Organic Chemistry and Biochemistry
Tel: 26510 08387
The primary goal of our lab is to understand biological processes at the molecular & atomic level, with the aim of using this knowledge to tackle specific problems in human health and disease. Special focus is given on cancer diagnostics, theranostics, tumor homing and tumor responsive drug delivery vehicles. We design and develop bioimaging agents (NIR, SWIR), inhibitors for a diverse class of therapeutic targets, theranostics, drug carriers, formulates to optimize the selective delivery of drugs in the disease site and for therapeutic and diagnostic purposes. For the most promising compounds we evaluate their in vivo biodistribution as also their cell uptake using our recently established and ISO:17025 accredited LC-MS platform (BAC LAB). Our research encompasses a wide variety of projects directed towards the development of strategies and methods from the rational design, rapid chemical, chemico-enzymatic and KTGS synthesis, experimental screening of chemical libraries (small synthetic molecules, natural products, peptides, peptidomimetics) for a wide variety of therapeutic targets. For this, we utilize modern robotic synthetic and NMR methodologies complemented by numerous biophysical (fluorescence, CD, ITC, DSC), bioimaging and bioinformatic techniques to characterize the dynamic, structural and thermodynamic properties of the studied systems as also their interactions. Our lab operates under the ISO:17025 accreditation.
|Current research in our lab is underway to explore:|
- (i) Near InfraRed Imaging agents (NIRI, NIRII, SWIR) and their application as cancer theranostics
- (ii) Drug delivery (development of drug delivery vehicles) and ProDrugs
- (iii) Design, synthesis and evaluation of Peptide-Drug Conjugates, prodrugs, small ligands, peptides and peptidomimetics
- (iv) Plants as sources of bioactive compounds; Formulation of Natural Products to amplify their therapeutic potency
- (v) Pharmacokinetics (Our lab operates under the ISO:17025 accreditation).
Organic Chemistry IV, Spectroscopy of Organic Molecules, Spectroscopic and physicochemical methods, Chemistry of Peptides and Proteins, Laboratory of Peptide and Protein Chemistry, Laboratory of Organic Chemistry I, Laboratory of Organic Chemistry II.
|Fellowship and awards:|
- Greek State Scholarship Foundation (IKY) (1995, 1997, 1998, 1999).
- Greek State Scholarship Foundation award (IKY) for excellence in undergraduate studies (1999).
- Marie Curie (2001, Univ. Florence, PARABIO, Italy).
- FEBS Summer Fellowship (2002, SONNMR, Univ. Utrecht, Netherlands).
- NATO fellowship (2001, International School, Erice, Sicily)
- EMBO fellowship (2002, EMBO practical course, Lucca, Italy).
- EMBO fellowship (2005, EMBO practical course, Basel, Switzerland).
- Greek State Scholarship Foundation award (IKY) for excellence in postgraduate studies (2002 Graduate Program in Bioinorganic Chemistry).
- Fellowship from the Greek Ministry of Education on the basis of student and research proposals qualifications (“Heracletos: Fellowships for Basic Research”);
- Leonidas Zervas Award (2004);
- EMBO long term fellowship & Medical Research Council fellowship (2004-2008, Medical Research Council, Laboratory of Molecular Biology, Cambridge, UK);
- Gardiki-Kouidou Award (2007, 59th HSBMB, Athens);
- Erasmus Teaching Mobility (STA) (2008, CNRS, Marseille, France)
- Alexander Onassis foundation fellowship for the 59th Meeting of Nobel Laureates, Lindau, Germany (2009).
- 1st Award from the “Institute for The Study And Education On Thrombosis And Antithrombotic Therapy” (2017)
- Awardee of a prestigious Academy of Athens award(Academy of Sciences, Humanities and Fine Arts) in the field of study and therapy of cancer/heart diseases for his studies on the discovery of the first agent bearing triple antiplatelet activity. (21/12/2018) short interview here.
Our Bioanalysis and Pharmacokinetics Lab operates under the ISO/IEC:17025 accreditation
-  The patent WO 2013091883 has been filed (along with MRCT, LMB, Cambridge) towards the establishment of an electronic tuning methodology to construct GPCR subtype selective ligands.
-  A system and method for the production, assignment and biological evaluation of natural product analogues
-  Greece Industrial property Organization, patent no. 1009100: the smallest on line bioreactor for rapid biotransformation of natural products and ligand-protein interaction monitoring.
-  GEMCITABINE DERIVATIVES AND METHODS OF FORMING GEMCITABINE DERIVATIVES (REF M36357).
-  Novel PI3K inhibitors and applications thereof (No. 10 2020 202 356.5)
-  PRESS -PRotEin S-Sulfenylation server–our server predicts cysteine residues of a protein that are prone to undergo modification to sulfenic acid using SVM, Bioinformatics, in press
-  DIAB-DB: A Web-Accessible Database for the Prediction of Diabetes Drugs. our server predicts diabetes drugs through 2 axes; a) comparison by similarity with a curated database of anti-diabetic drugs and experimental compounds, and b) inverse virtual screening of the input molecules chosen by the users against a set of protein targets identified as key elements in diabetes.
