EFMC-ASMC 2023

Opening Lecture
Synthetic and Medicinal Chemistry for Biologics (IL01)

Prof. Jeffrey BODE

ETH ZURICH, Zürich, Switzerland
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Prof. Jeffrey BODE

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http://www.bode.ethz.ch

The explosion of biological molecules as therapeutic modalities is transition to a new generation of modified proteins, antibodies, capsids, and bioconjugates through combinations of recombinantly produced biologics and synthetic molecules. This frontier requires new synthetic methods suitable for preparing and modifying homogeneous, folded biomolecule molecules. To achieve this, we are developing new chemical and chemoenzymatic reactions that offer the chemoselectivty, rapid reaction kinetics, and compatibility with physiological conditions required for advancing the field. These efforts have led to new platforms for chemical protein synthesis, modification and bioconjugation of commercial antibodies, and site specific modification and elaboration of recombinant proteins. Together, these new synthetic methods blur the lines between synthetic and biological molecules and open a plethora of new therapeutic approaches.

EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Industry
Discovery and Characterization of Potent, Efficacious and Orally Available Antimalarial Plasmepsin X Inhibitors (PR02)

Dr Teresa DE HARO GARCIA

UCB, Braine l'Alleud, Belgium

EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Academia
Targeted Protein Degradation via Molecular Glues (PR01)

Dr Georg WINTER

RESEARCH CENTER FOR MOLECULAR MEDICINE OF THE AUSTRIAN ACADEMY OF SCIENCES, Vienna, Austria

Synthesis of Fluorinated Molecules Using Modern Synthetic Tools (IL04)

Dr Tatiana BESSET

INSA OF ROUEN, Mont-Saint-Aignan, France
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Dr Tatiana BESSET

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Different synthetic approaches for the synthesis of original fluorinated molecules will be presented including new tools based on transition metal catalyzed C-H bond functionalization and the design of original reagents.

MicroCycle: A Machine Learning Driven, Automated and Integrated Platform for Drug Discovery (IL03)

Dr Cara BROCKLEHURST

NOVARTIS, Basel, Switzerland
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Dr Cara BROCKLEHURST

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"MicroCycle: A Machine Learning Driven, Automated and Integrated Platform for Drug Discovery"

What if we could develop an integrated drug discovery platform to accelerate drug discovery, which utilises micro-scale chemistry, real-time biological and physicochemical characterisation and machine learning driven compound design? At NIBR this is a reality! Our automated medicinal chemistry ‘design-make-test-analyse’ cycle is powered by machine learning, enables sequential multi-parameter optimisation and generates knowledge in a timeframe never before possible. We have built MicroCycle; a modular technology platform which benefits from recent advances in plate based micro-scale chemistry, micropurification,[1]in-situ quantification and machine learning thus ensuring rapid access to high quality chemical matter already formatted for assay. Furthermore, by reorienting existing high throughput assay technology we can generate a full package of relevant data on each set of compounds in every learning cycle.

Next Generation Design-Make-Test-Analysis-Cycles (IL14)

Dr Clara CHRIST

BAYER, Berlin, Germany
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Dr Clara CHRIST

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"Next Generation Design-Make-Test-Analysis-Cycles"

Digital tools are changing the way scientists are working in drug discovery projects. We will show examples how scientists can profit from the recent advances in machine learning and physics-based computational approaches. Examples from our research will be given.

Making Difficult-to-Make Molecules: Photochemistry as an Enabling Tool (IL25)

Dr Susannah COOTE

UNIVERSITY OF BATH, Bath, United Kingdom
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Dr Susannah COOTE

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"Making Difficult-to-Make Molecules: Photochemistry as an Enabling Tool"

Application of photochemical transformations in creative synthetic approaches to interesting strained products, especially four-membered rings.

