EFMC-ACSMEDI MedChem Frontiers 2019

First Time Disclosure
The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders (IL09)

Dr Yves P. AUBERSON

NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
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Dr Yves P. AUBERSON

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Yves P. Auberson obtained his Ph.D. in 1990 at the Swiss Federal Institute of Technology in Lausanne, Switzerland. He joined the Novartis Institute for BioMedical Research in Basel, Switzerland in 1992, after a post-doctoral training in chemical biology at Affymax in Palo Alto, USA. He is currently Executive Director in Global Discovery Chemistry, where his research group develops tracers for clinical imaging. Previously, he was Head of Chemistry for Neuroscience, and played a leading role in the discovery and development of drug candidates for the treatment of epilepsy, Alzheimer’s disease and narcolepsy. He is President of the European Federation of Medicinal Chemistry (EFMC), and of the Division of Medicinal Chemistry and Chemical Biology of the Swiss Chemical Society.

Derivatives of 1,3,5-triazine as a New Trend in the Search for the 5-HT₆ Receptor Ligands with Therapeutic Perspectives (PL01)

Prof. Jadwiga HANDZLIK

MEDICAL COLLEGE OF JAGIELLONIAN UNIVERSITY, Krakow, Poland
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Prof. Jadwiga HANDZLIK

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Jadwiga Handzlik is Associate Professor of Medicinal Chemistry in the Department of Technology and Biotechnology of Drugs, Jagiellonian University, Medical College in Cracow. She completed her Ph.D. in medicinal chemistry at the Faculty of Pharmacy, JU MC in Cracow in the group of. Prof. Katarzyna Kieć-Kononowicz (2006). In 2013, she received Doctor of Sciences Degree in pharmacy (habilitation) for work on pharmacophore features responsible for discrimination between GPCRs and MDR-protein targets. She is co-founder (2007) and activist of Polish Medicinal Chemistry Society, Participant of several COST actions and Co-organizer of Drug Discovery and Development course for international students at the Faculty of Pharmacy JU MC (2018). Her scientific expertise concerns computer-aided design and synthesis of GPCRs ligands and MDR modulators, including experience in screening in vitro and in vivo. Recently, her main interest is focused on serotonin receptors 5-HT6.

Systems Pharmacology Links GPCRs with Retinal Degenerative Disorders (PL02)

Prof. Krzysztof PALCZEWSKI

CASE WESTERN RESERVE UNIVERSITY, Cleveland, United States
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Prof. Krzysztof PALCZEWSKI

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Dr. Krzysztof (Kris) Palczewski is an internationally recognized vision scientist and a professor at the University of California – Irvine in the Department of Ophthalmology. He is the Leopold Chair and the founding member of the Center for Translational Vision Research at Gavin Herbert Eye Institute. His discoveries are well documented as evidenced by more than 550 scientific articles, an h-index of 111, and being cited over 43,000 times. Dr. Palczewski holds 22 patents with two of his invented drugs currently undergoing clinical trials. He has received several international awards including the 2015 Bressler Award in Vision Science and the inaugural 2014 Beckman-Argyros Award in Vision Research. He is the only scientist to win both the Cogan Award for the most promising young vision scientist (1996) and the Friedenwald Award for continuously outstanding ophthalmology research (2014). He is a recipient of Paul Kayser International Award for Retina Research from Retina Research Foundation (2018) and a member of Polish Academy of Arts and Sciences (PAU, foreign member).

Next Generation Pain Therapeutics for the Opioid Crisis: Design of Bifunctional Nociceptin/Mu Opioid GPCR Ligands as non-Addicting Analgesics (PL03)

Dr Nurulain ZAVERI

ASTRAEA THERAPEUTICS, Mountain View, United States
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Dr Nurulain ZAVERI

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Dr. Zaveri is the Founder, President and Chief Scientific Officer of Astraea Therapeutics, a preclinical discovery company she founded in 2009, whose mission is medication development for under-served diseases of the central nervous system (such as opioid and substance abuse and addiction, chronic pain and Parkinson’s disease). A PhD medicinal chemist by training, Dr. Zaveri is a recognized expert in the field of G-protein coupled receptor-targeted- and ion channel-targeted drug discovery for CNS medications, that are being advanced into medication development. Before her entrepreneurial venture at Astraea Therapeutics, Dr. Zaveri was Principal Investigator and Director of the Drug Discovery Program at the Stanford Research Institute International in Menlo Park, CA, for 16 years. Dr. Zaveri is a Fellow of the American Association of Pharmaceutical Scientists (AAPS). Dr. Zaveri is the lead inventor on over 12 patents and has authored over 60 research publications and 10 reviews/book chapters in fields of her research. Dr. Zaveri also serves on several NIH grant review committees and is a long-time member of ACS and the MEDI Section.

