3rd Alpine Winter Conference on Medicinal and Synthetic Chemistry

KL01 - Attenuating Oncogenic Transcription with Small Molecules

Prof. Angela KOEHLER

MIT KOCH INSTITUTE FOR INTEGRATIVE CANCER RESEARCH, Cambridge, United States
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Prof. Angela KOEHLER

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Angela Koehler is the Samuel A. Goldblith Career Development Professor in Applied Biology in the Department of Biological Engineering at MIT and an intramural member of the David H. Koch Institute for Integrative Cancer Research at MIT. She is also an Institute Member of the Broad Institute and a Founding Member of the MIT Center for Precision Cancer Medicine. Her research group aims to discover and develop functional small-molecule probes of targets emerging from patient-based genomics, including targets deemed recalcitrant to small molecule drug discovery efforts, such as transcription factors, RNA-binding proteins or cytokines. Selected probes may be developed into imaging agents, diagnostic tools, or therapeutic leads.

Angela received her B.A. in Biochemistry and Molecular Biology from Reed College in 1997. There she worked under the guidance of Professor Arthur Glasfeld on structural and biochemical studies of proteins that recognize tRNA or DNA. In 2003, she received her Ph.D. in Chemistry from Harvard University where she worked with Professor Stuart Schreiber to develop novel technologies for identifying and characterizing interactions between proteins and small molecules. Upon graduation, she became an Institute Fellow in the Chemical Biology Program at the Broad Institute and a Group Leader for the NCI Initiative for Chemical Genetics.

At MIT, Angela serves at the Faculty Director of the High-Throughput Sciences Facility in the Swanson Biotechnology Center. She is a co-Director of the MIT Biomedical Engineering Undergraduate Program and a member of the Committee on Pre-Health Advising. Angela has served on the Chemists in Cancer Research Executive Advisory Board for AACR. Awards include being named a Genome Technology Young Investigator and a Broad Institute Merkin Fellow as well as the Novartis Lectureship in Chemistry, the Ono Pharma Breakthrough Science Award, the AACR-Bayer Innovation and Discovery Award and the MIT Junior Bose Award for Excellence in Teaching. Angela serves as a consultant or scientific advisory board member to several pharmaceutical or biotechnology companies and has founded two biotechnology companies, Ligon Discovery and Kronos Bio.

KL03 - Functionalization of N-Heterocycles using Li, Mg, and Zn Organometallics

Prof. Paul KNOCHEL

LUDWIG MAXIMILIANS UNIVERSITY, Munich, Germany
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Prof. Paul KNOCHEL

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http://www.knochel.cup.uni-muenchen.de/index.php?id=8,0,0,1,0,0

Paul Knochel was born 1955 in Strasbourg (France). He did his undergraduate studies at the University of Strasbourg (France) and his Ph.D at the ETH-Zürich with Prof. D. Seebach. He spent 4 years at the CNRS at the University Pierre and Marie Curie in Paris with Prof. J.-F. Normant and one year of post-doctoral studies at Princeton University in the laboratory of Prof. M. F. Semmelhack. In 1987, he accepted a position as Assistant Professor at the University of Michigan. In 1991, he became Full Professor at this University and in 1992, he moved to Philipps-University at Marburg (Germany) as C4-Professor in Organic Chemistry. In 1999, he moved to the Chemistry Department of Ludwig-Maximilians-University in Munich (Germany). His research interests include the development of novel main-group organometallic reagents for organic chemistry, asymmetric catalysis and natural product synthesis. Prof. Knochel received many distinguished prices as e.g. the Berthelot Medal of the Academie des Sciences (Paris) (1992), the IUPAC Thieme Prize (1994), the Otto-Bayer-Prize (1995), the Leibniz-Prize (1996), the Arthur C. Cope Scholar Award (2005), Karl-Ziegler-Prize (2009), the Nagoya Gold Medal of Organic Chemistry (2012), the H. C. Brown Award (2014) and Paul Karrer gold medal (2015). He is author of over 900 publications (H index = 97).

KL02 - Drug Discovery: Where are we Headed?

Dr Wendy YOUNG

MPM CAPITAL, Brisbane, CA, United States
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Dr Wendy YOUNG

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Wendy Young is a biotechnology, pharma, and life sciences executive and board advisor with more than 25 years of experience in the discovery and development of innovative new medicines for patients. Wendy has held key senior roles at Genentech, Celera Genomics, and Johnson & Johnson Company. Prior to joining MPM, Wendy was the Senior Vice President at Genentech where she actively built and led the small molecule drug discovery organization. Under her leadership, more than 25 clinical candidates, in the areas of oncology, immunology, neurology, and anti-infectives, progressed into development. Additionally, Wendy led the BTK discovery program and is co-inventor of fenebrutinib which is currently in Phase 3 trials for multiple sclerosis. Prior to joining Genentech, Wendy held roles of increasing scientific leadership at Celera Genomics and Scios, a J&J company. Wendy is an inventor and/or author on more than 70 published patents and manuscripts. Known for her strong passion and contributions within the scientific community, Wendy has been involved with the American Chemical Society (ACS) for 20 years. In 2017, she was elected as the ACS National Chair of the Medicinal Chemistry Division (MEDI), and she currently serves as an associate editor of The Journal of Medicinal Chemistry. In 2018, Wendy was inducted as an ACS Fellow for her lifelong service to chemistry, society and medicine, and in 2019 highlighted as “One of the Top 20 Women in Biopharma” by Endpoint News. In 2020 she was awarded the prestigious Earle B. Barnes Award for Leadership in Chemical Research Management. Wendy earned her Ph.D. from Princeton University, having studied in the laboratories of Edward C. Taylor. At Princeton, and in collaboration with Eli Lilly, Wendy worked on folate analogs as antitumor agents and Alimta® was an outcome of this collaboration. Thereafter, as an American Cancer Society Fellow, she performed post-doctoral studies in the laboratories of Samuel Danishefsky at Sloan-Kettering Cancer Center and was part of the team that completed the total synthesis of Taxol®.