-  Multidimenisional-Fingerprint analysis and Rapid Assignment of Complex Mixtures, coming soon
|Editorial Board Member of International Journals|
|COMMISSIONS OF TRUST (selected)|
- 2009-Present Ad Hoc reviewer for several peer reviewed Journals oriented in drug discovery, medicinal chemistry, cancer and biophysics
- 2009-Present Expert evaluator for several National/International proposals
- 2017- Expert evaluator for H2020 proposals
|AUTHOR OF ACADEMIC BOOKS||TRANSLATION OF ACADEMIC BOOKS|
Nuclear Magnetic Resonance Spectroscopy, (2018), Simmetria, ISBN: 978-960-266-504-6
Organic Chemistry 6, Marc Loudon, Jim Parise, (2019), ISBN: 9789925563616
|PUBLICATIONS IN INTERNATIONAL JOURNALS|
-  Hajji, N.; et al., Arginine deprivation alters microglial polarity and synergizes with radiation to eradicate non-arginine-auxotrophic glioblastoma tumors. J. Clin. Invest. 2022, 132 (6). (Work appeared in the News: https://www.itv.com/news/london/2022-03-03/exciting-finding-say-scientists-to-tackle-deadliest-type-of-brain-tumour)
-  Kyrkou, S. G.; et al., Design Principles Governing the Development of Theranostic Anticancer Agents and Their Nanoformulations with Photoacoustic Properties. Pharmaceutics 2022, 14 (2).
-  Alexandri, E., et al., NMR and computational studies reveal novel aspects in molecular recognition of unsaturated fatty acids with non-labeled serum albumin. Febs J. 2022 in press
-  Koprivica, I.; et al., Phenethyl ester of rosmarinic acid attenuates autoimmune responses during type 1 diabetes development in mice. Life Sci 2022, 288, 120184.
-  Hernychova, L.; et al., Serum albumin as a primary non-covalent binding protein for nitro-oleic acid. Int. J. Biol. Macromol. 2022, 203, 116-129.
-  Tsiailanis A., et al., Exploration of betalains and determination of the antioxidant and cytotoxicity profile of orange and purple Opuntia spp. cultivars in Greece. Plant Foods for Human Nutrition 2022, in press
-  Ganai, et al., DBU mediated one-pot synthesis of triazolo triazines: Via Dimroth type rearrangement. RSC Advances, 2022, 12(4), pp. 2102–2106
-  Diamantis D., et al., Biotin-Yellow a biotin guided NIR turn-on fluorescent probe for cancer targeted diagnosis, Sensors and Actuators B Chemical 2021, 337:129807
-  Tourwé D, et al., Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability. Bioorg Med Chem Lett. 2021, 43, 128086. doi: 10.1016/j.bmcl.2021.128086.
-  Kougioumtzi A., et al., Development of novel GnRH and Tat(48-60) based luminescent probes with enhanced cellular uptake and bioimaging profile, Dalton Transactions, 2021, 50 (26), 9215-9224.
-  Vrettos EI, et al., Development of programmable gemcitabine-GnRH pro-drugs bearing linker controllable “click” oxime bond tethers and preclinical evaluation against prostate cancer. Eur J Med Chem. 2021; 211:113018.
-  Tsiailanis, A. D.; et al., Development of a DHA-Losartan hybrid as a potent inhibitor of multiple pathway-induced platelet aggregation. J Biomol Struct Dyn 2021, 1-12.
-  Tsiailanis, A. D.; et al., Chemical Profiling, Bioactivity Evaluation and the Discovery of a Novel Biopigment Produced by Penicillium purpurogenum CBS 113139. Molecules 2021, 27 (1).
-  Zoi, V.; et al. Curcumin and Radiotherapy Exert Synergistic Anti-Glioma Effect In Vitro. Biomedicines 2021, 9 (11).
-  Vlachou, M.; et al., Biophysical Evaluation and In Vitro Controlled Release of Two Isomeric Adamantane Phenylalkylamines with Antiproliferative/Anticancer and Analgesic Activity. Molecules 2021, 27 (1).
-  Tsagogiannis, E.; et al., Characterization of Protocatechuate 4,5-Dioxygenase from Pseudarthrobacter phenanthrenivorans Sphe3 and In Situ Reaction Monitoring in the NMR Tube. Int J Mol Sci 2021, 22 (17).
-  Sayyad, N.; et al., Development of niosomes for encapsulating captopril-quercetin prodrug to combat hypertension. Int J Pharm 2021, 609, 121191.
-  Pritsas, A.; et al., Valorisation of stachysetin from cultivated Stachys iva Griseb. as anti-diabetic agent: a multi-spectroscopic and molecular docking approach. J Biomol Struct Dyn 2021, 39 (17), 6452-6466.
-  Matsoukas, J.; et al., Myelin Peptide-Mannan Conjugate Multiple Sclerosis Vaccines: Conjugation Efficacy and Stability of Vaccine Ingredient. Vaccines (Basel) 2021, 9 (12).
-  Chontzopoulou, E.; et al., Molecular investigation of artificial and natural sweeteners as potential anti-inflammatory agents. J Biomol Struct Dyn 2021, 1-13.
-  Andreadelis, I.; et al., Charting the structural and thermodynamic determinants in phenolic acid natural product – cyclodextrin encapsulations. J Biomol Struct Dyn 2021, 39 (7), 2642-2658.
-  Tomou EM, et al., Anti-Ageing Potential of S. euboea Heldr. Phenolics, Molecules. 2021 May 25;26(11):3151.
