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
AL003 - How PROTACs Work: Molecular Recognition and Design Principles
Prof. Herbert WALDMANN
NAUTA PHARMACOCHEMISTRY AWARD FOR MEDICINAL CHEMISTRY AND CHEMICAL BIOLOGY
AL001 - Pseudo Natural Products – Chemical Evolution of Natural Product Structure
Prof. Mike WARING
UCB EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY
AL002 - 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
PR004 - 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
PR002 - 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)
LE025 - 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
PR003 - Chemical Biology Tools for Enlightening Drug Discovery
 

Plenary Speakers

Prof. Benoit DEPREZ
PL001 - Boosting « Chance and Necessity » with Experience and Molecular Creativity
Prof. Eric MISKA
PL002 - The Shape and Modification of RNA in Health and Disease
Prof. Sarah E. REISMAN
PL003 - Necessity is the Mother of Invention: Natural Products and the Chemistry They Inspire
Prof. Outi VAARALA
PL004 - Drivers of Innovation in Drug Discovery
 
 

Invited Speakers

Dr Louise WALPORT
LE092 - De Novo Cyclic Peptides as Chemical Tools to Explore Epigenetic Regulation
Dr Karine ALVAREZ
LE085 - Addressing Current Challenges in Antiviral Therapies Against Emerging RNA Viruses
Prof. Michelle ARKIN
LE029 - Fragment-Based Approaches to Stabilize Protein-Protein Interactions
Dr Andrea BECCARI
LE086 - Embrace Complexity: in Silico Polypharmacological Profiling to Repurpose Medicines and Design New Drugs
Dr Amy BITTNER MCCRACKEN
LE020 - Inhibiting the MYC Oncogene through Cell Active Max-E47 (ME-47)
Dr Benjamin BLASCO
LE033 - The Global Antibiotic R&D Partnership: Helping to Advance the Discovery & Development of New Treatments for Bacterial Infections
Prof. Jeffrey BODE
LE064 - Molecular Vending Machines for the On-Demand Synthesis of Drug-Like Molecules
Prof. Pascal BONNET
LE081 - A Novel Fragment-Based Ligand Design Tool : Application to Kinase Research
Dr Andreas BRUNSCHWEIGER
LE022 - A DNA Barcode with Enhanced Chemical Stability for DNA-encoded Library Design
Prof. Youngjoo BYUN
LE101 - Medicinal Chemistry in the Development of Molecular Imaging Probes Targeting Prostate-Specific Membrane Antigen
Dr Sébastien CAMPAGNE
LE074 - Fundamental Basis for SMN2 Specific Splicing Correction by Small Molecules and Bulge Repair Mechanism
Dr Lisa CANDISH
LE065 - Photocatalysis in Drug Discovery
Prof. Connor COLEY
LE050 - A Perspective on AI and Automation for the Medicinal Chemistry Lab Virtual Presentation
Dr David DAVIES
LE035 - Discovery and Preclinical Development of ANT3310, a Broad-Spectrum β-Lactamase Inhibitor which Potentiates Meropenem Against Carbapenem-Resistant Bacteria
Prof. Charlotte DEANE
LE051 - The Power and Pitfalls of Machine Learning in Early Stage Drug Discovery
Dr Lourdes ENCINAS
LE034 - Novel Tetrazole Inhibitor of Mycobacterium Tuberculosis Tryptophan Synthase
Mr Lluc FARRERA SOLER
EFMC-YMCS Prize 2021
LE016 - A Mating Mechanism to Generate Diversity for the Darwinian Selection of DNA-encoded Synthetic Molecules
Dr Yann FORICHER
LE073 - Targeting RNA with Small Molecules, A New Therapeutic Strategy
Dr David FREEMAN
LE019 - Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9/Cyclin T1 for MYC-Dependent Cancers
Dr Marta FRIGOLE-VIVAS
LE042 - Leveraging Biomolecular Condensates for Drug Discovery
Dr Amanda GARNER
LE072 - Enabling Technologies for Revealing Druggable Paths in RNA Biology
Prof. Matthew GAUNT
LE009 - New Synthetic Chemistry to Probe the Biology of Modified Nucleic Acids
Prof. Matthias GEHRINGER
LE047 - Discovery of Covalent Protein Kinase Inhibitors Targeting Cysteines in the Hinge Region
