Education

Biography

In 2007, Dr. De Marco was obtained degree in CTF- Chemistry and Pharmaceutical Technologies of the Faculty of Pharmacy, University of Bologna, discussing the Thesis "Bio-isosters and models of xantonic derivatives as aromatase inhibitors". In 2012, Ph.D. in Chemical Sciences; title of the thesis: "Synthesis of modified amino acids and insertion of peptides and mimetics. Structural aspects and impact on biological activity", supervisor Prof. L. Gentilucci, Dept. of Chemistry “G. Ciamician”, University of Bologna.

In 2013, Dr. De Marco won the fellowship "Young Investigator Programme- year 2013" by Umberto Veronesi Foundation, Milan-Rome, obtained for a competitive project entitled: "Tryptophan: Investigation and synthesis of new molecules for pain treatment in patients with stages advanced of cancer".

Dr. De Marco is the author of 36 printed papers on journals with IF, reviews included. Initially, her research was dedicated to the asymmetric synthesis of amino acids, and their introduction into biologically active peptide and mimetics, in particular opioid peptides and integrin inhibitors. More recently, Dr. De Marco started studying small-size heterocycles, such as oxazolidinones, imidazolidinones, lactams, macrolactams, etc. for the preparation of conformationally defined scaffolds in medicinal chemistry. In the last years she started studying the nanomaterials and their applications in several fields.

Research Interest

1. Asymmetric synthesis of amino acids, and their introduction into biologically active peptide and mimetics, opiod peptides and integrin inhibitors.
2. Synthesis of small-size heterocycles, oxazolidinones, imidazolidinones, hydanytoines  for the preparation of conformationally defined scaffolds in medicinal chemistry.
3. Study of conformational analisys by 2D-NMR, gCOSY, ROESY, NOESY
4. Synthesis of nanostructured materials and bind with peptide ligands for the detection of markers of inflammatory disease.
5. Studies for the development of functionalized polimeric materials for biomedical applications
6. Tumor targeting peptidomimetics: synthesis and biomedical applications
7. Expertice: Solid-Phase Synthesis, LC-MS, RP-HPLC preparative, IR, NMR

Scientific Activities

Awards

1996- Finalist "Chemistry Games" organized by the Italian Chemical Society (SCI), ranked 4th at the regional level.

Membership

Member of the Italian Chemistry Society (SCI)
Member of the European Peptide Society (EPS)

