GEORGIADIS RESEARCH GROUP

NATiONAL AND KAPODISTRIAN UNIVERSITY OF ATHENS

60. Discovery of the First-in-Class Inhibitors of Hypoxia Up-Regulated Protein 1 (HYOU1) Suppressing Pathogenic Fibroblast Activation.
D. Papadopoulou, V. Mavrikaki, F. Charalampous, C. Tzaferis, M. Samiotaki, K. D. Papavasileiou, A. Afantitis, N. Karagianni, M. C. Denis, J. Sanchez, J. R. Lane, Z. F. Brotzakis, G. Skretas, D Georgiadis, A. N. Matralis, and G. Kollias
Angewandte Chemie, International Edition in English, 2024, e202319157

59. Diastereoselective Synthesis of Phosphinic Dipeptide Isosteres: Domino Chirality Transfer during a Stereocontrolled P-Michael Reaction.
A Lelis, N. Skoulikas, M. Papathanasopoulou, K. Voreakos and D Georgiadis*
Organic Letters, 2023, 25 (36), 6623-6627

58. Phosphinic Peptides as Tool Compounds for the Study of Pharmacologically Relevant Zn-Metalloproteases.
D Georgiadis*, N. Skoulikas, A. Papakyriakou and E. Stratikos
ACS Pharmacology & Translational Science, 2022, 5 (12), 1228-1253

57. Practical Synthesis of Phosphinic Dipeptides by Tandem Esterification of Aminophosphinic and Acrylic Acids under Silylating Conditions.
P. Kokkala, K. Voreakos, A. Lelis, K. Patiniotis, N. Skoulikas, L. Devel, A. Ziotopoulou, E. Kaloumenou and D. Georgiadis*
Molecules, 2022, 27 (4), 1242

56. ERAP2 Inhibition Induces Cell-Surface Presentation by MOLT-4 Leukemia Cancer Cells of Many Novel and Potentially Antigenic Peptides.
I. Temponeras, G. Stamatakis, M. Samiotaki, D. Georgiadis, H. Pratsinis, G. Panayotou and E. Stratikos*
International Journal of Molecular Sciences, 2022, 23 (3), 1913

55. Inhibitor-Dependent Usage of the S1′ Specificity Pocket of ER Aminopeptidase 2.
A. Mpakali, D. Georgiadis, E. Stratikos and P. Giastas
ACS Medicinal Chemistry Letters, 2022, 13 (2), 218-224

54. Conformational Dynamics Linked to Domain Closure and Substrate Binding Explain the ERAP1 Allosteric Regulation Mechanism.
Z. Maben, R. Arya, D. Georgiadis, E. Stratikos and L. J. Stern*
Nature Communications, 2021, art no 5302

53. The ERAP1 Αctive Site Cannot Productively Access the N-Terminus of Antigenic Peptide Precursors Stably Bound Onto MHC Class I.
G. Mavridis, A. Mpakali, J. Zoidakis, M. Makridakis, A. Vlahou, E. Kaloumenou, A. Ziotopoulou, D. Georgiadis, A. Papakyriakou and E. Stratikos*
Scientific Reports, 2021, art no 16475

52. Ligand‐Directed Modification of Active Matrix Metalloproteases: Activity‐based Probes with no Photolabile Group.
M. Kaminska, P. Bruyat, C. Malgorn, M. Doladilhe, E. C.‐Lajeunesse, C. F. Gaillard, M. De Souza, F. Beau, R. Thai, I. Correia, A. Galat, D. Georgiadis, O. Lequin, V. Dive, S. Bregant and L. Devel*
Angewandte Chemie, International Edition in English, 2021, 131 (33), 18420-18427

51. A Carbodiimide-Mediated P–C Bond-Forming Reaction: Mild Amidoalkylation of P-Nucleophiles by Boc-Aminals .
P Kokkala, T Rajeshkumar, A Mpakali, E Stratikos and K. D. Vogiatzis* and D. Georgiadis*
Organic Letters, 2021, 23 (5), 1726-1730

50. A Reliable Enantioselective Route to Mono-Protected N1-Cbz Piperazic Acid Building Block.
E. Papadaki, D. Georgiadis and M. Tsakos*
Molecules, 2020, 25 (24) , 5939

49. The Discovery of Insulin-Regulated Aminopeptidase (IRAP) Inhibitors: A Literature Review.
D. Georgiadis* , A. Ziotopoulou, E. Kaloumenou, A. Lelis and A. Papasava
Frontiers in Pharmacology, 2020, 11 , art no 585838

