George Papageorgiou

PUBLICATIONS

Granted Patents

• Corrie, J.E.T.; Ogden, D.; Papageorgiou, G. “Anionically substituted 7-nitroindoline derivatives and their

uses”, US 7,737,169; EP1757585.

• Corrie, J.E.T.; Papageorgiou, G. “1-Acyl-7-nitroindoline derivatives, their preparation and their uses as

photocleavable precursors”, US 6,765,014; EP1161418

• Corrie, J.E.T.; Papageorgiou, G. “Process for nitrating photocleavable compounds”, EP1377548.

Patent Application

• Corrie, J.E.T.; Papageorgiou, G. “7-Nitroindoline derivatives and their uses”, WO2004085394.

Application Note - Sigma RBI

• Corrie, J.; Ogden, D.; Canepari, M.; Papageorgiou, G.” Nitroindolinyl-caged L-glutamate - A new tool for

investigating glutamate-gated ion channels”, Celltransmissions, 2001, 17, 19-20.

Book Chapter

• Abdel-Aal AB.M., Raz R., Papageorgiou G., Offer J. (2020) Synthesis of Amide Backbone-Modified

Peptides. In: Hussein W., Skwarczynski M., Toth I. (eds) Peptide Synthesis. Methods in Molecular

Biology, Vol 2103. Humana, New York, NY

•

Journal Articles

55. Joshi, D.; Milligan, J.C.; Zeisner, T.U.; O’Reilly, N.; Diffley, J.F.X.; Papageorgiou, G.* “An improved method for

the incorporation of fluoromethyl ketones into solid phase peptide synthesis techniques”, RSC Advances,

2021, submitted.

54. Milligan, J.C.; Zeisner, T.U.; Papageorgiou G.; Joshi, D., Soudy, C.; Ulferts, R.; Wu, M.; Lim, C.-T.; Tan, K.-

W.; Florian Weissmann, F.; Canal, B.; Fujisawa, R.; Deegan, T.; Nagara, H.; Bineva-Todd, G.; Basier, C.;

Curran, J.H.; Howell, M.; Beale, R.; Labib, K.; O’Reilly, N.; Diffley, J.F.X. “Identifying SARS-Cov-2 antiviral

compounds by screening for small molecule inhibitors of nsp5 main protease”, Biochem. J., 2021, submitted.

53. Higashi, T.L.; Eickhoff, P; Sousa, J.S.; Locke, J.; Nans, A.; Flynn, H.R.; Snijders, A.P.; Papageorgiou, G.;

O’Reilly, N.; Chen, Z.A.; O’Reilly, F.J.; Rappsilber, J.; Costa, A.; Uhlmann, F. “Structure-based mechanism

for DNA entry into the cohesin ring”, Mol. Cell, 2020, 79, 917–933.

52. Atkinson, B.N.; Steadman, D.; Mahy, W.; Zhao, Y.; Sipthorp, J.; Bayle, E.D.; Svensson, F.; Papageorgiou, G.;

Jeganathan, F.; Frew, S.; Monaghan, A.; Bictash, M.; Jones, E.Y.; Fish, P.V. “Scaffold-hopping identifies

furano[2,3-d]pyrimidine amides as potent Notum inhibitors”, Bioorg. Med. Chem. Letts, 2020, 30, 126751-

126758.

51. Willis, N.J.; Bayle, E.D.; Papageorgiou, G.; Steadman, D.; Atkinson, B.N.; Mahy, W.; Paul V. Fish, P.V. "An

improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a

superior electrophilic chlorinating agent", Beilstein J. Org. Chem., 2019, 15, 2790-2797.

50. Burlina, F.; Abdel-Aal, A-B.M; Raz, R.; Pinzuti, I.; Papageorgiou, G.; Li, J.; Antrobus, R.; Martin, R.M.;

Kunzelmann S.; Stieglitz, B.; Offer, J. “Auxiliary-assisted chemical ubiquitylation of NEMO and linear

extension by HOIP”, Commun. Chem. 2019, 2, 111. doi.org/10.1038/s42004-019-0211-7

49. Palma-Cerda, F.; Papageorgiou, G.; Barbour, B.; Auger, C.; Ogden, D. “Photolysis of a caged, fastequilibrating

glutamate receptor antagonist, MNI-caged γ-D-glutamyl-glycine, to investigate transmitter

dynamics and receptor properties at glutamatergic synapses”, Front. Cell. Neurosci., 2018, 12, 465.

doi.org/10.3389/fncel.2018.00465.

