RICT 2023

PL10 - Modulation of Protein – Protein Interactions by Means of Peptidomimetics

Prof. Steven BALLET

VRIJE UNIVERSITEIT BRUSSEL, Brussels, Belgium

PL20 - Peptide, A Manifesto

Prof. Philippe KAROYAN

SORBONNE UNIVERSITÉ, VILLEBON SUR YVETTE, France

PL19 - Expansion of the Druggable Genome through Rational Approaches to Molecular Glue Discovery

Dr Rohan BECKWITH

NEOMORPH INC., San Diego, United States
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Dr Rohan BECKWITH

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Rohan Beckwith, Ph.D. is Vice President of Chemistry at Neomorph Inc., bringing over 20 years of experience in Drug Discovery, 10 in the field of targeted protein degradation. Prior to joining Neomorph, Rohan served as Director, Medicinal Chemistry at Novartis Institutes for BioMedical Research, Boston, USA. At Novartis, Rohan established a molecular glue degrader initiative, led the glue degrader platform, seeded several molecular glue degrader programs and delivered a clinical candidate. In addition to developing glue degraders for CRBN and DCAF15 E3 ligases, he also demonstrated that VHL could function as an effective glue ligase system. In addition, Rohan has worked on over 20 research projects across various therapeutic areas, such as HECT E3 ligase inhibitors, modulators of RNA processing, Wnt pathway modulators, IAP, spinal muscular atrophy, synthetic RNA delivery, cytokine receptors, chemokine receptors and kinases. He has led multi-disciplinary teams in chemical biology and target identification efforts, as well as hit-to-lead and lead optimization. Prior to joining Novartis, Rohan conducted postdoctoral training with Prof. Huw Davies in the field of rhodium carbenoid-mediated C-H activation. He received his Ph.D. in synthetic organic chemistry from University of Nottingham, U.K. and before that his MSci. Chem from Bristol University, U.K.

PL16 - Discovery of the Clinical Candidate ACT-777991, a Potent CXCR3 Antagonist with Therapeutic Potential in Autoimmune Diseases

Dr Eva CAROFF

IDORSIA PHARMACEUTICALS LTD, Allschwil, Switzerland
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Dr Eva CAROFF

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Eva Caroff studied science focusing on mathematics, physics and chemistry and obtained a MSc in Chemistry from the Haute Alsace University, France, combined with a Chemistry Engineering Diploma from the Ecole Nationale Superieure de Chimie de Mulhouse, France, in 1997. She performed her PhD studies under the supervision of Prof. W. D. Woggon at the Institute of Organic Chemistry in Basel, Switzerland.

Following post-doctoral studies in the group of Prof. S. Roberts at Liverpool University, UK, and at Axovan AG in Allschwil, Switzerland, Dr. Caroff joined Actelion Pharmaceuticals Ltd. in Allschwil, Switzerland, as a medicinal chemist, in 2003. Dr. Caroff started her career as a laboratory head and project leader, and evolved as a group leader, now working since 2018 at Idorsia Pharmaceuticals Ltd in Allschwil, Switzerland. As project leader, together with her team, Dr. Caroff discovered 2 molecules that are now undergoing clinical studies, namely selatogrel (phase 3 ongoing) and ACT-777991 (phase 1 completed).

Dr. Caroff and her group continue to aim at identifying novel drugs interfering with biological mechanisms associated with immune diseases. Dr. Caroff has published approx. 30 scientific papers and patent applications.

PL04 - Electrochemistry in High-Throughput

Dr Nessa CARSON

ASTRAZENECA, Macclesfield, United Kingdom
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Dr Nessa CARSON

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Nessa Carson was born in Warrington, England. She received her MChem degree from Oxford University, before completing postgraduate studies in catalysis and organic methodology at the University of Illinois at Urbana-Champaign.