Will Chemputers Dream of Electric Drugs (IL23)

Prof. Leroy CRONIN

UNIVERSITY OF GLASGOW, Glasgow, United Kingdom
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Prof. Leroy CRONIN

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"Why Chemputers Will Dream of Electric Drugs"

Can chemputers, robots that can potentially make any molecule, take AI-designs of drugs and make them in the lab? In this talk Lee Cronin will discuss chemputation, the process of turning code into molecules, the use of theory to design new makable molecules, and the concept of a chemical programming language to help all chemists around the world exchange reproducible laboratory protocols.

New Catalytic Approaches for Simplifying Complex Amine Synthesis (IL06)

Prof. Darren J. DIXON

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Prof. Darren J. DIXON

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In this presentation, new “synthesis inspired” user-friendly broad scope catalytic strategies for forging the key carbon-carbon bonds of key late stage synthetic intermediates en route to various complex alkaloid natural products will be described.

Taking Molecular Glue Degraders to New Heights (IL24)

Dr Etienne DONCKELE

MONTE ROSA THERAPEUTICS, Basel, Switzerland
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Dr Etienne DONCKELE

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Etienne performed his undergraduate research with Prof. Barry M. Trost at Stanford University and carried out one-year placement in medicinal chemistry at the Broad Institute of MIT and Harvard. He obtained his Ph.D. in organic chemistry at the ETH Zürich under the supervision of Prof. François Diederich. After a postdoctoral stay at Caltech in the group of Prof. Brian Stoltz in natural product synthesis, Etienne gained experience across multiple phases of drug discovery throughout Philochem AG (a Swiss subsidiary of the Philogen group) first as a research scientist before taking on the role of Deputy Head of Chemistry. He worked on the development of the DNA-encoded chemical library platform and on multiple medicinal chemistry projects. Etienne joined Monte Rosa Therapeutics in 2021 and is currently an Associate Director in chemistry where is thriving to develop novel molecular glue degraders on various indication areas. Etienne is a named inventor on 6 patent applications and has authored more than 20 scientific publications.

Making and Breaking of C-S Bonds Using Metal Catalysis (IL15)

Dr Ivana FLEISCHER

UNIVERSITY OF TÜBINGEN, Tuebingen, Germany

Genochemetic Diversification of Natural Products (IL13)

Prof. Rebecca GOSS

UNIVERSITY OF ST ANDREWS, St Andrews, United Kingdom

Chemical Probes and their Relevance for Drug Discovery Programs – Examples from the Endocannabinoid System (IL05)

Dr Uwe GRETHER

F. HOFFMANN-LA ROCHE, Basel, Switzerland
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Dr Uwe GRETHER

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"Chemical Probes and their Relevance for Drug Discovery Programs – Examples from the Endocannabinoid System"

Chemical probes are of utmost importance for bringing drugs from the laboratory through the clinic and ultimately to the market. Optionally, they can carry one or more additional reporter groups to meet specific application requirements. Chemical probes support and affect all research and discovery phases: target verification and validation; assay development; lead optimization; and biomarker engagement in the context of preclinical studies and human trials. On the example of the cannabinoid receptor type-2 (CB2R) and monoacylglycerol lipase (MAGL), two highly health-relevant targets of the endocannabinoid system, the design, synthesis and application of chemical probes in different research and development stages will be discussed.

Novel Modes of Enzyme Inhibition (IL26)

Dr Anders JOHANSSON

ASTRAZENECA, Molndal, Sweden
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Dr Anders JOHANSSON

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"Novel Modes of Enzyme Inhibition"

Achieving good oral bioavailability and high potency can be a challenge, especially for intracellular protein targets. For certain enzymes, we have discovered a novel mode of inhibition, allowing for the optimization of permeability and bioavailability, but at the same time achieving high potency inhibitors of the target enzyme.

Multicomponent Alkene Cross-Coupling by Base Metal Catalysis (IL20)

Dr Ming Joo KOH

NATIONAL UNIVERSITY OF SINGAPORE, Singapore, Singapore

The beautiful simplicity of rearrangements – towards ideal reactions? (IL10)
Chemistry Europe Speaker

Prof. Nuno MAULIDE

UNIVERSITY OF VIENNA, Vienna, Austria
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Prof. Nuno MAULIDE

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"Can Chemistry Generate Biological Questions?"

