizes the KTN domain of the Shewanella denitrificans Kef potassium efflux system. C. Pliotas, S. C. Grayer, S. Ekkerman, A. K. N. Chan, J. Healy, P. Marius, W. Bartlett, A. Khan, W. A. Cortopassi, S. A. Chandler, T. Rasmussen, J. L. P. Benesch, R. S. Paton, T. D. W. Claridge, S. Miller, I. R. Booth, J. H. Naismith, S. J. Conway. Biochemistry, 2017, 56, 4219.
65. Clinical advances of hypoxia-activated prodrugs in combination with radiation therapy. I. N. Mistry, M. Thomas, E. D. Calder, S. J. Conway, E. M. Hammond. Int. J. Radiation Oncol. Biol. Phys., 2017, 98, 1183.
61. Isoxazole-derived amino acids are bromodomain-binding acetyl-lysine mimics: incorporation into histone H4 peptides and histone H3. A. R. Sekirnik (née Measures), D. S. Hewings, N. H. Theodoulou, L. Jursins, K. Lewendon, L. E. Jennings, T. P. C. Rooney, T. D. Heightman, S. J. Conway. Angew. Chem. Int. Ed., 2016, 55, 8353.
60. Design, synthesis and evaluation of molecularly targeted hypoxia-activated prodrugs. L. J. O’Connor, C. Cazares-Körner, J. Saha, C. N. G. Evans, M. R. L. Stratford, E. M. Hammond, S. J. Conway. Nature Protocols, 2016, 11, 781.
59. The photochemical thiol-ene reaction as a versatile method for the synthesis of glutathione S-conjugates targeting the bacterial potassium efflux system Kef. J. Healy, T. Rasmussen, S. Miller, I. R. Booth, S. J. Conway. Org. Chem. Front., 2016, 3, 439.
57. Efficient synthesis of 2-nitroimidazole derivatives and the bioreductive clinical candidate Evofosfamide (TH-302). L. J. O’Connor, C. Cazares-Körner, J. Saha, C. N. G. Evans, M. R. L. Stratford, E. M. Hammond, S. J. Conway. Org. Chem. Front., 2015, 2, 1026.
55. Quantitative hopanoid analysis enables robust pattern detection and comparison between laboratories. C-W. Wu, L. Kong, M. Bialecka-Fornal, S. Park, A. L. Thompson, G. Kulkarni, S. J. Conway, D. K. Newman. Geobiology, 2015, 13, 391.
54. Small molecule inhibitors of bromodomain-acetyl-lysine interactions. M. Brand, A. Measures, B. Wilson, W. A. Cortopassi, R. Alexander, M. Höss, T. P. C. Rooney, D. S. Hewings, R. Paton, S. J. Conway. ACS Chem. Biol., 2015, 10, 22.
52. Synthesis of highly water-soluble adamantyl phosphoinositide derivatives. M. Gregory, M-X. Yin, M. McConville, E. Williams, A. N. Bullock, S. J. Conway, A. B. Holmes. Aust. J. Chem., 2015, 68, 543.
51. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. D. A. Hay, O. Fedorov, S. Martin, C. Wells, S. Picaud, M. Philpott, O. P. Moteiro, C. M. Rogers, S. J. Conway, T. P. C. Rooney, A. Tumber, C. Yapp, P. Filippakopoulos, M. E. Bunnage, S. Müller, S. Knapp, C. J. Schofield, P. E. Brennan. J. Am. Chem. Soc., 2014, 136, 9308.
50. A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation–π interaction. T. P. C. Rooney, P. Filippakopoulos, O. Fedorov, S. Picaud, D. A. Hay, S. Martin, A. Tumber, C. M. Rogers, M. Philpott, M. Wang, A. L. Thompson, T. D. Heightman, D. C. Pryde, A. Cook, R. S. Paton, S. Müller, S. Knapp, P. E. Brennan, S. J. Conway. Angew. Chem. Int. Ed., 2014, 53, 6126.