IL23 - Flow-based Methods for Chemical Peptide and Protein Synthesis".

Prof. Nina HARTRAMPF

UNIVERSITY OF ZURICH, Zürich, Switzerland
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Prof. Nina HARTRAMPF

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Nina Hartrampf is an Assistant Professor at the University of Zurich in Switzerland. Her group’s current research interests are the development of new flow-based methods for peptide synthesis and modification, and their application to the investigation of post-translationally modified peptides and proteins.

She received her Bachelor’s degree in Chemistry and Biochemistry as well as a Master’s degree in Chemistry from the Ludwig-Maximilians-Universität München. In 2013, she joined the group of Prof. Dr. Dirk Trauner for her graduate studies in natural product synthesis. After graduating in 2017, she joined the group of Prof. Bradley L. Pentelute at Massachusetts Institute of Technology. Her postdoctoral work focused on the rapid high-fidelity synthesis of peptides and proteins using automated flow chemistry. Additional work included reaction development in flow, development of peptide-drug conjugates for targeted delivery and the synthesis of nonribosomal peptides. In March 2020, she started her independent career in the Department of Chemistry at the University of Zurich as Assistant Professor for “Next Generation Synthesis” (tenure track).

In 2019, her work was acknowledged with a “Bert Schram Award“ of the American Peptide Society, and in 2021 she was awarded the “Bachem Award for Peptide Science” by the Austrian Peptide Society.

IL24 - Prins Cyclization in Natural Product Synthesis

Prof. Ang LI

SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, Shanghai, China
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Prof. Ang LI

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Ang Li was born in Jilin, China. He obtained his B.Sc. degree at Peking University (China), where he worked with Prof. Zhen Yang. He earned his Ph.D. degree at The Scripps Research Institute (USA) in 2009 and carried out postdoctoral research at Institute of Chemical and Engineering Sciences (Singapore) in 2010, under the supervision of Prof. K. C. Nicolaou. He joined the faculty of Shanghai Institute of Organic Chemistry (SIOC), Chinese Academy of Sciences in 2010. He works on the chemical synthesis of natural products and elucidation of their modes of action. He received Tetrahedron Young Investigator Award for Organic Synthesis in 2017 and Thieme−IUPAC Prize in Synthetic Organic Chemistry in 2020.

IL25 - Taming Multifaceted Nickel Catalysts: An Academic Fascination

Prof. Ruben MARTIN

INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA, Tarragona, Spain
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Prof. Ruben MARTIN

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Ruben Martin was born in Barcelona in 1976. He received his Ph.D in 2003 at the Universitat de Barcelona with Prof. Antoni Riera, working on the total synthesis of glycosidases inhibitors. In January 2004 he moved to the Max-Planck-Institut für Kohlenforschung as a Humboldt postdoctoral fellow with Prof. Alois Fürstner, where he worked on the application of novel iron catalysts for cross-coupling and Alder-ene type reactions. In September 2008 he joined the ICIQ as a group leader. His current research interests concern the discovery and development of synthetically useful organometallic methodologies. Rubén Martín was promoted to Associate Professor in July 2013.In october 2013, he became ICREA (Catalan Institution of Research and Advanced Studies) Research Professor. During his time at ICIQ, he has received the 2010 RSEQ Young Investigator Award, 2011 Thieme Chemistry Journal Award, 2011 Eli Lilly Young Research Investigator Award, 2015 RSEQ Excellent Research Award, 2011 ERC Starting Grant, 2017 Marcial Moreno Lectureship Award, 2017 OMCOS Award, 2017 Liebig-Lectureship Award, 2018 Pharmaron Lectureship Award, 2018 Bristol-Myers-Squibb Lectureship Award, 2018 Genentech Lectureship Award, 2018 ChemSocRev Pioneering Investigator Award, 2018 Hirata Award, 2018 IOCF Lectureship Award, 2018 Banc Sabadell Award to Sciences and Engineering, 2019 ParazaPharma Lectureship Award, 2019 Boehringer Ingelheim Award, 2019 MIT/Merck Lectureship Award, 2019 Novartis Chemistry Lectureship Award and 2020 Arthur C. Cope Scholar Award.