She started in industry as a synthetic chemist for AMRI, then moved within the company to run the high-throughput automation facility on behalf of Eli Lilly in Windlesham, working across both the discovery and process chemistry arenas. She then worked in reaction optimization and data management using automation at Pfizer and then Syngenta. Nessa recently moved to AstraZeneca as Digital Champion in Early Chemical Development, where she focusses on making life easier for chemists and analysts with data management and accessible digital tools.

She was recently awarded the Salters' Institute Centenary Award for early-career chemists with the potential to make an outstanding long-term contribution to the chemical industry, and maintains a website of useful chemistry resources, https://supersciencegrl.co.uk.

PL12 - Development of SARS Coronavirus 3CL Protease Inhibitors with an Electrophilic aryl-ketone Warhead

Prof. Yoshio HAYASHI

TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES, Tokyo, Japan
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Prof. Yoshio HAYASHI

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Yoshio Hayashi is a professor at Tokyo University of Pharmacy and Life Sciences. His research focuses on peptide chemistry and medicinal chemistry. He created several peptide drug candidates such as Plinabulin (Phase III), negamycin derivative, myostatin inhibitory peptide and SARS-CoV 3CL protease inhibitor for the treatment of cancer, genetic disease, muscle disorder and corona viral infection, respectively. In peptide chemistry, he has recently developed efficient reagents in disulfide formation for the synthesis of cyclic peptides and peptide hybrid molecules.

He received his Ph.D. in 1990 from Faculty of Pharmaceutical Science, Kyoto University. After working for two companies, he joined former Professor Yoshiaki Kiso’s group at Kyoto Pharmaceutical University as a lecturer in 2001, and later became an associate professor. In 2007, he became a professor at Tokyo University of Pharmacy and Life Sciences. In 2009, he was awarded the Pharmaceutical Society of Japan Award for Divisional Scientific Promotions.

Currently, he serves as Vice president of the Pharmaceutical Society of Japan (PSJ), Vice chairperson of two Divisions (Organic Chemistry and Medicinal Chemistry) of PSJ, and Trustee of the Japanese Peptide Society.

PL03 - Discovery of Novel Microbiome-Sparing Antibiotics with Activity Against Gram-Negative Pathogens

Prof. Paul J. HERGENROTHER

UNIVERSITY OF ILLINOIS, Urbana, United States
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Prof. Paul J. HERGENROTHER

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Paul J. Hergenrother was born in 1972 and raised in Akron, Ohio. He attended the University of Notre Dame, where he received his B.S. in Chemistry in 1994. He moved to the University of Texas at Austin, conducting graduate research under the direction of Professor Stephen F. Martin, graduating with his PhD in 1999. He then moved as an American Cancer Society postdoctoral fellow to Harvard University, where he worked in the laboratory of Professor Stuart L. Schreiber. He established his own laboratory in the Department of Chemistry at the University of Illinois at Urbana-Champaign in 2001, and in 2013 was named the Kenneth L. Rinehart Endowed Chair in Natural Products Chemistry.

Professor Hergenrother is the co-founder of Vanquish Oncology, and through Vanquish an anticancer compound discovered by the Hergenrother lab completed a Phase 1 clinical trial and has begun Phase 2 studies. The Hergenrother lab has codified the eNTRy rules for compound accumulation in Gram-negative bacteria, and they and others have now used these rules to develop compounds with activity against Gram-negative pathogens. In spring of 2020, while UIUC was shut down due to the COVID-19 pandemic, Prof. Hergenrother led the team that developed a novel saliva-based assay for SARS-CoV-2, a simple protocol that bypasses the need for RNA isolation and as such is inexpensive, returns rapid results, and can be used on scale. The University of Illinois administered over 1,000,000 of these tests on its campus during Fall 2020, typically testing ~10,000 people a day, and with Emergency Use Authorization this test has now been used over 20 million times worldwide.

The Hergenrother laboratory seeks to use small molecules to identify and validate novel targets for the treatment of intractable diseases, including cancer and multi-drug resistant bacteria.