Can chemical curiosity be the driving force behind biology? In this talk we will address selected case studies from our own research which aim to showcase how chemical ingenuity and “blue skies curiosity” can be harnessed for valuable contributions to biological problems.

From BRD4 to KRAS: 12 Years of Oncology Small Molecules (IL16)

Dr Darryl MCCONNELL

BOEHRINGER INGELHEIM, Vienna, Austria
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Dr Darryl MCCONNELL

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"From BRD4 to KRAS: 12 Years of Oncology Small Molecules"

Twelve years ago, one of the hottest oncology targets was the epigenetic reader protein BRD4 which contains a highly druggable pocket for small molecules. Now the field is focused on drugging KRAS which contains arguably the most difficult to drug pocket medicinal chemists have faced to date. The talk will replay the highlights and challenges of this twelve year journey at Boehringer Ingelheim.

Structure Based Identification of Novel Albumin Binders for Half-Life Extensions of Proteins and Peptides (IL11)

Dr Maria MÉNDEZ PÉREZ

SANOFI, Frankfurt, Germany
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Dr Maria MÉNDEZ PÉREZ

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Dr. María Méndez Pérez is currently the head of SMD Medicinal chemistry and global IDD portfolio coordinator at Sanofi. Her team focuses on supporting drug-discovery programs in the areas of immunology and neurological diseases, focusing thereby on the implementation of novel technologies and workflows with the aim to shorten the DMTA cycle. María obtained her Ph.D. in organic chemistry from the Universidad Autónoma of Madrid in 2001, followed by postdoctoral research in catalysis at the MPI in Mülheim an der Ruhr and in theoretical chemistry at the TU in Berlin. She started her industrial career at Sanofi in 2006, where as medicinal chemist, she has worked with several target classes, modalities and disease areas in all discovery phases. As project leader or co-leader, she has contributed to the delivery of clinical candidates in the areas of diabetes and neuroscience.

Innovation in Synthetic Fluorine Chemistry through Use of Flow (IL02)

Prof. Timothy NOËL

UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands

Synthesis of Glycosylated Natural Products or Analogues of Biological Interest (IL17)

Dr Stéphanie NORSIKIAN

INSTITUT DE CHIMIE DES SUBSTANCES NATURELLES, Gif-sur-Yvette, France

Phenotypic Screen to NLRP3 lead (IL12)

Dr Daniel OEHLRICH

JANSSEN RESEARCH AND DEVELOPMENT, Beerse, Belgium

Challenges and Opportunities in CNS Drug Discovery (IL07)

Dr Frauke POHLKI

ABBVIE, Ludwigshafen, Germany

Covalent Chemical Biology with Natural Products and Novel Synthetic Warheads (IL19)

Prof. Thomas POULSEN

AARHUS UNIVERSITY, Aarhus C, Denmark
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Prof. Thomas POULSEN

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Electrophiles are subject to strong interest within chemical biology and biomedicine. The discovery of novel, biologically relevant electrophiles can enable e.g. bioconjugation to native proteins for the preparation of biopharmaceuticals or provide new warhead-classes for targeted covalent inhibitors or fragments for screening. In my talk, I will provide examples from our most recent projects focused on electrophilic compounds, which span from fully synthetic constructs to natural products. I will discuss the different synthetic strategies involved and assessment of biological performance in biochemical and cellular contexts.

Enabling Technologies to Drive the MSD Portfolio (IL08)

Dr Rebecca RUCK

MERCK, SHARP & DOHME, Rahway, United States
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Dr Rebecca RUCK

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"Enabling Technologies to Drive the MSD Portfolio"

The development and application of new enabling technologies is critical to the ideal preparation of our Active Pharmaceutical Ingredients. This talk will include how we think about these investments and recent utilization.

