| Monday April 8, 2024 |
| 15:00 | Registration |
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| 16:30 | Company Workshop by WuXi AppTec |
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| 17:30 | Opening of the Symposium and Welcome address |
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| Plenary lecture 1 |
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| 17:45 | Some Transferrable Lessons in Drug Discovery (PL01) |
Dr Mark MURCKO
(DEWPOINT THERAPEUTICS, Boston, MA, United States) |
| 18:30 | Welcome Reception |
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| Tuesday April 9, 2024 |
| New Chemistries for the Preparation of DNA-Encoded Libraries |
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| Session Chair |
Prof. Daniel HARKI
(UNIVERSITY OF MINNESOTA, Minneapolis, MN, United States) |
| 09:00 | Recent Advances in DNA-encoded Library Technology at GSK (IL01) |
Dr Melissa GRENIER-DAVIES
(GLAXOSMITHKLINE, Cambridge, MA, United States) |
| 09:30 | Development of SAR-CoV-2 Mpro Inhibitors Using DNA-Encoded Chemical Libraries (IL02) |
Prof. Damian YOUNG
(BAYLOR COLLEGE OF MEDICINE, Houston, TX, United States) |
| 10:00 | A Hybrid of mRNA Display and DNA-Encoded Libraries for Discovery of Extended Rule of 5 Molecules (OC01) |
Dr Seino JONGKEES
(VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands) |
| 10:15 | DELs in Cells - Direct Screening for Molecular Glue (OC02) |
Dr Rico Gerup PETERSEN
(VIPERGEN, Copenhagen, Denmark) |
| 10:30 | Coffee break & Exhibition |
|
| 11:00 | Fragment-Based Drug Discovery |
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| Session Chair |
Dr Gregg SIEGAL
(ZOBIO BV, Leiden, The Netherlands) |
| 11:00 | Fragment-Based Drug Design of Allosteric SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2) Inhibitors (IL03) |
Dr Alison WOOLFORD
(ASTEX PHARMACEUTICALS, Cambridge, United Kingdom) |
| 11:30 | The Art of Crafting a Mode of Action: Site Selective Hit Discovery (IL04) |
Dr Johan VEERMAN
(ZOBIO BV, Leiden, The Netherlands) |
| 12:00 | Development and Crystallographic Screening of a Fully Sociable and Diverse Fragment Library (OC03) |
Mr Philipp JANSSEN
(UNIVERSITY OF MÜNSTER, Muenster, Germany) |
| 12:15 | Fragment-Based Drug Discovery of Photopharmacological Agents (OC04) |
Mr Kim Tai TRAN
(IMPERIAL COLLEGE LONDON, London, United Kingdom) |
| 12:30 | Lunch & Exhibition |
|
| 13:00 | Company Workshop by Thermo Fisher Scientific |
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| 14:00 | Protein-protein Interactions |
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| Session Chair |
Prof. Terry MOORE
(UNIVERSITY OF ILLINOIS, Chicago, IL, United States) |
| 14:00 | Unlocking the 14-3-3 Interactome for Drug Discovery (IL05) |
Prof. Luc BRUNSVELD
(EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands) |
| 14:30 | From Protein Structures to Bioactive Proteomimetics (IL06) |
Prof. Tom GROSSMANN
(VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands) |
| 15:00 | Native Mass Spectrometry as a Tool for Rapid Elucidation and Modulation of Transient Protein-Protein Interactions (OC05) |
Prof. Clinton VEALE
(UNIVERSITY OF CAPE TOWN, Cape Town, South Africa) |
| 15:15 | Development of New SARS-CoV-2 NSP13 Inhibitors as a Promising Strategy to Block Viral Replication (OC06) |
Dr Valentina Noemi MADIA
(SAPIENZA, UNIVERSITY OF ROME, Roma, Italy) |
| 15:30 | Coffee break & Exhibition |
|
| 16:00 | Plenary lecture 2 |
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| 16:00 | The Polarities of Drug Discovery (PL02) |
Dr Hayley BINCH
(F. HOFFMANN-LA ROCHE, Basel, Switzerland) |
| 16:45 | Poster Session |
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| 16:45 | Poster session 1 (odd numbers) |
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| 18:00 | End of the scientific programme |
|
| 18:30 | City Tour - Utrecht Hotspots' walk |
