פרופ' ג'ררדו ביק

פרופ'
פרופסור חבר
פרופ' ג'ררדו ביק
טלפון: 
פקס: 
דוא"ל: 
משרד: 
מנחה את תלמידי המחקר: 

קורות חיים

Curriculum vitae

Academic Background

 

 

From-To

Institution

Area of specialization

Degree

1986-1990

The Hebrew University of Jerusalem

Medicinal Chemistry

Ph. D.

1984-1986

The Hebrew University of Jerusalem

Organic Chemistry

M. Sc.

1980-1983

The Hebrew University of Jerusalem

Chemistry

B. Sc.

 

 

previous Employment

 

 

From-To

Institution

Research area

Title

October 2002-present

Bar Ilan University

Nanobiotechnology

Associate Professor

September 1998-2002

Bar Ilan University

Peptidomimetics and Genetic Chemistry

Senior Lecturer

1996-1998

Rhone Poulenc Rorer (France-Paris)

Genetic Chemistry

Associate Research Fellow

1994-1996

Rhone Poulenc Rorer (France-Paris)

Genetic Chemistry

Senior  Research Scientist

1992-1994

Rhone Poulenc Rorer

Peptidomimetics

Research Scientist

1991-1992

InstitutPasteur

Lyon France

Peptidomimetics

Post –Doc.

 

