George Papageorgiou




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-


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.

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.

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-


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-


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,


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-


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-


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.

Qualifications and history

Loughborough University
PhD Organic Chemistry
Loughborough University
MSc Medicinal Chemistry
Queen Mary College London, UK
BSc (Hons) Chemistry
Guest Editor of "Organic Synthesis and Asymmetry" of the open access journal “Symmetry”
FRSC Fellow of the Royal Society of Chemistry
CSci Chartered Scientist - The Science Council
CChem MRSC Chartered Chemist Member of the Royal Society of Chemistry
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Last updated : 05 May 2021 02:02