Empowering Organic Synthesis: From Unique Methods to Complex Natural Products (IL09)

Prof. David SARLAH

UNIVERSITY OF ILLINOIS, Urbana, United States
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Prof. David SARLAH

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This talk will cover recent synthetic efforts from Sarlah Lab, ranging from bottom-up synthesis of aminoglycosides to highly strained peptides.

Novel, Reversible DCAF1 Ligands Expand the TPD-Toolbox (IL21)

Dr Martin SCHRÖDER

NOVARTIS, Basel, Switzerland
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Dr Martin SCHRÖDER

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Martin Schröder is a structural biologist with several years of experience in chemical biology and drug discovery. He is currently working as an Innovation Fellow in the Chemical Biology and Therapeutics department at Novartis with a focus of structure-guided drug design. While working in his PhD with the SGC, he contributed to the development and characterization of several chemical tool compounds. At Novartis he presently supporting several projects by providing biophysical assays and structural insights in ligand-protein complexes.

Dr Anna VULPETTI

NOVARTIS, Basel, Switzerland
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Dr Anna VULPETTI

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Anna Vulpetti has over 25 years of experience in drug discovery in Pharma, at Pharmacia & Upjohn, Pharmacia, Pfizer, and since 2006 at Novartis. She is an Associate Director and Senior Principal Data Scientist in the Global Discovery Chemistry department at Novartis with experience from hit finding technologies to hit-to-lead optimization. By working interdisciplinary across different disease areas, she impacted multiple pipeline projects through molecular designs and knowledge in structural chemistry and biophysics.

Machine Learning to Accelerate Design-Make-Test Cycles (IL18)

Dr Marwin SEGLER

MICROSOFT RESEARCH, Cambridge, United Kingdom

Natural Product Synthesis Through the Lens of Informatics (IL27)

Prof. Ryan SHENVI

SCRIPPS RESEARCH, La Jolla, United States

Disrupting the YAP-TEAD Protein-Protein Interaction with Small Molecules - Discovery of Drug Candidate NVP-IAG933 (IL22)

Dr Nicolas SOLDERMANN

NOVARTIS, Basel, Switzerland

Development of Selective mTOR Inhibitors for the Treatment of Cancer and Neurological Disorders (OC05)

Dr Chiara BORSARI

UNIVERSITY OF MILAN, Milan, Italy

EFMC-YMCS 2022 Best Oral Communication (OC09)
Epitope Identification Using In-Silico Approaches, a Case Study: Nanobodies Binding to MGlu5 Receptor

Ms Floriane ESHAK

UNIVERSITY PARIS CITÉ, Paris, France

Direct Access to Unnatural Drug-Like Molecules by Photocatalytic Late-Stage Functionalization (OC07)

Prof. Olga GARCIA MANCHENO

UNIVERSITY OF MÜNSTER, Münster, Germany
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Prof. Olga GARCIA MANCHENO

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Prof. Dr. Olga García Mancheño is professor for organic chemistry at the University of Münster (WWU). She obtained her PhD in Chemistry in 2005 at the University Autonomous of Madrid under the supervision of Prof. J.C. Carretero. After her postdoc in the group of Prof. C. Bolm at RWTH Aachen, she carried out her habilitation at the WWU Münster. In 2013, she was appointed as professor for organic chemistry at the University of Regensburg and, in 2017, to her current position at the University of Münster. Her research aims at developing new, efficient synthetic methodologies in organic chemistry, with especial focus on the design of novel catalytic systems and their application in catalysis, including photocatalysis and asymmetric anion-binding catalysis, and late-stage functionalization towards valuable small and drug building-blocks.

Selected Awards: International Isotope Society IIS-CED Prize 2022, ORCHEM EJOC Lecture Award 2022, ERC Consolidator Grant (2017), ORCHEM Prize 2016, Young Researcher Award WWU Münster (2013), Thieme Chemistry Journal Award 2012, Extraordinary Doctorate-Award 2006 (U.A.M.), Lilly Investigation Award, Spanish II Edition (2004).