Libraries of Fluorogenic Substrates with Natural and Unnatural Amino Acids as a Tool in Design of Active and Specific Probes for Investigation of Proteolytic Enzymes (IL01)

Prof. Marcin DRAG

WROCLAV UNIVERSITY OF TECHNOLOGY, Wroclaw, Poland
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Prof. Marcin DRAG

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Marcin Drąg was born in Świdnica (Poland) in 1975. He earned his M.Sc. degree from Department of Chemistry at University of Wroclaw in 1999. Next, he moved to Department of Chemistry at Wroclaw University of Science and Technology, where he earned his Ph.D. in organic and bioorganic chemistry working on new inhibitors of metallo- ad cysteine proteases under supervision of prof. Pawel Kafarski. His Ph.D. thesis was awarded the best thesis in organic chemistry by Polish Chemical Society and Sigma-Aldrich (2004). In 2003 he was appointed Assistant Professor at Wroclaw University of Science and Technology and shortly after (2004) adjunct position. In years 2005-2008 he conducted postdoctoral research at The Burnham Institute for Medical Research (currently SBP Medical Discovery Institute) in La Jolla, CA (USA) in prof. Guy Salvesen laboratory. In 2011 he received Doctor of Sciences Degree in chemistry (habilitation) for work on new types of combinatorial libraries to investigate proteolytic enzymes. In 2016 he received Professor title in chemistry from President of Poland. From July 2018, prof. Drag holds also Adjunct Professor position at Sanford Burnham Prebys Medical Discovery Institute (La Jolla, California, USA). Prof. Drag supervised four Ph.D. students (all cum laude) and 5 post-docs. He is an author of more than 100 publications in per-reviewed scientific journals (for example: Nature Reviews Drug Discovery, Nature Chemical Biology, Nature Protocols, Chemical Reviews, Journal of the American Chemical Society, PNAS). His research interests in chemical biology include the design and synthesis of substrates, inhibitors and activity-based probes to decipher the mechanism of action and the function of proteases in health and disease with particular focus on use of unnatural amino acids.

MMP-9 at the Synapse in the Brain and Mind (IL02)

Prof. Leszek KACZMAREK

NENCKI INSTITUTE OF EXPERIMENTAL BIOLOGY, Warsaw, Poland
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Prof. Leszek KACZMAREK

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Leszek Kaczmarek, is a professor and head of the Laboratory of Neurobiology at the Nencki Institute, Warsaw; Poland. His major research achievements include: (i) discovery of c-Myc protein role in regulation of the cell cycle; (ii) discovery of the learning-related gene (c-fos) expression in the mammalian brain; (iii) revealing apoptotic component of excitotoxicity in the adult brain; (iv) discovery of specific role of cyclin D2 in the adult brain neurogenesis; (v) discovery of involvement of matrix metalloproteinases in neuronal plasticity, epileptogenesis, learning and memory; (vi) defining the role of the central amygdala in appetitive learning and memory. He has published over 200 research papers, cited ca. 10 000 times. L. Kaczmarek was invited as a lecturer to more than 100 international and national meetings and over 250 times to talk on research seminars, workshops, etc.; promoted over 40 PhDs; and was PI or coordinator on over 50 domestic and international grants. He was postdoc at the Temple University (Philadelphia, USA), as well as visiting professor at the: University of Catania (Italy), McGill University (Montreal Canada), UCLA (Los Angeles, USA), Institute of Photonic Sciences, ICFO, Castelldefels, Spain. He served on numerous program and grant committees, editorial and advisory boards, as well as authorities of Polish and international scientific societies and organizations. At present he chairs the Division of Biological and Agriculture Sciences of the Polish Academy of Sciences (PAN). Labe webpage: http://neurogene.nencki.gov.pl

Metalloproteinase Cleavage Control of Interferon Alpha and Gamma Dampens Inflammation and Anti-Viral Immunity (IL03)

Prof. Christopher OVERALL

UNIVERSITY OF BRITISH COLUMBIA, Vancouver, Canada
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Prof. Christopher OVERALL

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Professor Christopher Overall is a Tier 1 Canada Research Chair in Protease Proteomics and Systems Biology at the University of British Columbia, Vancouver, Canada, a Senior Fellow of the Freiburg Institute of Advanced Studies, Albert-Ludwigs Universität Freiburg, Germany, where he is now an Honorary Professor. He completed his undergraduate degrees in Adelaide, Australia, PhD at the University of Toronto, and Post-Doctoral training in Protein Engineering with Dr Michael Smith, Nobel Laurette. He was inducted as a fellow into the Royal Society of Canada, Academy of Science in 2018 and is Chair of the HUPO Chromosome Centric Human Proteome Project. He is best known for his development of N-Terminomic proteomic methodology for the discovery of protease substrates in vivo, thereby establishing the field of degradomics. He has used these techniques to reveal new biological roles for proteases in immunity and disease as well as new treatments to correct protease deficiency in an immunodeficiency disease. His > 270 papers have high impact with an h-index of 87.