48. A Systematic Re-examination of Processing of MHCI-Bound Antigenic Peptide Precursors by Endoplasmic Reticulum Aminopeptidase 1.
G. Mavridis, R. Arya, A. Domnick, J. Zoidakis, M. Makridakis, A. Vlahou, A. Mpakali, A. Lelis, D. Georgiadis, R. Tampé, A. Papakyriakou, L. J. Stern and E. Stratikos*
Journal of Biological Chemistry, 2020, 295 (21) , 7193-7210

47. Mechanism for Antigenic Peptide Selection by Endoplasmic Reticulum Aminopeptidase 1.
P. Giastas, A. Mpakali, A. Papakyriakou, A. Lelis, P. Kokkala, M. Neu, P. Rowland, J. Liddle, D. Georgiadis and E. Stratikos *
Procceedings of the National Academy of Sciences, U.S.A., 2019, 116 (52) , 26709-26716

46. Novel Matrix Metalloproteinase 12 Selective Radiotracers for Vascular Molecular Imaging.
J. Toczek, T. Bordenave, K. Gona, H.-Y. Kim, F. Beau, D. Georgiadis, I. Correia, Y. Ye, M. Razavian, J.-J. Jung, O. Lequin, V. Dive, M. M. Sadeghi* and L. Devel*
Journal of Medicinal Chemistry, 2019, 62 (21) , 9743-9752

45. Editing the Immunopeptidome of Melanoma Cells Using a Potent Inhibitor of Endoplasmic Reticulum Aminopeptidase 1 (ERAP1).
D. Koumantou, E. Barnea, A. Martin-Esteban, Z. Maben, A. Papakyriakou, A. Mpakali, P. Kokkala, H. Pratsinis, D. Georgiadis , L. J. Stern, A. Admon and E. Stratikos *
Cancer Immunology Immunotherapy, 2019, 68 , 1245-1251

44. Inhibitors of ER Aminopeptidase 1 and 2: From Design to Clinical Application.
K. Voreakos, L. Devel and D. Georgiadis , A. Mpakali, D. Koumantou and E. Stratikos *
Current Medicinal Chemistry, 2019, 26 (15) , 2715-2729

43. Late-Stage Diversification of Phosphinic Dehydroalanine Pseudopeptides Based on a Giese-Type Radical C-Alkylation Strategy.
K. Voreakos, L. Devel and D. Georgiadis*
Organic Letters, 2019, 21 (12) , 4937-4401

42. Synthesis and Structural/Functional Characterization of Selective M14 Metallocarboxypeptidase Inhibitors Based on Phosphinic Pseudopeptide Scaffold: Implications on the Design of Specific Optical Probes.
G. Covaleda, P. Gallego, J. Vendrell, D. Georgiadis, J. Lorenzo, V. Dive, F. X. Aviles,* D. Reverter* and L. Devel*
Journal of Medicinal Chemistry, 2019, 62 (4) , 1917-1931

41. Ligand-induced Conformational Change of Insulin-Regulated Aminopeptidase: Insights on Catalytic Mechanism and Active Site Plasticity.
A. Mpakali, E. Saridakis, K. Harlos, Y. Zhao, P. Kokkala, D. Georgiadis, P. Giastas and Stratikos, E*
Journal of Medicinal Chemistry, 2017, 60 (7) , 2963-2972

40. Critical Role of the Inter-domain Interactions on the Conformational Change and Catalytic Mechanism of Endoplasmic Reticulum Aminopeptidase 1.
A. Stamogiannos, Z. Maben, A. Papakyriakou, A. Mpakali, P. Kokkala, D. Georgiadis, L. J. Stern and E. Stratikos*
Biochemistry, 2017, 56 (10), 1546-1558

39. Optical Imaging of MMP-12 Active Form in Inflammation and Anheurysm.
M. Razavian, T. Bordenave, D. Georgiadis, F. Beau, J. Zhang, R. Golestani, J. Toczek, J.-J. Jung, Y. Ye, H.-Y. Kim, J. Han, V. Dive, L. Devel and M. M. Sadeghi*
Scientific Reports, 2016, 6, art. no 38345

38. Synthesis and in Vitro and in Vivo Evaluation of MMP-12 Selective Optical Probes.
T. Bordenave, M. Helle, F. Beau, D. Georgiadis, L. Tepshi, M. Bernes, Y. Ye, L. Levenez, E. Poquet, H. Nozach, M. Razavian, J. Toczek, E. A. Stura, V. Dive, M. M. Sadeghi and L. Devel*
Bioconjugate Chemistry, 2016, 27 (10) , 2407-2417