Publications

1. Gentilucci, L.; Squassabia, F.; De Marco, R.; Artali, R.; Cardillo, G.; Tolomelli, A.; Spampinato, S.; Bedini, A.Investigation of the interaction between the atypical agonist c[YpwFG] and MOR. FEBS Journal, 2008, 275, 2315
2. Gentilucci, L.; Cardillo, G.; Tolomelli, A.; De Marco, R.; Garelli,A.; Spampinato, S.; Spartà, A.; Juaristi, E. Synthesis and Conformational Analysis of Cyclotetrapeptide Mimetic beta-Turn Templates and Validation as 3D Scaffolds. Chem Med Chem, 2009, 4, 517-23
3. Gentilucci, L.; Cardillo, G.; Tolomelli, A.; Squassabia, F.; De Marco, R.; Chiriano,G. Cyclopeptide analogs for generating new molecular and 3D diversity. Comb Chem High Throughput Screen 2009,12, 929-39.
4. Gentilucci, L.; Cardillo, G.; Spampinato, S.; Tolomelli, A.; Squassabia, F.; De Marco, R.; Bedini, A.; Baiula, M.; Belvisi, L.; Civera, M. Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimetics. J Med Chem 2010,1,106-18.
5. Gentilucci, L.; Cerisoli, L.; De Marco, R., Tolomelli, A. A simple route towards peptide analogues containing substituted (S)- or (R)-tryptophans.Tetrahedron Letters 2010, 51, 2576-79.
6. Bedini, A.; Baiula, M.; Gentilucci, L.; Tolomelli, A.; De Marco, R.; Spampinato, S. Peripheral antinociceptive effects of the cyclic endomorphin-1 analogue c[YpwFG] in a mouse visceral pain model. Peptides 2010, 31, 2135-2140.
7. Gentilucci, L.; De Marco, R.; Cerisoli, L. Chemical Modifications Designed to Improve Peptide Stability: incorporation of Non-Natural Amino Acids, Pseudo-Peptide Bonds, and Cyclization. Curr Pharm Des 2010, 16, 3185-3203.
8. L. Gentilucci, A. Tolomelli, R. De Marco, S. Spampinato,A. Bedini, and R. Artali. The Inverse Type II b-Turn on D-Trp-Phe, a Pharmacophoric Motif for MOR Agonists. Chem. Med. Chem. 2011, 9, 1640-53.
9. L. Gentilucci, A. Tolomelli, R. De Marco, C. Tomasini, and S. Feddersen, Synthesis of Constrained Peptidomimetics Containing 2-Oxo-1,3-oxazolidine-4-Carboxylic Acid. Eur. JOC 2011, 11, 4925-30.
10. L. Gentilucci, R. De Marco, A. Tolomelli, S. Feddersen, S. Spampinato, A. Bedini, R. Artali. A novel family of minimalist opioid peptides deprived of the classic pharmacophores. Pharmacological Reports, 2011, 63, 212.
11. R. De Marco, L. Gentilucci, A. Tolomelli, S. Feddersen, S. Spampinato, A. Bedini, R. Artali. Design and synthesis of opioid peptide analogues and mimetics. Pharmacological Reports, 2011, 63, 223.
12. R. De Marco, A. Tolomelli, M. Campitiello, P. Rubini, L. Gentilucci. Expedient Synthesis of Pseudo-Pro-Containing Peptides: Towards Constrained Peptidomimetics and Foldamers. Org. Biorg. Chem. 2012, 10, 2307-2317.
13. L. Gentilucci, A. Tolomelli, R. Artali, R. De Marco. Molecular docking of opioid peptides and analogues, a powerful tool for the design of selective agonists and antagonists, and for the investigation of atypical ligand-receptor interactions. Curr. Med. Chem. 2012, 19, 1587-1601.
14. D. Fabbri, A. Adamiano, G. Falini, R. De Marco, I. Mancini. Analytical pyrolysis of dipeptides containing proline and amino acids with polar side chains. Novel 2,5-diketopiperazine markers in the pyrolysates of proteins. J. Anal. Appl. Pyrolysis. 2012, 95, 145-155.
15. R. De Marco, A. Tolomelli, A. Bedini, S. Spampinato, L. Gentilucci. Opioid activity profiles of di- and tripeptides lacking of a protonable N-terminus. J. Med. Chem. 2012, 55, 10292-10296.
16. R. De Marco, A. Greco, S. Rupiani, A. Tolomelli, C. Tomasini, S. Pieraccini, L. Gentilucci. In-peptide synthesis of di-oxazolidinone and dehydroamino acid -oxazolidinone motifs as -turn inducers. Org. Biorg. Chem 2013, 11, 4316-4326.
17. R. De Marco, A. Tolomelli, A. Greco, L. Gentilucci. Controlled solid phase peptide synthesis using N-Carboxyanhydrides and PEG resins in water. Sustainable Chemistry & Engineering 2013,11, 4273-4420.
18. R. De Marco, A. Greco, L. Gentilucci. Lab, Preparazione di peptidi biologicamente attivi in condizioni ecocompatibili ed elevata atom-economy. LAB 2013, 7, 32-33. Corresponding author
19. S. D. Dattoli, R. De Marco, M. Baiula, S. Spampinato, A. Greco, A. Tolomelli, L. Gentilucci. Synthesis and assay of retro-α4ß1 integrin-targeting motifs Eur. J. Med. Chem. 2014, 73, 225-232.
