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.

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.

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.

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.

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.

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)

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.