37. Optimization and Structure-Activity Relationships of Phosphinic Pseudotripeptide Inhibitors of Aminopeptidases that Generate Antigenic Peptides.
P. Kokkala, A. Mpakali, F.-X. Mauvais, A. Papakyriakou, I. Daskalaki, I. Petropoulou, S. Kavvalou, M. Papathanasopoulou, S. Agrotis, T.-M. Fonsou, P. Van Endert, E. Stratikos* and D. Georgiadis*
Journal of Medicinal Chemistry, 2016, 59 (19) , 9107-9123

36. Silencing or Inhibition of Endoplasmic Reticulum Aminopeptidase 1 (ERAP1) Suppresses Free Heavy Chain Expression and Th17 Responses in Ankylosing Spondylitis.
L. Chen, A. Ridley, A. Hammitzsch, M. H. Al-Mossawi, H. Bunting, D. Georgiadis, A. Chan, S. Kollnberger and P. Bowness*
Annals of the Rheumatic Diseases, 2016, 75 (5) , 916-923

35. Crystal Structure of Insulin-Regulated Aminopeptidase with Bound Substrate Analogue Provides Insight on Antigenic Epitope Precursor Recognition and Processing.
A. Mpakali, E. Saridakis, K. Harlos, Y. Zhao, A. Papakyriakou, P. Kokkala, D. Georgiadis, and Stratikos, E*
Journal of Immunology, 2015, 195 (6) , 2842-2851

34. Probing the Mechanism of Morita-Baylis-Hillman Acetatesʼ (MBHAs) Allylic Substitution by Using the Silyl Phosphonite Paradigm: Scope and Applications of a Versatile Transformation.
Μ. Kalyva, Α.L. Zografos, E. Kapourani, E. Giambazolias, L. Devel, A. Papakyriakou, V. Dive, Y. G. Lazarou, and D. Georgiadis*
Chemistry - A European Journal, 2015, 21 (3) , 3278-3289

33. Autoimmune Disease-Associated Variants of Extracellular Endoplasmic Reticulum Aminopeptidase 1 Induce Altered Innate Immune Responses by Human Immune Cells.
Y. A. Aldhamen, Y. Pepelyayeva, D. P. W. Rastall, S. S. Seregin, E. Zervoudi, D. Koumantou, C. F. Aylsworth, D. Quiroga, S. Godbehere, D. Georgiadis, E. Stratikos, and A. Amalfitano*
Journal of Innate Immunity, 2015, 7 (3) , 275-289

32. Phosphinic Peptides as Potent Inhibitors of Zinc-Metalloproteases Inhibitors.
D. Georgiadis* and V. Dive
Topics in Current Chemistry, 2015, 360, 1-38

31. A New Transcriptional Role for Matrix Metalloproteinase-12 in Antiviral Immunity.
D. Marchant, C. Bellac, T. Moraes, S. Wadsworth, A. Dufour, G. Butler, L. M. Bilawchuk, R. Hendry, A. Robertson, C. Cheung, J. Ng, L. S. Ang, Z. Luo, K. Heilbron, M. Norris, W. Duan, T. Bucyk, A. Karpov, L. Devel, D. Georgiadis, R. Hegele, H. Luo, D. Granville, V. Dive, B. McManus* and C. Overall*
Nature Medicine, 2014, 20, 493-502

30. A Rationally Designed Inhibitor Targeting Antigen-Trimming Aminopeptidases Enhances Antigen Presentation and Cytotoxic T-Cell Responses.
E. Zervoudi, E. Saridakis, J. R. Birtley, S. S. Seregin, E. Reeves, P. Kokkala, Y. A. Aldhamen, A. Amalfitano, I. M. Mavridis, E. James, D. Georgiadis* and Stratikos, E*
Procceedings of the National Academy of Sciences, U.S.A., 2013, 110 (49), 19890-19895

29. A Pan Photoaffinity Probe for Detecting Active Forms of Matrix Metalloproteinases.
C. Nury, B. Czarny, E. Cassar-Lajeunesse, D. Georgiadis, S. Bregant, V. Dive *
ChemBioChem, 2013, 14 (7), 107-114

28. A Common Single Nucleotide Polymorphism in Endoplasmic Reticulum Aminopeptidase 2 Induces a Specificity Switch That Leads to Altered Antigen in Protein Crystallization.
I. Evnouchidou, J. Birtley, S. Seregin, A. Papakyriakou, E. Zervoudi, M. Samiotaki, G. Panayotou, P. Giastas, O. Petrakis, D. Georgiadis, A. Amalfitano, E. Saridakis, I. M. Mavridis, and Stratikos, E *
Journal of Immunology, 2012, 189 (7), 2383-2392