20. R. De Marco, S. Spampinato, A. Bedini, L. Gentilucci. Synthesis of Tripeptides Containing D-Trp Substituted at the Indole Ring, Assessment of Opioid Receptor Binding and in Vivo Central Antinociception. J. Med. Chem. 2014, 57, 6861-6866.
21. A. Greco, S. Tani, R. De Marco, L. Gentilucci. Synthesis and Analysis of the Folding Properties of 5-Aminomethyloxazolidine-2,4-dione Scaffolds as β2-Homo-Friedinger Lactam Analogs. Chem. Eur. J. 2014, 20, 13390-13404.
22. R. De Marco, L. Cavina, A. Greco, L. Gentilucci. One-step preparation of dehydroalanine equipped with a chiral auxiliary, and application to the stereoselective synthesis of substituted D-Tryptophans. Amino Acids 2014, 46, 2823-2839.
23. A. Greco, R. De Marco, S. Tani, D. Giacomini, P. Galletti, A. Tolomelli, E. Juaristi, L. Gentilucci. Convenient synthesis of the antibiotic linezolid via a unprecedented oxazolidine-2,4-dione intermediate derived from the chiral building block isoserine. Eur. JOC . 2014, 7614-7620.
24. J. Piekielna, L. Gentilucci, R. De Marco, R. Perlikowska, A. Adamska, J. Olczak, M. Mazur, R. Artali, J. Modranka, T. Janecki, C. Tömböly, A. Janecka. Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine. Bioorg. Med. Chem. 2014, 22, 6545-6551.
25. R. De Marco, G. Ricci, S. Schinelli, L. De Cola, L. Prodi, L. Gentilucci. AsthmaZoè: Nanostructured materials for detention of markers of asthma and other correlated inflammatory diseases. European Respiratory News 2014, 3, 141-142.
26. R. De Marco, G. Mazzotti, A. Greco, S. D. Dattoli, M. Baiula, S. Spampinato, L. Gentilucci. 5-Aminomethyloxazolidin-2,4-dione Hybrid α/β-dipeptide scaffolds as inductor of constrained conformations: applications to the synthesis of integrin antagonists. Biopolymers: Peptide Science 2015, 104(5), 636-649.
27. A. Greco, R. De Marco, L. Maggini, L. De Cola, L. Gentilucci. Selective Integrin-mediated Adhesion of Cancer Cells onto c[RGDfK]-functionalized Zeolite L Monolayers. Bioconjugate Chem., 2015, 26, 1873-1878.
28. R. De Marco, A. Janecka. Strategies to improve bioavailability and in vivo efficacy of the endogenous opioid peptides Endomorphin-1 and Endomorphin-2. Curr. Top. Med. Chem. 2016, 16(2), 141-155.
29. R. De Marco; E. Juaristi, A. Tolomelli, L. Gentilucci. Integrin Ligands with Hybrid α/β- Peptide Structure: Bioactivity, Stability, and Conformational Aspects. Medicinal Research Reviews 2016, 36(3), 389-424.
30. R. De Marco, A. Greco, G. Mazzotti, L. Gentilucci. Heterocyclic Scaffolds in the Design of Peptidomimetic Integrin Ligands: Synthetic Strategies, Structural Aspects, and Biological Activity. Curr. Top. Med. Chem. 2016, 16(3), 346-359.
31. R. Perlikowska, J. Piekielna, L. Gentilucci, R. De Marco, M. C. Cerlesi, G. Calo, R. Artali, C. Tomboly, A. Kluczyk, A. Janecka. Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration Eur. J. Med. Chem. 2016, 109, 276-286.
32. R. De Marco, A. Bedini, S. Spampinato, L. Gentilucci. Fine-Tuning the Selectivity Profile of Analogues of the Cyclotetrapeptide CJ-15,208: Versatile Picklocks for All Opioid Receptors. J. Med. Chem 2016, 59, 9255-9261.
33. L. Gentilucci, F. Gallo, F. Meloni, M. Mastandrea, B. Del Secco, and R. De Marco. Controlling Cyclopeptide Backbone Conformation with /α-Hybrid Peptide–Heterocycle Scaffolds. Eur. JOC. 2016, 19, 3243-3251.
34. J. Piekielna, R. De Marco, L. Gentilucci, M. C. Cerlesi, G. Calo’, C. Tomboly, R. Artali, A. Janecka. Redoubling the ring size of an Endomorphin-2 analog transforms a centrally acting mu-opioid receptor agonist into a pure peripheral analgesic. Peptide Science 2016, 106(3), 309-317.
35. L. Gentilucci, P. Tosi, A. Bauer, R. De Marco. Modern tools for the chemical ligation and synthesis of modified peptides and proteins. Future Medicinal Chemistry. 2016, 8, (18), 2287-2304.
36. A. Adamska-Bartłomiejczyk, R. De Marco, L. Gentilucci, A. Kluczyk, A. Janecka. Design and characterization of opioid ligands based on cycle-in-macrocycle scaffold. Bioorg. Med. Chem. 2017, 25(8), 2399-2405.
37. R. De Marco, L. Gentilucci. Tryptophan-Containing Non-Cationizable Opioid Peptides–A new Chemotype with Unusual Structure and In vivo Activity. Future Medicinal Chemistry 2017.