Isolation and Biological Activities of Natural Products and Analogues from the Adriatic Coral Eunicella Cavolini (OC02)

Prof. Dean MARKOVIC

UNIVERSITY OF RIJEKA, Rijeka, Croatia
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Prof. Dean MARKOVIC

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Dean Marković studied at the Faculty of Science, University of Zagreb and received his PhD at EPF-Lausanne (2005) mentored by Prof. dr. sc. Pierre Vogel. After postdoctoral studies at Yale University (2006) and UIUC Urbana-Champaign (2007) in the group of prof. dr. sc. John Hartwig as a fellow of the Swiss National Science Foundation and F. Hoffmann-La Roch Foundation, he held the position of scientific associate at EPFL (2008-2011). He completed his habilitation at the University of Paris Descartes (2012). As an associate professor, he teached at the University of Osijek (2015-2016) and at the University of Rijeka (2016-2021), where he was promoted to full professor in 2021. He was a visiting professor at the University of Rijeka (2010-2012) and at Riga Technical University (2016) and at the University of Picardy Jules Verne (2017). His research interests include the chemistry of natural compounds, novel CO2 catalytic methodologies, mechanistic studies and physical-organic aspects of metal-catalyzed reactions, and CO2 chemistry.

High-Throughput Protac Synthesis and Direct to Biology Assaying for Rapidly Evaluating Targeted Protein Degradation (OC04)

Dr Afjal MIAH

GLAXOSMITHKLINE, Stevenage, United Kingdom
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Dr Afjal MIAH

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Afjal joined GSK in 2006 and has worked on multiple hit-to-lead and lead optimisation projects in respiratory, immuno-inflammation and cancer. Afjal has been working in the targeted protein degradation field since 2012, where he has gained extensive experience leading projects in discovery and lead optimisation of PROTACs and E3 ligases. He helped design and manage the development of GSK’s proprietary PROTAC monomer library, and more recently, Afjal has collaborated with GSK's Discovery High Throughput Chemistry (DHTC) group, to develop an integrated biology and chemical screening platform (D2B) for the synthesis of PROTACs. This is now routinely used by all PROTAC projects in an HTC fashion and has had significant impact on reducing cycle times.

His research interests include new modalities in protein degradation such as molecular glues, novel E3 Ligases and the ubiquitin proteasome system.

RSC Medicinal Chemistry Lectureship
Time to Shine for Constrained Peptides in Medicinal Chemistry (OC11)

Prof. Christoph NITSCHE

AUSTRALIAN NATIONAL UNIVERSITY, Canberra, Australia

Design and Optimization of High Performance KSPi ADCs With Increased Tumor Selectivity: Enhancing the Therapeutic Window by Legumain-Mediated ADC Activation (OC03)

Dr Anne-Sophie REBSTOCK

VINCERX, Monheim am Rhein, Germany
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Dr Anne-Sophie REBSTOCK

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Anne-Sophie Rebstock graduated from INSA Rouen, a french engineering school, in 2001. She obtained a PhD in organic chemistry in 2004 in Pr. Quéguiner Group under the supervision of Prof. Mongin. After 2 postdocs in medicinal chemistry in Johnson & Johnson and the Wolston institute for Biomedical Research, she worked in Bayer for 14 years, both in the Cropscience and Pharma divisions. In 2022, she joined Vincerx Pharma as head of medicinal chemistry where she is thriving to develop Vincerx’ innovative bioconjugation platform to further improve safety in both the small molecule and antibody drug conjugates fields. Anne-Sophie has contribued to 13 papers and 55 patents.

Discovery of Imidazo[1,2-a]Pyridine Carboxamide BAY 1165747, a Long-Acting Soluble Guanylate Cyclase Stimulator for Resistant Hypertension (OC06)

Dr Alexandros VAKALOPOULOS

BAYER, Wuppertal, Germany
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Dr Alexandros VAKALOPOULOS

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Alexandros studied chemistry at the University of Hannover in Germany and received his PhD in 2000 in the field of marine natural product synthesis. He began his industrial career at Bayer in the field of semi-synthetic pharmaceutical active compounds based on natural products in 2001. He then worked as a medicinal chemist on various indication areas in Drug Discovery and made numerous contributions to various development assets in the field of cardiovascular and oncological diseases. In addition to his experience in the hit-to-lead process and late research projects, he also dealt in depth with DMPK topics and DEL chemistry. Alexandros has contributed to 87 scientific papers and patents.