48. Fets, L.; Driscoll, P.C.; Grimm, F.; Jain, A.; Nunes, P.M.; Gounis, M.; Doglioni, G.; Papageorgiou, G.;

Ragan, T.J.; Campos, S.; Silva dos Santos, M..; MacRae, J.I.; O’Reilly, N.; Wright, A.J.; Benes, C.H.;

Courtney, K.D; House, D.; Anastasiou, D. “MCT2 mediates concentration-dependent inhibition of glutamine

metabolism by MOG”, Nature Chem. Biol., 2018, 14, 1032-1042.

47. Edgington, R.; Spillane, K.; Papageorgiou, G.; Wray, W.; Ishiwata, H.; Labarca, M.; Leal-Ortiz, S.; Reid, G.;

Webb, M.; Foord, J.S.; Melosh, N.; Schaefer, A. “Functionalisation of detonation nanodiamond for

monodispersed, soluble DNA-nanodiamond conjugates using mixed silane bead-assisted sonication

disintegration”, Nature Scientific Reports, 2018, 8,728.

46. Abdel-Aal, A-B.M.; Papageorgiou, G.; Raz, R.; Quibell, M.; Burlina, F.; Offer, J. “A backbone amide protecting

group for overcoming difficult sequences and suppressing aspartimide formation”, J. Pept. Sci., 2016, 22, 360-

367.

45. Abdel-Aal, A-B.M.; Papageorgiou, G.; Quibell, M.; Offer, J. “Automated synthesis of backbone protected

peptides”, Chem. Comm., 2014, 50, 8316-8319.

44. Burlina, F.; Papageorgiou, G.; Morris, C.; White, P.D.; Offer, J. “In situ thioester formation for protein ligation

using a-methylcysteine”, Chem. Sci., 2013, 5, 766-770.

43. Papageorgiou, G.; Beato, M.; Ogden, D. “Synthesis and photolytic evaluation of a nitroindoline-caged

glycine with a side chain of high negative charge for use in neuroscience”, Tetrahedron, 2011, 67, 5228-

5234.

42. Trigo, F.F.; Bouhours, B.; Rostaing, P.; Papageorgiou, G.; Corrie, J.E.T.; Triller, A.; Ogden, D.; Marty, A.

“Presynaptic miniature gabaergic currents in developing interneurons”, Neuron, 2010, 66, 235-247.

41. Trigo, F.F.; Papageorgiou, G.; Corrie, J.E.T.; Ogden, D. “Laser photolysis of DPNI-GABA, a tool for

investigating the properties and distribution of GABA receptors and for silencing neurons in situ”, J. Neurosci.

Methods, 2009, 181, 159-169.

40. Papageorgiou, G.; Ogden, D.; Corrie, J.E.T. “An antenna-sensitised 1-acyl-7-nitroindoline that has good

solubility properties in the presence of calcium ions and is suitable for use as a caged L-glutamate in

neuroscience”, Photochem. Photobiol. Sci., 2008, 7, 423-432.

39. Papageorgiou, G.; Corrie, J.E.T.; “Synthesis of an anionically substituted nitroindoline-caged GABA reagent

that has reduced affinity for GABA receptors”, Tetrahedron, 2007, 63, 9668-9676.

38 Zhang, Z.; Papageorgiou, G.; Corrie, J.E.T.; Grewer, C. “Pre-steady-state currents in neutral amino acid

transporters induced by photolysis of a new caged alanine derivative”, Biochemistry, 2007,46, 3872-3880.

37. Papageorgiou, G.; Ogden, D.; Kelly, G.; Corrie, J.E.T.; “Synthetic and photochemical studies of substituted

1-acyl-7-nitroindolines” Photochem. Photobiol. Sci., 2005, 4, 887-896.

36. Papageorgiou, G.; Corrie, J.E.T. “A strategy to avoid anomalous O-alkylation of 4-hydroxyindole by diethyl

bromomalonate” J. Heterocycl., Chem., 2005, 42, 1101-1104.

35. Papageorgiou, G.; Barth, A.; Corrie, J.E.T. “Flash photolytic release of alcohols from photolabile

carbamates or carbonates is rate-limited by decarboxylation of the photoproduct” Photochem. Photobiol.

