Inhibitors based on the Snare Motif

Hayden and G. Murray Hamilton. Pepmetics Inc., 1762-1st Avenue N.W., Calgary, Alberta, Canada T2N OBI and Therapy Group, Defence Research Establishment Suffield, Medicine Hat, Alberta, Canada Botulinus neurotoxins are zinc proteases which cleave the SNARE proteins of synaptic vesicles thereby preventing neurotransmitter release. The SNARE complex is a four helix bundle made up of three proteins which each contain the repeating SNARE motif AAxxA, where A is...

Spectroscopy

Solmajer and R. Jerala Laboratory for Molecular Modeling and NMR Spectroscopy, National Institute of Chemistry, POB 660, Hajdrihova 19, 1001, Ljubljana, Slovenia DNA gyrase is a well-established antibacterial target, because it is restricted to prokaryotic organisms. Novel DNA gyrase inhibitors are still searched in order to overcome the limitations of the known inhibitors connected with resistance and cytotoxicity. In our efforts to find new lead compounds, the...

Biological Implications

Papazacharias, A. Galanis and P. Cordopatis Laboratory of Pharmacognosy and Chemistry of Natural Products, Department of Pharmacy, University of Patras, Patras, Greece Over the last decade the devolepement on technology and methodology in NMR Spectroscopy was achieved in concert with the detailed analysis and exploitation of NMR data, especially these that can provide geometrical information (NOEs - Nuclear Overhausser Enhancement, paramagnetism, relaxation times, 3- HNHa...

And the T cell Receptor

Plebanski2 'Head, Immunology and Vaccine Laboratory, 2Head, Vaccine Development and Infectious Disease Laboratory, The Austin Research Institute, Studley Road, Heidelberg, VIC 3084, Australia. The major histocompatibility complex on the surface of antigen presenting cells presents peptides to the T cell receptor. Recognition of peptide-MHC by T cells activates them as well as initiating a sequence of signals in T cells which enables a T cell dependent specific immune...

Glutamate Semialdehydes

Magrioti3, T. Makridisb and G. Kokotosb aChemical Laboratories, Agricultural University of Athens, Greece bLaboratory of Organic Chemistry, Department of Chemistry, University of Athens, Greece 2-Amino-oleic acid is of great interest, because it is used as a tissue treatment for advanced generation bioprostheses. Efficient methodology for the synthesis of enantiopure 2-amino-oleic acid was developed using either tert-butyl or methyl as key-intermediates....

Molecular Biology and Drug Design

Tsakalidis1 'Department of Computer Engineering and Informatics, University of Patras, 26500 Patras, Molecular structure-based drug design is an art and a science. As graphics hardware has matured and software continues to mature, the applications of computer algorithms on molecular biology provides a rigorous basis for many drug design efforts. In this paper we try to present the basic principles in molecular graphics as long as it concerns molecular representations and...

Antitumor activity of Lasparaginase

L-Asparaginase is unique among cancer chemotherapeutic agents for at least two reasons. First, the enzyme can exert its cytotoxic activity at sites far removed from the tumor itself. Secondly, L-asparaginase is a catalytic protein and one molecule of the enzyme will degrade thousands molecules of L-asparagine per minute. Its cytotoxicity is based on a biochemical difference between sensitive and resistant cells. Unlike normal cells, the malignant cells can only synthesize L-asparagine slowly...

Studies on Release by Buffer and Rat Plasma

Cancer Research Institute and Department of Pharmacology, University of California San Francisco, California, 94143-0450 Present address School of Pharmacy Dept. of Pharmacognosy Panepistimiopolis Zografou This paper is dedicated to the memory of Professor Demitrios Papahadjopoulos This experimental article provides data concerning of the encapsulation of vinorelbine (VNR) in various liposomal composition which was achieved using different ammonium and sodium salts. The amount of VNR trapped...

Peptides Bound to LPS

Kidric National Institute of Chemistry, Hajdrihova 19, SI-1000 Ljubljana, Slovenia Lipopolysaccharide LPS, endotoxin induced Gram-negative sepsis and septic shock remain lethal in up to 60 of cases, and LPS antagonists that neutralize its endotoxic action are the subject of intensive research. In the last decade peptidic antagonists have become increasingly important in providing leads for treatment of LPS-mediated diseases. In an effort to determine the molecular motifs of...