Dr Carmen GIL
LE084 - Searching for Drugs against Pandemic Viruses
Dr Darren GREEN
LE049 - Driving Lead Optimization with BRADSHAW
Prof. György KESERU
LE046 - Covalent Fragment Approaches in Drug Discovery
Prof. Angela KOEHLER
LE017 - Chemical Probe Discovery for Recalcitrant Targets Virtual Presentation
Dr Urban KOSAK
LE097 - Selective Butyrylcholinesterase Inhibitors for Alleviating Symptoms of Dementia
Dr Brian LANMAN
LE045 - Inhibiting KRAS: Strategies, Structures, and Lessons Learned in the Invention of Sotorasib
Dr Cristina MAYOR-RUIZ
LE001 - Strategies to Discover Molecular Glue Degraders at Scale
Dr Dieter MURI
LE010 - Tritiation of Pharmaceuticals Via Late Stage C-H Functionalization
Dr Gerhard MÜLLER
LE080 - The Phosphatase Family: a Widely Neglected Target Space for Small-Molecule Drug Discovery
Dr Frank NARJES
LE061 - The discovery of the Clinical Candidate AZD0284, a Orally Bioavailable Inverse Agonist of RORG for the Treatment of Psoriasis
Prof. Zaneta NIKOLOVSKA-COLESKA
LE013 - Disrupting hDot1L and MLL Oncofusion Protein Interactions as a Novel Therapeutic Strategy
Dr Mikako OGAWA
LE100 - Evaluation of Cancer Immunity and Development of Novel Radiolabeling Method with Astatin-211 Virtual Presentation
Prof. Defang OUYANG
LE078 - Opportunity and Challenge of Artificial Intelligence (AI) in Drug Delivery Virtual Presentation
Prof. Sebastien PAPOT
LE057 - Tumor Activated Therapy
Dr Alex PAUTSCH
LE091 - Chemical Probes and How to Find Them
Dr Dijana PESIC
LE062 - Macrolide Inspired Macrocycles as Effective Disruptors of the IL-17A/IL-17RA Interaction
Prof. William POMERANTZ
LE014 - New Opportunities for Studying the Function of the Nucleosome Remodeling Factor, NURF, Through Inhibition and Degradation
Prof. Eugen PROSCHAK
LE093 - Chemical Probes for Targets in Lipid Signalling
Dr Renaud PRUDENT
LE038 - EDELRIS Keymical Space™ and GPCR : Identification of Allosteric Binders by AS-MS
Dr Jean QUANCARD
LE060 - Tipping the Balance: MALT1 Inhibitors with Paradoxical Effects on the Immune System
Prof. Fraydoon RASTINEJAD
LE018 - Transcription Factors as Drug-Discovery Targets
Prof. Andrea RENTMEISTER
LE058 - Investigating and Controlling mRNAs Via Chemo-enzymatic Modification
Prof. Tobias RITTER
LE011 - Late-Stage Functionalizations
Dr Marc ROBILLARD
LE056 - Chemically-Triggered Payload Release in-vivo
Prof. Judith ROLLINGER
LE005 - Big Data Analyses for the Discovery of Lead Structures from Nature
Dr Fanny ROUSSI
LE006 - Design of Naturally Inspired Anti-Cancer Compounds that Modulate Cholesterol Homeostasis
Dr Jörg SCHEUERMANN
LE021 - Innovating DNA-encoded Chemical Library Technology for Better Ligand Discovery
Prof. Roger SCHIBLI
LE099 - Radiotheragnostics from Bench-to-Bedside Virtual Presentation
Prof. Wenqing SHUI
LE037 - Adapting the Affinity MS Technology to GPCR Ligand Discovery Virtual Presentation
Prof. Kristian STROMGAARD
LE041 - Targeting Protein-Protein Interactions of Receptor Complexes
Dr Nicolas THOMÄ
LE002 - Haven't Got a Glue: Protein Surface Variation for the Design of Molecular Glue Degraders
Prof. Guy VAN DEN MOOTER
LE068 - Formulation Strategies for Compounds with Challenging Physicochemical Properties
Dr Jarrod WALSH
LE039 - High Throughput Affinity Screening for Rapid Hit Discovery and Prosecuting Intractable Targets
Dr Dingyan WANG
LE076 - Uncertainty Quantification: Considering the Reliability of Artificial Intelligence in Drug Design Virtual Presentation
Prof. Daniel WATTERSON
LE095 - Beyond Amyloid and Tau: Exploring Alternative Therapeutic Targets Using an Integrative Approach
Prof. Feng ZHU
LE077 - Innovative Therapeutic Target Discovery based on OMIC Technology and Machine Learning Virtual Presentation
 

