Sep 302013

Over the recent years, drug discovery via high throughput screening (HTS) has moved beyond the boundaries of pharmaceutical companies and been successfully integrated into research programs of many academic institutes. These efforts have taken advantage of the availability of diverse libraries of small molecules, either as pure entities or natural product extracts. However, identification of candidate drugs benefits from an in-depth understanding of potential pitfalls of HTS, which can include (i), storage of compound libraries (ii), stability and cost of assay reagents (iii), robustness of the assay and (iv), access to bioinformatics to analyze the wealth of data that results from performing multiple assays on 250,000 – 500,000 compounds. Beyond these challenges, successful HTS is an iterative process requiring close co-operation with programs of structural biology, medicinal chemistry and clinical research.

With these issues in mind, the Innovative Approaches for Identification of Antiviral Agents Summer School (IAAASS) aims to provide an informal and interactive environment to review the application of HTS techniques to identification of novel and clinically-significant antiviral drugs. The Summer School is targeted to researchers at an early stage in their career, combining examples of drug discovery from internationally-recognized experts in the field with informal, small-group thematic discussion sessions. Evening sessions will allow students to present their work in the form of either a poster or oral presentations and receive feedback from their colleagues. The Organizing Committee welcomes you to the Hotel Flamingo, Santa Margherita di Pula, located on the south tip of Sardinia, and looks forward to sharing with you their experience on current and future strategies for identifying novel antiviral agents targeted to clinically-significant diseases.


The Organizing Committee would like to thank the following:
Regione Autonoma Sardegna, for their generous financial support for the meeting;

Università di Cagliari, for logistical support;

Gemma Marcias and Luca Zinzula for website preparation.

The meeting is being held in partnership with:
European Society for Virology (ESV)
Società Italiana di Virologia (SIV)
Società Italiana di Microbiologia Generale e Biotecnologie Microbiche (SIMGBM)
Università di Cagliari, PhD program in “Human and Environmental Biology and Biochemistry”

IAAASS 2012 Participants

 IAAASS 2012 Participants  Comments Off on IAAASS 2012 Participants
Sep 262013
Sep 262013

Stefano Alcaro (*1966) obtained his doctoral degree in Pharmacology, Pharmacognosy and Toxicology at the Università La Sapienza di Roma. After his PhD he continued with a postdoctoral fellowship in the laboratory of Computional Chemistry of the Department of Chemistry at the Columbia University, New York (Prof. W. Clark Still team). On 1996 he has got his first permanent position as Medicinal Chemistry researcher at the Faculty of Pharmacy at the Università Magna Græcia of Catanzaro. From 2002 to 2011 he was Associate Professor in the same scientific sector (CHIM/08) at the University of Catanzaro. From 2011 he is Full Professor in the same academic institution. His main teaching course at the Università Magna Græcia of Catanzaro is Medicinal Chemistry and Toxicology I.
Stefano Alcaro is co-author of about 100 original publications on peer reviewed international journals, 4 books chapters, 2 international diffused volumes and over 100 national and international communications. His research interests are related to drug design and hit identification of bioactive compounds by means of computational methods especially in the fields of anticancer and antiviral therapies.

Daniel Appella was graduated from the University of Wisconsin-Madison, 1998, with Ph.D. in Organic Chemistry. He continued with a postdoc at MIT, also working in the area of organic chemistry. He was an assistant professor at Northwestern University, in the Chemistry Department, from 2001 to 2004. In 2005 he moved to NIH as a tenure track PI, promoted to tenure at NIH in 2008. Currently, he is Chief of the Synthetic Bioactive Molecules Section, one of the labs in the Laboratory of Bioorganic Chemistry that is part of the National Institute of Diabetes and Digestion and Kidney Diseases (NIDDK). Appella’s laboratory research uses synthetic organic chemistry to create new molecules with unique biological activity with the potential to evolve into a new strategy for diagnosing or treating a disease. Within their research, most of the time goes for the molecules synthesis, and the use of a large amount of molecular modeling and biophysical techniques to study the molecules they make. Different projects of the Appella’s group are: A) exploration of the incorporation of carbocyclic rings and sidechains into the backbone of several different peptide nucleic acids (PNAs) in order to provide the basis for design of PNA-based sensors and to develop new diagnostic techniques based on our modified PNAs; B) examination of sidechain-bearing polyamines as molecular scaffolds for the display of RNA binding groups, in order to develop syntheses of these polyamines, making combinatorial libraries of these molecules, and studying their binding properties to two important RNA targets (TAR RNA and RRE RNA of HIV); C) inspired by a recent identification of a few novel molecules that reactivate mutant p53 to bind its DNA target, the 3rd research topic is to design a new class of molecules that reactivate mutant p53 in order to probe the unique mechanism that allows small organic molecules to restore normal activity to a mutant protein.