Protein-Ligand Interactions: How Medicinal Chemistry Contributes to the Understanding of Molecular Recognition (IL17)

Dr Marc NAZARE

FMP, Berlin, Germany
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Dr Marc NAZARE

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Marc Nazare is a group leader medicinal chemistry at the Leibniz Institut fuer Molekulare Pharmakologie FMP, Berlin, Germany. He studied chemistry at the University of Karlsruhe and obtained his PhD in organic chemistry in 1999 under the guidance of Prof. Herbert Waldmann working on a natural product total synthesis. He started his career in the pharmaceutical industry at Aventis (now Sanofi) in Frankfurt, as a medicinal chemist and project leader. Over the years he has been working on kinase-, GPCR-, protease- and ion channel projects covering both early and late stage research. Marc Nazare contributed to several clinical candidates of Factor Xa inhibitors and P2Y12 antagonists programs for the treatment of thrombosis. In 2013, he joined the Leibniz Institute for Molecular Pharmacology FMP to establish the medicinal chemistry group in the chemical biology department. His research interest is focused on the structure-based design and optimization of chemical probes and imaging tools for chemical biology.

Adventures in Targeting Protein Lipdation: Breaking Drug Resistance Using Fragment Deconstruction and Chemical Biology (IL18)

Prof. Edward TATE

IMPERIAL COLLEGE LONDON, London, United Kingdom
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Prof. Edward TATE

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Edward Tate is Professor of Chemical Biology in the Department of Chemistry at Imperial College London, and a Satellite Group Leader and the Francis Crick Institute. He completed his Ph.D. in organic chemistry at the University of Cambridge in the group of Prof. Steve Ley. Following postdoctoral research in chemistry and biology on an 1851 Research Fellowship at CNRS Gif sur Yvette and Ecole Polytechnique and the Pasteur Institute in Paris, he moved to Imperial College London on a BBSRC David Phillips Fellowship, where he was promoted to a Chair in 2014. He leads a team of more than 50 scientists working on the design and application of chemical approaches to understand and manipulate living systems, with a particular focus on drug target discovery and validation. He is a Fellow of the Royal Societies of Chemistry (FRSC) and of Biology (FRSB), and Director of Imperial’s Centre for Drug Discovery Science. He received the 2012 Wain Medal, the 2013 MedImmune Protein and Peptide Science Award, the 2014 Norman Heatley Award, and a 2015 Cancer Research UK Programme Foundation Award in recognition of his group’s research in chemical biology and drug discovery. Website: http://www.imperial.ac.uk/people/e.tate.

Tankyrase Inhibitors : Evidence for Therapeutic Potential in Immuno-Oncology

Dr Luc VAN HIJFTE

MERCACHEMSYNCOM, Nijmegen, The Netherlands

Design of Orexin 1 Receptor Selective Antagonists (IL11)

Dr Uta LESSEL

BOEHRINGER INGELHEIM PHARMA GMBH & CO KG, Biberach an der Riss, Germany
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Dr Uta LESSEL

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Uta Lessel, Principal Scientist in Computational Chemistry within the Department Medicinal Chemistry, working on early projects (special fields of interest: virtual screening, phenotypic screening and macrocycles) study of Pharmaceutical sciences at the University of Düsseldorf PhD in Pharmaceutical Chemistry from the University of Düsseldorf Postdoc at a research institute in Brunswick (Germany) and at the University of Cologne joined Boehringer Ingelheim in 1998.

Next Generation GPR119 Agonists as Potential Treatment for Cardiometabolic Diseases (IL12)

Dr Lothar SCHWINK

SANOFI, Frankfurt Am Main, Germany
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Dr Lothar SCHWINK

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Lothar studied chemistry at the Philipps-University in Marburg (Germany) were he earned his doctoral degree for his work on asymmetric catalysis under the supervision of Prof. Paul Knochel in 1997. During a postdoctoral stay at the University of California, Irvine, in Prof. Larry Overman’s group, he completed the total synthesis of aloperine and succeeded in assembling a strategic intermediate for asparagamine A. Since 1999, Lothar is leading research teams directed towards the optimization of small molecule drug candidates for metabolic diseases at Sanofi or its predecessor companies. Examples include natural product derived enzyme inhibitors, and several modulators of nuclear hormone and G-protein coupled receptors.

G Protein-Coupled Receptors: the Structural Basis for their Pharmacology (IL10)

Dr Chris TATE

MRC LABORATORY OF MOLECULAR BIOLOGY, Cambridge, United Kingdom
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Dr Chris TATE

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Chris obtained his PhD from the University of Bristol (1989) and then moved to the University of Cambridge (Dept of Biochemistry). After obtaining a research fellowship at Girton College (Cambridge) he moved to the LMB to work in Richard Henderson's group on the serotonin transporter. Chris then worked on the E. coli multidrug transporter EmrE and obtained both 2D and 3D crystals as well as a 3D structure using cryo-EM. In 2005 he started working on the development of conformational thermostabilisation of GPCRs, which resulted in the structure of the 1-adrenoceptor. Subsequent work has focused on understanding the molecular basis of GPCR pharmacology through structure determination of the 1-adrenoceptor and adenosine A2A receptor in multiple different conformations bound to ligands of different efficacy. In 2016 mini-G proteins were developed as a tool for the structure determination of GPCRs in the fully active state. Structures have been determined either by X-ray crystallography of receptors coupled to either mini-Gs or mini-Go, or by electron cryo-microscopy of receptors coupled to mini G protein bound to  subunits.