פירסומים

  1. Maldiney, T., Byk, G., Wattier, N., Seguin, J., Khandadash, R., Bessodes, M., Richard, C., Scherman, D.: Synthesis and functionalization of persistent luminescence nanoparticles with small molecules and evaluation of their targeting ability. Int. J. Pharmaceutics, (2012), 423, 102-107.
  2. Khandadash, R., Partouche, S., Weiss, A., Margel, S. and Byk, G. A Fully Synthetic Phage- Like System II: Synthesis and Live Cell Screening of Combinatorial Libraries of Peptides on Sub-Cellular Sized Microspheres. The Open Optics Journal, (2011) 5, 17-27.
  3. Byk G.; Machtey V.; Khandadash R.: A Novel Dimension for Merrifield Synthesis: NPPS, Nano-Particle-Peptide-Synthesis BIOPOLYMERS (2011), 96, 449-450.
  4. Khandadash R.; Machtey V.; Weiss A. and Byk, G.: A Nanometric Platform for Synthesis and Biological Evaluation of Peptides BIOPOLYMERS (2011) 96, 451-452.
  5. Machtey, V., Gottlieb, H. and Byk, G. Total synthesis of structures proposed for quinocitrinines A and B and their analogs. Microwave energy as efficient tool for generating heterocycles. ARKIVOC, 2011, IX, 308-324.
  6. Byk, G., Partouche, S., Weiss, A. Margel, S. and Khandadash, R.: Fully Synthetic Phage-Like System for Screening Mixtures of Small Molecules in Live Cell. J. Comb. Chem. 2010, 12 (3),  332–345.
  7. Mirkin F, Eini H, Douvdevani A, Byk G.: New degradable cationic peptides for modulated gene delivery. Adv Exp Med Biol. (2009) 611:245-6. Peptides for Youth, Emmanuel Escher, William D. Lubell, Susan Del Valle Edt. PEPTIDES FOR YOUTH V611,  245-246 (2009) 
  8. Kun H, Byk G, Mastai Y. Effects of antifreeze protein fragments on the properties of model membranes. Adv Exp Med Biol. (2009) 611:85-6.
  9. Byk, G; Mozes, T: Tetramic acid peptide derivatives as cytotoxyc compounds. Biopolymers (2009) 9(4), 339-339.
  10. Khandadash, R., Partouche, S., Margel, S. and Byk, G.: Towards a fully synthetic “phage-display like” system for high-throughput screening. J.  Pept.  Sci.  (2008) 14( 8), 139.  
  11. Davidov G, Mozes T, Khandadash R, Diestel R, Sasse  F,  Byk G: Versatile methods for synthesizing acyl-tetramic acids peptide analogs . J.  Pept.  Sci (2008) 14( 8), 59 .
  12. Gerardo Byk, Mirit Cohen-Ohana and Daniel Reichman. Fast and Versatile Microwave-Assisted Intramolecular Heck Reaction in Peptide Macrocyclization Using Microwave Energy. Biopolymers 2006, 81, 274-282.
  13. Gerardo Byk and Eihab Kabha. A Solid-Supported Stereoselective Multicomponenent Reaction: One-Pot Generation of Three Asymmetric carbons. SYNLETT, 2006, 5, 747-749.
  14. Gerardo Byk, David Visnovezky and Daniel Raichman. Fast and Versatile Backbone Modifications and Peptide Macrocyclization Using Microwave Energy. Biopolymers Pept. Sci. 2005, 80, 531.
  15. Gerardo Byk, Tamar Tennenbaum, Shlomo Margel and Shirly Partush.  Towards in vivo screening of small molecules: Micron sized monodispersed polystyrene for synthesis, tagging and biological screening of small molecules. Biopolymers Pept. Sci. 2005, 80, 597-598.
  16. Julia Mazar, Boris Rogachev, Gad Shaked, Nadav Y. Ziv, David Czeiger,Cidio Chaimovitz, Moshe Zlotnik, Igor Mukmenev,Gerardo Byk and Amos Douvdevani. Involvement of Adenosine in the Anti-inflammatory Action of Ketamine. Anesthesiology (2005)102(6), 1174-1181.
  17. Gerardo Byk and Eihab Kabha. Anomalous regiselective MCR4 Biginelli reaction II: One pot parallel synthesis of spiro heterobicyclic aliphatic rings. Journal of Combinatorial Chemistry (2004), 6(4), 596-603.
  18. Alexander Aizikovich, Vladimir Kuznetsov, Sofia Gorohovsky, Amalia Levy, Simha Meir, Gerardo Byk and Garry GellermanA new application of diphenylphosphorylazide (DPPA) reagent: convenient transformations of quinolin-4-one, pyridin-4-one and quinazolin-4-one derivatives into 4-azido and 4-amino counterparts. Tetrahedron Lett.,(2004) 45, 4241-4243
  19. Vladimir Kuznetsov, Sofia Gorohovsky, Amalia Levy, Simcha Meir, Vladimir Shkoulev, Naim Menashe, Moshe Greenwald,  Alexander Aizikovich, Dror Ofer, Gerardo Byk and Garry Gellerman. Approaches for introducing high molecular diversity in scaffolds: Fast Parallel Synthesis of Highly Substituted 1H-quinolin-4-one Libraries. Molecular Diversity, (2004),  8(4),  437-448.
  20. Gerardo Byk and Eihab Kabha: Regioselective MCR4 reaction: One pot synthesis of spiro heterobicyclic aliphatic rings generated from natural amino acids. Biopolymers, 71(3), 235 (2003)
  21. Gerardo Byk, Elisha Haas, Varda Itah and Inbar Rofman. A versatile method for fast and selective introduction of multiple probes into peptides using solid phase synthesis. Applications to biophysical models. Biopolymers 71(3), 470 (2003).