Jonas Blomberg (*1944) is a professor emeritus of Clinical Virology at Uppsala University. MD 1974 at the School of Medicine at Göteborg University and PhD 1977 at Medical Biochemistry, GU. He was then a post-doc 1979-1981 at the National Cancer Institute under Dr John Stephenson, on Retroviruses. He became assistant Professor 1981 (Virology) in Lund, and professor (Clinical Virology, chair), at the Medical Faculty of Uppsala University 1996. He is a professor emeritus there since 2011. He is since 1979 a board certified clinical virology specialist, heading diagnostic virology labs at Lund and Uppsala. I was the main supervisor of 14 PhD students. He has published 190 papers in peer reviewed journals. The lines of investigation are 1. Diagnosis of microbial disease. Being a clinical virologist, this is a natural preoccupation. It is currently dominated by the development of broadly targeted multiplex techniques for detection of pathogen nucleic acid, and antibodies to pathogens. 2. Retroviruses. Human retroviruses, HTLV, HIV, XMRV and human endogenous retroviruses were studied. Much of the study is done with bioinformatics, where he collaborated with ass. prof. Göran Sperber in the creation of RetroTector, a bioinformatics tool for detecting and characterizing proviral sequences in genomic databases. The bioinformatics and the multiplex methods are useful for basic retroviral research and for diagnostic development. Currently, the disease myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS) is in my focus.

Maria José Camarasa obtained her PhD In Chemistry by the Universidad Complutense of Madrid. She was Head of the Chemotherapy Department of IQM-CSIC; Vice-Director of Medicinal Chemistry Institute (IQM-CSIC); President of the Spanish Society of Medicinal Chemistry (SEQT) (2004-2007); member of the executive board of the Chemistry Area of ANEP (2005-2008), coordinator of Medicinal Chemistry. She is actually Research Professor (Full professor) at the Medicinal Chemistry Institute of CSIC (IQM-CSIC), Madrid, Spain; co-coordinator of the Chemical Science and Technologies area of the CSIC; Head the of nucleosides and analogues group and Member of the executive board of International Society for Nucleosides, Nucleotides and Nucleic Acids (IS3Na). She was awarded in 2001 with the prestigious René Descartes-Prize of the European Commission.
Her research interests are the Medicinal Chemistry, drug-design and discovery, antivirals, anticancer, antiinfectives, pro-drugs, organic chemistry, carbohydrates, nucleosi(ti)des, peptides.

Mamuka Kvaratshelia Mamuka Kvaratskhelia obtained his Ph.D. degree in Biochemistry from the Russian Academy of Sciences, continued his career in the Biological Chemistry Department at the Unilever-John Innes Center (Norwich) and University of Dundee, United Kingdom and is currently working at the National Cancer Institute (NCI), Frederick, MD. He is actually Associate Professor at The Ohio State University, College of Pharmacy, Center for Retrovirus Research and Comprehensive Cancer Center, Columbus, OH. Research in the Kvaratskhelia laboratory focuses on elucidating the composition and architecture of key HIV replication complexes and exploiting the knowledge obtained for discovery of new anti-retroviral therapies. His research look with particular interest at the biochemistry of HIV integration, in order to define molecular interactions essential for HIV replication and uncover new structural targets for developing antiretroviral compounds; and the allosteric inhibitors of HIV integrase, to discover novel types of clinically useful agents that could complement current antiviral therapies. Particular interest is addressed to the proteomics approach to better understating the complex network of virus-host interactions required for HIV infection.