IL26 - Computationally Augmented Total Synthesis

Dr Timothy NEWHOUSE

YALE UNIVERSITY, New Haven, United States
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Dr Timothy NEWHOUSE

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Tim was born in New Hampshire and grew up in New England, northeastern U.S. He received his B.A. in Chemistry from Colby College (2005) in Waterville, ME, where he was mentored by Prof. Dasan M. Thamattoor. He completed his Ph.D. studies in 2010 at The Scripps Research Institute in La Jolla, CA, with Prof. Phil S. Baran. During his time at Scripps, he also worked in the laboratories of Prof. Donna G. Blackmond. He then returned to the east coast for postdoctoral studies with Prof. E.J. Corey at Harvard University. He joined the faculty at Yale in 2013, and as of 2018 he is an Associate Professor at Yale University in the Department of Chemistry. Tim’s research focuses on computational strategies and synthetic methodologies. He has received numerous awards, including the ACS Cope Scholar award, NSF CAREER Award, Sloan Research Fellowship, Camile Dreyfus Teacher Scholar Award, Genentech Research Innovation Award, and Amgen Young Investigator Award.

IL09 - Enabling Fragment-based Drug Discovery (FBDD) with Automated Synthesis Technologies

Dr Rachel GRAINGER

ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
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Dr Rachel GRAINGER

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Rachel Grainger obtained her MChem from University of Bath in 2010, before moving to Queen Mary University of London to complete her PhD on transition metal catalysis with Prof. Igor Larrosa. She spent two years working with Prof. Matthew Gaunt at the University of Cambridge as a Postdoctoral Research Associate focussing on the development of nanoscale HTE for organic synthesis. In March 2017 she joined Astex Pharmaceuticals’ Sustaining Innovation Postdoctoral program where she established automated synthesis capabilities (HTE and flow) within the company. As of 2019, Rachel is Senior Research Associate in Astex’s Synthesis Technology Group, her role involves the development and implementation of cutting-edge technologies (robotic enabled HTE, photoredox, flow etc.) to enable synthetic challenges on live drug discovery projects.

IL10 - Rapid Development of Robust Reactions and Multi-Step Syntheses

Prof. Alexei LAPKIN

UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
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Prof. Alexei LAPKIN

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Alexei Lapkin graduated with an MChem from Novosibirsk State University, specialising in membrane gas separation. He then worked at Boreskov Institute of Catalysis prior to moving to the University of Bath where he was employed as a research officer, which allowed him to complete his PhD in the area of multiphase membrane catalysis. His research interests are digitalisation of R&D and developing clean chemical manufacturing processes.

IL11 - High-Throughput Experimentation Capabilities to Accelerate Discovery Chemistry

Dr Iulia STRAMBEANU

JOHNSON AND JOHNSON, King of Prussia, United States
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Dr Iulia STRAMBEANU

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Iulia joined Janssen in July 2019 and is the head of High-Throughput Experimentation within the Global Discovery Chemistry department, leading a global team to champion innovative chemistry technologies and platforms to accelerate drug discovery and early development. Iulia’s research expertise includes catalysis, automation and parallel chemistry techniques (HTE, parallel med chem) with a focus on solving problems on medicinal chemistry projects. Prior to Janssen, Iulia spent close to 5 years at GSK where she was part of both the Process and Medicinal Chemistry departments, applying HTE and catalysis to discover and develop more efficient routes to APIs. Iulia received her PhD in organic chemistry from University of Illinois, Urbana-Champaign in 2014, working with Prof. M. Christina White and her BA in Chemistry and Physics from Lake Forest College, IL.

IL01 - Intracellular Oligonucleotide Distribution and Protein Binding

Dr Alice GHIDINI

ASTRAZENECA, Gothenburg, Sweden
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Dr Alice GHIDINI

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Dr Alice Ghidini has a broad background in nucleic acids technology gained during her doctoral and postdoctoral studies in the labs of three pioneers of the field, Roger Stromberg (Karolinska Institute), Peter Dervan (California Institute of Technology), and Jonathan Hall (ETH Zurich). During her studies in their laboratories, she accumulated expertise on the interaction between oligonucleotides and proteins/RNA targets, specifically though her work on RNA-based artificial enzymes, PNA triplexes, and antisense technologies. She lately developed the first single strand oligonucleotide-based PROTAC proof of concept, designed to degrade RNA-binding proteins. In 2021 she joined the Oligonucleotide platform of AstraZeneca as an Assistant Principal Scientist in the Biophysics department where she is studying the influence of ASOs’ proteins binding on their toxicity and potency.

IL04 - Lessons in Transcellular Membrane Permeability Re-Learned

Dr Mike HANN

GSK MEDICINES RESEARCH CENTRE, Stevenage, United Kingdom
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Dr Mike HANN

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After completing his PhD in organic chemistry in 1980, Mike has worked in Pharma R&D initially as a medicinal chemist and then as a computational chemist. He joined Glaxo in 1986 and was responsible for helping initially build and then lead the computational chemistry department. He went on to lead the biophysics and protein crystallography activities including developing fragments theory and practice in lead identification. His current role is in looking at new technologies in early discovery to help reduce attrition in drug discovery, with particular interest in chemical biology, target tractability, drug distribution at cellular and subcellular resolution. Mike is a GSK Senior Fellow Alumni and an Adjunct Professor in the chemistry department at Imperial College London.