Designing Synthetic Gene Regulators (SynGR) (IL04)

Prof. Aseem ANSARI

UNIVERSITY OF WISCONSIN-MADISON, Madison, United States
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Prof. Aseem ANSARI

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Aseem Zoe Ansari is a Professor of Chemical Genomics and Synthetic Biology at the University of Wisconsin-Madison (https://ansarilab.biochem.wisc.edu/research.html). Professor Ansari received his Ph.D. from Northwestern University followed by postdoctoral training at Harvard University and MIT. At UW-Madison, the Ansari group creates synthetic gene regulators (SynGRs) to control stem cell fate and tackle “undruggable” genome-based diseases. Integrating chemistry, genomics, molecular medicine and bioinformatics, the Ansari group has recently created a designer gene switch that can find and fix the diseased gene that causes an incurable neuronal disease (Friedreich’s ataxia). The molecular design strategy permits the precision-targeting of other genes whose malfunctions cause a wide array of diseases (Erwin et al., Science 2017). Professor Ansari has received a few honors and awards, including: The CAREER award from the U.S. National Science Foundation (NSF), Research Excellence Award from the W. M. Keck Foundation, Basil O'Connor Starter Scholar Award from the March of Dimes Foundation, the Japan Society for Promotion of Science (JSPS) fellowship, the Resident Tutorship at Winthrop House from Harvard, and the first prize for graduate research from Sigma Xi Research society at Northwestern.

Exploring Bacterial Genomes for Natural Product Discovery and Development (IL05)

Prof. Alessandra S. EUSTAQUIO

UNIVERSITY OF ILLINOIS AT CHICAGO, Chicago, United States
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Prof. Alessandra S. EUSTAQUIO

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Dr. Eustaquio has been an Assistant Professor in the Department of Medicinal Chemistry and Pharmacognosy of the University of Illinois at Chicago (UIC) since August 2015. She also holds an appointment with the Center for Biomolecular Sciences. The Eustaquio laboratory aims to contribute to drug discovery and development from natural products. Bacterial metabolites account for the majority of antibiotics in use in the clinic today. The Eustaquio lab uses open-source bioinformatics tools to predict the biosynthetic potential of bacteria based on their genome sequences (genome mining). We then carry out genetic engineering to activate expression of silent genes and obtain the encoded antibiotics. We are also interested in understanding antibiotic biosynthesis and transcriptional regulation. Finally, we are interested in developing synthetic biology tools to facilitate access to natural and engineered compounds. Before joining UIC, Dr. Eustaquio was a Principal Scientist at Pfizer, Medicinal Chemistry, Natural Products group. Prior to that, she had done postdoctoral training at the University of California San Diego, obtained a PhD in Pharmaceutical Biology from the University of Tuebingen, Germany, and a B.Sc. in Pharmacy & Biochemistry from the University of São Paulo, Brazil.

Integrative Screening Identifies a Novel Node in the Oncogenic YAP/HIPPO Pathway (IL06)

Dr Mathias FREDERIKSEN

NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH (NIBR), Basel, Switzerland

Charting New Paths in Multi-Target Drug Discovery for Alzheimer’s Disease (IL13)

Prof. Maria Laura BOLOGNESI

UNIVERSITY OF BOLOGNA, Bologna, Italy
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Prof. Maria Laura BOLOGNESI

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Maria Laura Bolognesi holds the position of Professor of Medicinal Chemistry and Director of the Chemistry and Pharmaceutical Technologies degree program at the Alma Mater Studiorum - University of Bologna. She received her PhD in Pharmaceutical Sciences in 1996 and carried out postdoctoral work at the University of Minnesota. Her research explores the development of small molecules in the neurodegenerative and neglected tropical disease therapeutic areas. Maria Laura has a track record of more than 160 publications in high-ranked scientific journals, including patents and patent applications, and numerous invited talks worldwide. She was awarded the positions of Distinguished Visiting Professor at the Complutense University of Madrid in 2009, Pesquisador Visitante Especial at the University of Brasilia in 2014 and Professeur Invité at Université Caen Normandie in 2018. She is also an Associate Editor of Journal of Medicinal Chemistry and serves in the Advisory Board of the European Federation of Medicinal Chemistry.

Chemical Biology for Drug Discovery: A Click and Play Approach Exemplified by ERK1/2 Probes (OC03)

Dr Charlotte GRIFFITHS-JONES

ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
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Dr Charlotte GRIFFITHS-JONES

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Charlotte Griffiths-Jones gained a PhD from Cardiff University in 2004 then undertook a post doc in Cambridge under the supervision of prof Steve Ley. After 1 year at GSK working in the technology development lab, she moved to Astex in 2007 where she is now an Associate Director. Charlotte has worked on a number of fragment based drug discovery projects from early stage right through to clinical development. This includes the recently launched oncology drug Erdafitinib.