Thierry Langer (*1962) began his career at Leopold-Franzens-University of Innsbruck in 1992 after completing a post doctoral fellowship at the Université Louis Pasteur, Strasbourg, France with Prof. C.-G. Wermuth. Since that time, he established the Computer Aided Molecular Design Group, was appointed Associate Professor of Pharmaceutical Chemistry in 1997, and served as Head of the Institute of Pharmaceutical Chemistry and of the Pharmaceutical Chemistry Department in 1998 and 1999. His research interests range from medicinal chemistry, including theoretical pharmaceutical chemistry, drug design, and pharmacophore modeling as well as QSAR and 3DQSAR molecular modeling techniques. His scientific work, which has culminated in more than 160 original articles, book chapters, and invited reviews, together with more than 200 lectures and poster presentations at scientific meetings, led to the founding of the spin-off company Inte:Ligand GmbH, in which he also was CEO from 2003 to 2008. With April 2008, Prof. Langer has left University of Innsbruck to been appointed CEO of Prestwick Chemical Inc., Strasbourg-Illkirch, France. Prof. Langer holds an M.S. degree in Pharmacy and a Ph.D. in Medicinal Chemistry from the University of Vienna, Austria. He is fluent in English, French, and German.

Stephan Ludwig obtained in 1993 his PhD at the Institute of Virology of University of Giessen. After the Habilitation (2000) in Molecular Biology at the Julius-Maximilians-Universität Würzburg, he was research assistant at the Institute of Virology, University of Giessen (1993-1994). In 1995 he became group leader at the Institute for Medical Radiation and Cell Research (MSZ), University of Wuerzburg, from 2001 to 2002 he earned a senior research fellowship at the MSZ. Stephan Ludwig was University Professor at the Institute of Molecular Medicine (IMM), University of Duesseldorf (2002-2004). Since 2004 he is University Professor and Director at the Institute for Molecular Virology (IMV) at the Center for Molecular Biology of Inflammation (ZMBE), University of Muenster. He was Managing Director of ZMBE (2006-2008) and he is actually Vice-Rector for Research at the Westfälische Wilhelms-Universität. Within his affiliation we count: since 2007 the Scientific coordination of the service platform “Integrated Functional Genomics” (IFG), University of Muenster; since 2008 the coordination of the nationwide research network “FluResearchNet” (initiated and supported by the German Ministry for Education an Research – BMBF) and since 2009 the coordination of the “National Platform for Zoonoses Research” (initiated and supported by the BMBF).
Research at the Institute of Molecular Virology (headed by Prof. Dr. Stephan Ludwig) focusses on intracellular signal transduction pathways and their impact on viral infection and inflammation with a major interest for: influenza viruses, via gathering knowledge about the cellular processes which control virus replication; signalling pathways involved in inflammatory responses, with the molecular analysis of pro-inflammatory cytokine expression and signalling mechanisms during the acute-phase response and the analysis of signalling pathways during inflammatory activation of the endothelium.

