MedChem 2013
Constrained Peptides and Macrocycles – New Opportunities for Drug Discovery

Head of Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, The University of Queensland, Brisbane, Qld 4072, Australia Senior Principal Research Fellow, National Health and Medical Council of Australia Email: d.fairlie@imb.uq.edu.au Homepage: http://fairlie.imb.uq.edu.au/ Research Field: Chemistry, biochemistry, pharmacology (including protease/enzyme inhibitors, GPCR modulators, protein/peptide mimics, PPI modulators, drug design and discovery). Education: Undergraduate (University of Adelaide, South Australia); Postgraduate (Australian National University, Canberra, Australia) and University of New South Wales (Australia); Postdoctoral (chemistry depts, Stanford University, California, USA and University of Toronto, Ontario, Canada). Professional Experience as Lecturer/Assistant Professor, Associate Professor and Professor (Canberra, Perth, Brisbane); Chief Scientific Officer, Scientific Director and Consultant for a range of pharma and biotech companies in USA, Europe, SE Asia & Australia.

Jan Hoflack is Chief Scientific Officer and Head of Drug Discovery at Oncodesign, a leading biotechnology company in Dijon, France that provides on the one hand advanced oncology pharmacology models and services to pharmaceutical clients, and that is on the other hand involved in kinase inhibitor based Drug Discovery partnerships. Before joining Oncodesign in 2008, Jan filled senior executive roles in drug discovery at Merrell Dow (now Sanofi) in Strasbourg, at Novartis, Basel, Switzerland, and at AstraZeneca where he founded the Astra Structural Chemistry Laboratory in Gothenburg, Sweden. In 2000, Dr. Hoflack joined Johnson & Johnson’s Janssen Pharmaceutica in Beerse, Belgium, to lead the European medicinal chemistry and enabling biology teams.

Dr Hamid Hoveyda is currently the Director of Medicinal Chemistry & Development at Euroscreen SA, Gosselies, Belgium, where he has been employed since 2007. Previous to this, his industrial employers included Tranzyme Pharma (Sherbrooke, Canada), and Affymax Research Institute (Santa Clara, CA, USA) – a subsidiary of GSK at the time. He received his academic training in chemistry both in Canada (PhD, UBC) and in the USA (NSERC postdoctoral fellow at Harvard University).

Senior Fellow at the Institute for Advanced Study of the TU München, Department Chemie; Emeritus of Excellence. Kessler studied Chemistry in Leipzig and Tübingen. Ph.D. 1966 in Organic Chemistry (with E. Müller). Already 1971 he became Full Professor of Organic Chemistry at the Goethe University in Frankfurt. In 1989 he moved to Technische Universität München. Since his retirement (2008) until now he is Senior Fellow and Carl von Linde Professor at the Institute for Advanced Study. Research fields: Conformational design of biomolecules, especially peptides and peptidomimetics in drug design. Application of constraint peptides for coating of biomaterials and for molecular imaging via PET. Development of novel NMR spectroscopic techniques and its application for small molecules, proteins and their mutual interactions.

After a PhD in organic chemistry obtained from the University of Zurich (1983), D. Obrecht spent two years of postdoctoral studies working in Prof. R. E. Ireland’s group at the California Institute of Technology on the total synthesis of avermectin. He then joined the Central Research Laboratories of F. Hoffmann-La Roche in Basle where he worked on several drug discovery projects. In 1989 he started a project with the aim to find small molecule peptidomimetics of exposed protein epitopes. In 1993 he was awarded Roche Lecturer, and 1994 he started a combinatorial chemistry project which he headed in 1996. End of 1996 he co-founded Polyphor with his brother Dr. Jean-Pierre Obrecht. The main expertises of D. Obrecht are synthetic organic chemistry with particular emphasis on macrocycles, medicinal chemistry and drug discovery. He is currently CSO of the the company Polyphor and author of 65 publications and 32 patents, including key patents on the Protein Epitope Mimetics (PEM) Technology and products.