IL03 - Molecular Chameleonicity and Cell Permeability of Drugs and PROTACs in the bRo5 Space

Prof. Jan KIHLBERG

UPPSALA UNIVERSITY, Uppsala, Sweden
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Prof. Jan KIHLBERG

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Professor Jan Kihlberg holds a chair in Organic Chemistry at Uppsala University, Sweden since 2013. His key research interests are to understand what properties convey cell permeability, aqueous solubility and target binding to drugs and PROTACs in the beyond rule of 5 space and to translate this knowledge into guidelines for design. His group is also involved in synthesis of macrocycles as ligands for difficult-to-drug targets. He has published 167 peer reviewed articles, 16 research reviews and four book chapters Before moving to Uppsala Prof. Kihlberg spent ten years at AstraZeneca R&D in Gothenburg, seven of which as Director of Medicinal Chemistry. He obtained his PhD in organic chemistry at Lund University in 1988.

IL02 - Monitoring Drug Selectivity and Target Engagement Across Systems – Thermal Shift Assay in Drug Discovery

Dr Anna RUTKOWSKA-KLUTE

GSK, Heidelberg, Germany
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Dr Anna RUTKOWSKA-KLUTE

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After completing her PhD in molecular biology, Anna has worked as postdoc at European Molecular Biology Laboratory (EMBL) Heidelberg in the field of chemical biology. At Cellzome/GSK since 2014, Anna was first focusing on the development of methods to measure direct drug-target binding in cellular systems (e.g. the thermal shift assay, the click-probe based approach) as well as their application to support drug discovery at GSK and to and cellular drug disposition. Currently, Anna is a GSK Associate Fellow and works as a Scientific Leader in the Functional Genomics department leading the Cellular Assays and Biomarker Group aiming on in depth pre-clinical characterization of drug mode of action to support development of new treatments in the context of oncology diseases.

IL17 - Concept of Pharmacologic Target-Mediated Drug Disposition (TMDD) in Large-Molecule and Small-Molecule Compounds

Prof. Guohua AN

THE UNIVERSITY OF IOWA COLLEGE OF PHARMACY, Iowa City, United States
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Prof. Guohua AN

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After receiving her MD from Taishan Medical College and MS in Clinical Pharmacology from Fudan University, Dr. An joined Ruijin Hospital for 2 years as a clinical pharmacist and research scientist. Then she pursued a further study and got her PhD degree in Pharmaceutical Sciences from SUNY at Buffalo. Her graduate research focused on the role of transporter on the pharmacokinetics and pharmacodynamics of anticancer agent. Her research was further expanded after she joined the R&D group of Abbott, where she gained extensive hands on experience in clinical drug development, PK/PD modeling and simulation. Prior to joining University of Iowa, Dr. An has worked at University of Florida as an Assistant Professor for one and half years. Her research interests include building mechanism-based pharmacokinetic and pharmacodynamic modeling of small molecules (such as tysosine kinase inhibitors) and large molecules (such as Epo); understanding the mechanisms of poor brain penetration and offering novel approaches to overcome it; evaluating the transporter- and enzyme-based herbal-drug interactions.

IL18 - Understanding the PKPD and ADME of PF-07059013: An Allosteric Modulator of a High Abundance Target

Dr Kevin BEAUMONT

ASTRAZENECA, Cambridge, United Kingdom
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Dr Kevin BEAUMONT

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Kevin Beaumont has worked in the pharmaceutical industry for 37 years. Throughout that time he has worked extensively in the drug metabolism field, especially as it relates to drug discovery support. His major area of expertise is in the modulation of physicochemistry to affect drug disposition and in prediction of human pharmacokinetics. He is author on over 50 peer reviewed publications. Kevin has spent the majority of his career at Pfizer in both the UK and US. In 2020,Kevin returned to the UK and is currently with AstraZeneca supporting Oncology R&D with DMPK expertise.

IL16 - General Introduction to TMDD

Dr David FAIRMAN

GSK, Cambridge, United Kingdom
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Dr David FAIRMAN

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David Fairman is a Senior Director in the Clinical Pharmacology, Modelling and Simulation group at GSK. He specialises in translational pharmacology within the early drug development phase and biologics PKPD. He has worked extensively on developing translational mechanistic models and leading collaborations developing QSP models covering areas including asthma and diabetes. Previous experience includes translational and clinical PKPD modelling at MedImmune and preclinical modelling at Pfizer (Sandwich UK). David has a BsC in pharmacology from the Open University, an MsC in Modelling & Simulation from the University of Manchester and has authored or co-authored over 15 scientific papers and is a co-inventor on patents covering 4 novel biological agents.

IL19 - Importance of Mechanistic Models in AHD Prediction (IL)

Dr Birgit SCHOEBERL

NOVARTIS INSTITUTE FOR BIOMEDICAL RESEARCH, Cambridge, MA, United States
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Dr Birgit SCHOEBERL

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Dr. Birgit Schoeberl currently serves a Global Head of Modeling and Simulation, PK Sciences at Novartis. Before joining Novartis, Birgit served as interim Senior Vice President, Scientific Value, at GNS Healthcare. During her time at GNS, she focused on applying causal machine learning to drug development. Prior to GNS, she was a member of the founding team at Merrimack Pharmaceuticals and where she spent over 12 years in different roles. In her latest role as Head of Discovery and Early Development, she gained broad experience in oncology drug discovery and development. Birgit and her leadership team were responsible for multiple preclinical and early clinical programs. Birgit received her Chemical Engineering degree from the Technical University in Karlsruhe, Germany, and her Ph.D. in Biological Engineering from the Max Planck Institute for Dynamics of Complex Technical Systems in Magdeburg. She was a post-doctoral fellow in the laboratories of Douglas Lauffenburger and Peter Sorger in the Biological Engineering Department at MIT.