-  Kiriakidi S, et al., Interplay of cholesterol, membrane bilayers and the AT1R: A cholesterol consensus motif on AT1R is revealed. Comput Struct Biotechnol J. 2021 Dec 3;19:110-120.
-  Georgiou N, et al., Rational Design and Synthesis of AT1R Antagonists. Molecules. 2021 May 14;26(10):2927.
-  Syriopoulou A, et al., Ligand-Receptor Interactions and Drug Design. Methods Mol Biol. 2021;2266:89-104.
-  Chontzopoulou E, et al., On the Rational Drug Design for Hypertension through NMR Spectroscopy. Molecules 2021, in press
-  Vrettos EI, et al., Construction of Peptide-Drug Conjugates for Selective Targeting of Malignant Tumor Cells Methods Mol Biol. 2021;2207:327-338.
-  Chatzigiannis CM, et al., 2D DOSY NMR: A Valuable Tool to Confirm the Complexation in Drug Delivery Systems. Methods Mol Biol. 2021;2207:235-246.
-  Chatziathanasiadou MV, et al., Unveiling the Thermodynamic Aspects of Drug-Cyclodextrin Interactions Through Isothermal Titration Calorimetry. Methods Mol Biol. 2021;2207:187-198.
-  Tsiailanis AD, et al., Encapsulation of Small Drugs in a Supramolecule Enhances Solubility, Stability, and Therapeutic Efficacy Against Glioblastoma Multiforme. Methods Mol Biol. 2021;2207:175-186.
-  Tsiailanis AD, et al., Advancing the Therapeutic Efficacy of Bioactive Molecules by Delivery Vehicle Platforms, Curr Med Chem 2021;28(14):2697-2706.
-  Diamantis DA et al., Bioinspired tailoring of fluorogenic thiol responsive antioxidant precursors to protect cells against H2O2-induced DNA damage. Free Radic Biol Med. 2020 in press
-  Tsiailanis AD, et al., Enhancement of glioblastoma multiforme therapy through a novel Quercetin-Losartan hybrid. Free Radic Biol Med. 2020 in press
-  Vrettos E. et al., Single peptide backbone surrogate mutations to regulate angiotensin GPCR subtype selectivity, Chem Eur. J., (Journal Cover!)
-  Manta K, et al., Preparation and biophysical characterization of Quercetin inclusion complexes with β-cyclodextrin derivatives for the preparation of possible nose-to-brain Quercetin delivery systems. Mol Pharm. 2020, in press
-  Liapakis G., et al., Discovery of a stable tripeptide targeting the N-domain of CRF1 receptor. Amino Acids. 2020, in press
-  Papaemmanouil C, et al., Unveiling the interaction profile of rosmarinic acid and its bioactive substructures with serum albumin. J Enzyme Inhib Med Chem. 2020 Dec;35(1):786-804. doi: 10.1080/14756366.2020.1740923.
-  Perez-Sanchez H, et al., DIA-DB: A Database and Web Server for the Prediction of Diabetes Drugs. J Chem Inf Model. 2020, in press
-  Chayrov R, et al., Synthetic Analogues of Aminoadamantane as Influenza Viral Inhibitors-In Vitro, In Silico and QSAR Studies. Molecules. 2020 doi: 10.3390/molecules25173989.
-  Andreadelis I, et al., Charting the structural and thermodynamic determinants in phenolic acid natural product – cyclodextrin encapsulations. J Biomol Struct Dyn. 2020 Apr 6:1-19. doi: 10.1080/07391102.2020.1751716.
-  Chatzikonstantinou AV, et al., The NMR tube bioreactor. Methods Enzymol. 2020; 633:71-101. doi: 10.1016/bs.mie.2019.10.032. Epub 2019 Dec 26.
-  Kiriakidi S, et al., Exploring the role of the membrane bilayer in the recognition of candesartan by its GPCR AT1 receptor. Biochim Biophys Acta Biomembr. 2020 1862(3):183142. doi: 10.1016/j.bbamem.2019.183142.
-  Tomou EM. Et a., NMR-based chemical profiling, isolation and evaluation of the cytotoxic potential of the diterpenoid siderol from cultivated Sideritis euboea Heldr., Molecules, 2020,
-  Pritsas A, et al., Valorisation of stachysetin from cultivated Stachys iva Griseb. as anti-diabetic agent: a multi-spectroscopic and molecular docking approach. J Biomol Struct Dyn. 2020 Jul 31:1-15.
-  Chatzikonstantinou AV, et al., Lipase immobilized on magnetic hierarchically porous carbon materials as a versatile tool for the synthesis of bioactive quercetin derivatives. Bioresource Technology Reports, 2020, in press
-  Leonis G, et al., Antihypertensive activity and molecular interactions of irbesartan in complex with 2-hydroxypropyl-β-cyclodextrin. Chem Biol Drug Des. 2020 Jul;96(1):668-683.
-  Goulas V, Valorization of Carob Fruit Residues for the Preparation of Novel Bi-Functional Polyphenolic Coating for Food Packaging Applications. Molecules. 2019 24(17). pii: E3162. doi: 10.3390/molecules24173162.
