EFMC-ISMC 2022

XXVII EFMC International Symposium on Medicinal Chemistry

 Nice, France    September 4-8, 2022

EFMC Award Lectures

Prof. Alessio CIULLI
PROUS INSTITUTE - OVERTON AND MEYER AWARD FOR NEW TECHNOLOGIES IN DRUG DISCOVERY
How PROTACs Work: Molecular Recognition and Design Principles
Prof. Herbert WALDMANN
NAUTA PHARMACOCHEMISTRY AWARD FOR MEDICINAL CHEMISTRY AND CHEMICAL BIOLOGY
Pseudo Natural Products – Chemical Evolution of Natural Product Structure
Prof. Mike WARING
UCB EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY
Small Molecule Drugs and where to find them - Approaches to Hit Generation and Lead Optimisation

Prize Lectures

Prof. Michael E. JUNG
IUPAC-RICHTER PRIZE 2022
Drug Discovery in Academia: A Drug For Glioblastoma Multiforme
Dr Marie-Helene LARRAUFIE
EFMC PRIZE FOR A YOUNG MEDICINAL CHEMIST OR CHEMICAL BIOLOGIST IN INDUSTRY
Chemical Biology Strategies Applied to Phenotypic Screening and Targeted Protein Degradation Discovery Programs
Dr Modesto REMUINAN
GALAPAGOS AWARD LECTURE (Award-winning Team: Bioversys/University of Lille/GSK)
Rejuvenating Ethionamide for Treatment of Tuberculosis - TRICky, but Possible
Dr Raphaël RODRIGUEZ
KLAUS GROHE PRIZE 2022
Discovery of a Druggable Copper-signaling Pathway that Drives Cell Plasticity and Inflammation
Prof. Olalla VÁZQUEZ
EFMC PRIZE FOR A YOUNG MEDICINAL CHEMIST OR CHEMICAL BIOLOGIST IN ACADEMIA
Chemical Biology Tools for Enlightening Drug Discovery
 

Plenary Speakers

Prof. Benoit DEPREZ
Discovery of Lead Compounds and Drug Candidates : Opportunities Unique to the World of Small Molecules
Prof. Eric MISKA
New Biology and Therapeutic Approaches from RNA Shape and Modification
Prof. Sarah E. REISMAN
Necessity is the Mother of Invention: Natural Products and the Chemistry They Inspire
Prof. Outi VAARALA
Drivers of Innovation in Drug Discovery
 
 