Peter Matyus achieved his M.S. in Synthetic Organic Chemistry at in 1975; the M. Litt. (Doctor title) in 1980; and the Degree in Medicinal Chemistry at the Technical University Budapest 1981. He obtained his habilitation at the A. Szent-Györgyi Univ., Szeged on 1997; and the C.Sc., D.Sc. at the Hungarian Academy of Sciences. He pursuived with several Postdoctoral Fellowships of the A.v. Humboldt-Foundation (Inst. für Organische Chemie und Biochemie), University of Bonn (H. Wamhoff) (1982-1984, 1989, 1990); of the Ciba-Geigy Foundation for Promotion of Sciences Japan (Inst. for Chem. Res.), University of Kyoto (K. Tanaka) 1992-93; and the fellowship of the Australian Natl. University (John Curtin School of Medical Research) (G. Barlin) Canberra 1993 (1 month), and on 1994 (3 months). From 1997 he is the Head of the Department of Organic Chemistry at the Semmelweis University. Since 2008 he is the Director of the Drug Discovery and Safety Centre at the Semmelweis University. His memberships: 1999-2007 Chair of the Division of Organic and Medicinal Chemistry of the Hungarian Chemical Society (re-elected twice); 2007-2011 President of the Hungarian Chemical Society; 2002-2006 Member of the Council of Scientists, INTAS (EU, Brussels; re-elected); International Advisory Board of ChemMedChem. Associate Editor of Future Med. Chem; 2004-2010 Member of the Executive Committee, and Chair of Education and Training Committee of European Federation for Medicinal Chemistry (re-elected); Member of Medicinal Chemistry Subcommittee of IUPAC; Member of ACS; Founder and Board member of Paul Ehrlich MedChem Euro-PhD Network. He also won several awards such as: Zemplén-Prize, Hungarian Academy of Sciences 1989; ‘Nívó’-Prize, Hungarian Chemical Society, 1996. Genius Prize, Committee of the Hungarian Inventors, (twice) 1996, 1998; Jedlik Ányos Prize, Hungarian Patent Office, 2002; Kazay Prize, Hungarian Pharmaceutical Society, 2004; Than Károly Prize, Hungarian Chemical Society, 2005; Náray-Szabó Gábor Prize, Hungarian Chemical Society, 2006; Bruckner Prize, Hungarian Academy of Sciences 2009; PhD-Educational Prize, Semmelweis University, 2011. His research interests are medicinal chemistry of cardiovascular and central nervous systems, molecular modelling and synthesis of biologically active compounds; synthetic and mechanistic chemistry of pyridazines and nitrogen containing heterocycles.

Thomas Mertens studied Chemistry in Bonn and Medicine in Cologne (1968-1976). He obtained the MD Thesis (Dr. med.) on 1976 and his Habilitation on 1984. Thomas Mertens was medical assistant, training in internal medicine and surgery (1976–1977); he continued with a research fellowship for the postdoctoral training in immunology, virology and diagnostics, Institute of Virology, University of Cologne (1977–1985). In 1983 he reached the Board Certification in Microbiology and Epidemiology of Infectious Diseases. In 1985 he became Professor (C2) at the Institute of Virology, University of Cologne, from 1991 to 1998 he was Professor (C3), in the Dept. of Virology, Ulm University. He was Temporary Director of the Dept. Medical Hygiene, Ulm University Hospital from 1991 to 1992; and Dean of Studies at the Medical Faculty, Ulm University from 2003 to 2006. Since 1998 he is the Director of the Institute of Virology at the Ulm University Hospital. His research focuses: mechanisms of resistance of antiviral substances towards herpes viruses; the analysis of the biological function of the viral gene UL97; new targets for antiviral interference against human cytomegalovirus (HCMV); molecular mechanisms and functional relevance of host-cell genes modulation by HCMV; viral tegument proteins and Morphogenesis of HCMV; new organ culture model for analysis of HCMV infection; the characterization and function of G-protein coupled receptor homologs of HCMV; and the Clinical Virology.

Ali Mirazimi received his Ph.D In infection Biology in 2000 from the Department of Microbiology, Tumour biology and Cell biology at Karolinska Institute. Short after, he received a junior lecturer position at Karolinska Institute. At 2002 he received a position as Molecular virologist at Swedish Institute for Infectious Disease control. At 2006 he achieved Associate professor position at Karolinska Institute. He has been the head of the BSL-4 Virology Unit at Centre for Microbiological Preparedness at Swedish Institute for Infectious disease control. Today, he is Coordinator for a large collaborative research program with focus on Crimean Congo hemorrhagic fever virus, which founded by European commission. He has also a position as strategically advisor for Swedish national Veterinary Institute. His group is interested to understand the molecular pathogenesis of emerging viruses. The major focus is the role of Innate Immunity for controlling the viral replication cycle. He is also interested to investigate the virus-host cell interaction and virus biology.