PL18 - A Tricycle Journey to in vivo Degraders of the Oncogenic Transcription Factor BCL6

Prof. Swen HOELDER

THE INSTITUTE OF CANCER RESEARCH, Sutton, United Kingdom
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Prof. Swen HOELDER

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Professor Hoelder studied chemistry at the University of Muenster (Germany). He completed his PhD in organic chemistry at the Technical University in Berlin in the team of Professor S. Blechert. Following his PhD, Professor Hoelder spent two years in the lab of Professor P.G. Schultz at the University of California, Berkeley establishing methods to identify novel enzymes through selection from large protein libraries.
Professor Hoelder then joined the department of Medicinal Chemistry at Hoechst Marion Roussel (now Sanofi), a major pharmaceutical company, where he predominately worked on diabetes therapies. In 2005, he joined Altana Pharma to work on cancer therapies, where he led a team of chemists that discovered two pre-clinical candidates.
Professor Swen Hoelder now leads the Medicinal Chemistry 4 team within the Centre for Cancer Drug Discovery (CCDD) at The Institute of Cancer Research in London. In 2022 he became the Head of Chemistry within the CCDD and the interim Director of the Centre for Protein Degradation. To find out more please visit https://www.icr.ac.uk/our-research/researchers-and-teams/professor-swen-hoelder

PL02 - Identification of CDK8 Inhibitors as Inducers of Tendon Cell Differentiation through Phenotypic Screening and Chemoproteomics

Dr Jean-Baptiste LANGLOIS

NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
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Dr Jean-Baptiste LANGLOIS

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Jean-Baptiste Langlois obtained is PhD in organic chemistry from the University of Geneva (Switzerland), where he worked on asymmetric catalysis in the group of Prof. Alexakis. In 2012, he moved to the Massachusetts Institute of Technology (Cambridge, USA) to perform his post-doctoral studies with Prof. Buchwald. Jean-Baptiste came back to Switzerland in 2013 to start his career as medicinal chemist. First, in a startup company named PIQUR Therapeutics focusing on the discovery of new PI3K inhibitors and eventually at the Novartis Institutes for Biomedical Research in Basel, where he is currently a senior principal scientist and project team leader. Over the past years, Jean-Baptiste acquired a quite diverse experience, working successively in the fields of autoimmune disorders, oncology and musculoskeletal diseases. Jean-Baptiste received the young investigator in medicinal chemistry prize from the French Société de Chimie Thérapeutique in 2022.

PL08 - Leucettinib-21, A DYRK1A Inhibitor Drug Candidate Aiming at the Correction of Cognitive Disorders in People with Down Syndrome or Alzheimer’s Disease

Dr Laurent MEIJER

PERHA PHARMACEUTICALS, Roscoff, France
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Dr Laurent MEIJER

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Laurent MEIJER obtained Doctorate degrees from the Universities of Lille (M. Durchon) and Paris VI (P. Guerrier). He went for a post-doctoral training at the Stanford University Hopkins Marine Laboratory (D. Epel) (1978-’79) and was appointed by the CNRS in October 1979. He went on sabbatical (1985-’86) at the University of Washington, Seattle (E. Krebs). He was a Visiting Professor (2001-2004) at the Rockefeller University, New York (P. Greengard). As a CNRS Research Director he was heading a team of 21 co-workers (‘Protein Phosphorylation & Human Disease’ group), at the ‘Station Biologique de Roscoff’, till June 2011.

He is now Chair and Chief Scientific Officer of ManRos Therapeutics and of Perha Pharma, two small biotech companies focused on the development of kinase inhibitors targeting cystic fibrosis (ManRos), cognitive disorders associated with Alzheimer’s disease and Down syndrome, and prevention of Hearing Loss induced by ototoxic products or acoustic trauma (Perha Pharma). Aged 70, he is author of >365 scientific articles, and co-inventor in 47 patents. He was the main editor of 6 books and has received numerous honours. He has participated to >210 conferences, and organized 8 conferences. He has directed many post-doctoral researchers, doctoral students and Master 2 students.