-  Renziehausen, A., et al., Encapsulation of temozolomide in a calixarene nanocapsule improves its stability and enhances its therapeutic efficacy against glioblastoma. Mol. Cancer Therapeutics, 2019, in press
-  Renziehausen, A., et al., The Renin Angiotensin System (RAS) mediates bifunctional growth regulation in melanoma and is a novel target for therapeutic intervention, Oncogene, 2019, 38:2320-2336
-  Yilmaz., M., et al., Inclusion of Quercetin in Gold Nanoparticles Decorated with Supramolecular Hosts Amplifies its Tumor Targeting Properties, 2019, ACS Appl. Bio Mater. , in press(JOURNAL COVER!)
-  Primikyri, A. et al., Probing the interaction of a quercetin bioconjugate with Bcl-2 in living human cancer cells with in-cell NMR spectroscopy, Febs Lett., 2019, 3367-3379. (EDITOR’S CHOICE!)
-  Heřmánková et al., Redox properties of individual quercetin moieties, Free Radic Biol Med., 2019, 30897-4.
-  Sayyad N., et al., Development of bioactive gemcitabine-D-Lys6-GnRH prodrugs with linker-controllable drug release rate and biopharmaceutical profile. Eur. J. Med. Chem., 2019, in press
-  Mubarak M., et al., Development and validation of simple step protein precipitation UHPLC-MS/MS methods for quantitation of temozolomide in cancer patient plasma samples,J. Pharm. Biomed. Anal.,2019,162:164-170.
-  Chatziathanasiadou M., et al.,Development of a validated LC-MS/MS method for the in vitro and in vivo quantitation of sunitinib in glioblastoma cells and cancer patients, J. Pharm. Biomed. Anal.,2019, 5;164:690-697.
-  Ntountaniotis D. et al., Host-guest interactions between candesartan and its prodrug candesartan cilexetil in complex with 2-hydroxypropyl-β-cyclodextrin: on the biological potency for Angiotensin II antagonism. Mol Pharm. 2019, in press
-  Mihailidou AS, et al., Non-Genomic Effects of Aldosterone. Vitam Horm. 2019;109:133-149.
-  Magafa V. et al., Novel stable analogues of the Neurotensin NT(8-13) C-terminal hexapeptide containing unnatural amino acids, Amino Acids, 2019, in press
-  Chantzopoulou E., et al., A Sweet Drug? Repurposing an Old Artificial Sweetener as a Novel Lipoxygenase Inhibitor, 2019,
-  Andreadelis I., et al., On the Architectural and Thermodynamic Aspects of Caffeic Acid and Rosmarinic Acid Encapsulation in 2-hydroxypropyl-beta-Cyclodextrin, 2019
-  Mubarak M. et al., Development of a novel conjugatable sunitinib analogue validated through in vitro and in vivo preclinical settings, Journal of Chromatography B, 2018, 1092:515-523
-  Diamantis, D., et al., Exploring the oxidation and iron binding profile of a cyclodextrin encapsulated quercetin complex unveiled a controlled complex dissociation through a chemical stimuli, Biochim. Biophys. Acta, 2018, 1862(9):1913-1924
-  Vrettos E., et al., On the Design Principles of Peptide – Drug Conjugates for Targeted Drug Delivery to the Malignant Tumor Site, Beilstein J. Org. Chem. 2018, 14, 930–954(INVITED)
-  Chayrov R., et al., Tailoring Acyclovir Prodrugs with Enhanced Antiviral Activity: Rational Design, Synthesis, Human Plasma Stability and In Vitro Evaluation, Amino Acids, 2018, 50(8):1131-1143.
-  Gerogianni P., et al., Lipophilic ester and amide derivatives of rosmarinic acid protect cells against H2O2-induced DNA damage and apoptosis: the potential role of intracellular accumulation and labile iron chelation, Redox Biol.2018, 15, 548-556
-  Tsiailanis A., et al. Designing natural product hybrids bearing triple antiplatelet profile and evaluating their human plasma stability, Methods Mol. Biol., 2018;1824:371-385 (INVITED)
-  Kyriakou, E. et al., Three Regioselectively Acylated Flavonoid Aglycone Derivatives in Equimolar Yield at One Blow, ChemistrySelect,2018, 3, 5207-5211.
-  Chatziathanasiadou MV, et al., Amplifying and broadening the cytotoxic profile of quercetin in cancer cell lines through bioconjugation, Amino Acids, 2018, 50(2):279-291
-  Ishiguro, S; et al., Co-treatment with a C1B5 peptide of protein kinase Cg and a low dose of gemcitabine strongly attenuated pancreatic cancer growth in mice through T cell activation. Biochem. Biophys. Res. Comm. 2018, 495(1):962-968
-  Chatzikonstantinou A., et al.; Enriching the biological space of natural products, through real time biotransformation monitoring: the NMR tube bioreactor, Biochim. Biophys. Acta, 2018, 1862(1):1-8
-  Vrettos E. et al., Unveiling and Tackling Guanidinium Peptide Coupling Reagent Side Reactions towards the Development of Peptide-Drug Conjugates, RSC Advances, 2017, in press
-  Kellici T., et al., Rational design and structure-activity relationship studies of quercetin-amino acid hybrids targeting the anti-apoptotic protein Bcl-xL, Org Biomol. Chem., 2017, in press
-  Stylos E., et al. Tailoring Naringenin Conjugates with Amplified and Triple Antiplatelet Activity Profile: Rational Design, Synthesis, Human Plasma Stability and In Vitro Evaluation, Biochim. Biophys. Acta, 2017, in press
-  Liosi Α. , et al., Exploring the interactions of irbesartan and irbesartan-2-hydroxypropyl-b-cyclodextrin complex with model membranes, Biochim. Biophys. Acta, 2017, 1859(6):1089-1098
-  Moschonas I., et al. Molecular requirements involving human platelet protease-activated receptor-4 mechanism of activation by peptide analogues of its tethered-ligand, Platelets, 2017, in press
-  Stylos E., et al., LC-MS/MS based bioavailability determination of the major classes of phytochemicals, J Chromatogr B, 1047:15-38 (INVITED)
-  Charisiadis P, et al., Determination of Polyphenolic Phytochemicals using Highly Deshielded -OH 1 H-NMR Signals Phytochem. Anal. 2017, May;28(3):159-170.
