EFMC-ACSMEDI Medicinal Chemistry Frontiers 2024

Joint Symposium on Medicinal Chemistry

 Utrecht, The Netherlands    April 8-11, 2024

Programme



15:00

Registration

16:30

Company Workshop by WuXi AppTec

17:30

Opening of the Symposium and Welcome address

Plenary lecture 1

17:45

Some Transferrable Lessons in Drug Discovery (PL01)

Dr Mark MURCKO
DEWPOINT THERAPEUTICS, Boston, MA, United States
18:30

Welcome Reception

New Chemistries for the Preparation of DNA-Encoded Libraries

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

Fragment-Based Drug Discovery

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

Protein-protein Interactions

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

Plenary lecture 2

16:00

The Polarities of Drug Discovery (PL02)

Dr Hayley BINCH
F. HOFFMANN-LA ROCHE, Basel, Switzerland

Poster Session

16:45

Poster session 1 (odd numbers)

18:00

End of the scientific programme

18:30

City Tour - Utrecht Hotspots' walk

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

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

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

13:00

Company Workshop by Schrodinger

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

Plenary lecture 3

16:00

Cancer Drug Discovery Using Fragment-Based Methods (PL03)

Prof. Stephen W. FESIK
VANDERBILT UNIVERSITY, Nashville, United States

Poster Session

16:45

Poster session 2 (even numbers)

18:00

End of the scientific programme

20:00

Symposium Banquet

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

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

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