His major work is focused on pharmacological chemical inhibitors of disease-relevant protein kinases. Over 3 decades of work in this area has led to the discovery of numerous inhibitors (olomoucine, roscovitine, purvalanol, paullones, indirubins, hymenialdisine, aloisines, meriolins, leucettines, leucettinibs, etc...). One of them, roscovitine, has reached clinical trials against various diseases, and Leucettinib-21 is about to enter phase 1 clinical trial. The key kinase targets in the laboratory are namely cyclin-dependent kinases, cdc2-like kinases, dual specificity tyrosine phosphorylation activated kinases.

PL05 - Stabilizing Relevant GPCR Conformations to Discover Therapeutic Antibodies

Dr Christel MENET

CONFO THERAPEUTICS, Brussels, Belgium
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Dr Christel MENET

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Christel joined Confo Therapeutics as CSO in 2016. She was one of the first chemists to join Galapagos and later became Director of Medicinal Chemistry. She is an inventor of filgotinib, which has since reach market under the brand ‘Jyseleca’ for rheumatoid arthritis, among other indications. Prior to Galapagos, Christel worked at Faust Pharmaceuticals (now Domain Therapeutics), a biotechnology company specializing in GPCR drug discovery. She is an inventor on over 25 patent applications and has over 20 years of R&D experience. Christel completed a PhD in Organic Chemistry at the University of Manchester (UK) in the lab of Prof Jonathan Clayden.

PL14 - BacPROTACs Mediate Targeted Protein Degradation in Bacteria

Prof. Francesca Ester MORREALE

THE FRANCIS CRICK INSTITUTE, London, United Kingdom
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Prof. Francesca Ester MORREALE

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Dr Francesca Ester Morreale is a Group Leader at the Francis Crick institute (London, UK). Her lab focuses on enabling antibiotic discovery by targeted protein degradation, integrating chemical biology and structural biology.
>br/> Dr Morreale obtained her PhD in Pharmaceutical Sciences in 2014 from the University of Messina (Italy) supervised by Prof. Alba Chimirri. After completing her PhD, she started a postdoc in the group of Prof. Helen Walden at the MRC Protein Phosphorylation and Ubiquitylation Unit (University of Dundee, UK), co-supervised by Prof. Alessio Ciulli. In 2017 Dr Morreale joined the group of Dr Tim Clausen at the Research Institute of Molecular Pathology (IMP) in Vienna, Austria. As a postdoc in the Clausen lab, she led a proof-of-concept study translating targeted protein degradation to bacteria, a technology she is further developing in her independent research group.

PL11 - Structural Biology Supporting Medicinal Chemistry of Purine Receptors

Prof. Christa MÜLLER

UNIVERSITY OF BONN, Bonn, Germany
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Prof. Christa MÜLLER

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Christa Müller studied pharmacy at the University of Tübingen, Germany, and received her Ph.D. in Pharmaceutical/Medicinal Chemistry from the same university. After postdoctoral stays with John W. Daly (1989-1990 and 1992) in the Laboratory of Bioorganic Chemistry at the National Institutes of Health in Bethesda, Maryland, USA, she became Associate Professor of Pharmaceutical Chemistry at Würzburg University in Germany. Since 1998 she is full professor of Pharmaceutical & Medicinal Chemistry at Bonn University and a founder of the Pharma-Center Bonn and the Bonn International Graduate School of Drug Sciences (BIGS DrugS).

Her scientific interests are focused on the medicinal chemistry, structural biology, and molecular pharmacology of purine-binding membrane proteins (purine receptors, ectonucleotidases), orphan G protein-coupled receptors and G proteins, and recently also on coronavirus therapeutics. Disease indications include neurodegenerative and inflammatory diseases, cancer, and infections. She has published more than 500 scientific papers and patents in the field of medicinal chemistry and pharmacology. Among a number of awards, she received the Nauta Pharmacochemistry Award for Medicinal Chemistry and Chemical Biology by the European Federation of Medicinal Chemistry (EFMC) in 2018. Since 2021, she acts as Editor-in-Chief of ACS Pharmacology & Translational Science.