Identification and in-vivo Efficacy Studies of a Nicotinamide Derivative as Novel NNMT Inhibitor (OC04)

Dr Sven RUF

SANOFI-AVENTIS DEUTSCHLAND GMBH, Frankfurt am Main, Germany
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Dr Sven RUF

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Dr. Sven Ruf completed his PhD studies in synthetic organic chemistry with Prof. Regitz at the University of Kaiserslautern in 1999. Afterwards he spent the year 2000 with postdoctoral studies in the group of Prof. Trost at Stanford University. In 2001 he joined the medicinal chemistry department of the Sanofi-Aventis Deutschland GmbH and currently holds the position of a senior scientist. He has been responsible for the lead discovery strategies deployed in several early resarch projects and is a team and project leader at the Sanofi research site in Frankfurt

Multiple Targeting - The Histamine H3 Receptor Pharmacophore as Central Element (IL14)

Prof. Holger STARK

HEINRICH HEINE UNIVERSITY DÜSSELDORF, Duesseldorf, Germany
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Prof. Holger STARK

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Prof. Dr. Dr. h.c.Holger Stark studied pharmacy and finished his PhD in Medicinal Chemistry at the Free University of Berlin. He focused on neurotransmitter research with emphasis on histamine as well as dopamine receptor subtypes and expanded this on lipid signalling. In 2000 he became full professor at the Goethe University in Frankfurt, Germany and went in 2013 to the Heinrich Heine University in Düsseldorf, Germany where he has his actual position. He founded some start-up companies on cancer therapeutics (Warburg Glycomed, PSites Pharma) and has received several prices for his successful research as well as for teaching. He is co-inventor of pitolisant (Wakix®), the first histamine H3 receptor antagonist with market approval, and has prepared some back-up candidates in different leads for various targets. Since 2004 Holger Stark is editor-in-chief of the Archiv der Pharmazie – Chemistry in Life Sciences, one of the oldest journals on Medicinal Chemistry.

Mining the Protein Kinase Cysteinome (IL22)

Dr Tjeerd BARF

ACERTA PHARMA BV, Oss, The Netherlands
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Dr Tjeerd BARF

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Dr. Barf is one of the founders of Acerta Pharma. He has extensive experience in pharmaceutical Research and Development and contributed to delivery of several clinical candidates in the metabolic disease, autoimmune and oncology space. He successfully exploited the covalent binding paradigm for kinases, resulting in the discovery of acalabrutinib. Tjeerd joined the pharmaceutical industry in 1997 and served in various project and line management roles at Pharmacia & Upjohn, Biovitrum, Organon, Schering-Plough and MSD. He holds a PhD in Medicinal Chemistry and MSc in Organic Chemistry from the University of Groningen, The Netherlands.

Safety First: Covalent Inhibitors from a Safety Perspective (IL20)

Dr Mickael MOGEMARK

ASTRAZENECA, Mölndal, Sweden
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Dr Mickael MOGEMARK

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Mickael Mogemark is a medicinal chemist/ chemical toxicologist at AstraZeneca Gothenburg. He was awarded his Ph. D in chemistry from Umeå University, Sweden in January 2005. He joined AstraZeneca as a medicinal chemist in 2004 where he has worked across several therapy areas. His research interests are focused on chemical toxicology and on the development of novel therapeutic agents.

Adventures in Functional Assignment and Inhibition of Metallo-Enzymes (IL21)

Prof. Christopher J. SCHOFIELD

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Prof. Christopher J. SCHOFIELD

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Chris Schofield studied for a degree in chemistry at the University of Manchester (1979-1982). In 1982 he moved to Oxford for DPhil studies with Jack Baldwin on the synthesis and biosynthesis of antibiotics. In 1985 he became a Departmental Demonstrator in the Dyson Perrins Laboratory, and in 1990 Lecturer in Chemistry and Fellow of Hertford College. In 1998 he became Professor of Chemistry, and in 2011 was appointed Head of Organic Chemistry. He is a Fellow of the Royal Society. His research group works at the interface of chemistry, biology and medicine. His work has opened up new fields in antibiotic research, oxygen sensing and gene regulation in organisms ranging from bacteria to plants and animals. His work has identified new opportunities for medicinal intervention that are being pursued by numerous academic and commercial laboratories.

Capturing and Applying Knowledge to Guide Compound Optimisation (OC10)

Dr Nick FOSTER

OPTIBRIUM, Litlington, United Kingdom
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Dr Nick FOSTER

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Nick graduated with a degree in Applied Biochemistry in 1993 before joining the Medical Research Council working on protein folding within Cambridge University's Chemistry Department and the Laboratory for Molecular Biology (LMB) until 2001. After this, Nick helped establish the ADME/PK laboratory of Camitro and remained part of the operational team (within BioFocus) until 2009 when he joined the sales and marketing team as Associate Director of Business Development, Europe. Nick joined Optibrium as Head of Commercial Operations in 2012. The company develops pioneering software for small molecule design, optimisation and data analysis

Learning the Art of Chemical Synthesis with Deep Neural Networks and Discipline Scale Data (IL23)

Prof. Mark WALLER

UNIVERSITY OF WOLLONGONG, Wollongong, Australia
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Prof. Mark WALLER