  22. Tom Einbinder, Yuval Sufaro, Igor Yusim, Gerardo Byk, Jutta Passlick-Deetjen, Cidio Chaimovitz and Amos Douvdevani: Correction of anemia in uremic mice by genetically modified peritoneal mesothelial cells. Kidney International, Vol. 63 (2003), 2103-2112     
  23. Sofia Gorohovsky, Simha Meir, Vladimir Shkoulev, Gerardo Byk and Garry Gellerman: A Facile Two-step Synthesis of Novel ring-A double substituted Tryptophan Building Blocks for Combinatorial Chemistry. SYNLETT 10, 1411-1414 (2003)                              
  24. Francoise Leclercq , Mirit Cohen-Ohana, Nathalie Mignet , Andrea Sbarbati,Jean  Herscovici, Daniel Scherman and Gerardo Byk : Design, Synthesis and Evaluation of Gadolinium Cationic Lipids As Tools for Biodistribution Studies of Gene Delivery Complexes. Bioconjugate Chem. 14, 112-119 (2003).   
  25. Nathalie Mignet, Gerardo Byk, Barbara Wetzer and Daniel Scherman. DNA complexes with reducible cationic lipid for gene transfer.  Methods in Enzymology  373, 357-69, (2003)
  26. Gerardo Byk: Cationic Lipid Based Gene Delivery, in : Pharmaceutical Perspectives of Nucleic Acid Based Therapy. Edited by Ram I. Mahato and Sung Wan Kim Part 3(15), pg 302-333 (2002).    
  27. Carriere, Marie; Tranchant, Isabelle; Niore, Pierre-Antoine; Byk, Gerardo; Mignet, Nathalie; Escriou, Virginie; Scherman, Daniel; Herscovici, Jean. Optimization of cationic lipid mediated gene transfer: structure-function, physico-chemical, and cellular studies. Journal of Liposome Research 12(1 & 2),  95-106, (2002) 
  28. Marks, Vered; Gottlieb, Hugo E.; Melman, Artem; Byk, Gerardo; Cohen, Shmuel; Biali, Silvio E. Journal of Organic Chemistry, (2001)  66(20),  6711-6718: Polyethylated Aromatic Rings: Conformation and Rotational Barriers of 1,2,3,4,5,6,7,8-Octaethylanthracene, 1,2,3,4,6,7,8-Heptaethylfluorene, and 1,2,3,4,5,6,7,8-Octaethylfluorene.    
  29. Wetzer, Barbara; Byk, Gerardo; Frederic, Marc; Airiau, Marc; Blanche, Francis; Pitard, Bruno; Scherman, Daniel. Reducible cationic lipids for gene transfer. Biochem. J. (2001),  356(3),  747-756.
  30. Raspaud, Eric; Pitard, Bruno; Durand, Dominique; Aguerre-Chariol, Olivier; Pelta, Juan; Byk, Gerardo; Scherman, Daniel; Livolant, Francoise.    Polymorphism of DNA/Multi-cationic Lipid Complexes Driven by Temperature and Salts. J. Phys. Chem. B (2001), 105(22), 5291-5297.                                
  31. Byk, Gerardo; Gottlieb, Hugo E.; Herscovici, Jean; Mirkin, Fiana.  New Regioselective Multicomponent Reaction: One Pot Synthesis of Spiro Heterobicyclic Aliphatic Rings J. Comb. Chem.  (2000), 2(6),  732-735.                                                
  32. Byk, Gerardo; Wetzer, Barbara; Frederic, Marc; Dubertret, Catherine; Pitard, Bruno; Jaslin, Gabrielle; Scherman, Daniel. Reduction-Sensitive Lipopolyamines as a Novel Nonviral Gene Delivery System for Modulated Release of DNA with Improved Transgene Expression. J. Med. Chem. (2000), 43(23), 4377-4387.              
  33. Byk, Gerardo; Scherman, Daniel.  Genetic chemistry: tools for gene therapy coming from unexpected directions.  Drug Dev. Res.  (2000), 50(3/4), 566-572.                     
  34. Soto, Javier; Bessodes, Michel; Pitard, Bruno; Mailhe, Philippe; Scherman, Daniel; Byk, Gerardo. Non-electrostatic complexes with DNA: Towards novel synthetic gene delivery systems. Bioorg. Med. Chem. Lett.  (2000), 10(9), 911-914.                        
  35. Frederic, Marc; Scherman, Daniel; Byk, Gerardo. Introduction of cyclic guanidines into cationic lipids for non-viral gene delivery. Tetrahedron Lett. (2000), 41(5), 675-679.
  36. Neves, Carole; Byk, Gerardo; Escriou, Virginie; Bussone, Florence; Scherman, Daniel; Wils, Pierre.  Novel Method for Covalent Fluorescent Labeling of Plasmid DNA That Maintains Structural Integrity of the Plasmid. Bioconjugate Chem. (2000), 11(1), 51-55. 
  37. Neves, C.; Escriou, V.; Byk, G.; Scherman, D.; Wils, P. Intracellular fate and nuclear targeting of plasmid DNA. Cell Biol. Toxicol. (1999), 15(3), 193-202.                 
  38. Neves, Carole; Byk, Gerardo; Scherman, Daniel; Wils, Pierre. Coupling of a targeting peptide to plasmid DNA by covalent triple helix formation. FEBS Lett.  (1999), 453(1, 2), 41-45.                  
  39. Schwartz, B.; Ivanov, M-A.; Pitard, B.; Escriou, V.; Rangara, R.; Byk, G.; Wils, P.; Crouzet, J.; Scherman, D. Synthetic DNA-compacting peptides derived from human sequence enhance cationic lipid-mediated gene transfer in vitro and in vivo. Gene Ther.  (1999), 6(2),  282-292.                             
  40. Ciolina, Carole; Byk, Gerardo; Blanche, Francis; Thuillier, Vincent; Scherman, Daniel; Wils, Pierre.    Coupling of Nuclear Localization Signals to Plasmid DNA and Specific Interaction of the Conjugates with Importin. Bioconjugate Chem.  (1999),  10(1),  49-55.