-  Kellici, T., et al., Mapping the Interactions and Bioactivity of Quercetin-(2-Hydroxypropyl)-β-Cyclodextrin Complex, International Journal of Pharmaceutics, 2016, 511(1):303-11
-  Argyros O., et al., Peptide-drug conjugate GnRH-sunitinib targets angiogenesis selectively at the site of action to inhibit tumor growth, Cancer Research, 2016,76(5):1181-92
-  Sakka M. et al., PRESS: protein S-sulfenylation server,Bioinformatics, 2016, 32(17):2710-2
-  Kellici, T., et al., The dynamic properties of angiotensin II type 1 receptor inverse agonists in solution and in the receptor site, Arabian Journal of Chemistry, 2016, in press
-  Milica Vujicic, et al., Ethyl Acetate Extract of Origanum vulgare L. ssp. hirtum Prevents Streptozotocin-Induced Diabetes in C57BL/6 Mice, J. Funct. Food., 2016, 81(7):H1846-53
-  Karakurt S., et al., Calixarenes in Biocatalysis and Cancer Therapy,Curr. Org. Chem., 2016, 10, 1043 – 1057 (Editor’s Choice) A press release has been also published in EurekAlert
-  Kellici T.F. et al., Leveraging NMR and X-ray Data of the Free Ligands to Build Better Drugs Targeting GPCRs: The Case of AT1R Curr. Med. Chem.2016, 23, 36-59 (JOURNAL COVER)
-  Kontogianni V. et al., Deconvoluting the synergistic antiplatelet activity of an olive leaf extract, J. Agric. Food Chem, 64 (22), 4511–4521
-  Goulas V., Stylos E., Chatziathanassiadou M., et al. Functional components of carob: linking the chemical and biological space, Int. J. Mol. Sci. 2016, 17(11), 1875 (INVITED)
-  Charisiadis P, et al., Determination of Polyphenolic Phytochemicals using Highly Deshielded -OH 1 H-NMR Signals Phytochem. Anal. 2016, in press
-  Siskos M., et al., 1H NMR chemical shift assignment, structure and conformational elucidation of hypericin with the use of DFT calculations – The challenge of accurate positions of labile hydrogens, Tetrahedron, 52, 8287-8293
-  Kounnis V. et al., Microcystin-LR shows cytotoxic activity against pancreatic cancer cells expressing the membrane OATP1B1 and OATP1B3 transporters, Anticancer Res.2015, in press
-  Geromichalou E et al., Regioselective chemical and rapid enzymatic synthesis of a novel redox – antiproliferative molecular hybrid, Eur J. Med. Chem. 2015, 96:47-57.
-  Kellici T.F. et al., Pharmaceutical compositions for antihypertensive treatments: a patent review, Expert Opin Ther Pat. 2015, in press
-  Siskos MG et al., Accurate ab initio calculations of O-HO and O-H(-)O proton chemical shifts: towards elucidation of the nature of the hydrogen bond and prediction of hydrogen bond distances. Org Biomol Chem. 2015; 13(33):8852-68.
-  Papaemmanouil C et al., Selective One-Dimensional Total Correlation Spectroscopy Nuclear Magnetic Resonance Experiments for a Rapid Identification of Minor Components in the Lipid Fraction of Milk and Dairy Products: Toward Spin Chromatography? J Agric Food Chem. 2015 63(22):5381-7.
-  Primikyri A et al., Understanding zinc(II) chelation with quercetin and luteolin: a combined NMR and theoretical study. J Phys Chem B. 2015;119(1):83-95.
-  Prodromidis M. et al, Preorganized composite material of polyaniline–palladium nanoparticles with high electrocatalytic activity to methanol and ethanol oxidation. International Journal of Hydrogen Energy, 2015, in press
-  Ferlemi A. et al., Rosemary tea consumption results to anxiolytic- and anti-depressant-like behavior of adult male mice and inhibits all cerebral area and liver cholinesterase activity; phytochemical investigation and in silico studies Chemico-Biological Interactions 2015, 237:47-57
-  Milica Vujicic, eta al., Tzakos A., Stojanovic I. Methanolic extract of Origanum vulgare ameliorates type 1 diabetes through antioxidant, anti-inflammatory and anti-apoptotic activity, Br J Nutr. 2015;113(5):770-82.