Sci., 2005, 4, 216-220.

34. Maier, W; Corrie, J.E.T.; Papageorgiou, G.; Laube, B.; Grewer, C. “Comparative analysis of inhibitory

effects of caged ligands for the NMDA receptor”, J. Neurosci. Methods, 2005, 142, 1-9.

33. Papageorgiou, G.; Corrie, J.E.T. “Optimised synthesis and photochemistry of antenna-sensitised 1-acyl-7-

nitroindolines”, Tetrahedron, 2005, 61, 609-616.

32. Papageorgiou, G.; Ogden, D.; Corrie, J.E.T. “An antenna-sensitized nitroindoline precursor to enable

photorelease of L-glutamate in high concentrations”, J. Org. Chem., 2004, 69, 7228-7233.

31. Papageorgiou, G.; Lukeman, M.; Wan, P.; Corrie, J.E.T. “An antenna triplet sensitizer for 1-acyl-7-

nitroindolines improves the efficiency for carboxylic acid photorelease”, Photochem. Photobiol. Sci., 2004, 3,

366-373.

30. Morrison, J.; Wan, P.; Corrie, J.E.T.; Papageorgiou, G. “Mechanisms of photorelease of carboxylic acids

from 1-acyl-7-nitroinolines in solutions of varying water content”, Photochem. Photobiol. Sci., 2002, 1, 960-

969.

29. Papageorgiou, G.; Corrie, J.E.T. “Regioselective nitration of 1-acyl-4-methoxyindolines leads to efficient

synthesis of a photolabile L-glutamate precursor”, Synth. Commun., 2002, 32, 1571-1577.

28. Canepari, M.; Nelson, L.; Papageorgiou, G.; Corrie, J.E.T.; Ogden, D. “Photochemical and pharmacological

evaluation of 7-nitroindolinyl- and 4-methoxy-7-nitroindolinyl-amino acids as novel, fast caged

neurotransmitters”, J. Neurosci. Methods, 2001, 112, 29-42.

27. Canepari, M.; Papageorgiou, G.; Corrie, J.E.T.; Watkins, C.; Ogden, D. “The conductance underlying the

parallel fibre slow EPSP in rat cerebellar Purkinje neurones studied with photolytic release of L-glutamate”, J.

Physiol.-Lond. 2001, 533, 765-772

26. Corrie, J.E.T.; Barth, A.; Papageorgiou, G. “Synthesis and characterisation of 13C and 15N isotopomers of a

1-acyl-7-nitroindoline”, J. Labelled Cpd. Radiopharm., 2001, 44, 619-626.

25. Papageorgiou, G.; Corrie, J.E.T. “Effects of aromatic substituents on the photocleavage of 1-acyl-7-

nitroindolines”, Tetrahedron, 2000, 56, 8197-8205.

24. Corrie, J.E.T.; Gradwell, M.J.; Papageorgiou, G. “Non-photochemical rearrangements of o-nitrobenzyl

compounds”, J. Chem. Soc., Perkin Trans. 1, 1999, 2977-2982.

23. Papageorgiou, G.; Ogden, D.C.; Barth, A.; Corrie, J.E.T. “Photorelease of carboxylic acids from 1-acyl-7-

nitroindolines in aqueous solution: rapid and efficient photorelease of L-glutamate”, J. Am. Chem. Soc.,

1999,121, 6503-6504.

22. Papageorgiou, G.; Corrie, J.E.T. “Synthetic and photochemical studies of N-arenesulfonyl amino acids”,

Tetrahedron, 1999, 55, 237-254.

21. Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “The functionalisation of electron rich aromatic compounds

with 1,3-oxazolidines and 1,3-dimethylimidazolidine”, Tetrahedron, 1997, 53, 14381-14396.

20. Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “The activation of aminals and aminol ethers by sulphur

dioxide and their reactions with electron rich aromatic compounds”, Tetrahedron, 1997, 53, 13361-13372.

19. Papageorgiou, G.; Corrie, J.E.T. “Synthesis and properties of carbamoyl derivatives of photolabile

benzoins”, Tetrahedron, 1997, 53, 3917-3932.

18. Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “The generation of iminium ions using chlorosilanes and their

reactions with electron rich aromatic heterocycles”, Tetrahedron, 1997, 53, 2941-2958.