  41. Byk, Gerardo; Scherman, Daniel. Novel cationic lipids for gene delivery and gene therapy.  Expert Opin. Ther. Pat.  (1998),  8(9),  1125-1141.
  42. Byk, Gerardo; Soto, Javier; Mattler, Christophe; Frederic, Marc; Scherman, Daniel.  Novel non-viral vectors for gene delivery: synthesis of a second-generation library of mono-functionalized poly-(guanidinium)amines and their introduction into cationic lipids.  Biotechnol. Bioeng.  (1998), 61(2),  81-87.
  43. Byk, Gerardo; Dubertret, Catherine; Escriou, Virginie; Frederic, Marc; Jaslin, Gabrielle; Rangara, Ravi; Pitard, Bruno; Crouzet, Joel; Wils, Pierre; Schwartz, Bertrand; Scherman, Daniel.    Synthesis, Activity, and Structure-Activity Relationship Studies of Novel Cationic Lipids for DNA Transfer. J. Med. Chem.  (1998), 41(2),  224-235.                                 
  44. Escriou, Virginie; Ciolina, Carole; Lacroix, Florence; Byk, Gerardo; Scherman, Daniel; Wils, Pierre.    Cationic lipid-mediated gene transfer: effect of serum on cellular uptake and intracellular fate of lipopolyamine/DNA complexes Biochim. Biophys. Acta (1998), 1368(2), 276-288.
  45. Byk, Gerardo; Dubertret, Catherine; Schwartz, Bertrand; Frederic, Marc; Jaslin, Gabrielle; Rangara, Ravi; Scherman, Daniel.    Novel nonviral vectors for gene delivery: synthesis and applications.  Lett. Pept. Sci.  (1997), 4(4/5/6),  263-267.
  46. Pitard, Bruno; Aguerre, Olivier; Airiau, marc; Lachages, Anne-Marie; Boukhnikachvili, Tsiala; Byk, Gerardo; Dubertret, Catherine; Herviou, Christian; Scherman, Daniel; Mayaux, Jean-Francois; Crouzet, Joel. Virus-sized self-assembling lamellar complexes between plasmid DNA and cationic micelles promote gene transfer. Proc. Natl. Acad. Sci. U. S. A.  (1997),  94(26),  14412-14417.
  47. Byk, Gerardo; Frederic, Marc; Scherman, Daniel. One pot synthesis of unsymmetrically functionalized polyamines by a solid phase strategy starting from their symmetrical polyamine-counterparts. Tetrahedron Lett.  (1997),  38(18),  3219-3222.
  48. Byk, Gerardo; Lelievre, Yves; Duchesne, Marc; Clerc, Francois F.; Scherman, Daniel; Guitton, Jean Dominique.    Synthesis and conformational analysis of peptide inhibitors of farnesyltransferase.    Bioorg. Med. Chem.  (1997), 5(1),  115-124.
  49. Byk, Gerardo and Scherman Daniel: Synthesis of novel (N-farnesyl)amino acids and their incorporation into peptides. Int. J. Peptide Protein Res. (1996), 47, 333-339.
  50. Bitan, Gal; Zeltser, Irena; Byk, Gerardo; Halle, David; Mashriki, Yaffa; Gluhov, Evgenia V.; Sukhotinsky, Inna; Hanani, Menachem; Selinger, Zvi; Gilon, Chaim.  Backbone cyclization of the C-terminal part of substance P. Part 1: The important role of the sulfur in position 11.  J. Pept. Sci.  (1996),  2(4),  261-269.
  51. Byk, Gerardo; Halle, David; Zeltser, Irena; Bitan, Gal; Selinger, Zvi; Gilon, Chaim.    Synthesis and Biological Activity of NK-1 Selective, N-Backbone Cyclic Analogs of the C-Terminal Hexapeptide of Substance P.  J. Med. Chem.  (1996),  39(16),  3174-3178.
  52. Byk, Gerardo; Duchesne, Marc; Parker, Fabienne; Lelievre, Yves; Guitton, Jean D.; Clerc, Francois F.; Becquart, Jerome; Tocque, Bruno; Scherman, Daniel; et al.    Local constrained shifty pseudopeptides inhibitors of ras-farnesyl transferase. Bioorg. Med. Chem. Lett.  (1995),  5(22),  2677-82.
  53. Grdadolnik, Simona Golic; Mierke, Dale F.; Byk, Gerardo; Zeltser, Irena; Gilon, Chaim; Kessler, Horst. Comparison of the Conformation of Active and Nonactive Backbone Cyclic Analogs of Substance P as a Tool To Elucidate Features of the Bioactive Conformation: NMR and Molecular Dynamics in DMSO and Water.  J. Med. Chem.  (1994),  37(14),  2145-52.
  54. Byk, Gerardo and McGregor, John L. Role of Type I Motif CSVTCG in the Thronbispondin Interaction with other Adhesive Proteins: Effect on Platelet Aggregation. Thrombosis-Haemostasis (1993) 69, 1009.
  55. Byk, Gerardo; Gilon, Chaim. Building units for N-backbone cyclic peptides.  1.  Synthesis of protected N-(-aminoalkylene)amino acids and their incorporation into dipeptide units.  J. Org. Chem.  (1992),  57(21),  5687-92.
  56. Saulitis, Juris; Mierke, Dale F.; Byk, Gerardo; Gilon, Chaim; Kessler, Horst. Conformation of cyclic analogs of substance P:  NMR and molecular dynamics in dimethyl sulfoxide. J. Am. Chem. Soc.  (1992),  114(12),  4818-27.
  57. Gilon, Chaim; Halle, David; Chorev, Michael; Selinger, Zvi; Byk, Gerardo.    Backbone cyclization:  a new method for conferring conformational constraint on peptides.  Biopolymers  (1991),  31(6),  745-50.