27. Practical Use of Glycerol in Protein Crystallization.
L. Vera, B. Czarny, D. Georgiadis, V. Dive and E. A. Stura *
Crystal Growth and Design, 2011, 11 (7), 2755-2762

26. The N Domain of Human Angiotensin-I Converting Enzyme: The Role of N-Glycosylation and the Crystal Structure in Complex with an N Domain Specific Phosphinic Inhibitor RXP407.
C. S. Anthony, H. R. Corradi, S. L. U. Schwager, P. Redelinghuys, D. Georgiadis, V. Dive, K. R. Acharya* and E. D. L. Sturrock *
Journal of Biological Chemistry, 2010, 285 (46), 35685-35693

25. Insights from Selective Non-Phosphinic Inhibitors of MMP-12 Tailored to Fit with a S1΄ Loop Canonical Conformation.
L. Devel, S. Garcia, B. Czarny, F. Beau, E. Lajeunesse, L. Vera, D. Georgiadis, E. Stura and V. Dive*
Journal of Biological Chemistry, 2010, 285 (46), 35900-35909

24. Third Generation of Matrix Metalloprotease Inhibitors: Gain in Selectivity by Targeting the Depth of the S1΄ Cavity.
L. Devel, B. Czarny, F. Beau, D. Georgiadis, E. Stura and V. Dive*
Biochimie, 2010, 92 (11), 1501-1508

23. High-Resolution Crystal Structures of Drosophila Melanogaster Angiotensin-Converting Enzyme in Complex with Novel Inhibitors and Antihypertensive Drugs.
M. Akif, D. Georgiadis, A. Mahajan, V. Dive, E. D. Sturrock, R. E. Isaac and K. R. Acharya*
Journal of Molecular Biology, 2010, 400 (3), 502-517

22. Phosphinic Tripeptides as Dual Angiotensin-Converting Enzyme C-Domain and Endothelin-Converting Enzyme-1 Inhibitors.
N. Jullien, A. Makritis, D. Georgiadis, F. Beau, A. Yiotakis and V. Dive*
Journal of Medicinal Chemistry, 2010, 53 (1), 208-220

21. A Modular Rearrangement Approach Toward Medicinally Relevant Phosphinic Structures.
V. Rogakos, D. Georgiadis,* V. Dive and A. Yiotakis*
Organic Letters, 2009, 11 (20), 4696-4699

20. Specific Targeting of Metzincin Family Members with Small-Molecule Inhibitors: Progress Towards a Multifarious Challenge.
D. Georgiadis* and A. Yiotakis
Bioorganic and Medicinal Chemistry, 2008, 16 (19), 8781-8794

19. A Versatile Annulation Protocol toward Novel Constrained Phosphinic Peptidomimetics.
Μ. Nasopoulou, D. Georgiadis, M. Matziari, V. Dive and A. Yiotakis*
Journal of Organic Chemistry, 2007, 72 (19), 7222-7228

18. The Structure of Testis Angiotensin-Converting Enzyme in Complex with the C Domain-Specific Inhibitor RXPA380.
H. R. Corradi, I. Chitapi, B. T. Sewell, D. Georgiadis, V. Dive, E. D. Sturrock* and K. R. Acharya*
Biochemistry, 2007, 46 (18), 5473-5478

17. Synthetic Strategies Towards Naturally Occuring Tetronic Acids.
A. L. Zografos and D. Georgiadis*
Synthesis , 2006, 3157-3188

16. Combined Use of Selective Inhibitors and Fluorogenic Substrates to Study the Specificity of Somatic Wild-Type Angiotensin-Converting Enzyme.
N. D. Jullien, P. Cuniasse, D. Georgiadis, A. Yiotakis and V. Dive*
F.E.B.S. Journal, 2006, 273 (20), 1772-1781

15. Rapid Access to the Tricyclic Spirotetronic Core of Abyssomicins.
A. L. Zografos, A. Yiotakis and D. Georgiadis*
Organic Letters, 2005, 7 (20), 4515-4518

14. Future Challenges Facing the Development of Specific Active-Site-Directed Synthetic Inhibitors of MMPs.
P. Cuniasse, L. Devel, A. Makaritis, F. Beau, D. Georgiadis, M. Matziari, A. Yiotakis and V. Dive*
Biochimie, 2005, 87 (3-4) , 393-342