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| Wednesday April 10, 2024 |
| 08:00 | EFMC-YSN | ACSMEDI-YMCC Programme for Early Career Researchers |
|
| 08:00 | Chair |
Dr Sean MCKENNA
(LEIDEN UNIVERSITY, Leiden, The Netherlands) |
| 08:00 | Panel Discussion
From Graduate Student to Young Professional: Career Perspectives from Industry, Academia and Beyond |
Dr Hayley BINCH (F. HOFFMANN-LA ROCHE, Basel, Switzerland)
Prof. Luc BRUNSVELD (EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands)
Dr Silvia ILLA TUSET (CRESSET, Royston, United Kingdom)
Dr Mark MURCKO (DEWPOINT THERAPEUTICS, Boston, MA, United States)
Dr Floris VAN DELFT (SYNAFFIX, Oss, The Netherlands) |
| 09:00 | Advances in Linkerology |
|
| Session Chair |
Dr Carolyn DZIERBA
(BRISTOL-MYERS SQUIBB, Cambridge, MA, United States) |
| 09:00 | Targeted Cancer Therapy with Best-in-Class Antibody-Drug Conjugates Based on Clinical-Stage GlycoConnect™ and HydraSpace Technologies (IL07) |
Dr Floris VAN DELFT
(SYNAFFIX, Oss, The Netherlands) |
| 09:30 | Catalent’s SMARTag® Technology: Novel Linker Solutions Enable Improved Tolerability of Solid Tumor-Targeting ADCs (IL08)
|
Dr Stepan CHUPRAKOV
(CATALENT PHARMA SOLUTIONS INC, Emeryville, United States) |
| 10:00 | Inducing Receptor Degradation as a Novel Approach to Target CC Chemokine Receptor 2 (CCR2)(OC07) |
Dr Natalia V. ORTIZ ZACARIAS
(LACDR, LEIDEN UNIVERSITY, Leiden, The Netherlands) |
| 10:15 | Targeted Protein Degradation of GPCRS: A Case Study of Novel CCR2 PROTACs (OC08) |
Mr Khaled ESSA
(LEIDEN UNIVERSITY, Leiden, The Netherlands) |
| 10:30 | Coffee break & Exhibition |
|
| 11:00 | Impact of Novel Modalities on Clinical Pipelines |
|
| Session Chair |
Dr Antonia F. STEPAN
(F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland) |
| 11:00 | Development of Orally Bioavailable Peptides Targeting an Intra-cellular Protein: From a Hit to a Clinical KRAS Inhibitor (IL09) |
Dr Ryuji HAYASHI
(CHUGAI PHARMACEUTICAL CO.,LTD., Kanagawa , Japan) |
| 11:30 | Targeted Protein Degradation Using Cereblon Molecular Glues (IL10) |
Dr Lyn H. JONES
(DANA FARBER CANCER INSTITUTE, Boston, MA, United States) |
| 12:00 | Peptides from Bench to Clinical Studies: Our Experience with CXCR4 (OC09) |
Dr Salvatore DI MARO
( UNIVERSITÀ DEGLI STUDI DELLA CAMPANIA, CASERTA, Italy) |
| 12:15 | Nizubaglustat, a Novel L-ido Azasugar in Development for GM1, GM2 Gangliosidoses and Niemann-Pick Type C Diseases (OC10) |
Dr Kyle LANDSKRONER
(AZAFAROS, Basel, Switzerland) |
| 12:30 | Lunch & Exhibition |
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| 13:00 | Company Workshop by Schrodinger |
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| 14:00 | A Focus on Early Career Investigators |
|
| Session Chair |
Dr Rita PETRACCA
(UTRECHT UNIVERSITY, Utrecht, The Netherlands) |
| 14:00 | Targeting Challenging Proteins Using an Integrative Antibody Discovery Approach (IL11) |
Dr Francesco APRILE
(IMPERIAL COLLEGE LONDON, London, United Kingdom) |
| 14:15 | Dynamics and Mechanism of CRISPR-Cas9 through the Lens of Computational Methods (IL12) |
Dr Giulia PALERMO
(UNIVERSITY OF CALIFORNIA RIVERSIDE, Riverside, United States) |
| 14:30 | Discovery of Hedgehog Acyltransferase (HHAT) Inhibitors as a Novel Strategy to Stop Hedgehog Signalling in Cancer (OC11) |
Dr Efthymios S. GAVRIIL
(IMPERIAL COLLEGE LONDON, London, United Kingdom) |
| 14:45 | Selective Substrate Identification Using Chemically Modified Phage Display (OC12) |
Mr Franco FAUCHER
(STANFORD UNIVERSITY, Stanford, United States) |
| 15:00 | Potent Bispecific T Cell Engagers Obtained by Tyrosine Click Chemistry (OC13) |
Ms Irene SHAJAN
(WAGENINGEN UNIVERSITY & RESEARCH, Wageningen, The Netherlands) |
| 15:15 | Borylated Cyclobutanes Via Thermal [2+2]-Cycloaddition (OC14) |
Dr Olha KOLODIAZHNA
(ENAMINE, Kyiv, Ukraine) |
| 15:30 | Coffee break & Exhibition |