  58. Byk, , Gerardo and Kabha, Eihab,  Regioselective MCR4 reaction: One Pot Synthesis of Spiro Hetetrobicyclic Aliphatic Rings generated from Natural Amino Acids: in Peptide Revolution:Genomics,Proteomics &Therapeutics Michael Chorev &Tomi K.Sawyer (Editors) American Peptide Society (2003) pg 104-105.
  59. Byk, Gerardo; Haas, Elisha; Ittah, Vardah and Rofman Inbar: A Versatile Method for Fast and Selective Introduction of Multiple Probes into Peptides Using Solid Phase Synthesis-Application to Biophysical Models.  In Peptide Revolution: Genomics,Proteomics &Therapeutics Michael Chorev &Tomi K.Sawyer (Editors) American Peptide Society (2003) pg 91-92.
  60. Byk, Gerardo; Engel, Dikla; Ittah, Vardah; Haas, Elisha: Peptide models for studying autonomous folding of subdomain sections of protein molecules.  In Peptides: The Wave of the Future, Proceedings of the Second International and the Seventeenth American Peptide Symposium, San Diego, CA, United States, June 9-14, 2001  (2001),  398-399
  61. Byk, Gerardo; Dubertret, Catherine; Schwartz, Bertrand; Frederic, Marc; Jaslin, Gabrielle; Scherman, Daniel.  Synthesis, characterization and use of novel nonviral vectors for gene delivery.  Editor(s): Tam, James P.; Kaumaya, Pravin T. P.    Pept. Proc. Am. Pept. Symp., 15th  (1999),  Meeting Date 1997,     823-824.  Publisher: Kluwer,  Dordrecht, Netherlands.
  62. Byk, Gerardo; Frederic, Marc; Scherman, Daniel.    Unsymmetrically functionalized polyamine libraries by a solid phase strategy starting from their symmetrical polyamine-counterparts.  Editor(s): Tam, James P.; Kaumaya, Pravin T. P.    Pept. Proc. Am. Pept. Symp., 15th  (1999),  Meeting Date 1997,     47-48.  Publisher: Kluwer,  Dordrecht, Netherlands
  63. Bitan, G.; Byk, G.; Mashriki, Y.; Hanani, M.; Halle, D.; Selinger, Z.; Gilon, C.    Structure-activity relationship studies of new backbone-cyclic substance  P  analogs. Editor(s): Kaumaya, Pravin T. P.; Hodges, Robert S.    Pept.:  Chem., Struct. Biol., Proc. Am. Pept. Symp., 14th  (1996),  Meeting Date 1995,     697-698.  Publisher: Mayflower Scientific,  Kingswinford, UK
  64. Byk, G.; Burns, C.; Duchesne, M.; Parker, F.; Lelievre, Y.; Guitton, J. D.; Clerc, F. F.; Commercon, A.; Tocque, B.; et al.    Constrained pseudopeptides as inhibitors of Ras-farnesyl transferase: Structure-activity relationship studies.  Editor(s): Kaumaya, Pravin T. P.; Hodges, Robert S.    Pept.:  Chem., Struct. Biol., Proc. Am. Pept. Symp., 14th  (1996),  Meeting Date 1995,     213-214.  Publisher: Mayflower Scientific,  Kingswinford, UK
  65. Byk, G.; Scherman, D. Synthesis of backbone-modified (N-farnesyl) amino acids and their incorporation into peptides.  Editor(s): Kaumaya, Pravin T. P.; Hodges, Robert S.    Pept.:  Chem., Struct. Biol., Proc. Am. Pept. Symp., 14th  (1996),  Meeting Date 1995,     107-108.  Publisher: Mayflower Scientific,  Kingswinford, UK
  66. Byk, Gerardo; McGregor, John L. Peptide analogs derived from the thrombospondin type I repeat (CSVTCG) inhibit platelet aggregation.  Editor(s): Schneider, Conrad H.; Eberle, Alex N.    Pept. 1992, Proc. Eur. Pept. Symp., 22nd  (1993),  Meeting Date 1992,     827-8.  Publisher: ESCOM,  Leiden, Neth
  67. Gilon, Chaim; Zeltser, Irena; Rashti-Bahar, Vered; Muller, Dan; Bitan, Gal; Halle, David; Bar-Akiva, Giora; Selinger, Zvi; Byk, Gerardo. Backbone cyclization as a tool for imposing conformational constraint on peptides.  Editor(s): Yanaihara, Noboru.    Pept. Chem. 1992, Proc. Jpn. Symp., 2nd  (1993),  Meeting Date 1992,     482-5.  Publisher: ESCOM,  Leiden, Neth
  68. Gilon, C.; Halle, D.; Chorev, M.; Selinger, Z.; Byk, G.. SAR studies of cycloseptide:  Effects of cyclization and charge at position 6.  Editor(s): Smith, John A.; Rivier, Jean E.    Pept.:  Chem. Biol., Proc. Am. Pept. Symp., 12th  (1992),  Meeting Date 1991,     476-7.  Publisher: ESCOM,  Leiden, Neth
  69. Gilon, Chaim; Halle, David; Chorev, Michael; Selinger, Zvi; Goldshmith, Rafi; Byk, Gerardo.    Backbone-to-end cyclic tachykinins:  a new approach to conformationally restricted peptides.  Editor(s): Giralt, Ernest; Andreu, David.    Pept. 1990, Proc. Eur. Pept. Symp., 21st  (1991),  Meeting Date 1990,     404-6.  Publisher: ESCOM Sci. Publ.,  Leiden, Neth
  70. Byk, Gerardo; Gur, Erez; Halle, David; Chorev, Michael; Selinger, Zvi; Gilon, Chaim.  A new route to prepare conformationally restricted cyclic peptides as demonstrated by a potent NK-1 selective substance P analog.  Editor(s): Rivier, Jean E.; Marshall, Garland R.    Pept.:  Chem., Struct. Biol., Proc. Am. Pept. Symp., 11th  (1990),  Meeting Date 1989,     984-5.  Publisher: ESCOM Sci. Pub.,  Leiden, Neth