Cocktails For 19F NMR Fragment Screening: From Theory to Applications Using Enamine’s Stock Chemical Space (OC08)

Prof. Dmytro VOLOCHNYUK

ENAMINE LTD, Kyiv, Ukraine
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Prof. Dmytro VOLOCHNYUK

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Prof. Dmitriy Volochnyuk at present shares his time as senior scientific advisor of ENAMINE LTD, Head of Medicinal Chemistry Department at the Institute of Organic Chemistry NAS of Ukraine and Professor of Chemistry at the Institute of High Technologies of Taras Shevchenko National University of Kyiv. He received his PhD in Organic Chemistry in 2005 and Dr.Sci in Organic and Organomettalic Chemistry in 2011. Having been previously working at the key positions in CRO industry (2006–2010: Director of Chemistry at Enamine Ltd; 2010–2014: Executive Director at Curplyx–Macrochem; 2014 – 2017: New business development director at Life Chemicals), Prof. Volochnyuk has over 15-year experience in managing chemical outsourcing projects and is an expert in fluoroorganic, organophosphorus, heterocyclic, combinatorial and medicinal chemistry as well as in cheminformatics. He is an author of more than 180 scientific publications and 3 monograph chapters.

First time disclosure
Discovery of the clinical candidate BI 1810631 (Zongertinib), a Selective HER2 Inhibitor for the Treatment of HER2 Exon 20 Insertion Driven Tumors (OC10)

Dr Birgit WILDING

BOEHRINGER INGELHEIM, Vienna, Austria
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Dr Birgit WILDING

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Birgit Wilding is a Scientific Director in Medicinal Chemistry at Boehringer Ingelheim in Vienna, Austria. Since joining Boehringer Ingelheim in 2018, Birgit has led and impacted several drug discovery programmes in oncology research, and successfully delivered three development candidates. Birgit obtained her PhD in organic synthesis and biocatalysis at Graz University of Technology, in collaboration with the Austrian Centre of Industrial Biocatalysis (acib), followed by a position as postdoctoral researcher at acib. She then moved to the CRUK Drug Discovery Unit at the Institute of Cancer Research in London, UK as Postdoctoral Fellow in Synthetic Medicinal Chemistry. As medicinal chemist, Birgit has worked across modalities, including small molecule reversible and covalent inhibitors, as well as degraders, in early as well as late-stage projects. At both, the Institute of Cancer Research and Boehringer Ingelheim, Birgit contributed to drug discovery programmes which resulted in compounds now investigated in clinical trials.

Divergent Synthesis as an Emergent Tool for Drug Discovery (OC01)

Prof. Alexandros ZOGRAFOS

ARISTOTLE UNIVERSITY OF THESSALONIK, THESSALONIKI, Greece
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Prof. Alexandros ZOGRAFOS

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Alexandros L. Zografos graduated as a chemist in 1996 from National University of Athens. After earning his PhD in 2001 under the supervision of Prof. Olga Igglessi-Markopoulou at National Technical University of Athens, he pursued postdoctoral studies first at The Scripps Research Institute, under the guidance of Prof. Phil S. Baran and then at Columbia University with Prof. Scott Snyder, before moving back to Greece to work as a senior researcher at National University of Athens and at NCRS Demokritos Institute. In 2009, he began his independent career at Aristotle University of Thessaloniki where currently he is Associate Professor. He is recipient of Hildegrad award of the National Academy of Athens and the Fulbright Visiting Scholar Award. His group is working on the exploration of divergent total synthesis of natural products and the development of biomimetic methodologies for the aerobic oxidation of complex substrates.