PL13 - Inhibitors of the Mitochrondrial Sirtuins 3 and 5

Prof. Christian A. OLSEN

UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark
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Prof. Christian A. OLSEN

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Christian A. Olsen was born in Copenhagen in 1974. He received his M.Sc. from the Technical University of Denmark in 2000 and his Ph.D. from the Royal Danish School of Pharmacy in 2004. After independently working on the development of novel peptidomimetics, he did his postdoctoral fellowship with Prof. Ghadiri at The Scripps Research Institute. In 2010 he returned to a faculty position at the Technical University of Denmark and in 2014 he accepted his current position as professor at the University of Copenhagen. He is recipient of the Lundbeck Foundation Fellowship (2010), the EFMC award for a young medicinal chemist in academia (2014), and an ERC Consolidator Grant in 2016. His research interests include foldamers, HDAC inhibitors and quorum sensing modulators, as well as investigation of protein lysine acylation.

PL07 - Discovery of GLPG3970, A First-in-class SIK2/SIK3 Inhibitor Evaluated in Clinical Trials for the Treatment of Autoimmune and Inflammatory Diseases

Dr Christophe PEIXOTO

GALAPAGOS, Romainville, France
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Dr Christophe PEIXOTO

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Christophe Peixoto joined Galapagos in 2006 as associate scientist in chemistry and he’s now Associate Director in Medicinal chemistry. Prior to Galapagos, Christophe worked at Proskelia an Aventis spin-off in the bone disease area from 2002 and 2006. After his bachelor’s degree in chemistry, he started his career as technician at Aventis Pharma in 1998 working on the synthesis of anti-infective agents. He is an inventor on over 12 patents application including the discovery of GLPG3970. He has over 20 years of research experience.

PL01 - Fragment-based Design of Methionine Adenosyl Transferase (MAT2a) Inhibitors with Anti-tumour Effect

Dr Marianne SCHIMPL

ASTRAZENECA, Cambridge, United Kingdom
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Dr Marianne SCHIMPL

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Marianne Schimpl is a structural biologist with expertise in fragment-based drug discovery, structure-guided drug design, target analysis, protein kinases, PARP-family enzymes and protein ubiquitination. In her current role as Associate Principal Scientist at AstraZeneca, she is supporting oncology programmes with structural insights. Marianne studied biotechnology in Austria, Australia and Canada before moving to Scotland for PhD and postdoctoral studies at the University of Dundee. An interest in structural enzymology led to a position in the Drug Discovery Programme at the Beatson Institute for Cancer Research in Glasgow, and then to joining AstraZeneca in 2015. Since then, Marianne is has seen several small molecule drug discovery programmes from hit finding through to clinical evaluation. She has a particular interest in fragment-based lead generation and the application of structural insights in the drug discovery process.

PL15 - Metallo-Enzymes - From Functions to Drugs

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; from 2011-2021 he was Head of Organic Chemistry at Oxford. He is presently Director of Chemistry at the Ineos Oxford Institute for Antimicrobial Research (IOI). 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; it has helped enable discovery of new medicines.

PL17 - Bifunctional Molecules for Exploring and Treating Human Disease

Prof. David SPIEGEL

YALE UNIVERSITY, New Haven, United States
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Prof. David SPIEGEL

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http://www.spiegelgroup.yale.edu

David A. Spiegel was born in New York City, and grew up in Teaneck, New Jersey. From a very young age, he was fascinated by the chemistry and biology of small molecules, and at 16 began doing research in a neuroanesthesiology laboratory at the University of Iowa. He went on to attend Harvard University where he conducted research under the guidance of Professor Yoshito Kishi. After graduating from Harvard, David began in Yale University’s M.D./Ph.D. program. There he conducted graduate research in Professor John Wood’s laboratory focusing on developing synthetic approaches toward the phomoidrides. During the course of these studies, he discovered that trialkylborane-water complexes could function as H-atom donors in free radical reactions. Following graduation from Yale, Professor Spiegel moved back to Harvard for postdoctoral studies under the guidance of Professor Stuart L. Schreiber. There he focused on developing an oligomer-based method for small-molecule synthesis to enable the rapid assembly of skeletally diverse small molecules starting from simple monomers. David began as an assistant Professor at Yale in June of 2007. Since that time, he has been fortunate to be named recipient of the Camille and Henry Dreyfus New Faculty Award, the NIH Director’s New Innovator Award, Ellison Foundation New Scholar Award,

Bill and Melinda Gates Foundations Grand Challenges Explorations Award and is the recipient of an Alfred P. Sloan Foundation Fellowship.