Born in 1970 at Dietwiller in France. After having obtained his PharmD and Master diplomas in Strasbourg, Pierre did his PhD thesis in Prof. Wermuth’s laboratory - Strasbourg. He is currently leading the Medicinal Chemistry of the Infectious Diseases and Vaccines at Tibotec, a division of Janssen Pharmaceutica. Until recently, Pierre was the Head of the Hepatitis C Disease Area in the same company. Together with his group he delivered several drug candidates currently being evaluated in the clinics, including TMC435, a potential best in class Hepatitis C Virus (HCV) protease inhibitor being currently in late Ph3 clinical development, for which he was the project leader and TMC647055 a HCV NS5B non-nucleosidic polymerase inhibitor in Phase 2 clinical trial. Aside from his current assignment, Pierre has initiated a collaboration with Janssen Animal Health, which has delivered novel drug candidates for the treatment of animal diseases. Prior to Tibotec, Pierre worked in the US at ArQule, Woburn, MA then in Oncology at Johnson and Johnson Exton (formally 3-Dimensional Pharmaceuticals) in PA. Pierre’s field of expertise covers both Medicinal Chemistry research on small molecules (including protease inhibitors and nucleosides) and early development. His worked has been recognized by several distinctions including the Philip B. Hofmann Research Scientist Awards in 2009 and 2013. He is an author and inventor of more than 150 original articles, book chapters and patent applications.

Prof Alexander Dömling (Chair of Drug Design at the University of Groningen) devotes his academic life to the structure based design and discovery of bioactive compounds for difficult targets such as protein protein interactions. At the University of Pittsburgh he introduced the “google-like” and web-based technology ANCHOR.QUERY together with Carlos Camacho. ANCHOR.QUERY and the congeners NUCLEO.QUERY and TPP.QUERY can screen very large (billions) of virtual compounds in just seconds for pharmacophores and based on key interacting fragments, e.g. large amino acid side chains of amino acids (in PPIs) or nucleotides or the cofactor thiamine. Interestingly the resulting virtual hits can be instantaneously synthesized using convergent and fast multicomponent reaction chemistry (MCR) in order to test the virtually generated hypothesis. The indication areas Alexander Dömling is interested in are cancer immunology, infectious diseases and metabolic disorders. He has published more than 150 scientific articles, reviews and patents. Additionally Alexander Dömling is a serial entrepreneur trying to make the expression “from bench to bedside” become true. - a.s.s.domling@rug.nl - http://www.drugdesign.nl/

Wael Houssen is a postdoctoral research fellow at the Institute of Medical Sciences, University of Aberdeen working with Professor Marcel Jaspars. He has BSc (Pharmacy), MSc (Pharmacognosy) and PhD (Chemistry). The aim of his current work is to utilise synthetic biology to engineer novel cyclic peptides for several applications. This work was inspired by his previous successful work at the University, starting with his PhD and continuing through his post-doctoral position, focusing on studying the biosynthesis of post-translationally modified ribosomal cyclic peptides e.g. patellamides in cyanobacteria. The engineered biosynthetic machinery Wael Houssen is developing can indeed be used in vitro to generate valuable variants at a feasible rate to meet the demand of the high throughput screening systems and for materials applications. He has published more than 25 research articles, two book chapters and hold two patents.

Peter Timmerman is Chief Scientific Officer (CSO) at Pepscan Therapeutics, Lelystad, the Netherlands. He also holds a chair as Professor in Protein Mimetic Chemistry in the Faculty of Science at the University of Amsterdam (UvA). He studied Chemistry at the Vrije Universiteit (Amsterdam), and obtained his PhD summa cum laude from the University of Twente. In 1995, he was recipient of the Dutch Backer prize for the best Dutch thesis in Organic Chemistry. He did post-doctoral research at the ETH in Zürich and was Assistant Professor in Supramolecular Chemistry and Technology at the University of Twente. He is co-author of over 80 scientific articles.