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Dr. Mark P Waller is the founder of Pending.AI, a startup based in Sydney, Australia. The company is developing AI solutions to empower scientists in the pharmaceutical industry to design, make, and test new drugs to treat diseases. Mark was formerly at Shanghai University in Shanghai, China, where he was an Eastern Scholar Professor in the department of Physics. Prior to that he was in the Organic Chemistry Institute at University of Münster, Germany where he worked towards getting his Habilitation on adaptive multi-scale modeling. Mark first went to Germany over 12 years ago as a post-doc at the Max-Planck-Institut für Kohlenforschung where he worked on NMR. He obtained his PhD from the University of Sydney in Charge Density, and before that he carried out his undergraduate studies at the University of Tasmania where he obtained a Bachelor of Science.

Applications of Artificial Intelligence in Drug Discovery – Separating Hype From Utility (IL24)

Dr Patrick WALTERS

RELAY THERAPEUTICS, Cambridge, MA, United States
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Dr Patrick WALTERS

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Pat Walters heads the Computation & Informatics group at Relay Therapeutics in Cambridge, MA. His group focuses on novel applications of computational methods that integrate computer simulations and experimental data to provide insights that drive drug discovery programs. Prior to joining Relay, he spent more than 20 years at Vertex Pharmaceuticals where he was Global Head of Modeling & Informatics. Pat is a member of the editorial advisory board for the Journal of Medicinal Chemistry, and previously held similar roles with Molecular Informatics, and Letters in Drug Design & Discovery. Pat received his Ph.D. in Organic Chemistry from the University of Arizona where he studied the application of artificial intelligence in conformational analysis. Prior to obtaining his Ph.D., he worked at Varian Instruments as both a chemist and a software developer. Pat received his B.S. in Chemistry from the University of California, Santa Barbara.

Augmented Intelligence for Compound Design (OC09)

Dr Michal WARCHOL

ARDIGEN, Krakow, Poland
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Dr Michal WARCHOL

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Dr. Michał Warchoł serves as a Director of Ardigen AI Labs, leading the development and applications of statistical learning methods in Ardigen's projects. He did a PhD in Statistics at the Institute of Statistics, Biostatistics and Actuarial Sciences at Université Catholique de Louvain in Belgium. Part of his research program was conducted at the Department of Statistics at Columbia University in New York. Prior to joining Ardigen, Dr. Warchoł co-founded DeepArt UG, company providing novel image processing algorithms based on deep learning. He obtained a master degree in mathematics at the Jagiellonian University and a bachelor degree in finance at the Cracow University of Economics in Poland. The last year of his master program was done at the Department of Statistics at École polytechnique fédérale de Lausanne in Switzerland.

Targeted Protein Degradation with Small Molecules: how PROTACs Work (IL07)

Prof. Alessio CIULLI

UNIVERSITY OF DUNDEE, Dundee, United Kingdom
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Prof. Alessio CIULLI

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Alessio Ciulli holds the Personal Chair of Chemical and Structural Biology at the School of Life Sciences, University of Dundee. His research interests are in chemical biology, structural biology and drug discovery of protein-protein interactions (PPIs) within the chromatin and ubiquitin-proteasome systems. Of particular interest are the development and application of small molecules approaches for inducing protein degradation, and chemical genetics and fragment based drug design approaches to target protein surfaces and PPIs. Alessio graduated in Chemistry (2002) from his hometown Florence under the late Ivano Bertini and obtained his PhD from the University of Cambridge (Chemistry, 2006), studying as a Gates Cambridge Scholar under the supervision of Chris Abell and in collaboration with Astex Pharmaceuticals. Following post-doctoral research on fragment-based drug design with Chris Abell and Tom Blundell, and an HFSP visiting Fellowship at Yale University to begin collaboration with Craig Crews (2009), he was awarded a BBSRC David Phillips Fellowship and returned to Cambridge to start his independent career in 2010. In 2013 Alessio was awarded an ERC Starting Grant and moved his laboratory to the School of Life Sciences at Dundee to take up a Readership and Principal Investigator role within the Division of Biological Chemistry and Drug Discovery. He was promoted to Professor in October 2016. He is a Fellow of the Royal Society of Chemistry. Alessio is the recipient of several prizes and awards, including: - 2014 Talented Young Italian award - 2015 EFMC Prize for Young Medicinal Chemist in Academia - 2015 ICBS Young Chemical Biologist Award - 2016 RSC Capps Green Zomaya Award in medicinal computational chemistry - 2016 MedChemComm Emerging Investigator Lectureship.

Drugging Challenging E3 Ligases: A Novel Multidisciplinary Approach to Identify Small-Molecules that Bind FBW7 (OC02)

Ms Miriam MARTINEZ CARTRO

UNIVERSITY OF BARCELONA, Barcelona, Spain
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Ms Miriam MARTINEZ CARTRO

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Míriam Martínez-Cartró obtained her bachelor's degree in Pharmacy at the University of Barcelona. She is currently a PhD student under the supervision of Prof. Xavier Barril and Dr. Carles Galdeano at the Faculty of Pharmacy of the University of Barcelona. Her PhD project is focused on the identification and characterization of chemical probes able to bind relevant SCF-E3 ligase through the application of a multidisciplinary approach that combines structure-based drug design and biophysical techniques for hit identification. During her PhD she carried out a placement in the Structural Genomics Consortium of Oxford under the supervision of Prof. Frank von Delft to perform X-Ray crystallography of small-molecules for therapeutic interest.