-  Susumu Ishiguro et al., Involvement of angiotensin II type 2 receptor (AT2R) signaling in human pancreatic ductal adenocarcinoma (PDAC): a novel AT2R agonist effectively attenuates growth of PDAC grafts in mice, Cancer Biol Ther. 2015 Feb;16(2):307-16.
-  Tahsin F. Kellici et al., Investigation of the interactions of silybin with 2-hydroxypropyl-β-cyclodextrin through biophysical techniques and computational methods, Mol Pharm.201512(3):954-65.
-  Kellici T. et al., Rational Drug Design Paradigms: The Odyssey for designing better Drugs. Comb Chem High Throughput Screen. 2015, in press
-  Tahsin F. Kellici et al., Rational Drug Design and Synthesis of Molecules Targeting the Angiotensin Receptors AT1 and AT2, Molecules. 2015; 20(3):3868-97.
-  Magnani F., et al., Tzakos A* Electronic tuning of angiotensin II selectivity to its GPCRs AT1R and AT2R, ACS Chemical Biology, in press, DOI: 10.1021/cb500063y
-  Primikiri A., et al., Tzakos A* Direct binding of Bcl-2 family proteins by quercetin triggers its pro-apoptotic activity, ACS Chemical Biology, in press
-  Karampelas T., et al. GnRH-Gemcitabine Conjugates for the Treatment of Androgen-Independent Prostate Cancer: Pharmacokinetic Enhancements Combined with Targeted Drug Delivery, Bioconjugate Chemistry, 25, 813-823
-  Stamatopoulou V., et al., On the Role of the appended P19 domain in type A RNAs of bacterial RNase P, Biochemistry, 53, 1810-1817
-  Ntountaniotis D. et al. The application of solid state NMR spectroscopy to study Candesartan Cilexetil (TCV-116) membrane interactions. Comparative study with the AT1R antagonist drug olmesartan. Biochim. Biophys Acta, , in press
-  Stathopoulos P., et al., Tzakos* A., A rapid and efficient method for the synthesis of selectively S-Trt or S-Mmt protected Cys-containing peptides, Amino Acids, 46, 1367-1376
-  Charisiadis P., et al. 1H NMR as a Structural and Analytical Tool of Intra-and Inter-molecular Hydrogen Bonds of Phenol Containing Natural Products and Model Compounds, Molecules, in press
-  Charisiadis P., et al. Dynamic changes in composition of extracts of natural products as monitored by in situ NMR: the role of entropy, Magn Reson Chem, in press
-  Ferlemi AV. et al., Phytochemical analysis, in silico studies and in vivo evaluation of rosemary tea on behavioral parameters and AChE activity,
-  Tahsin Kellici et al., Rational Drug Design Paradigms: The Odyssey for designing better Drugs, Combinatorial Chemistry & High Throughput Screening, in press
-  Primikyri A et al., Understanding Zinc(II) Chelation with Quercetin and Luteolin: A Combined NMR and Theoretical Study. J Phys Chem B. 2014, in press
-  Tzakos A.G*., et al., Novel Oncology Therapeutics: Targeted Drug Delivery for Cancer, J Drug Deliv. 2013;2013:918304
-  Siskos M., et al. Investigation of solute-solvent interactions in complex phenol compounds at a molecular level: accurate ab initio calculations of solvent effects on 1H NMR chemical shifts, Org Biomol Chem. 2013 Nov 14;11(42):7400-11
-  Charisiadis P. et al., Entropy Driven Dynamic Changes in Composition of Extracts of Natural Products Monitored by in situ NMR, submitted
-  Kounnis, V, et al., Microcystin LR is a new candidate molecule for the development of novel therapeutics against pancreatic cancer specifically expressing the OATP1B3 transporter, submitted
-  Apostolopoulos V., et al. Targeting antigens to dendritic cell receptors for vaccine development, J DrugDeliv., in press
-  Athena A Papadopoulou et al., Enzymatic hybridization of α-lipoic acid with bioactive compounds in ionic solvents, Bioresource Technology, in press
-  Stathopoulos P., et al., Side reactions in the SPPS of Cys-containing peptides, Amino Acids, 2013 May;44(5):1357-63
-  Kontogianni, V., et al. Tzakos A*. Olive leaf extracts as a natural source of potent advanced glycation end products (AGE) inhibitors, J. Med Food., in press
-  Froudarakis M., et al., (2013) Revisiting bleomycin from pathophysiology to safe clinical use, Critical Reviews in Oncology Hematology, in press
-  Kontogianni, V., et al., Tzakos, A.*, (2013) Phytochemical profile of Rosmarinus officinalis and Salvia officinalis extracts and correlation to their antioxidant and anti-proliferative activity, FoodChem., in press
-  Buxhofer-Ausch V., et al. (2013) Tumor-specific expression of organic anion-transporting polypeptides (OATPs) as novel targets for improved cancer therapy, J Drug Deliv., in press
-  Kontogianni, V., et al., Hydrogen Bonding Probes of Phenol-OH Groups: Shielding Ranges, Solvent Effects and Temperature Coefficients of 1H NMR Shieldings and OH Diffusion Coefficients, Org. Biomol. Chem, in press
-  Malini Nagulapalli et al., Andreas G. Tzakos*, (2012) Recognition Pliability is Coupled to Structural Heterogeneity: a Calmodulin – Intrinsically Disordered Binding Region Complex, Structure, 2012, 20(3), 522-533.