OC06 - Towards the Design of Cell Division Cycle 25 Phosphatases Inhibitors as Anticancer Agents

Dr Carmen CERCHIA

UNIVERSITY OF NAPLES FEDERICO II, Naples, Italy
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Dr Carmen CERCHIA

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Dr Carmen Cerchia obtained the Ph.D. in Pharmaceutical Sciences in 2016 at the Department of Pharmacy, University of Naples Federico II, Italy, under the supervision of Prof. Antonio Lavecchia. She then joined the group of Prof. Jürgen Bajorath at the Department of Life Science Informatics, B-IT, Rheinische Friedrich-Wilhelms-Universität, Bonn, Germany, for one year, as visiting researcher. From 2018 to mid-2021, she held Postdoctoral Fellowships at Department of Pharmacy, University of Naples Federico II, where she has been appointed fixed-term researcher (RtdA) since December 2021. Her research interests are in the field of drug discovery and computational chemistry, in particular large-scale compound data mining and virtual screening methodologies applied to biological targets involved in cancer and metabolic diseases.

OC04 - Dissociative Inhibitors of Thymidylate Synthase Homodimer Accelerate its Proteasomal Degradation and Inhibit Cancer Growth in Vivo

Prof. Maria Paola COSTI

UNIVERSITY OF MODENA AND REGGIO EMILIA, Modena, Italy
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Prof. Maria Paola COSTI

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She has completed her Ph.D in Medicinal chemistry from the University of Modena and Reggio Emilia and was a visiting scientist at the University of California San Francisco (UCSF) in 1991. She is professor of Medicinal Chemistry at the Department of Life Science, leading the Drug discovery and biotechnology group. Her main field of research is the discovery and development of new drugs against the folate dependent enzymes and, more recently, relevant targets of the Hippo pathway. She has published about 170 papers and book chapters in international journals, 18 patents, and is serving as an editorial board member of some international journals. Member of the MITO oncology group, translational science, and other networks and foundation (Paul Erlich Network, ESF). Coordinator of several collaborative European projects and Programme (LIGHTS, NMTrypI, European Lead Factory QHL Programme Plan); scientific manager (Optobacteria, EUTransbio) or participant (MM4TB) and coordinator of different AIRC project (Associazione Italiana per la ricerca sul cancro). COST ACTIONS participant and vice-chair. She is a discoverer of new drug leads in the field of anti-Leishmania agents. She is a co-founder of two SMEs TydockPharma srl and QuadrEL srl.

OC05 - Rational Design of Light-Controlled Bioactive Compounds for Photopharmacology

Mr Piermichele KOBAURI

UNIVERSITY OF GRONINGEN FSSC, Groningen, The Netherlands
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Mr Piermichele KOBAURI

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Piermichele Kobauri obtained his MChem degree under the supervision of Prof. Marco Lolli at the University of Turin, Italy, working on the application of pharmacophore modeling and molecular docking for the design of strigolactone analogues. After his graduation in 2016, he completed internships at the University of Turin, designing and synthesizing compounds to target Leishmaniasis, and at the University of Copenhagen, Denmark, working on the development of GABA analogues. In March 2017 he started his Ph.D. under the guidance of Prof. Ben Feringa at the University of Groningen, focussing on rational, structure-based drug design approaches for photopharmacology

OC03 - Discovery of a Selective ALK2 Kinase Inhibitor for the Treatment of a Rare Genetic Bone Disease

Dr Thomas ULLRICH

NOVARTIS PHARMA AG, Basel, Switzerland
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Dr Thomas ULLRICH

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Thomas obtained his PhD from the University of Technology in Vienna, Austria, in 1999 and joined the National Institutes of Health in Bethesda, MD, as a Post-doctoral Fellow for two years working on the synthesis of opioid receptor ligands. He then started his industrial career with Novartis in Vienna before moving to Switzerland in 2008 and becoming a Group Leader and Director in Medicinal Chemistry. Thomas’s team has advanced several drug candidates into clinical trials to treat musculo-skeletal diseases, in particular rare bone disorders, sarcopenia, and tendon injuries.

IL12 - Exploring and exploiting propellanes

Prof. Ed ANDERSON

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Prof. Ed ANDERSON

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Ed Anderson is Professor of Organic chemistry at the University of Oxford. He has research interests across synthetic organic chemistry, with a particular focus on the development of new synthetic methods, and the synthesis of bioactive molecules. In the former area, his research encompasses catalysis (including transition metal, asymmetric, and photoredox catalysis), bioisosteres, the reactivity of heteroatom-substituted alkynes, and mechanistic study. His work in target-oriented synthesis included antiparasitic natural products, polyketides, and the development of cascade processes in synthesis. Ed was an undergraduate at Oxford, then moved to Cambridge for his PhD with Prof Andrew Holmes. After postdoctoral research with Profs Erik Sorensen (Scripps Research Institute) and Ian Paterson (Cambridge), he took up an EPSRC Advanced Research Fellowship at Oxford, and was appointed as a Lecturer in 2009, with promotion to Professor in 2016. He is the recipient of the 2019 Novartis Chemistry Lectureship and the 2020 RSC Bader award, and is currently the head of Organic Chemistry at Oxford.