 

Patents

  1. Scherman, Daniel; Bessodes, Michel; Pitard, Bruno; Soto, Javier; Byk, Gerardo.  Oligobenzimidazole derivatives and their use as DNA transfection agents. (Aventis Pharma S.A., Fr.).    PCT Int. Appl.  (2001),     56 pp. Patent  written in French.    Application: WO  2000-2000FR3087  20001106.  Priority: FR  99-13934  19991105; US  2000-174648  20000105.  CAN 134:336672    AN 2001:338501
  2. Byk, Gerardo; Frederic, Marc; Hofland, Hans; Schermann, Daniel.  Amidine-containing lipopolyamines, their synthesis and use in transfection. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1999),     83 pp. Patent  written in French.    Application: WO  99-FR740  19990330.  Priority: FR  98-4121  19980402; US  98-85845  19980518.  CAN 131:267946    AN 1999:659366
  3. Byk, Gerardo; Dubertret, Catherine; Pitard, Bruno; Scherman, Daniel.  Transfecting compositions comprising DNA-binding, disulfide bond-containing compounds and their use in gene therapy. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1999),     51 pp.  CODEN: PIXXD2  WO  9938821  A2  19990805 . Patent  written in French.    Application: WO  99-FR162  19990128.  Priority: FR  98-1065  19980130; US  98-77026  19980306.  CAN 131:140459    AN 1999:495250
  4. Byk, Gerardo; Dubertret, Catherine; Scherman, Daniel.  Preparation of lipopolyamine-related compounds for transferring nucleic acids into cells. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1998),     80 pp. Patent  written  in French.    Application: WO  98-FR1041  19980525.  Priority: FR  97-6549  19970528.  CAN 130:38711    AN 1998:793121
  5. Byk, Gerardo; Scherman, Daniel; Schwartz, Bertrand; Dubertret, Catherine.  Lipopolyamines as transfection agents and pharmaceutical uses thereof. (Rhone-Poulenc Rorer S.A., Fr.; Byk, Gerardo; Scherman, Daniel; Schwartz, Bertrand; Dubertret, Catherine).    PCT Int. Appl.  (1997),     81 pp. Patent  written in French.    Application: WO  96-FR1774  19961108.  Priority: FR  95-13490  19951114.  CAN 127:46039    AN 1997:440187   
  6. Byk, Gerardo; Scherman, Daniel; Schwartz, Bertrand. Nucleic acid-containing compositions containing transfecting agents and nucleic acid condensing agents and their use in transfection. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1996),     53 pp.  CODEN: PIXXD2  WO  9625508  A1  19960822  Patent  written in French.    Application: WO  96-FR248  19960215.  Priority: FR  95-1865  19950217.  CAN 125:240223    AN 1996:609959
  7. Byk, Gerardo; Dubertret, Catherine; Scherman, Daniel.  Lipopolyamines as transfection agents and pharmaceutical uses thereof. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1996),     36 pp.  CODEN: PIXXD2  WO  9617823  A1  19960613  Patent  written in French.    Application: WO  95-FR1595  19951204.  Priority: FR  94-14596  19941205.  CAN 125:160332    AN 1996:506088
  8. Gilon, Chaim; Zelinger, Zvi; Byk, Gerardo.  Preparation of backbone cyclic peptides as drugs and pharmaceutical compositions containing them. (Hebrew University of Jerusalem, Israel).    Eur. Pat. Appl.  (1993),     48 pp.  CODEN: EPXXDW  EP  564739  A2  19931013  Patent  written in English.    Application: EP  92-309016  19921002.  Priority: IL  91-99628  19911020.  CAN 121:206022    AN 1994:606022

קורסים

כימיה של פפטידים וקומבינטורית

כימיה אורגנית מתקדמת

מעבדה בכימיה אורגנית א'

סמינר בכימיה ביו-אורגנית לתלמידי מחקר

קולוקיום מחלקתי

תחומי מחקר

ננוביוטכנולוגיה, טכנולוגיות סריקה קומבינטורית, העברת גנים על ידי נשאים לא וירלים. כימיה קומבינטורית. סינתזה טוטלית של חומרי טבע.

ראה פרטים באתר האישי: http://www.wix.com/gerardobyk/nanobiotechnology

 

נושאי המחקר במעבדה כוללים:

 

1. בנית פלטפורמה לטכנולוגיה סריקה רחבת ממדים בתאים או בחיות למציאת מולקולות בעלות זיקה חזקה לתאי סרטן. ליישום בתחום התרופות ודיאגנוסטיקה

 

2. סינתזה טוטלית של חומרי טבע, פיתוח מטודוליגיה סינתתית-אורגנית למטרה זאת

 

3. נשאים לא ויראלים להעברה וביטוי גנים לטיפול גנטי.

 

Nanobiotechnology, high-throughput technologies for life cell and in vivo screening of small molecules for tissue targeting, tumor targeting.

 

Non viral vectors for gene delivery and expression of foreign gens for gene therapy.

Organic synthesis of natural products. Development of organic methods.

For more details see personal web page: www.wix.com/gerardobyk/nanobiotechnology

 

1.Nanobiotechnology for drug discovery and diagnostics

2.Total synthesis of natural products

3. combinatorial chemistry and combinatorial screening technologies

4. Non viral gene delivery for gene therapy

 

Combinatorial Chemistry: Towards the chemistry of the 21st century

In the last twenty years, pharmaceutical companies have invested significant efforts in developing robotics and miniaturization for biological screening purposes. As a result of these efforts, the capacity of biologists to perform in vitro high-throughput screening of chemicals for drug discovery was dramatically improved. The main limitation of this new screening technology lies in the capacity of the chemists to furnish biologists with great diversity and number of products.