The Ubiquitin System (IL08)

Prof. Huib OVAA

LEIDEN UNIVERSITY MEDICAL CENTER, Leiden, The Netherlands
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Prof. Huib OVAA

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Huib Ovaa, Professor Leiden University Medical Center, Department of Cell and Chemical Biology, Leiden, the Netherlands Education/training: Maters’s 01-07-1997, studies Chemistry, Main subject Organic Synthesis, Leiden University the Netherlands. Doctorate/PhD 03-10-2001 Phd, title of thesis ‘Synthetic Organic Chemistry’, supervisor J.H. van Boom/H.S. Overkleeft, Leiden University the Netherlands. Positions and employment: 2015-present: Professor Leiden University Medical Center; 2016-present: Professor Leiden University; 2016-present Guest Researcher Netherlands Cancer Institute (NKI); 2012-2016: Extraordinary Professor Leiden University; 2010-2013:0.1FTE C.S.O. UbiQ Bio B.V.; 2009-2016: Tenured staff member Netherlands Cancer Institute (NKI); 2005-2012: Assistant Professor, Leiden University, the Netherlands; 2004-2009: Junior group leader, Netherlands Cancer Institute (NKI); 2004-2005: Guest Researcher, Leiden University; 2003-2004: Instructor in Pathology, Harvard Medical School, Boston, U.S.A.; 2001-2003: Post-doctoral fellow, Harvard Medical School, Boston U.S.A. Research Field: Chemical Biology. My group specializes in the development of novel techniques to profile cellular enzymatic activities associated primarily with ubiquitin-mediated proteasomal degradation and antigen presentation. We use an organic synthesis driven approach in order to gain further understanding of the cellular processes under investigation by preparing small molecule-activity modulators and synthetic protein- reporters on enzymatic activities by both rational design and by en masse screening of small molecule libraries followed by hit-optimization and subsequent development of research tools.

Small-Molecule Modulation of Cereblon Protein Level (OC01)

Dr Christian STEINEBACH

UNIVERSITY OF BONN, Bonn, Germany
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Dr Christian STEINEBACH

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Christian Steinebach completed his undergraduate studies in Pharmacy (state examination) at the University of Bonn, Germany. In 2015, he became a licensed Pharmacist and got the Carl-Friedrich-Mohr award. He received his MSc in Drug Development in 2016. Since then he is performing his PhD studies in Pharmaceutical Chemistry supervised by Prof. Michael Gütschow at the Pharmaceutical Institute in Bonn. In 2018, he successfully applied for a PhD-related scholarship from the Bonn International Graduate School of Drug Sciences. His scientific work is devoted to the Medicinal Chemistry of Proteolysis Targeting Chimeras (PROTACs), to the design and synthesis of bioactive molecules acting by a new modality of targeted degradation of disease causing proteins, as well as to general questions about the utilization of the ubiquitin-proteasome system.

The Discovery and Development of the Clinical FAAH Inhibitor JNJ-42165279 (OC06)

Prof. James BREITENBUCHER

UNIVERSITY OF CALIFORNIA SAN FRANCISCO, San Francisco, United States
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Prof. James BREITENBUCHER

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Dr. Breitenbucher has over 20 years of drug discovery experience and is currently Professor at the Institute for Neurodegenerative Diseases at UCSF. Prior to joining UCSF, Dr. Breitenbucher was senior director of Chemistry at Dart Neurosciences. During his 8 years at DNS he built a robust department that discovered 10 novel pre-clinical candidates for 7 different biological mechanisms for the treatment of Stroke, Alzheimer’s, and Parkinson’s Disease. Prior to DNS Guy was a research fellow at Johnson & Johnson as head of the Pain Discovery Chemistry. At J&J, Dr. Breitenbucher worked on or led drug discovery projects on 10 different biological mechanisms which advanced compounds into pre-clinical or clinical development. Dr. Breitenbucher received his B.Sc. and M.Sc. in chemistry at California State University at Long Beach and his Ph.D. in organic chemistry at University of California at Riverside. Dr. Breitenbucher is co-author on over 50 peer reviewed scientific papers, an inventor on over 40 patents.