IL15 - No Strain, No Gain: Advances in the Synthesis and Design of New Classes of Building Blocks

Prof. Kevin BROWN

INDIANA UNIVERSITY, Bloomington, United States
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Prof. Kevin BROWN

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Kevin grew up in the suburbs of Chicago and after graduating high school moved to central New York to pursue an undergraduate degree at Hamilton College. Here Kevin became interested in organic chemistry by working in the labs of Ian Rosenstein. Upon graduation, Kevin moved to Boston College and received his Ph.D. in organic chemistry with Professor Amir Hoveyda in 2008. C. Upon completion of his graduate studies he began a Ruth L. Kirschstein National Institutes of Health funded postdoctoral fellowship in the laboratories of E. J. Corey at Harvard University. In 2011, Kevin began his intendent academic career at Indiana University. He has initiated a program of research that is generally directed towards the development of new methods and strategies in chemical synthesis. For these efforts, Kevin has been awarded a Sloan fellowship, NSF CAREER awards and the Amgen and Novartis Early Career Awards. In 2017, Kevin was promoted to Associate Professor and in 2021 he was promoted to full Professor.

IL13 - The Next Generation of BCPs: Exploring Substitutions on the Bridge

Dr Xiaoshen MA

MERCK & CO., INC, Boston, United States
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Dr Xiaoshen MA

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I am currently a senior scientist in the Department of Discovery Chemistry at Merch Research Laboratories in Boston, Massachusetts. In addition to my research for pipeline programs, I also conduct independent research as side projects in the development of novel synthetic methods accessing pharmaceutically relevant structures. We recently reported a series of publications focused on the synthesis of novel bicyclo[1.1.1]pentanes (BCPs), especially BCP analogues with substituents on the methylene positions. I hope to share with you our journey towards the discovery of these methodologies as well as some unpublished results. Before joining Merck, I conducted my PhD studies under the supervision of Prof. Seth B. Herzon at Yale University focusing on the topics of alkene hydrofunctionalization via hydrogen atom transfer mechanism, late-stage C H functionalization of (+)-pleuromutilin derivatives, and the host-release-factor in 0marine symbiotic systems.

IL14 - Synthesis and Functionalization of Cyclopropane Derivatives

Dr Sophie ROUSSEAUX

UNIVERSITY OF TORONTO, Toronto, Canada
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Dr Sophie ROUSSEAUX

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Sophie Rousseaux is an Assistant Professor in the Department of Chemistry at the University of Toronto. She also holds a Canada Research Chair (Tier 2) in Organic Chemistry since 2016. Her group’s research interests include organic synthesis, catalysis, and organometallic chemistry. She is particularly interested in the synthesis and functionalization of small rings and nitrile-containing building blocks. Prior to joining the faculty at U of T in 2015, Sophie obtained her PhD from the University of Ottawa, working with Prof. Keith Fagnou and with Prof. Stephen L. Buchwald (MIT). She carried out postdoctoral studies as an NSERC postdoctoral fellow and Glasstone Research Fellow at the University of Oxford, working with Prof. Harry Anderson.

IL22 - Studies with Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors

Dr Agustin CASIMIRO-GARCIA

PFIZER, United States
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Dr Agustin CASIMIRO-GARCIA

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Agustin Casimiro-Garcia is an Associate Research Fellow in the Pfizer Medicine Design group in Cambridge, MA, USA. He has worked at Pfizer since 2000. His research at Pfizer has been in the areas of cardiovascular and metabolic diseases, inflammation and immunology disorders, fibrotic diseases, and more recently oncology. His current research interests include phenotypic drug discovery, covalent inhibition, and approaches to pursue challenging targets. Agustin obtained his Ph.D. in Medicinal Chemistry from Purdue University and carried out postdoctoral studies at Rensselaer Polytechnic Institute.

IL20 - Lysine-Targeting Covalent Inhibitors

Dr Matthew CHEESEMAN

THE INSTITUTE OF CANCER RESEARCH, Sutton, United Kingdom
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Dr Matthew CHEESEMAN