 

Traditionally, drug discovery involved the optimization of lead structures, most likely derived from biological sources, through a multi-step process of serial synthesis and screening. This approach is extremely costly, as each compound will have been individually handcrafted in solution by a synthetic chemist. The need to find more cost-effective methods of drug development, combined with the recent advances in robotic screening which enable the testing of hundreds of thousands of products per year, has led pharmaceutical companies to examine combinatorial synthetic strategies as a means of accelerating drug discovery programs, and increasing the chemical diversity of their compound libraries.

 

Chemists in academia are aware that novel synthetic tools must be developed in order to meet the increasing requirements of the high-throughput biological screening technology. For this purpose, the use of robotics in organic synthesis may significantly improve the diversity of synthetic libraries, and may allow the finding of new organic reactions. The emerging technology, the so-called ‘Combinatorial Chemistry’, is based on the simple premise that the greater the diversity of compounds tested, the better the chance of finding one that can be developed into a drug or other industrial lead. Although it is theoretically not limited to any specific family of chemical species, the scope of this approach is actually limited as a result of the restrained organic reactions available for synthesis on solid supports, and by the limited quantity of available multi-reagent organic reactions. A main goal of the laboratory of peptidomimetics and genetic chemistry will be to discover and develop new tools for extending the scope of combinatorial chemistry, and the application of these new tools to drug discovery.

http://pubs.acs.org/doi/abs/10.1021/cc900156z

The laboratory will focus on the design and delivery of biologically active molecules and complexes for drug research and clinical applications.

 

Some tasks of the laboratory:

Development of new technologies for automation and miniaturization of organic synthesis: Multicomponent and multistep organic synthesis on solid supports for high throughput synthesis.

http://pubs.acs.org/doi/abs/10.1021/cc900156z

http://pubs.acs.org/doi/abs/10.1021/cc000056p?source=chemport

https://www.thieme-connect.de/DOI/DOI?10.1055/s-2006-932498

http://pubs.acs.org/doi/abs/10.1021/cc049962i?source=chemport

 

Discovery of molecules with interesting biological activity using screening approaches such as combinatorial chemistry and multiple organic synthesis, and rational approaches starting from the natural substrates, especially from peptide sequences.

 

http://springer.metapress.com/content/x24u058q453q1034/

http://onlinelibrary.wiley.com/doi/10.1002/bip.20411/abstract;jsessionid=13FE5EBC1C5FB365F20B8D52A27E5BDC.d01t02

 

Definition of the bioactive conformation of biologically active analogs derived from synthetic molecules, or from natural compounds whose pharmacological characteristics are well known.

http://onlinelibrary.wiley.com/doi/10.1002/bip.20411/abstract;jsessionid=13FE5EBC1C5FB365F20B8D52A27E5BDC.d01t02

 

Development of integrated nanotechnology both for high-throughput organic synthesis and in vivo biological screening.

A new "phage display-like" synthetic system is generated using 2 mm cross-linked mono-dispersed microspheres bearing a panel of fluorescence tags and peptides that are directly synthesized on the microspheres or small molecules covalently conjugated to them. The new system allows screening mixtures of ligands bound to the microspheres using flow-cytometry analysis of the microspheres after incubation with a live cells model PC-3 cell-line in analogy to phage-display peptide method. The advantage of the proposed system is the possibility of screening non natural peptides, combinatorial libraries and small molecules that cannot be expressed and screened using phage display libraries. Two libraries are screened resulting in peptide DUP-1(1-12)2Ala and small molecule Rak-2 both individually synthesized and validated in an independent binding assay. Finally, the cellular fate of DUP-1(1-12)2Ala in PC-3 cell line is demonstrated using confocal laser scanning microscopy.

 

 

Figure 1. Design of a phage-like synthetic system and steps of the analysis technique. Background microscopy pictures in steps 2, 3 and 4 are real representations of the steps as seen by inverted microscopy.

 

http://pubs.acs.org/doi/abs/10.1021/cc900156z

http://www.benthamscience.com/open/tooptsj/articles/V005/SI0011TOOPTSJ/17TOOPTSJ.pdf

 

 

Fig. (1). Steps of live cell screening using a phage-like synthetic system.

 

 

Development of novel targeted imaging systems for diagnostics in collaboration with French scientists: http://sciencedirect.dogsoso.com/science/article/pii/S0378517311006260

 

 

2. Gene therapy

Synthetic DNA delivery agents are of crucial importance for gene therapy as an alternative to viral vectors, since they display potentially less risks in terms of immunogenicity and propagation.

 

A great deal of work is still needed for obtaining improved gene expression after non-viral gene delivery, especially regarding the in vivo final localization of the DNA complexes. Based on recently published results, the introduction of a targeting moiety into non-viral gene delivery systems promises improved gene expression in the targeted area as result of the accumulation of the complexes.

http://pubs.acs.org/doi/abs/10.1021/bc025567e?source=chemport

The laboratory aims to develop non-viral gene delivery systems specifically targeted to tumors. Specific tumor receptors are of particular interest. Thus, targeting ligands addressed to these receptors will allow a selective localization of the therapeutic gene or drug in the tumor area. Coupling of these ligands to complexes carrying suicide genes will promote the specific elimination of tumor cells, resulting in tumor reduction or elimination.