Potential of Natural Cannabinoids and Synthetic Cannabinoids in Neuroprotection (IL16)

Prof. Rafael FRANCO

UNIVERSITY OF BARCELONA, Barcelona, Spain
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Prof. Rafael FRANCO

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I am Molecular Neuropharmacologist coming with Biochemistry and Molecular Biology background. I did a first postdoc stay in the lab of Prof. Geoffrey Burnstock in UCL (Univ College London) where I get acquainted with purinergic nerves and purinergic actions. Back in Spain I founded one of the first labs in Europe devoted to the work from a molecular point of view of G protein-coupled receptors (GPCRs). Other stays abroad were: in Max Planck Institute Dortmund with Prof. Rolk Kinne, in Harvard Medical School with Prof. Cox Terhorst and in Pasteur Institute with Prof. Ara Hovanessian. My laboratory is internationally known for the discovery of GPCR heteromers and for research on their physiological relevance. The main focus is the central nervous system and we now have taken a translational approach for which we collaborate with Medicinal Chemistry laboratories in different Countries. GPCRs in our portfolio include, among other, those for adenosine, cannabinoids, epinephrine, orexin, dopamine and ghrelin. We are interested in neurodegenerative diseases and in drug addiction (cocaine, ethanol and amphetamine) I have circa 400 papers mainly in international journal and h index as of Nov 2018 is: 68. Number of citations is >15,000.

Cannabinoid Receptor Type 2 Modulation to Improve Outcomes for Cartilage Repair in the Osteoarthritic Joint (IL15)

Prof. Katarzyna STAROWICZ-BUBAK

INSTITUTE OF PHARMACOLOGY, POLISH ACADEMY OF SCIENCES, Krakow, Poland
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Prof. Katarzyna STAROWICZ-BUBAK

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Katarzyna Starowicz (PhD, DSc) is a neuropharmacologist leading Department of Neurochemistry based at the Institute of Pharmacology Polish Academy of Sciences (www.if-pan.krakow.pl). her education includes M.Sc. degree in Biotechnology from the Jagiellonian University (2000), PhD in Pharmacology at the Medical Sciences at the Utrecht University (2005) and Habilitation in Medical Biology at the Faculty of Medicine of the Jagiellonian University Medical College (2013). After receiving a PhD degree she started a postdoctoral fellowship in Endocannabinoid Research Group under the supervision of prof. Vincenzo Di Marzo. After completing the postdoctoral fellowship she returned to Poland where she have established and maintained a laboratory focused on understanding of the mechanisms of chronic pain and on the characteristics of endogenous system involved in the transmission of pain stimuli with particular attention to endocannabinoid system. Subsequently, my research interests expanded to include the issue of degenerative joint disease (particularly osteoarthritis, OA). Please visit http://www.painlab.pl for more details and full description of current research interests. Laureate of the Powroty / Homing program of the Foundation for Polish Science, the habilitation scholarship of L'Oréal Poland for Women and Science in 2012 and the National Science Centre Award in Life Science in 2016. Member of British Journal of Pharmacology Editorial Board. President of the Alumni Association of the Foundation for Polish Science (2017-2019). V-ce President of the Board of National Agency for Academic Exchage (NAWA, www.nawa.gov.pl).

Discovery of Best in-class, Novel, Selective, Potent and Peripheral FLT3 Inhibitors, a New Way to Treat Neuropathic Pain (OC05)

Dr Dominique SURLERAUX

BCI PHARMA, Liège, Belgium
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Dr Dominique SURLERAUX

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Dominique Surleraux is Chief Executive officer (CEO) of BCI Pharma. BCI Pharma was founded in March 2013 and is actually located in France (Montpellier) and Belgium (Liège). Dominique Surleraux has a Ph.D in organic chemistry from university of Namur (BE) and a master in drug design (Lille, FR). Dr. Dominique Surleraux started his career at Janssen Phamaceutica (J&J (BE), 5 years), then moved to Tibotec (J&J (BE), 7 years) and was managing worldwide anti-infective research for J&J. He then moved to France and supervised the HCV research (60 scientists) for idenix Pharmaceutical, a Boston based company acquired by MSD (4b$). He was directly involved on the discovery of blockbusters (Prezista (HIV protease Inh.) and Simeprevir (HCV protease Inh.) and bring more than 10 drugs in clinical development. He is inventor/co-inventor of more than 100 patents.

Discovery of OAT-2068 - A Potent, Selective, Orally Bioavailable Inhibitor of Mouse Chitotriosidase and its In Vivo Activity in the Bleomycin-Induced Pulmonary Fibrosis Model in Mice (OC07)

Dr Agnieszka BARTOSZEWICZ

MOLECURE S.A, Warszawa, Poland
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Dr Agnieszka BARTOSZEWICZ

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Agnieszka completed her PhD studies in organic chemistry under the supervision of Prof. Belén Martín-Matute at Stockholm University, Sweden in 2012. Afterwards she spent 2 years as a postdoctoral fellow in the group of Prof. Gregory Fu at Caltech, Pasadena, CA, USA. She joined Oncoarendi Therapeutics SA in 2015 as a medicinal chemist. Agnieszka is currently a team and project leader at Oncoarendi working on design and synthesis of small molecule inhibitors targeting chitinase-like-proteins.

DPD-inspired Small Heterocyclic Libraries Characterized as Novel LsrK Kinase Inhibitors: an Opportunity to Fight Antimicrobial Resistance (OC08)

Dr Anna KARAWAJCZYK

SELVITA, Krakow, Poland