 Giorgio Palù received the Specialty diplomas in Oncology (1976) and General Pathology (1978), was appointed Postdoctoral Fellow and Research Associate at the Tumor Institute, Jules Bordet, Université Libre, Bruxelles (1975), the Chester Beatty Research Institute-Royal Marsden Hospital, Royal Cancer Institute, London University, UK (1976-79), the Depart. of Pharmacology, Yale University, New Haven, CT (1979-80), Assistant Professor in Microbiology, University of Parma (1980-82), Associate Professor in Virology, University of Padova, Medical School (1983-1989), Visiting Professor, Depart. of Molecular Biochemistry and Biophysics, Yale University, 1982,1984,1986; Division of Virology, National Institute for Medical Research, Mill Hill, London, UK, 1980,1985,1987; Division of Human Retrovirology, Dana Farber Cancer Institute, Harvard Medical School, Full Professor of Microbiology and Virology (since 1989), University of Padova Medical School. Director of the Institute of Microbiology, University of Padova, Medical School (1991-1999), of the Depart. of Histology, Microbiology and Medical Biotechnologies, University of Padova, Medical School (1999-2002); Head of the Unit of Clinical Microbiology and Virology, Padova University Hospital/Veneto Region (since 1996); Member of the Executive Committee of the Interdipartimental Centre for Innovative Biotechnologies, Padova University (since 1992); the Interuniversity Consortium of Nanotechnologies (since 2003); the Galilei Scientific Park (since 2001); the Padua start-up company incubator (since 2003); the Tissue-Tech Consortium (since 2004); the Biotechnological Association for Oncology Research (ABO, since 2003). Coordinator, PhD Course/School in Virology (since 1998) and in Biomedicine (since 2007); Member of the Board of the International PhD Programmes in Molecular Medicine, University of Ulm, Germany (since 2008), in Biomedicine and Translational Neurosciences, Temple University, Philadelphia, USA (since 2011); Pro-Rector, University of Padova (Foreign affairs and international research, 2002-2004); Dean, Faculty of Medicine and Surgery, University of Padova (2004-2011), Director of the Padova GMP Project (Cell-factory of the Veneto Region – Italy); Director of the Department of Molecular Medicine, University of Padova (since 2012). He is also Head of the Center of Biomedicine, Clinical Microbiology and Virology and GMP facility of the Padua University Hospital. He has a long-standing experience in the study of pathogenesis of viral infections and the design of viral and non-viral vectors for gene transfer, somatic gene therapy and vaccinology and for regenerative medicine. He has made relevant contributions in the study of antimicrobial therapy and resistance and anticancer therapy with more than 350 publications and 10 patents. His basic research has provided a platform for finding new targets for antiviral therapy and new antivirals based on peptides and small molecules able to disrupt the interface of protein-protein interactions essential for viral replication.

Sep 262013

Approaches for Identification of Antiviral
Agents Summer School (IAAASS)

September 30 – October 4, 2012
Santa Margherita di Pula, Sardinia

Provisional Program

Sunday, September 30th – Registration Day

13:00 pm Buffet lunch

Afternoon – Free

7.00 pm Welcoming Remarks

7.15 pm Development of new antiviral agents: from peptides to small molecules, Giorgio Palù, University of Padova, Italy

8.00 pm Informal Dinner

Monday, October 1st


Morning session

Plenary lectures

9.00 – 9.45 am A dynamic interplay between HIV-1 integrase subunits as a new therapeutic target, Mamuka Kvaratskhelia, The Ohio State University, Columbus, USA.

9.55 – 10.40 am Influenza viruses and host cell signaling – towards identification of novel targets for antiviral therapy, Stephan Ludwig, University of Muenster, Germany.

10.50 – 11.10 am Coffee break

11:15 – 12.00 pm  Multi-targeting with one single drug, Peter Matyus, Semmelweis University, Hungary

12.10 – 12:55 pm Therapy of Human Cytomegalovirus – actual situation, problems and future perspectives, Thomas Mertens, Universitätsklinikum Ulm, Germany

1:00 pm Lunch

Afternoon session

3.30 – 5:00 pm Thematic Group Discussions

5:00 – 6.00 pm Coffee break/ Poster Session 1

Short Talks

6.00 – 6.15 pm From a Protein Crystal to an Effective Hepatitis C Vaccine: The Hard Way of Structural Biology, Valeria Fadda, University of St Andrews, St Andrews (UK)

6.15 – 6.30 pm Structural and functional analysis of a dendrimer microbicide against HIV-1 env, Cath Latham, Burnet Institute, Australia

6.30 – 6.45 pm Study of the role of gp120 disulfide bridges and N-glycans in HIV capture and transmission, Leen Mathys, Rega Institute for Medical Research, Belgium

6.45 – 7.00 pm Synthesis and biological evaluation of new dual inhibitors of HIV-1 associated functions, Rita Meleddu, University of Cagliari,  Italy.