|
| 16:00 | Plenary lecture 3 |
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| 16:00 | Cancer Drug Discovery Using Fragment-Based Methods (PL03) |
Prof. Stephen W. FESIK
(VANDERBILT UNIVERSITY, Nashville, United States) |
| 16:45 | Poster Session |
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| 16:45 | Poster session 2 (even numbers) |
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| 18:00 | End of the scientific programme |
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| 20:00 | Symposium Banquet |
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| Thursday April 11, 2024 |
| 09:00 | Emerging Synthetic Methodologies |
|
| Session Chair |
Prof. Iwan DE ESCH
(VU AMSTERDAM, Amsterdam, The Netherlands) |
| 09:00 | From Molecules to Molecular Surfaces and Back Again. Exploiting the Synergy between Electrochemistry and Organic Synthesis (IL13) |
Prof. Kevin MOELLER
(WASHINGTON UNIVERSITY, Saint Louis, MO, United States) |
| 09:30 | Click Chemistry in Drug Discovery: The Story of CIC-39, a SOCE Modulator for the Treatment of Rare Genetic Myopathies (IL14) |
Prof. Tracey PIRALI
(UNIVERSITY OF PIEMONTE ORIENTALE, Novara, Italy) |
| 10:00 | Innovative Synthetic Methods to Accelerate Drug Discovery (OC15) |
Dr Stefan SCHIESSER
(ASTRAZENECA, Mölndal, Sweden) |
| 10:15 | Late-Stage Functionalization in Drug Discovery: from Academic Collaborations to Applications in Medicinal Chemistry (OC16) |
Dr Antonio MISALE
(JOHNSON & JOHNSON PHARMACEUTICAL R&D, Toledo, Spain) |
| 10:30 | Coffee break & Exhibition |
|
| 11:00 | Targeting Immune Checkpoints with Small Molecules |
|
| Session Chair |
Prof. Eddy SOTELO PÉREZ
(UNIVERSITY OF SANTIAGO DE COMPOSTELA, Santiago de Compostela, Spain) |
| 11:00 | Discovery of Quemliclustat, a Potent and Selective Small Molecule Inhibitor of CD73 (IL15) |
Dr Jenna L. JEFFREY
(ARCUS BIOSCIENCES, Hayward, CA, United States) |
| 11:30 | Discovery of a Highly Specific, Potent, and Orally Efficacious LMP7 (β5i) Inhibitor (IL16) |
Dr Markus KLEIN
(MERCK KGAA, Darmstadt, Germany) |
| 12:00 | Preclinical Development of Innovative TLR4 Modulators as Vaccine Adjuvants and Immunotherapeutics (OC17) |
Prof. Francesco PERI
(UNIVERSITY OF MILANO-BICOCCA, Milano, Italy) |
| 12:15 | Leveraging New Chemical Modalities for Reprogramming IDO1 Half-Life in Cancer Immunotherapy (OC18) |
Dr Rita Maria Concetta DI MARTINO
(UNIVERSITY OF PIEMONTE ORIENTALE, Novara, Italy) |
| 12:30 | Lunch & Exhibition |
|
| 13:00 | Company Workshop by Iktos |
|
| 14:00 | Recent Advances in Neurodegenerative Diseases |
|
| Session Chair |
Dr Luc VAN HIJFTE
(SYMERES, Nijmegen, The Netherlands) |
| 14:00 | Discovery of a Potent and Brain Penetrant O-GlcNAcase (OGA) Inhibitor Able to Reduce Tau Pathology in a Preclinical Animal Model (IL17) |
Dr Peter BUIJNSTERS
(JOHNSON & JOHNSON PHARMACEUTICAL R&D, Beerse, Belgium) |
| 14:30 | In silico Enabled Discovery of KAI-11101, a Potent, Selective and Brain Penetrant DLK Inhibitor for the Treatment of Neurodegenerative Diseases (IL18) |
Dr H. Rachel LAGIAKOS
(SCHRÖDINGER, New York, NY, United States) |
| 15:00 | Hybrid Compounds for Neurodegenerative Diseases: from Small Molecules to Targeted Therapies (IL19)
Chemistry Europe Talk |
Prof. Maria Joao MATOS
(UNIVERSITY OF SANTIAGO DE COMPOSTELA, Santiago de Compostela, Spain) |
| 15:30 | Discovery of a Brain Penetrant Covalent BTK Inhibitor with a Novel Asn-484 Interaction (OC19) |
Mr George VANDEVEER
(BIOGEN, Stoneham, United States) |
| 15:45 | Fighting Chronic Neuroinflammation with Novel P2X7 Receptor Antagonists: An Intriguing Therapeutic Approach to the Neurodegenerative Diseases (OC20) |
Dr Imane GHAFIR EL IDRISSI
(UNIVERSITY OF BARI ALDO MORO, Bari, Italy) |
| 16:00 | Closing Ceremony & Poster Prizes Ceremony |
|
| 16:15 | End of the scientific programme |
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