Invited Speakers

Dr Louise WALPORT
De Novo Cyclic Peptides as Chemical Tools to Explore Epigenetic Regulation
Dr Karine ALVAREZ
Addressing Current Challenges in Antiviral Therapies Against Emerging RNA Viruses
Prof. Michelle ARKIN
Fragment-Based Approaches to Stabilize Protein-Protein Interactions
Dr Andrea BECCARI
Embrace Complexity: in Silico Polypharmacological Profiling to Repurpose Medicines and Design New Drugs
Dr Amy BITTNER MCCRACKEN
Inhibiting the MYC Oncogene through Cell Active Max-E47 (ME-47)
Prof. Jeffrey BODE
Molecular Vending Machines for the On-Demand Synthesis of Drug-Like Molecules
Prof. Pascal BONNET
A Novel Fragment-Based Ligand Design Tool : Application to Kinase Research
Dr Marco BORGOGNO
Discovery of Selective NKCC1 Inhibitors for the Treatment of Core Symptoms in Autism, Down Syndrome, and Brain Disorders with Defective NKCC1/KCC2 Ratio
Dr Andreas BRUNSCHWEIGER
A DNA Barcode with Enhanced Chemical Stability for DNA-encoded Library Design
Prof. Youngjoo BYUN
Medicinal Chemistry in the Development of Molecular Imaging Probes Targeting Prostate-Specific Membrane Antigen
Dr Sébastien CAMPAGNE
Fundamental Basis for SMN2 Specific Splicing Correction by Small Molecules and Bulge Repair Mechanism
Dr Lisa CANDISH
Photocatalysis in Drug Discovery
Prof. Connor COLEY
A Perspective on AI and Automation for the Medicinal Chemistry Lab Virtual Presentation
Dr Michael J. DART
eIF2B Activators Beyond ISRIB: New Integrated Stress Response Inhibitors
Dr David DAVIES
Discovery and Preclinical Development of ANT3310, a Broad-Spectrum β-Lactamase Inhibitor which Potentiates Meropenem Against Carbapenem-Resistant Bacteria
Prof. Charlotte DEANE
The Power and Pitfalls of Machine Learning in Early Stage Drug Discovery
Dr Lourdes ENCINAS
Novel Tetrazole Inhibitor of Mycobacterium Tuberculosis Tryptophan Synthase
Mr Lluc FARRERA SOLER
EFMC-YMCS Prize 2021
A Mating Mechanism to Generate Diversity for the Darwinian Selection of DNA-encoded Synthetic Molecules
Dr Yann FORICHER
Targeting RNA with Small Molecules, A New Therapeutic Strategy
Dr David FREEMAN
Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9/Cyclin T1 for MYC-Dependent Cancers
Dr Marta FRIGOLE-VIVAS
Leveraging Biomolecular Condensates for Drug Discovery
Prof. Tanja GAICH
Title to be announced
Dr Amanda GARNER
Enabling Technologies for Revealing Druggable Paths in RNA Biology
Prof. Matthew GAUNT
New Synthetic Chemistry to Probe the Biology of Modified Nucleic Acids
Prof. Matthias GEHRINGER
Discovery of Covalent Protein Kinase Inhibitors Targeting Cysteines in the Hinge Region
Dr Carmen GIL
Searching for Drugs against Pandemic Viruses. A Case Study
Dr Darren GREEN
Driving Lead Optimization with BRADSHAW
Prof. Gyorgy KESERU
Covalent Fragment Approaches in Drug Discovery
Prof. Angela KOEHLER
Attenuating Oncogenic Transcription with Small Molecules Virtual Presentation
Dr Sanja KOSTRUN
Macrolide Inspired Macrocycles as Effective Disruptors of the IL-17A/IL-17RA Interaction
Dr Brian LANMAN