-  Koutsotoli A., Tzakos, A.G.* (2012) Host – pathogen crosstalking: The mastery of taking the helm of the host, Structure, 2012, invited
-  Kyriakou, E., Primikyri, A., Charisiadis, P., Katsoura, M., Gerothanassis, I., Stamatis, H., and Tzakos A*, (2012) Unexpected Enzyme-Catalyzed Regioselective Acylation of Flavonoid Aglycones & Rapid Product Screening, Org. Biomol. Chem, 2012, 10 (9), 1739 – 1742.
-  Primikyri, A., et al., Tzakos A*, Gerothanassis I. (2012) Fine-Tuning the Diffusion Dimension of -OH Groups for the Application of High Resolution DOSY NMR in Mixture Analysis of Organic Compounds, Tetrahedron, 68, 6887-6891.
-  Tzakos A, et al., (2012) Exploration of the antiplatelet activity profile of betulinic acid on human platelets, J. Agr. Food. Chem., in press (DOI: http://dx.doi.org/10.1021/jf3006728).
-  Vasilopoulou, C. Kontogianni, V., Linardaki, Z., Iatrou, G., Lamari, F., Nerantzaki, A., Gerothanassis, I., Tzakos, A.*, Margarity., M.* (2012) Phytochemical composition of “mountain tea” from Sideritis clandestina subsp. clandestina and evaluation of its behavioural and oxidant/antioxidant effects on adult mice Eur. J. of Nutr., DOI 10.1007/s00394-011-0292-2, in press (awarded also by the HSN in the 5th HS for Neuroscience Meeting).
-  Charisiadis P., et al., (2012) A Rapid and Direct Low Micromolar NMR method for the Simultaneous Detection of Hydrogen Peroxide and Phenolics in Plant Extracts, J. Agr. Food Chem., in press
-  Koutsotoli A., Tzakos, A.G.* (2012) Targeting the Diseasome Complexity with Natural Sources, in press (invited)
-  Tzakos A.* (2012),Intrinsic Protein Disorder as a Drug Target in Oncology: Designing Drugs Targeting Plasticity, Biochem & Pharmacol1:e107. doi:10.4172/bcpc.1000e107, (invited)
-  Pappas, C., Tzakos, A., Gerothanassis, I., On the Hydration State of Amino Acids and their Derivatives at Different Ionization States: A Comparative Multinuclear NMR and Crystallographic Investigation, (invited)
-  Valentinos Kounnis, Elli Ioachim, Martin Svoboda, Andreas Tzakos, Ioannis Sainis, Theresia Thalhammer, Georg Steiner, Evangelos Briasoulis (2011) Expression of organic anion-transporting polypeptides 1B3, 1B1, and 1A2 in human pancreatic cancer reveals a new class of potential therapeutic targets. Onco Targets Ther 4: 27-32.
-  Charisiadis P., Primikyri A., Exarchou, V., Tzakos, A., Gerothanassis, I. (2011) Unprecedented Ultra High-Resolution Hydroxy Group 1H NMR Spectroscopic Analysis of Plant Extracts, J. Nat. Prod., 74, 2462-6.
-  Andreas G Tzakos*, Demosthenes Fokas, Charlie Johannes, Vassilios Moussis, Eleftheria Hatzimichael, Evangelos Briasoulis (2011) Targeting oncogenic protein-protein interactions by diversity oriented synthesis and combinatorial chemistry approaches. Molecules 16: 6. 4408-4427 05 (invited)
-  Vassiliki Stamatopoulou, Chrisavgi Toumpeki, Andreas Tzakos, Anastassios Vourekas, Denis Drainas (2010) Domain architecture of the DRpp29 protein and its interaction with the RNA subunit of Dictyostelium discoideum RNase P. Biochemistry 49: 50. 10714-10727
-  Konstantinos Skobridis, Maria Kinigopoulou, Vassiliki Theodorou, Emilia Giannousi, Alison Russell, Rakhee Chauhan, Roberta Sala, Nicola Brownlow, Serafim Kiriakidis, Jan Domin, Andreas G Tzakos, Nick J Dibb (2010) Novel imatinib derivatives with altered specificity between Bcr-Abl and FMS, KIT, and PDGF receptors. ChemMedChem 5: 1. 130-139
-  Ioannis Sainis, Demosthenes Fokas, Katerina Vareli, Andreas G Tzakos, Valentinos Kounnis, Evangelos Briasoulis (2010) Cyanobacterial cyclopeptides as lead compounds to novel targeted cancer drugs. Mar Drugs 8: 3. 629-657 03
-  Dimitrios H Roukos, Andreas Tzakos*, George Zografos (2009) Current concerns and challenges regarding tailored anti-angiogenic therapy in cancer. Expert Rev Anticancer Ther 9: 10. 1413-1416
-  Sarath Chandra Janga, Andreas Tzakos (2009) Structure and organization of drug-target networks: insights from genomic approaches for drug discovery. Mol Biosyst 5: 12. 1536-1548.