49. Understanding the structural requirements for activators of the Kef bacterial potassium efflux system. J. Healy, S. Ekkerman, C. Pliotas, M. Richard, W. Bartlett, S. C. Grayer, G. Morris, S. Miller, I. R. Booth, S. J. Conway, T. Rasmussen. Biochemistry, 2014, 53, 1982.
48. Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands. L. E. Jennings, A. R. Measures, B. G. Wilson, S. J. Conway. Future Med. Chem., 2014, 6, 179.
47. CH-01 is a hypoxia-activated prodrug that sensitizes cells to hypoxia/reoxygenation through inhibition of Chk1 and Aurora A. A. C. Cazares-Körner, I. M. Pires, I. D. Swallow, S. C. Grayer, L. J. O’Connor, M. M. Olcina, M. Christlieb, S. J. Conway, E. M. Hammond. ACS Chem. Biol., 2013, 8, 1451.
46. Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. D. S. Hewings, O. Fedorov, P. Filippakopoulos, S. Martin, S. Picaud, A. Tumber, C. Wells, M. M. Olcina, K. Freeman, A. Gill, A. J. Ritchie, D. W. Sheppard, A. J. Russell, E. M. Hammond, S. Knapp, P. E. Brennan, S. J. Conway. J. Med. Chem., 2013, 56, 3217.
44. The design and synthesis of 5- and 6- isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains. D. Hay, O. Fedorov, P. Filippakopoulos, S. Martin, M. Philpott, D. S. Hewings, S. Uttakar, T. D. Heightman, S. J. Conway, S. Knapp, P. E. Brennan. Med. Chem. Commun., 2013, 4, 140.
43. NAADP activates two-pore channels on T cell cytolytic granules to stimulate exocytosis and killing. L. C. Davis, A. J. Morgan, J-. L. Chen, C. Snead, D. Bloor-Young, M. N. Stanton-Humphreys, S. J. Conway, E. Shenderov, G. C. Churchill, J. Parrington, V. Cerundolo, A. Galione. Curr. Biol., 2012, 22, 2331.
42. Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. D. S. Hewings, T. P. C. Rooney, L. E. Jennings, D. Hay, C. J. Schofield, P. E. Brennan, S. Knapp, S. J. Conway.† J. Med. Chem., 2012, 55, 9393.
39. Wavelength-orthogonal photolysis of neurotransmitters in vitro. M. N. Stanton-Humphreys, R. D. T. Taylor, C. McDougall, M. L. Hart, C. T. A. Brown, N. J. Emptage, S. J. Conway. Chem. Commun., 2012, 48, 657.
38. 3,5-Dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. D. S. Hewings, M. Wang, M. Philpott, O. Fedorov, P. Filippakopoulos, S. Picaud, C. Vuppusetty, B. Marsden, S. Knapp, S. J. Conway, T. D. Heightman, J. Med. Chem., 2011, 54, 6761. (Highlighted in Faculty 1000, recognised as highly cited by J. Med. Chem.).
37. KefF, regulatory subunit of the potassium efflux system KefC, shows quinone oxidoreductase activity. L. Lyngberg, J. Healy, W. Bartlett, S. Miller, S. J. Conway, I. R. Booth, T. Rasmussen. J. Bacteriol., 2011, 193, 4925.
35. Development of inositol-based antagonists for the D-myo-inositol 1,4,5-trisphosphate receptor. N. S. Keddie, Y. Ye, T. Aslam, T. Luyten, D. Bello, C. Garnham, G. Bulynck, A. Galione, S. J. Conway. Chem. Commun., 2011, 47, 242.
34. (-)-CHANA, a fluorogenic probe for detecting amyloid binding alcohol dehydrogenase HSD10 activity in living cells. K. E. A. Muirhead, M. Froemming, X. Li, K. Musilek, S. J. Conway, D. Sames, F. J. Gunn-Moore. ACS Chem. Biol., 2010, 5, 1105.