Inhibiting KRAS: Strategies, Structures, and Lessons Learned in the Invention of Sotorasib
Dr María MANEIRO
Antibody-Protac Conjugates: an Approach for Targeted Selective BRD4 Degradation in HER2+ Phenotypes
Dr Cristina MAYOR-RUIZ
Strategies to Discover Molecular Glue Degraders at Scale
Dr Hannes MIKULA
Next-level Chemical Tools for Ultrafast Bioorthogonal Bond-Cleavage Reactions
Dr Dieter MURI
Tritiation of Pharmaceuticals Via Late Stage C-H Functionalization
Dr Gerhard MÜLLER
The Phosphatase Family: a Widely Neglected Target Space for Small-Molecule Drug Discovery
Dr Frank NARJES
The discovery of the Clinical Candidate AZD0284, a Orally Bioavailable Inverse Agonist of RORG for the Treatment of Psoriasis
Prof. Zaneta NIKOLOVSKA-COLESKA
Disrupting hDot1L and MLL Oncofusion Protein Interactions as a Novel Therapeutic Strategy
Dr Mikako OGAWA
Evaluation of Cancer Immunity and Development of Novel Radiolabeling Method with Astatin-211 Virtual Presentation
Prof. Defang OUYANG
Opportunity and Challenge of Artificial Intelligence (AI) in Drug Delivery Virtual Presentation
Dr Alex PAUTSCH
Chemical Probes and How to Find Them
Prof. Jianfeng PEI
De Novo Drug Design Using 3D Deep Generative Models Virtual Presentation
Prof. Laura PIDDOCK
The Global Antibiotic R&D Partnership: Helping to Advance the Discovery & Development of New Treatments for Bacterial Infections
Prof. William POMERANTZ
New Opportunities for Studying the Function of the Nucleosome Remodeling Factor, NURF, Through Inhibition and Degradation
Prof. Eugen PROSCHAK
Chemical Probes for Targets in Lipid Signalling
Dr Renaud PRUDENT
EDELRIS Keymical Space™ and GPCR : Identification of Allosteric Binders by AS-MS
Dr Jean QUANCARD
Tipping the Balance: MALT1 Inhibitors with Paradoxical Effects on the Immune System
Prof. Fraydoon RASTINEJAD
Transcription Factors as Drug-Discovery Targets
Prof. Andrea RENTMEISTER
Investigating and Controlling mRNAs Via Chemo-enzymatic Modification
Dr Marc ROBILLARD
Chemically-Triggered Payload Release in-vivo
Prof. Judith ROLLINGER
Big Data Analyses for the Discovery of Lead Structures from Nature
Dr Fanny ROUSSI
Design of Naturally Inspired Anti-Cancer Compounds that Modulate Cholesterol Homeostasis
Dr Jörg SCHEUERMANN
Innovating DNA-encoded Chemical Library Technology for Better Ligand Discovery
Prof. Roger SCHIBLI
Radiotheragnostics from Bench-to-Bedside
Prof. Wenqing SHUI
Title to be announced Virtual Presentation
Prof. Kristian STROMGAARD
Targeting Protein-Protein Interactions of Receptor Complexes
Dr Nicolas THOMÄ
Haven't Got a Glue: Protein Surface Variation for the Design of Molecular Glue Degraders
Prof. Guy VAN DEN MOOTER
Formulation Strategies for Compounds with Challenging Physicochemical Properties
Dr Jarrod WALSH
High Throughput Affinity Screening for Rapid Hit Discovery and Prosecuting Intractable Targets
Prof. Daniel Martin WATTERSON
Beyond Amyloid and Tau: Exploring Alternative Therapeutic Targets Using an Integrative Approach
Prof. Feng ZHU
Title to be announced Virtual Presentation
 