8:30 pm Sardinian Dinner

Tuesday, October 2nd


Morning session

9.00 – 9.45 am Can novel antiretroviral strategies be deduced from the study of host-retrovirus interplay recorded in vertebrate genomes? Jonas Blomberg,  Uppsala University, Sweden.

9.55 – 10.40 am Feature-based Pharmacophores for Rapid Compound Profiling, Thierry Langer, Prestwick Chemical SAS, Strasbourg-Illkirch, France

10.50 – 11.10 am Coffee break

11:15 – 12.00 pm HIV/AIDS: One virus (HIV-1) and two challenging targets (GP120 and RT dimerization). Strategies for the design and discovery of inhibitors, María José Camarasa, Instituto de Qímica Médica (IQM-CSIC), Madrid, Spain

12.10 – 12:55 pm A Small Molecule Platform to Inhibit HIV through the Nucleocapsid Protein, Daniel H. Appella, National Institutes of Health, Bethesda, MD, USA

1:00 pm Lunch

Afternoon session

3.30 – 5:00 pm Thematic Group Discussions

5:00 – 6.00 pm Coffee break/ Poster Session 2

Short Talks

6.00 – 6.15 pm The mechanism of action of new HIV-1 reverse transcriptase dual inhibitors explored by kinetic studies and site direct mutagenesis, Angela Corona, University of Cagliari, Italy

6.15 – 6.30 pm Optimization of an in vitro assay to quantify HIV-1 Reverse Transcriptase (RT) dimerization, Tania Matamoros, Centro de Biología Molecular “Severo Ochoa”, CSIC-UAM, Madrid, Spain

6.30 – 6.45 pm Formation of HCV replication complex on membranous web: An interplay between viral and cellular factors, Vikas Saxena, Academia Sinica, Taipei, Taiwan

6.45 – 7.00 pm Transmitted and secondary antiretroviral drug resistance among Ethiopian patients, Andargachew Mulu Meharie, University of Leipzig, Leipzig, Germany

8:30 pm Sardinian Dinner

Wednesday, October 3rd


Morning session

9.00 – 9.45 am G-quadruplex nucleic acid conformations: potentially selective targets against viral and cancer diseases, Stefano Alcaro, Università “Magna Græcia” di Catanzaro, Italy

9.55 – 10.40 am High Throughput Screening for Inhibitors of Human Immunodeficiency Virus Ribonuclease H Activity, Stuart F.J. Le Grice, NCI, Frederick, MD, USA

10.50 – 11.10 am Coffee break
11:15 – 12.00 pm Innate Immunity and RNA viruses, Ali Mirazimi, Karolinska Institute, Sweden
12.10 – 12:55 pm to be announced

1:00 pm Lunch

Afternoon session

3.30 – 5:00 pm Thematic Group Discussions

5:00 – 6.00 pm Coffee break/ Poster Session 2

Short Talks

6.00 – 6.15 pm Biochemical evidence supporting the association of HIV-1 reverse transcriptase polymorphism R284K and resistance mutations M41L, L210W and T215Y, Gilberto Betancor, Centro de Biología Molecular “Severo Ochoa” (CSIC-UAM), Madrid, Spain

6.15 – 6.30 pm Characterization of retroviral resistance mechanisms against azidothymidine, Anna Schneider, Department of Biopolymers, University of Bayreuth, Germany

6.30 – 6.45 pm The Ephrin Receptor Tyrosine Kinase A2 is a Cellular Receptor for Kaposi’s Sarcoma-Associated Herpesvirus, Saipraisad Salvi, Institut für Klinische und Molekulare Virologie, Erlangen, Germany

6.45 – 7.00 pm Ebola virus recombinant VP35 (rVP35) as a paradigm model for dsRNA binding-mediated suppression of the interferon-α/β innate immune response, Luca Zinzula, University of Cagliari, Italy

Final remarks

8:30 pm Gala Dinner

Thursday, October 4th- Breakfast and Departure

credits Università degli Studi di Cagliari
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