PL06 - LipMete (Lipophilic Metabolism Efficiency) as a Simple Guide for Half-Life and Dosing Regimen Prediction of Oral Drugs

Dr Antonia F. STEPAN

F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland
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Dr Antonia F. STEPAN

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Antonia F. Stepan is a Section Head - Medicinal Chemistry at Roche. Antonia received her undergraduate degree from the ETH Zurich, Switzerland, and her Ph.D. from the University of Cambridge, UK, under the guidance of Professor Steven V. Ley.
After two years of postdoctoral studies with Professor K. C. Nicolaou at the Scripps Institute in La Jolla, California, Antonia joined the Pfizer Medicinal Chemistry Department at the end of 2008. Her research interest focuses on the discovery of novel medicines for the treatment of neurodegenerative diseases.
She has co-authored more than 50 peer-reviewed papers, reviews, and patents.

PL09 - Discovery of Linvencorvir (RG7907), a Hepatitis B Virus Core Protein Allosteric Modulator, for the Treatment of Chronic HBV Infection

Dr Wei ZHU

CHINA INNOVATION CENTER OF ROCHE (CICOR), Shanghai, China
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Dr Wei ZHU

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Dr. Wei Zhu is the Head of Medicinal Chemistry at China Innovation Center of Roche. He graduated from Lanzhou University (China) in 1999 as a Chemistry Bachelor, and obtained his Ph.D. in 2004 from Shanghai Institute of Organic Chemistry (China) under the supervision of Prof. Dawei Ma. From 2004 to 2009, he pursued postdoctoral studies firstly at European Institute of Chemistry & Biology (France) with Prof. Léon Ghosez, and then at University of Pittsburgh (USA) with Prof. Dennis Curran. He joined Roche in 2009 as a scientist. Since then, he has been taking increasing responsibilities and was appointed as Head of Medicinal Chemistry in early 2020. His research interest focuses on small molecule drug discovery in oncology, virology and immunology. He has led cross-functional teams to deliver several molecules into the clinic. He is corresponding author of peer-reviewed journals/book chapters, inventor of >50 patents, regularly invited speaker on multiple domestic/international forums, and invited reviewer for J. Med. Chem. and ACS Med. Lett.

OC07 - Discovery of an Oral, Rule-of-5 Compliant, IL-17A Protein-Protein Interaction Modulator (IL-17A PPIm) for the Treatment of Psoriasis and other Inflammatory Diseases.

Dr Mark D. ANDREWS

LEO PHARMA, Ballerup, Denmark
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Dr Mark D. ANDREWS

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After completing a DPhil in organic chemistry with Dr Mark Moloney at Oxford in 1995 I moved to Canada for 2 years, carrying out post-doctoral research with Prof. John Vederas at the University of Alberta. Returning to the UK, I spent a year as a temporary lecturer in organic chemistry at the University of Bristol, working with Prof. Tim Gallagher, before joining Pfizer at their Sandwich research site in 1998. At Pfizer I worked as a medicinal chemist on numerous targets across several therapeutic areas (Sexual Health, Obesity, Pain), helping to deliver clinical candidates and potential candidates for SSRIs, 5HT2C, MC4, TRPM8 and TRK (Tropomyosin receptor kinase).

Following the closure of Pfizer’s Sandwich site in 2011 I stayed in East Kent and joined Peakdale (now Concept life sciences), where I spent 3 years. In 2015, I moved to LEO pharma in Denmark, where I am now a Senior Principal Scientist, with responsibilities as a Medchem Lead/Project Lead, helping LEO discover new, safe and effective medicines to treat skin diseases.