13. Selective Agiotensin-Converting Enzyme C-Domain Inhibition is Sufficient to Prevent Angiotensin I-Induced Vasoconstriction.
J. H. van Esch, B. Tom, V. Dive, W. W. Batenburg, D. Georgiadis, A. Yiotakis, J. M. van Gool, R. J. de Bruijn, R. de Vries and A. H. Danser*
Hypertension, 2005, 45, 120-125

12. Phosphinic Peptides as Zinc Metalloproteinase Inhibitors.
V. Dive,* D. Georgiadis , M. Matziari, A. Makaritis, F. Beau, P. Cuniasse and A. Yiotakis
Cellular and Molecular Life Sciences, 2004, 61, 2010-2019

11. Structural Determinants of RXPA380, a Potent and Highly Selective Inhibitor of the Angiotensin-Converting Enzyme C-Domain.
D. Georgiadis , P. Cuniasse, J. Cotton, A. Yiotakis and V. Dive^
Biochemistry, 2004, 43 (25), 8048-8054

10. Phosphinic Peptides: Synthetic Approaches and Biochemical Evaluation as Zn-Metalloproteases Inhibitors.
A. Yiotakis,* D. Georgiadis , M. Matziari, A. Makaritis and V. Dive
Current Organic Chemistry, 2004, 8 (12), 1135-1158

9. Roles of the two Active Sites of Somatic Angiotensin-Converting Enzyme in the Cleavage of Angiotensin I and Bradykinin. Insights from Selective Inhibitors.
D. Georgiadis, F. Beau, B. Czarny, J. Cotton, A. Yiotakis and V. Dive*
Circulation Research, 2003, 93, 148-154

8. Diastereoselective Solution and Multipin-based Combinatorial Array Synthesis of a Novel Class of Potent Phosphinic Metalloprotease Inhibitors.
A. Makaritis, D. Georgiadis , V. Dive* and A. Yiotakis*
Chemistry - A European Journal, 2003, 9 (9), 2079-2094

7. Synthesis and Comparative Study on the Reactivity of Peptidyl-type Phosphinic Esters. Intramolecular Effects in the Alkaline and Acidic Cleavage of Methyl β-Carboxyphosphinates.
D. Georgiadis, V. Dive and A. Yiotakis*
Journal of Organic Chemistry, 2001, 66 (20), 6604-6610

6. A Highly Efficient Method for the Preparation of Phosphinic Pseudodipeptidic Blocks Suitably Protected for Solid-Phase Peptide Synthesis.
D. Georgiadis, M. Matziari and A. Yiotakis*
Tetrahedron, 2001, 57 (16), 3471-3478

5. Convenient Synthesis and Diversification of Dehydroalaninyl Phosphinic Peptide Analogues.
M. Matziari, D. Georgiadis, V. Dive and A. Yiotakis
Organic Letters, 2001, 3 (5), 659-662

4. Phosphinic Peptide Inhibitors as Tools in the Study of the Function of Zinc Metallopeptidases.
V. Dive,* K. Lucet-Levannier, D. Georgiadis, J. Cotton, S. Vassiliou, P. Cuniasse and A. Yiotakis
Biocemical Society Transactions, 2000, 28 (4), 455-460

3. Potent and Selective Inhibition of Zinc Aminopeptidase A (EC 3.4.11.7, APA) by Glutamyl Aminophosphinic Peptides. Importance of Glutamyl Amiphosphinic Residue in the P1 Position.
D. Georgiadis, G Vazeus, C. Llorens-Cortes, A. Yiotakis and V. Dive*
Biochemistry, 2000, 39 (5), 1152-1155

2. Phosphinic Pseudo-Tripeptides as Potent Inhibitors of Matrix Metalloproteinases: A Structure-Activity Study.
S. Vassiliou, A. Mucha, P. Cuniasse, D. Georgiadis, K. Lucet-Levannier, F. Beau, R. Kannan, G. Murphy, V. Knäuper, M.-C. Rio, P. Basset, A. Yiotakis and V. Dive*
Journal of Medicinal Chemistry, 1999, 42 (14), 2610-2620

1. A Convenient Method to Synthesize Phosphinic Peptides Containing an Aspartyl or Glutamyl Aminophosphinic Acid. Use of the Phenyl Group as the Carboxyl Synthon.
D. Georgiadis, M. Matziari, S. Vassiliou, V. Dive and A. Yiotakis*
Tetrahedron, 1999, 55 (51), 14635-14648

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