17. Papageorgiou, G.; Corrie, J.E.T. “Synthesis and evaluation of photolabile sulfonamides as potential

reagents for rapid photorelease of neuroactive amines”, J. Chem. Soc., Perkin Trans. 1, 1996, 1583-1592.

16. Fenton, D.E.; Papageorgiou, G. “Synthesis of unsymmetrical dinucleating ligands bearing nitrogen and

oxygen donor atoms”, Tetrahedron, 1996, 52, 5913-5928.

15. Heaney, H.; Papageorgiou, G.; “The use of bis(aminol) ethers derived from aliphatic primary amines in the

synthesis of secondary and tertiary amines”, Tetrahedron, 1996, 52, 3473-3486.

14. Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “The synthesis of 2-arylmethyltetrahydroisoquinolines from

bis(aminol) ethers involving two iminium salt intermediates”, Tetrahedron, 1995, 51, 10737-10750.

13. Adams, H.; Bailey, N.A.; Fenton, D.E.; Papageorgiou, G.; “A mononuclear copper (II) complex of an

unsymmetrical dinucleating ligand”, J. Chem. Soc., Dalton Trans., 1995, 1383-1386.

12. Bailey, N.A.; Fenton, D.E.; Papageorgiou, G.; Rodriguez de Barbarin, C.O. “Synthesis of unsymmetrical

dinucleating ligands from Mannich bases”, Synlett, 1994, 79-81.

11. Earle, M.J.; Fairhurst, R.A.; Heaney, H.; Papageorgiou, G. “A new synthesis of primary amines using tertbutylamine

as an ammonia equivalent: The triflic acid catalysed removal of N-tert-butyl groups from

carbamates”, Synlett., 1990, 621-623.

10. Brown, D.S.; Earle, M.J.; Fairhurst, R.A.; Heaney, H.; Papageorgiou, G.; Wilkins, R.F.; Eyley, S.C.

“Diastereoselective reactions of trialkylsilyl enol ethers with acyliminium ions”, Synlett., 1990, 619-621.

9. Cooper, M.S.; Earle, M.J.; Fairhurst, R.A.; Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “Tandem and

stepwise reactions of b-(3,4-dialkoxyphenyl)ethylamine bis(aminol) ethers in syntheses of N-arylmethyl-6,7-

dimethoxy-1,2,3,4-tetrahydroisoquinolines: A synthesis of sendaverine methyl ether”, Synlett., 1990, 617-

618.

8. Earle, M.J.; Fairhurst, R.A.; Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “A new route to secondary amines

from bis(alkoxymethyl)alkylamines. The activation of an aminomethyl group and protection of the product by

the same functional group”, Tetrahedron Lett., 1990, 31, 4229-4232.

7. Brown, D.S.; Burns, C.A.; Heaney, H.; Papageorgiou, G.; and Wilkins, R.F. “Dimethyl bis(5-

methylfurfuryl)ammonium chloride”, Acta Cryst., 1990, C46, 64-66.

6. Fairhurst, R.A.; Heaney, H.; Papageorgiou, G.; Wilkins, R.F.; Eyley, S.C. “Mannich reactions of

oxazolidines”, Tetrahedron Lett., 1989, 30, 1433-1436.

5. Cooper, M.S.; Fairhurst, R.A.; Heaney, H.; Papageorgiou, G.; and Wilkins, R.F. “Mannich reactions of

aryltrialkylstannanes in aprotic solvents”, Tetrahedron, 1989, 45, 1155-1166.

4. Fairhurst, R.A.; Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “The effect of sulphur dioxide on the Mannich

reactions of phenols”, Tetrahedron Lett., 1988, 29, 5801-5804.

3. Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “Mannich reactions of nucleophilic aromatic compounds

involving aminals and a-amino ethers activated by chlorosilane derivatives; Catalysis by

chlorotrimethylsilane”, J. Chem. Soc., Chem. Commun., 1988, 1161-1163.

2. Eyley, S.C.; Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “Mannich reactions of p-excessive heterocycles

using bis(dialkylamino)methanes and alkoxydialkylaminomethanes activated with acetyl chloride or sulphur

dioxide”, Tetrahedron Lett., 1988, 29, 2997-3000.

1. Heaney, H.; Papageorgiou, G.; Wilkins, R.F. “Mannich reactions of furan and 2-methylfuran using

preformed imonium salts”, Tetrahedron Lett., 1988, 29, 2377-2380.