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I grew up in the seaside town of Weymouth in Dorset. I completed my undergraduate degree in Chemistry at The University of Bath in 2002; during my final year project with the late Professor Jonathan Williams, I discovered a passion for research in general and organic synthesis in particular. I was lucky enough to stay in Bath to carry out my PhD under the supervision of Professor Steven Bull, developing new methodologies for asymmetric synthesis exploiting temporary stereocentres. After completing my PhD in 2006, I joined the research group of Professor Timothy Donohoe as a Postdoctoral Fellow to complete my education in organic synthesis, working on the total synthesis of polyhydroxylated pyrrolizidine natural products. All my work had focused on synthesis of molecules rather than their application, so at this point in my career I decided to change tack, and despite no previous experience, I moved into Medicinal Chemistry by joining the team led by Professor Keith Jones at the Institute of Cancer Research as a Postdoctoral Training Fellow. After four years learning all aspects of medicinal chemistry and drug discovery, I was promoted to Staff Scientist and then in 2019 to Senior Staff Scientist, leading the medicinal chemistry optimisation of multiple projects and recently pushing the first compound my team designed into clinical trials, a challenging but exciting journey. I have a passion for all aspects of medicinal chemistry and chemical biology, and applying synthetic strategies to improve the efficiency of compound optimisation. Until the pandemic, I taught pharmacokinetics to students at Imperial College London, and my academic research interests have focused novel strategies to target difficult to drug proteins and covalent inhibitors, and have published over 30 papers. I currently live in Sutton in south London with my wife and 5-year-old daughter, who takes up most of our free time. Like most people during lockdown, we re-discovered our love for long walks, and hope very much in the near future, we will re-discover our love for travel!

IL21 - Reversible-covalent Inhibitors of the Kinase Activity of FGFR4

Dr Robin FAIRHURST

NOVARTIS, Basel, Switzerland
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Dr Robin FAIRHURST

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Robin is currently an Associate Director in the Oncology Chemistry Group in Basel, Switzerland, serving as a Project Leader/Medicinal Chemist. He has occupied this position since 2007, contributing to several kinase inhibitor projects including the PI3Kα selective inhibitor alpelisib, the pan-PI3K inhibitor CLR457, and the FGFR4 inhibitor roblitinib, and more recently he has been involved in the discovery of DFF332, an allosteric inhibitor of the transcription factor HIF2α. Prior to this Robin spent 11 years in the Respiratory Disease Chemistry Group within Novartis in Horsham, England, contributing to several GPCR and enzyme inhibitor projects including the discovery of the once-daily inhaled β2-adrenoceptor agonist indacaterol. Robin started his industrial career in Ciba Central Research, Macclesfield, England, joining an organophosphorus chemistry group exploring modified nucleic acids for antisense applications. A position he held up until the merger of Ciba with Sandoz in 1996 that resulted in the formation of Novartis. He received a PhD in Chemistry from the University of Loughborough working with Professor Harry Heaney developing synthetic methodology around acyliminium ion chemistry, and made Postdoctoral studies with Professor Philip Magnus at the University of Texas at Austin working on the synthesis of the enediyne natural product dynemicin.

OC01 - Design and Synthesis of Novel RNA Binders for Therapeutic Applications

Dr Maurinne BONNET

ICN, Nice, France
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Dr Maurinne BONNET

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Maurinne Bonnet obtained a French national degree (Agrégation) to teach in 2017. After one year teaching physics and chemistry at the high school, she finally obtained a master degree in Fragrances and Fine chemistry in 2019 under the supervision of Pr Véronique Michelet at the University of Côte d’Azur, Nice. During her internship, she was interested on the development of new methodology using gold catalysts for the cycloisomerisation of alkynes. Maurinne started then a PhD in medicinal chemistry and she is currently a third year PhD student. She is working under the supervision of Dr Maria Duca, head of Targeting Nucleic Acid group at the University Côte d’Azur, Nice on the design, synthesis and biological evalution of new RNA ligand for therapeutic applications.

OC02 - Is Resistance Futile? Discovery of Clinical Candidate AZD3229, A Pan-Mutant C-KIT Inhibitor

Dr James SMITH

ASTRAZENECA, Cambridge, United Kingdom
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Dr James SMITH

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Originally from Bristol, UK, I completed both my undergraduate MChem and PhD Chemistry degrees at The University of Manchester (PhD in synthetic organic chemistry under supervision of Prof. John D. Sutherland). Following this I completed post-doctoral studies first at the Institute of Cancer Research in London (oncology medicinal chemistry with Prof. Keith Jones), and then at the University of Edinburgh (synthetic organic chemistry with Prof. Michael Greaney). I next settled to continue research as a medicinal chemist in the field of cancer therapeutics at Cancer Research UK Discovery Laboratories (Cambridge, UK) in 2008. I moved to join AstraZeneca (Cambridge, UK) in 2014, where as an associate director I currently lead a team of medicinal chemists and have contributed to multiple cancer drug discovery projects across the AZ portfolio.

IL05 - Innovative Strategies to Target Non-Coding RNAs with Synthetic Ligands

Dr Maria DUCA

UNIVERSITY OF CÔTE D'AZUR, Nice, France
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Dr Maria DUCA

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Dr. Maria DUCA is head of Targeting of Nucleic Acids research group in the Institute of Chemistry of Nice (Université Côte d’Azur - CNRS). After undergraduate studies in Pharmacy and Medicinal Chemistry (Faculty of Pharmacy, University of Bologna, Italy), she obtained her PhD in Molecular Biochemistry under the supervision of Dr. Paola B. Arimondo (National Natural History Museum, Paris, France) working on topoisomerase II inhibitors. A 2- year post-doctoral training in Sydney Hecht’s lab (Department of Chemistry, University of Virginia, USA) allowed her to pursue the study of nucleic acids working on targeted protein mutagenesis. After CNRS recruitment as a Research Scientist in 2007, her research activities focus on the targeting of non-coding RNAs using synthetic small molecules toward innovative therapeutic approaches for anticancer, antiviral and antimicrobial applications.