33. Mechanism of ligand-gated potassium efflux in bacterial pathogens. T. P. Roosild, S. Castronovo, J. Healy, S. Miller, C. Pliotas, T. Rasmussen, W. Bartlett, S. J. Conway and I. R. Booth. Proc. Natl. Acad. Sci. USA, 2010, 107, 19784.
31. Synthesis and biological evaluation of phosphatidylinositol phosphate affinity probes. S. J. Conway, J. Gardiner, S. J. A. Grove, M. K. Johns, Z.-Y. Lim, G. F. Painter, D. E. J. E. Robinson, C. Schieber, J. W. Thuring, L. S.-M. Wong, M.-X. Yin, A. W. Burgess, B. Catimel, P. T. Hawkins, N. T. Ktistakis, L. R. Stephens and A. B. Holmes. Org. Biomol. Chem., 2010, 8, 66.
28. Synthesis, photolysis studies and in vitro photorelease of caged TRPV1 agonists and antagonists. M. P. Van Ryssen, N. Avlonitis, R. Giniatulin, C. McDougall, J. L. Carr, M. N. Stanton-Humphreys, C. T. A. Brown, L. Khiroug and S. J. Conway. Org. Biomol. Chem., 2009, 7, 4695.
27. Synthesis and biological evaluation of a novel cardiolipin affinity matrix. M. K. Johns, M. Yin, S. J. Conway, D. E. J. E. Robinson, L. M.-M. Wong, R. Bamert, R. E. H. Wettenhall and A. B. Holmes, Org. Biomol. Chem., 2009, 7, 3691.
26. Increased InsP3Rs in the junctional sarcoplasmic reticulum augment Ca2+ transients and arrhythmias associated with cardiac hypertrophy. D. Harzheim, M. Movassagh, R. S.-Y. Foo, R. Oliver, T. Aslam, S. J. Conway, M. D. Bootman and H. L. Roderick, Proc. Natl. Acad. Sci. USA, 2009, 106, 11406.
25. A type 2 Ferrier rearrangement-based synthesis of D-myo-inositol 1,4,5-trisphosphate. N. S. Keddie, G. Bultynck, T. Luyten, A. M. Z. Slawin and S. J. Conway. Tetrahedron: Asymmetry, 2009, 20, 857. (Invited submission for Prof. George Fleet’s 65th birthday issue).
24. Caged AG10: new tools for spatially predefined mitochondrial uncoupling. N. Avlonitis, S. Chalmers, C. McDougall, M. N. Stanton-Humphreys, C. T. A. Brown, J. G. McCarron and S. J. Conway. Mol. BioSyst., 2009, 5, 450. (Highlighted in RSC Chemical Biology and Faculty of 1000).
21. Purinergic receptor-stimulated IP3-mediated Ca2+ release enhances neuroprotection by increasing astrocyte mitochondrial metabolism during ageing. J. Wu, J. D. Holstein, G. Upadhyay, D.-T. Lin, S. J. Conway, E. Muller, J. D. Lechleiter. J. Neurosci., 2007, 27, 6510.
19. The proapoptotic factors Bax and Bak regulate T cell proliferation through control of endoplasmic reticulum Ca2+ homeostasis. R. G. Jones, T. Bui, C. White, M. Madesh, C. M. Krawczyk, T. Lindsten, B. J. Hawkins, S. Kubek, K. A. Frauwirth, Y. L. Wang, S. J. Conway, H. L. Roderick, M. D. Bootman, H. Shen, J. K. Foskett and C. B. Thompson. Immunity, 2007, 27, 268.
17. Synthesis and biological action of novel 4-position-modified derivatives of D-myo-inositol 1,4,5-trisphosphate. D. Bello, T. Aslam, G. Bultynck, A. M. Z. Slawin, H. L. Roderick,M. D. Bootman and S. J. Conway. J. Org. Chem., 2007, 72, 5647.