I am a named inventor on 26 patents and an author of 31 papers/book chapters.

OC05 - Tackling LysS, a New Target for Tuberculosis

Dr Laura A.T. CLEGHORN

UNIVERSITY OF DUNDEE, Dundee, United Kingdom
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Dr Laura A.T. CLEGHORN

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Dr. Laura Cleghorn is the Tuberculosis Portfolio Manager at the Drug Discovery Unit (DDU) based at the School of Life Sciences, University of Dundee, Scotland. She obtained her BSc (hons) in Chemistry from the University of Edinburgh, following this she became a medicinal chemist working at Organon Laboratories before moving to the University of Leeds to complete a PhD in Chemistry. Laura joined the DDU in 2006 at the point of its inception, initially working as a medicinal chemist working on Human African Trypanosomiasis before changing focus to Tuberculosis (TB) in 2013. She currently leads a team focussed on identifying new chemical series that inhibit TB and with the aim of developing them towards pre-clinical drug candidates.

OC08 - Small-Molecule Inhibitor Targeting PD-1/PD-L1 Interaction Restores T-Cell Function

Prof. Helena FLORINDO

IMED - UNIVERSITY OF LISBON, Lisbon, Portugal
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Prof. Helena FLORINDO

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Helena Florindo graduated in Pharmaceutical Sciences in 2003 (University of Lisbon) and obtained her Ph.D. degree in Pharmaceutical Technology in 2008 (University of Lisbon), in collaboration with the University of London.
Currently, she is an Associate Professor with tenure and habilitation in the department of Pharmacy, Pharmacology, and Health Technologies at the Faculty of Pharmacy, University of Lisbon. Since 2015, she is the head of the BioNanoSciences – Drug Delivery & Immunoengineering Research Group, at the Research Institute for Medicines (iMed.ULisboa), University of Lisbon.
Helena is also a member of the Portuguese Medicines Agency Evaluation Board (INFARMED) and an expert to the European Medicines Agency (EMA), thus supporting the evaluation of marketing authorization procedures for new drugs and biologics. This knowledge also guides her research, which has been motivated by the immune-oncology field toward the rational development of functionalized nano/biomaterials as novel immunotherapies for cancer treatment. It includes the characterization of the anti-tumor effects induced by the combination of nano-vaccines with nano-therapeutics, including small molecules, designed to modulate the functions of key cells within tumor microenvironment, such as T cells, myeloid-derived cells, and tumor cells.

OC06 - Historical Evolution and Lessons Learned from an RSV Non Nucleosides Polymerase Inhibitor Program

Dr Sandrine GROSSE

JANSSEN, Beerse, Belgium
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Dr Sandrine GROSSE

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Sandrine studied chemistry at the Engineering School of Chemistry of Rennes (ENSCR, France) and completed a PhD in Organic Chemistry at the Institute of Organic and Analytical Chemistry (Orléans, France) under the supervision of Pr. Gérald Guillaumet in collaboration with GreenPharma (Synthesis, functionalization and biological evalution of novel heterocyclic systems. After a short period in production plant (Seqens, France) she joined Janssen Belgium, a company of Johnson and Johnson in 2014. She contributed to and led several hit-to-lead and lead optimization projects mainly in the areas of respiratory diseases or hepatitis. Her work has resulted in 15 published international patents and 8 articles.

OC03 - Scaffold out of the Blue: Azulenes for Medicinal Chemistry

Dr Jörg KLEY

BOEHRINGER INGELHEIM, Biberach an der Riss, Germany
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Dr Jörg KLEY

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Dr Jörg Kley Studied chemistry at the University of Freiburg, Germany and did his PhD at Tumor Biology Center, Freiburg, supervised by Prof. G. v. Kiedrowski (Synthesis and biochemical evaluation of phospholipid analogs)He did a PostDoc at Boehringer Ingelheim (Parallel synthesis to support hit-to-lead projects) before becoming visiting scientist at Imperial College, London, in the group of Prof. Donald Craig (Ireland-Claisen Rearrangements) Since 2000, Dr Kley is Head of a Medicinal Chemistry Lab at BI in Biberach, Germany. He Contributed to and lead numerous hit-to-lead and lead optimization projects in the areas of Oncology, Respiratory Diseases, and Metabolic Diseases. He is the Coinventor of a Phase 2 clinical compound for the treatment of Cystic Fibrosis.