-  Andreas G Tzakos, Laura E Easton, Peter J Lukavsky (2007) Preparation of large RNA oligonucleotides with complementary isotope-labeled segments for NMR structural studies. Nat Protoc 2: 9. 2139-2147
-  Latifa ElAntak, Andreas G Tzakos, Nicolas Locker, Peter J Lukavsky (2007) Structure of eIF3b RNA recognition motif and its interaction with eIF3j: structural insights into the recruitment of eIF3b to the 40 S ribosomal subunit. J Biol Chem 282: 11. 8165-8174
-  Vassiliki Theodorou, Konstantinos Skobridis, Andreas G Tzakos, Valentine Ragoussis (2007) A simple method for the alkaline hydrolysis of esters. Tetrahedron Letters 48: 8230-8233
-  Andreas G Tzakos, Laura E Easton, Peter J Lukavsky (2006) Complementary segmental labeling of large RNAs: economic preparation and simplified NMR spectra for measurement of more RDCs. J Am Chem Soc 128: 41. 13344-13345
-  Andreas G Tzakos, Christy R R Grace, Peter J Lukavsky, Roland Riek (2006) NMR techniques for very large proteins and rnas in solution. Annu Rev Biophys Biomol Struct 35: 319-342
-  Andreas G Tzakos, Nawazish Naqvi, Konstantinos Comporozos, Roberta Pierattelli, Vassiliki Theodorou, Ahsan Husain, Ioannis P Gerothanassis (2006) The molecular basis for the selection of captopril cis and trans conformations by angiotensin I converting enzyme. Bioorg Med Chem Lett 16: 19. 5084-5087
-  Andreas G Tzakos, Ioannis P Gerothanassis (2005) Domain-selective ligand-binding modes and atomic level pharmacophore refinement in angiotensin I converting enzyme (ACE) inhibitors. Chembiochem 6: 6. 1089-1103
-  A. Tzakos, P. Kursula, V. Theodorou, T. Tselios, C. Svarnas, J. Matsoukas, A. Troganis, V. Apostolopoulos, I. Gerothanassis.(2005) Structure and Function of the Myelin Proteins: Current Status and Perspectives in Relation to Multiple Sclerosis. Cur. Med. Chem. 12, 13, 1569-1587.
-  Andreas G Tzakos, Patrick Fuchs, Nico A J van Nuland, Anastasios Troganis, Theodore Tselios, Spyros Deraos, John Matsoukas, Ioannis P Gerothanassis, Alexandre M J J Bonvin (2004) NMR and molecular dynamics studies of an autoimmune myelin basic protein peptide and its antagonist: structural implications for the MHC II (I-Au)-peptide complex from docking calculations. Eur J Biochem 271: 16. 3399-3413
-  Andreas G Tzakos, Ioannis P Gerothanassis, Anastassios N Troganis (2004) On the structural basis of the hypertensive properties of angiotensin II: a solved mystery or a controversial issue? Curr Top Med Chem 4: 4. 431-444
-  Andreas G Tzakos, Athanassios S Galanis, Georgios A Spyroulias, Paul Cordopatis, Evy Manessi-Zoupa, Ioannis P Gerothanassis (2003) Structure-function discrimination of the N- and C- catalytic domains of human angiotensin-converting enzyme: implications for Cl- activation and peptide hydrolysis mechanisms. Protein Eng 16: 12. 993-1003
-  Athanassios S Galanis, Georgios A Spyroulias, Roberta Pierattelli, Andreas Tzakos, Anastassios Troganis, Ioannis P Gerothanassis, George Pairas, Evy Manessi-Zoupa, Paul Cordopatis (2003) Zinc binding in peptide models of angiotensin-I converting enzyme active sites studied through 1H-NMR and chemical shift perturbation mapping. Biopolymers 69: 2. 244-252
-  Andreas G Tzakos, Alexandre M J J Bonvin, Anasstasios Troganis, Paul Cordopatis, Mario L Amzel, Ioannis P Gerothanassis, Nico A J van Nuland (2003) On the molecular basis of the recognition of angiotensin II (AII). NMR structure of AII in solution compared with the X-ray structure of AII bound to the mAb Fab131. Eur J Biochem 270: 5. 849-860
-  Georgios A Spyroulias, Panagiota Nikolakopoulou, Andreas Tzakos, Ioannis P Gerothanassis, Vassiliki Magafa, Evy Manessi-Zoupa, Paul Cordopatis (2003) Comparison of the solution structures of angiotensin I & II. Implication for structure-function relationship. Eur J Biochem 270: 10. 2163-2173
-  I Gerothanassis, A Tzakos, A Troganis, P Cordopatis, A Bonvin, N van Nuland (2003) On the Molecular Basis of Hypertension: Structural Studies of ACE, AI AII and its analogues In: Hellenic Medical Pharmaceutical Review
-  Andreas Tzakos et al. (2002) Conformational Studies of a Myelin Basic Protein Epitope 74-85 Implicated in Multiple Sclerosis In: Bioactive Peptides in Drug Discovery and Design: Medical Aspects, Biomedical and Health Series, Edited by:J. Matsoukas and T. Mavromoustakos. 180-187 Ios Press, Amsterdam, the Netherland
-  A G Tzakos, A Troganis, I G Gerothanassis, N Assimomytis, V Magafa, E Manessi-Zoupa, E Bissyris, P Cordopatis (2001) Two Dimensional NMR Studies of Angiotensin II and Biologically Important Analogues In: Peptides (J.Martinez, Ed.), Editions EDK, Paris, (2001). Edited by:J.Martinez. Paris: Editions EDK