14. Inositol 1,4,5-trisphosphate supports the arrhythmogenic action of endothelin-1 on ventricular cardiac myocytes. A. Proven, H. L. Roderick, S. J. Conway, M. J. Berridge, J. K. Horton, S. J. Capper and M. D. Bootman. J. Cell Sci., 2006, 119, 3363.
13. In vitro photo-release of a TRPV1 agonist. J. L. Carr, K. N. Wease, M. P. Van Ryssen, S. Paterson, B. Agate, K. A. Gallagher, C. T. A. Brown, R. H. Scott and S. J. Conway. Bioorg. Med. Chem. Lett., 2006, 16, 208.
12. The spatial pattern of atrial cardiomyocyte calcium signalling modulates contraction. L. Mackenzie, H. L. Roderick, M. D. Bootman, M. J. Berridge, S. J. Conway, A. B. Holmes, and P. Lipp. J. Cell Sci., 2004, 117, 6327.
10. Bcl-2 functionally interacts with inositol 1,4,5-trisphosphate receptors to regulate calcium release from the ER in response to inositol 1,4,5-trisphosphate. R. Chen, I. Valencia, F. Zhong, K. S. McColl, H. L. Roderick, M. D. Bootman, M. J. Berridge, S. J. Conway, A. B. Holmes, G. A. Mignery, P. Velez and C. W. Distelhorst. J. Cell. Biol., 2004, 166, 179.
9. Production and characterization of reduced NAADP (nicotinic acid-adenine dinucleotide phosphate). R. A. Billington, J. W. Thuring, S. J. Conway, L. Packman, A. B. Holmes, and A. A. Genazzani. Biochem. J., 2004, 378, 275.
8. Regulation of InsP(3) receptor activity by neuronal Ca2+- binding proteins. N. N. Kasri, A. M. Holmes, G. Bultynck, J. B. Parys, M. D. Bootman, K. Rietdorf, L. Missiaen, F. McDonald, H. De Smedt, S. J. Conway, A. B. Holmes, M. J. Berridge, and H. L. Roderick. EMBO J., 2004, 23, 312.
7. Co-incident signalling between μ-opioid and M3 muscarinic receptors at the level of Ca2+ release from intracellular stores: lack of evidence for Ins(1,4,5)P3 receptor sensitization. D. S. K. Samways, W. H. Li, S. J. Conway, A. B. Holmes, M. D. Bootman, and G. Henderson. Biochem. J., 2003, 375, 713.
5. Phenylglycine derivatives as antagonists of group III metabotropic glutamate receptors expressed on neonatal rat primary afferent terminals. J. C. Miller, P. A. Howson, S. J. Conway, R. V. Williams, B. P. Clark, and D. E. Jane. Brit. J. Pharmacol., 2003, 139, 1523.
4. 2-Aminoethoxydiphenyl borate (2-APB) antagonises inositol 1,4,5-trisphosphate-induced calcium release, inhibits calcium pumps and has a use-dependent and slowly reversible action on store-operated calcium entry channels. C. M. Peppiatt, T. J. Collins, L. Mackenzie, S. J. Conway, A. B. Holmes, M. D. Bootman, M. J. Berridge, J. T. Seo, and H. L. Roderick. Cell Calcium, 2003, 34, 97.
3. Synthesis and biological evaluation of phospholane and dihydrophosphole analogues of the glutamate receptor agonist AP4. S. J. Conway, J. C. Miller, A. D. Bond, B. P. Clark, and D. E. Jane. J. Chem. Soc., Perkin Trans. 1, 2002, 1625.
2. Distinct intracellular calcium transients in neurites and somata integrate neuronal signals. F. W. Johenning, M. Zochowski, S. J. Conway, A. B. Holmes, P. Koulen, and B. E. Ehrlich. J. Neurosci., 2002, 22, 5344-5353.
1. Synthesis of phenylglycine derivatives as potent and selective antagonists of group III metabotropic glutamate receptors. S. J. Conway, J. C. Miller, P. A. Howson, B. P. Clark, and D. E. Jane. Bioorg. Med. Chem. Lett., 2001, 11, 777.