EFMC-ACSMEDI Medicinal Chemistry Frontiers 2024

Joint Symposium on Medicinal Chemistry

 Utrecht, The Netherlands    April 8-11, 2024

Programme



15:00

Registration

17:30

Opening of the Symposium and Welcome address

Plenary lecture 1

17:45

Medicinal Chemistry: Some Possible Future Directions (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

Site Directed Hit Discovery Using Biophysical Assays (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

12:45

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

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

Oral Communication 10

12:30

Lunch & Exhibition

12:45

Company Workshop by Schrodinger

A Focus on Early Career Investigators

Session Chair

Dr Rita PETRACCA
UTRECHT UNIVERSITY, Utrecht, The Netherlands
14:00

Antibody Discovery vs Challenging Proteins (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

Oral Communication 14

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 the Discovery of a Modulator of the Store-Operated Calcium Entry for the Treatment for 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
JANSSEN 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
UNIVERSITÀ DEL PIEMONTE ORIENTALE , Novara , Italy
12:30

Lunch & Exhibition

12:45

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 RESEARCH AND DEVELOPMENT, Beerse, Belgium
14:30

In silico enabled discovery of KAI-11101, a 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)

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