IL07 - Drugging RNA – A Structure-based Approach

Dr Jacques DUMAS

ARRAKIS THERAPEUTICS, Boston, United States
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Dr Jacques DUMAS

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Jacques Dumas grew up in France and has 30-years experience in drug discovery and development. He is a co-inventor of two marketed drugs in Oncology, Nexavar® and Stivarga®.
In January 2020, Jacques joined Arrakis, an innovative biotech company dedicated to the discovery of small molecules targeting RNA. He is currently Chief Scientific Officer (CSO) and oversees all R&D functions. From 2015 to 2019, Jacques was CSO at Tetraphase, a publicly traded company focused on fully synthetic tetracyclines (acquired by La Jolla in 2020) and played a key role in the US and EU approvals of eravacycline, a broad-spectrum antibiotic. Before joining Tetraphase, Jacques was CSO at Idenix (acquired by Merck in 2014) working on liver-targeted nucleosides and their applications in HCV and HCC. From 2007 to 2014, Jacques worked at AstraZeneca, most recently as VP of Strategy, Infectious Diseases. Prior to that he spent 15 years at Bayer Healthcare in Leverkusen, Germany and West Haven, CT.
Jacques attended Ecole Normale Supérieure in Paris, France. He holds a Ph.D. in Organic Chemistry from Paris VI University, and completed a Post-doctoral Fellowship at Stanford University.

IL06 - Targeting Transcription Factors for Treating Human Cancers and Auto Immune and Inflammatory Diseases

Dr Doriano FABBRO

CELLESTIA BIOTECH AG, arlesheim, Switzerland
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Dr Doriano FABBRO

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Doriano Fabbro, PhD in Biology, has 30 years of experience in drug discovery in big Pharma (Ciba-Geigy, Novartis) and Biotech (Piqur Therapeutics) following 10 years in academia (PhD at the Biocenter Basel, Switzerland then as Junior Group Leader in the Molecular Tumor-Biology at the Department of Research of the University Basel, Switzerland before joining Ciba-Geigy in 1991).

Until 2005 he was Executive Director for the Oncology Drug Discovery effort at the Novartis Institute for Biomedical Research (NIBR) and member of the NIBR Oncology Advisory Board overseeing significant part of NIBR’s global Oncology Drug Discovery portfolio from target discovery to clinical development. From 2005 to 2012 he was Executive Director of the NIBR Expertise Platform Kinases dedicated to global Kinase Drug Discovery Projects including integrated lead finding (FBS/HTS), profiling (biochemical and cellular), expression and purification, X-ray and NMR, biophysical methods, cell biology, target validation, phospho-proteomic of all indication areas of Novartis (Oncology, Immunology, Inflammation, Respiratory Disease, Muscle, Cardiovascular). From 2012 until 2019 he was CSO of Piqur Therapeutics (Basel Switzerland), a small company devoted to the discovery of PI3K/mTOR inhibitors (PQR309 in Phase-1). Since 2020 he is VP Research at Cellestia Biotech Basel working on Notch inhibitors. He also scientifically advises several pharmaceutical companies in the area of kinase drug discovery.

During his career he contributed to the development of the approved drugs Glivec® (Imatinib, BcrABL inhibitor), Tasigna® (Nilotinib, 2nd gen. BcrAbl inhibitor), Scemblix® (Asciminib or STAMP, 3d gen. BcrAbl inhibitor), Afinitor® (Everolimus, mTOR inhibitor), Rydapt® (Midostaurin, Kit and Flt-3 inhibitor), Piqray® (Alpelisib, PIK3a inhibitor) and many other compounds that are still in in various clinical phases like, Buparlisip (BKM120, PI3K inhibitor), Leniolisib (CDZ173, PIK3Kd inhibitor), Luminespib (hsp90 inhibitor) and CB103 (Notch inhibitor)

IL08 - Design of Zotatifin (eFT226), a First-in-Class Inhibitor of the RNA Helicase eIF4A

Dr Christian NILEWSKI

GENENTECH, South San Francisco, United States
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Dr Christian NILEWSKI

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Christian Nilewski conducted his undergraduate studies at the University of Dortmund and the University of Münster in Germany. A synthetic organic chemist by training, he received his PhD in 2011 from ETH Zurich (Switzerland) under the supervision of Prof. Dr. Erick M. Carreira and conducted postdoctoral studies with Prof. K. C. Nicolaou at The Scripps Research Institute (La Jolla, California) and Rice University (Houston, Texas). Christian started his career as a Medicinal Chemist in 2014 at eFFECTOR Therapeutics in San Diego, California, where he was involved in several oncology drug discovery projects and contributed to the design and discovery of first-in-class small molecule inhibitors of eukaryotic initiation factors eIF4A (eFT226/zotatifin) and eIF4E (currently undergoing preclinical development in collaboration with Pfizer). In 2019, Christian joined Genentech in South San Francisco, California, as a Senior Scientist in the Small Molecule Discovery Chemistry Department.