OC01 - Experiences from CETSA Screens for Hit Discovery versus Challenging Targets

Dr Alice LANNE

ASTRAZENECA, Macclesfield, United Kingdom
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Dr Alice LANNE

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Alice is a senior scientist in the High Throughput Screening group (HTS) at AstraZeneca. She joined the company in 2021 after obtaining a PhD from the University of Birmingham where she focused on identifying and profiling inhibitors of Mycobacterium tuberculosis. In her current role, Alice is part of the biochemical and biophysical screening team and routinely develops miniaturised assays, performs screens of up to 2 million compounds and builds triaging cascades to identify novel hit chemistry for lead generation. She has been heavily involved in building the affinity screening capability at AstraZeneca, including the high throughput Cellular Thermal Shift Assay (CETSA), Differential Scanning Fluorimetry (DSF) and Affinity Selection Mass Spectrometry (ASMS) platforms.

OC02 - Potential of Chloroalkene as Amide Bond Isostere

Prof. Tetsuo NARUMI

SHIZUOKA UNIVERSITY, Hamamatsu, Japan
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Prof. Tetsuo NARUMI

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Tetsuo Narumi received his Ph.D. in Pharmacy from Kyoto University under the direction of Prof. N. Fujii in 2008; spent the next year as a postdoctoral research associate with Prof. J. W. Bode in the Department of Chemistry, at the University of Pennsylvania; spent the next three years as an assistant professor with Prof. H. Tamamura in the Institute of Biomaterials and Bioengineering at Tokyo Medical and Dental University; and has been in the Department of Engineering at Shizuoka University ever since. His research activities are primarily concerned with chemistry to understand and control biological phenomena by means of organic and peptide chemistry methods. He is actively working on the development of novel peptidomimetics, including amide bond isosteres, for drug discovery targeting amyloid disease and viral infections such as HBV, HCV, and HIV.

OC04 - Unravelling the Potential of the Type 2 Lysophosphatidic Acid Receptor (LPA2) for Central Nervous System Pathologies

Prof. Silvia ORTEGA GUTIERREZ

COMPLUTENSE UNIVERSITY OF MADRID, Madrid, Spain
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Prof. Silvia ORTEGA GUTIERREZ

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Silvia is currently Associate Professor at Complutense University of Madrid, Spain. Her lines of research are mainly focused on medicinal chemistry and biological chemistry devoted to the validation and identification of new therapeutic targets as well as on the development of probes for the study of therapeutically relevant proteins. At present, she works in particular on the central nervous system (including the endogenous cannabinoid system and the lysophosphatidic acid receptors) and also on cancer and progeria. Her work has resulted in more than 75 publications in prestigious journals (such as Science, Nat. Neurosci., ACS Cent. Sci., Angew. Chem. Int. Ed. and J. Med. Chem.) and several international patents transferred and in exploitation by the industry. He has also supervised twelve PhD Theses, given invited lectures, and directed several research projects with both public and private funding.

Silvia obtained her PhD at Complutense University of Madrid (Cum Laude and Extraordinary Award). After that, she moved to The Scripps Research Institute (La Jolla, California, USA) with a Fulbright grant and then she joined the Department of Organic Chemistry at the Complutense University as Ramón y Cajal Researcher where she was promoted to Associate Professor in 2016. Her research career has been recognized with the different awards. Among them, stand out the "Young researchers Sigma-Aldrich Award" of the Spanish Royal Society of Chemistry and the "Runner-up Prize for a Young Medicinal Chemist in Academia" by the European Federation of Medicinal Chemistry.