The proposed research is intended to exploit RNA as a pharmaceutical target by the synthesis of rationally designed small molecules as lead structures and could potentially result in the development of novel antibiotics. The work will initially focus on substrates that bind specifically to the ribonucleic acid (RNA) components of the bacterial ribosome, which is a validated target for many known antibiotics. Additionally, technologies currently used for the global analysis of protein function, exemplified by the biotin-small molecule conjugates, will be explored for the identification of novel RNA components as potential targets for small molecule interactions with therapeutic significance. Finally, exploration of RNA tertiary structure will be performed by the synthesis of “dynamic libraries”, where the individual final products will be generated in the presence of the biological target, resembling the outcome of a natural selection. Our approach will be expandable to other RNA-domains, like the GTPase associated domain in 23S rRNA, target of the antibiotic thiostrepton, or the internal ribosome entry sites (IRES), which are important targets for the treatment of viral pathogens such as polio and hepatitis C.

This project represents an interdisciplinary approach, comprising of synthetic, spectroscopic, biological, and computational studies and is expected to elucidate the pharmacological profile of various RNA components and increase our understanding for their individual function. In addition to the obvious training opportunities for young researchers in the different scientific fields involved, its successful completion will place EU in the lead of the world stage in the field of RNA, will create new opportunities for the development of biotechnology and pharmaceutics and will improve overall our quality of life.


(Marie Curie Excellence Grants, “Study of RNA components by the Synthesis of Small Molecules”, Contract No. MEXT-CT-2006-039149, Dr. Dionisios Vourloumis, € 1.619.960, 2/2007–1/2011).




The present research aims at the development of innovative multidisciplinary approaches for the design, synthesis and evaluation of molecular, nano- and micro-scale functionalities for targeted delivery of therapeutic peptides and proteins (biopharmaceutics). New protein- and peptide-based drugs are being discovered every day and their increased availability offers new ways to treat diseases. However, the structure, physicochemical properties, stability, pharmacodynamics, and pharmacokinetics of these new biopharmaceutics place stringent demands on the way they are delivered into the body. Carrier-based drug delivery systems can improve the bioavailability and diminish the toxicity of Peptidic/Proteinic (P/P) drugs. Furthermore, the carrier specificity can be enhanced, through proper functionalization, and the release of the therapeutic peptide/protein can be controlled on demand. Artificial nanostructures being of the same size as biological entities can readily interact with biomolecules both on the cell’s surface and within the cell. Thus, the development of functionalized nanocarriers and nanoparticle-based microcarriers for P/P delivery is both an important scientific challenge and potentially a business breakthrough for the biopharmaceutical industry.

('NMP' INTEGRATED PROJECT, "Nanoscale Functionalities for Targeted Delivery of Biopharmaceutics", Contract No. NMP4-CT-2006-026723, Dr. Dionisios Vourloumis, € 537.000, 10/2006-9/2010).



Angiogenesis is the process by which new blood capillaries sprout from pre-existing blood vessels, and it is well recognized that angiogenesis is an important mechanism governing tumor growth and metastasis. The recent clinical success of Avastin® has provided a proof of principle for the potential of anti-angiogenic cancer therapy with anti-vascular enthothelial growth factor (VEGF) agents. This dimeric glycoprotein interacts with two high-affinity transmembrane tyrosine kinase receptors, VEGFR-1 (originally Flt-1) and VEGFR-2 (or human KDR), and results in the proliferation of the endothelial cells and their development into new blood vessels.

One of the potential therapeutic approaches utilizes VEGFR tyrosine kinase inhibitors that target the intracellular signal transduction. Within the last 5 years there has been considerable effort to produce selective VEGFR inhibitors, therefore structures of several nanomolar binders of VEGFR-2 have been obtained. Computational chemistry analysis of these results will lead to the design, synthesis and biological evaluation of novel VEGFR-2 inhibitors.

(ENTER2004, GSRT, “Design of Selective Inhibitors of Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2) Using Structural Methods for the Treatment of Cancer.” Contract No. 04EP63, Dr. Dionisios Vourloumis, € 58.500, 2/07-10/08)


[Top of page]

The secret of any online business is web hosting. Select the best hosting service reading offered by justhost.

Copyright © 2011, Chemical Biology Laboratory, IPC, NCSR "Demokritos". Web designed by Athanasios Papakyriakou using the Free Software Joomla!®