Synthetic LHRH Analogue in Solution

Analogue Chemical

Magafa and P. Cordopatis Department of Pharmacy, University ofPatras, 26504 Patras, Greece The pivotal role that LHRH and its analogues play in the modulation of reproductive functions have attracted considerable scientific interest because of their usefulness in the treatment of endocrine-based diseases such as prostate cancer, breast cancer, endometriosis and precocious puberty. Several LHRH agonists, represented by Leuprolide DLeu6, desGly' -LHRH-ethylamide...

Myelin Basic Protein Epitope MBPMi

Daliani2, P. Zoumpoulakis3, L. Probert2, A. Troganis4, P. Papathanassopoulos5, T. Mavromoustakos3 and J. Matsoukas1 1 Department of Chemistry, University of Patras, Patras, Greece 26500 2 Department of Molecular Genetics, Hellenic Pasteur Institute, Athens, Greece 11521 3 National Hellenic Research Foundation, Institute of Organic and Pharmaceutical Chemistry, 11635 Athens, Greece 4 Department of Chemistry, University of loannina, 45110 Ioannina, Greece 5 Department...

Larvae of the Gray Flesh

Poulos2 'institute of Organic and Pharmaceutical Chemistry, Vas. Constantinou 48, Athens 11635 2 University of Patras, Department of Chemistry, Patras 26500, Greece Larval extracts of the homometabolous insects i.e.Neobelleria Bullata -Insecta Diptera , cause immediate paralysis, followed by death when injected into adult flesh flies. These extracts contain endogenous toxins which are widely spread over the class of insects , called paralysins, and are...

Fluorometric Assays of Enzymes

Department of Chemistry, University of Athens, Panepistimiopolis, Zografou, Athens 15771, Greece This article describes the development of new fluorescent markers and their use in the solution or solid phase synthesis of fluorogenic and intramolecularly quenched fluorogenic substrates IQFS for proteases or lipases. The determination and study of several proteases, such as chymotrypsin, oxytokinase, prolylendopeptidase, aminopeptidase M, elastase and trypsin are reviewed. The results of an...

Influenza A Virus

B. Foscolos,1 G. Fytas,1 E. Padalko,2 J. Neyts2 and 'School of Pharmacy, Department of Phrmaceutical Chemistry, University of Athens, Panepistimioupoli-Zografou GR-15771 Athens, Greece. 2Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, The influenza A virus has been proved to be a serious threat for human life. Three pandemics have occurred in the last century, one of which the infamous Spanish flu of 1918 was responsible for...

Abstract

The novel amide linked Angiotensin II cyclic analogues y,e- cyclo 3, 5 - Sar1-Glu3-Lys5 ANG II 1 and y, e - cyclo 3, 5 - Sar'-Glu LysMle8 ANG II 2 have been designed, synthesized and bioassayed in anesthetized rabbits in order to further unravel structural ring cluster characteristics important for receptor activation. The two analogues were synthesized in particular to investigate differences in activity and conformation upon 1 replacement of aromatic residue Phe with aliphatic lie at position...

Synthesis Biological Evaluation NMR Solution Structural Models of New Oxytocin Analogues

Structure For Nmr Spectra 184 And 186

Raptis2, G. A. Spyroulias1, V. Magafa1, J. Slaninova3 and P. Cordopatis department of Pharmacy, University ofPatras, GR-265 04 Patras, Greece 2Technological Education Institute, Egaleo, GR-12210 Athens, Greece 3Department of Peptide Biochemistry, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of Czech Republic, Flemingovo square 2, Prague 6, CZ-166-10, We report the solid-phase synthesis of four oxytocin analogues in which the residues...

Monitoring Gene Delivery

Neal Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, U.K. The rational design and practical preparation of unsymmetrical polyamine carbamates and amides, based on steroid templates of cholesterol and the bile acid lithocholic acid as the lipid moiety, provides fluorescent molecular probes that condense DNA. These novel lipopolyamine conjugates mimic the positive charge distribution found in the triamine spermidine and the tetra-amine...