http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B7CV2-4B7GMMS-V&_user=856235&_coverDate=12%2F31%2F2003&_alid=1586318160&_rdoc=1&_fmt=high&_orig=search&_origin=search&_zone=rslt_list_item&_cdi=18066&_sort=r&_st=13&_docanchor=&view=c&_ct=1&_acct=C000046180&_version=1&_urlVersion=0&_userid=856235&md5=0a77dc501a5b66659317ebb56f4656d4&searchtype=a

 

3- Total synthesis of natural compounds with biological activities

Novel methodologies especially employing microwave energy are being developed in the laboratory for the synthesis of biological relevant natural compounds. The lab designs and develop synthetic methodologies for this aim and characterise the obtained molecules for final validation of the natural compounds structure.

http://www.arkat-usa.org/get-file/39666/

 

Particular research areas (projects):

1. Nano-biotechnology for drug discovery and diagnostics

2. Total synthesis of natural products

3. Combinatorial chemistry and combinatorial screening technologies

4. Non-viral gene delivery for gene therapy

 

OPEN POSITION

Bachelor or MSc students in chemistry, biophysics, biology, physics, biotechnology, biomedical engineering from any university or recognized college are asked to apply to Prof. Byk for MSc or PhD positions currently open.

 

פטנטים

  1. Scherman, Daniel; Bessodes, Michel; Pitard, Bruno; Soto, Javier; Byk, Gerardo.  Oligobenzimidazole derivatives and their use as DNA transfection agents. (Aventis Pharma S.A., Fr.).    PCT Int. Appl.  (2001),     56 pp. Patent  written in French.    Application: WO  2000-2000FR3087  20001106.  Priority: FR  99-13934  19991105; US  2000-174648  20000105.  CAN 134:336672    AN 2001:338501
  2. Byk, Gerardo; Frederic, Marc; Hofland, Hans; Schermann, Daniel.  Amidine-containing lipopolyamines, their synthesis and use in transfection. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1999),     83 pp. Patent  written in French.    Application: WO  99-FR740  19990330.  Priority: FR  98-4121  19980402; US  98-85845  19980518.  CAN 131:267946    AN 1999:659366
  3. Byk, Gerardo; Dubertret, Catherine; Pitard, Bruno; Scherman, Daniel.  Transfecting compositions comprising DNA-binding, disulfide bond-containing compounds and their use in gene therapy. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1999),     51 pp.  CODEN: PIXXD2  WO  9938821  A2  19990805 . Patent  written in French.    Application: WO  99-FR162  19990128.  Priority: FR  98-1065  19980130; US  98-77026  19980306.  CAN 131:140459    AN 1999:495250
  4. Byk, Gerardo; Dubertret, Catherine; Scherman, Daniel.  Preparation of lipopolyamine-related compounds for transferring nucleic acids into cells. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1998),     80 pp. Patent  written  in French.    Application: WO  98-FR1041  19980525.  Priority: FR  97-6549  19970528.  CAN 130:38711    AN 1998:793121
  5. Byk, Gerardo; Scherman, Daniel; Schwartz, Bertrand; Dubertret, Catherine.  Lipopolyamines as transfection agents and pharmaceutical uses thereof. (Rhone-Poulenc Rorer S.A., Fr.; Byk, Gerardo; Scherman, Daniel; Schwartz, Bertrand; Dubertret, Catherine).    PCT Int. Appl.  (1997),     81 pp. Patent  written in French.    Application: WO  96-FR1774  19961108.  Priority: FR  95-13490  19951114.  CAN 127:46039    AN 1997:440187   
  6. Byk, Gerardo; Scherman, Daniel; Schwartz, Bertrand. Nucleic acid-containing compositions containing transfecting agents and nucleic acid condensing agents and their use in transfection. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1996),     53 pp.  CODEN: PIXXD2  WO  9625508  A1  19960822  Patent  written in French.    Application: WO  96-FR248  19960215.  Priority: FR  95-1865  19950217.  CAN 125:240223    AN 1996:609959
  7. Byk, Gerardo; Dubertret, Catherine; Scherman, Daniel.  Lipopolyamines as transfection agents and pharmaceutical uses thereof. (Rhone-Poulenc Rorer S.A., Fr.).    PCT Int. Appl.  (1996),     36 pp.  CODEN: PIXXD2  WO  9617823  A1  19960613  Patent  written in French.    Application: WO  95-FR1595  19951204.  Priority: FR  94-14596  19941205.  CAN 125:160332    AN 1996:506088
  8. Gilon, Chaim; Zelinger, Zvi; Byk, Gerardo.  Preparation of backbone cyclic peptides as drugs and pharmaceutical compositions containing them. (Hebrew University of Jerusalem, Israel).    Eur. Pat. Appl.  (1993),     48 pp.  CODEN: EPXXDW  EP  564739  A2  19931013  Patent  written in English.    Application: EP  92-309016  19921002.  Priority: IL  91-99628  19911020.  CAN 121:206022    AN 1994:606022

קבוצת מחקר

רז חאנדדש, דוקטורנט

 

ויקטוריה מכטיי, דוקטורנטית

 

 

ולדימיר גוברי, מסטרנט

 

 

ליליה פרבר, קדם מסטרנטית.