 

Oral Communication

Dr Bauke ALBADA
Chemical Modification of Wild-type Proteins
Dr Paola B. ARIMONDO
Development of Bisubstrate Inhibitors to Tackle Epigenetics
Dr Giulia BERGONZINI
Visible-light Photocatalysis: a Powerful Tool in the Pursuit of New Pharmaceuticals
Dr Virgyl CAMBERLEIN
Discovery of Pseudomonas Aeruginosa Elastase LasB Inhibitors by in Situ Click Chemistry
Dr Laura CARZANIGA
Discovery of Clinical Candidate CHF-6366: a Super-soft Heterobifunctional Muscarinic Antagonist and β2-adrenoceptor Agonist (MABA) for the Inhaled Treatment of Respiratory Diseases
Prof. Christina CHAI
Tuning the Reactivity of the Natural Product Andrographolide: Towards Targeted Covalent Inhibitors for the Treatment of Inflammation
Dr Bryan CHOI
Accelerating Drug Discovery with the Integration of Affinity Selection Mass Spectrometry (ALIS)
Prof. Rebecca DEPREZ-POULAIN
First Selective Nanomolar Inhibitors of ERAP2 for Modulation of the Antigen Presentation
Dr Richard DOVESTON
Molecular Glues for the 14-3-3 Interactome
Prof. Karl GADEMANN
Reduce to the Max: Functionally Optimized Natural Products via Chemical Synthesis
Dr Herve GENESTE
In Silico Prediction of Brain Penetration - High Accuracy Achieved
Dr Francesco GRECO
NR2F6 Antagonists: in Vitro Pharmacology and Preclinical Data of a Potential Next Generation Immuno-oncology Therapy
Dr Gilles GUICHARD
Structure-Guided Design of Foldamer-Based Inhibitors of Protein-Protein Interactions
Dr Thomas HAYHOW
Discovery And Profiling of AZ'6421: an Oral ERa-Protac with an in vitro-in vivo Disconnect
Dr Timo HEINRICH
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106
Prof. Roderick HUBBARD
Photoactivated Covalent Capture of DNA-encoded Fragments to Identify Ligands for Challenging Targets
Dr Soufyan JERHAOUI
Discovery of JNJ-1245, a Novel and Potent Fluoroallylamide Mcl-1 Inhibitor for the Treatment of Hematologic Malignancies
Dr Manuela JORG
Identification and Structure-activity Relationship Profiling of Positive Allosteric Modulators Targeting Muscarinic Acetylcholine Receptors
Dr Anna JUNKER
Development of First PET Tracers for the Imaging of CD73 Expression in Triple-negative Breast Cancer
Ms Elizabeth A. LOPES
Dual Inhibition of P53-MDM2/4 Interactions With Spiropyrazoline Oxindoles
Ms Katherine MACFARLANE
Exploiting DNA-encoded Library Technology for the Discovery of Novel Antibody Recruiting Molecules Against LOX-1
Prof. Ana MARTINEZ
Modulation of TDP-43-pathy by Brain Penetrant Protein Kinase Inhibitors, a New Hope for ALS and Related Disorders
Dr Exequiel PORTA
Mining the Leishmania Kinome
Dr Filipa RAMILO-GOMES
New Generation of EZH2 Inhibitors for Cancer Therapy: A Computer-Aided Drug Design Approach in Epigenetics
Dr Stefano SAINAS
Human Dihydroorotate Dehydrogenase Inhibitor MEDS443: a Magic Bullet Against Coronaviruses
Dr Matthew SEGALL
Using AI to Derive Valuable Insights from Drug Discovery Data
Dr Alice SOSIC
Bis-3-chloropiperidines Targeting TAR RNA as a Novel Strategy to Impair the HIV-1 Nucleocapsid Protein
Dr Léopold THABAULT
Interrogating Lactate Dehydrogenases Oligomeric Interfaces Using (Stapled) Peptides And Small Molecules
Dr Boris VAUZEILLES
Fast Detection and Imaging of Hydrogen Peroxide with New Borinic Probes
Dr Anita WEGERT
A New Dual Mode of Action to Treat Pain - From Scratch to Pre-Clinical Candidate
Dr Erik WEIS
Iridium-catalyzed C-H Activation Methods for Late-stage Functionalization of Pharmaceuticals
Prof. Jukka WESTERMARCK
Protein Phosphatase 2A, a Druggable Tumor Suppressor for Cancer Therapy
Dr Birgit WILDING
Discovery of Novel Covalent, EGFR WT Sparing, HER2 Selective Inhibitors for the Treatment of Her2 Exon 20 Insertion Driven Tumours

First Time Disclosures

Dr Sophie BERTRAND
Discovery and Optimisation of Potent, Slow-dissociating Inhaled PI4KB Inhibitors
Dr Kenneth GRANBERG
Discovery of AZD5462, an Oral Agonist of the Relaxin Family Peptide Receptor 1 (RXFP1) for the Treatment of Cardiorenal Disease
Dr Uwe GRETHER
First Disclosure of Cannabinoid Receptor Type 2 Agonist Rg7774 – An Innovative Oral Treatment for Diabetic Retinopathy
Dr Peter HAEBEL
Discovery of BI 456906, a Novel Long-acting GCG/GLP-1 Receptor Dual Agonist for the Treatment of Patients With Obesity
Dr Pilar MANZANO-CHINCHON
Session Chair
Dr Leena OTSOMAA
Session Chair
Dr Roland PFAU
mPGES1 Inhibitors: First Time Disclosure of Clinical Candidate BI01029539 / GS-248
Dr Kai SCHIEMANN
First-time Disclosure of M1069, a Highly Selective Dual Inhibitor of Adenosine A2a/A2b Receptors With Improved Therapeutic Activity Compared to A2a Receptor Selective Antagonists
 

EFMC Prizes for Young Medicinal Chemist or Chemical Biologist in Academia and in Industry
Ceremony & Lectures