Oral Communication

Dr Bauke ALBADA
LE012 - Chemical Modification of Wild-type Proteins
Dr Paola B. ARIMONDO
LE030 - Development of Bisubstrate Inhibitors to Tackle Epigenetics
Dr Giulia BERGONZINI
LE066 - Visible-light Photocatalysis: a Powerful Tool in the Pursuit of New Pharmaceuticals
Dr Marco BORGOGNO
LE096 - Discovery of Selective NKCC1 Inhibitors for the Treatment of Core Symptoms in Autism, Down Syndrome, and Brain Disorders with Defective NKCC1/KCC2 Ratio
Dr Virgyl CAMBERLEIN
LE036 - Discovery of Pseudomonas Aeruginosa Elastase LasB Inhibitors by in Situ Click Chemistry
Dr Laura CARZANIGA
LE088 - 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
LE008 - Tuning the Reactivity of the Natural Product Andrographolide: Towards Targeted Covalent Inhibitors for the Treatment of Inflammation
Mr Bryan CHOI
LE040 - Accelerating Drug Discovery with the Integration of Affinity Selection Mass Spectrometry (ALIS)
Prof. Rebecca DEPREZ-POULAIN
LE094 - First Selective Nanomolar Inhibitors of ERAP2 for Modulation of the Antigen Presentation
Dr Richard DOVESTON
LE032 - Molecular Glues for the 14-3-3 Interactome
Prof. Karl GADEMANN
LE007 - Reduce to the Max: Functionally Optimized Natural Products via Chemical Synthesis
Dr Herve GENESTE
LE079 - In Silico Prediction of Brain Penetration - High Accuracy Achieved
Dr Francesco GRECO
LE063 - NR2F6 Antagonists: in Vitro Pharmacology and Preclinical Data of a Potential Next Generation Immuno-oncology Therapy
Dr Gilles GUICHARD
LE090 - Structure-Guided Design of Foldamer-Based Inhibitors of Protein-Protein Interactions
Dr Thomas HAYHOW
LE004 - Discovery And Profiling of AZ'6421: an Oral ERa-Protac with an in vitro-in vivo Disconnect
Dr Timo HEINRICH
LE070 - Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106
Prof. Roderick HUBBARD
LE024 - Photoactivated Covalent Capture of DNA-encoded Fragments to Identify Ligands for Challenging Targets
Dr Soufyan JERHAOUI
LE089 - Discovery of JNJ-1245, a Novel and Potent Fluoroallylamide Mcl-1 Inhibitor for the Treatment of Hematologic Malignancies
Dr Manuela JORG
LE031 - Identification and Structure-activity Relationship Profiling of Positive Allosteric Modulators Targeting Muscarinic Acetylcholine Receptors
Dr Anna JUNKER
LE102 - Development of First PET Tracers for the Imaging of CD73 Expression in Triple-negative Breast Cancer
Ms Elizabeth A. LOPES
LE069 - Dual Inhibition of P53-MDM2/4 Interactions With Spiropyrazoline Oxindoles
Ms Katherine MACFARLANE
LE023 - Exploiting DNA-encoded Library Technology for the Discovery of Novel Antibody Recruiting Molecules Against LOX-1
Dr Maria MANEIRO
LE003 - Antibody-Protac Conjugates: an Approach for Targeted Selective BRD4 Degradation in HER2+ Phenotypes
Prof. Ana MARTINEZ
LE098 - Modulation of TDP-43-pathy by Brain Penetrant Protein Kinase Inhibitors, a New Hope for ALS and Related Disorders
Dr Exequiel PORTA
LE083 - Mining the Leishmania Kinome
Dr Filipa RAMILO-GOMES
LE015 - New Generation of EZH2 Inhibitors for Cancer Therapy: A Computer-Aided Drug Design Approach in Epigenetics
Dr Stefano SAINAS
LE087 - Human Dihydroorotate Dehydrogenase Inhibitor MEDS443: a Magic Bullet Against Coronaviruses
Dr Matthew SEGALL
LE052 - Using AI to Derive Valuable Insights from Drug Discovery Data
Dr Alice SOSIC
LE075 - Bis-3-chloropiperidines Targeting TAR RNA as a Novel Strategy to Impair the HIV-1 Nucleocapsid Protein
Dr Léopold THABAULT
LE044 - Interrogating Lactate Dehydrogenases Oligomeric Interfaces Using (Stapled) Peptides And Small Molecules
Dr Boris VAUZEILLES
LE059 - Fast Detection and Imaging of Hydrogen Peroxide with New Borinic Probes
Dr Anita WEGERT
LE071 - A New Dual Mode of Action to Treat Pain - From Scratch to Pre-Clinical Candidate
Dr Erik WEIS
LE067 - Iridium-catalyzed C-H Activation Methods for Late-stage Functionalization of Pharmaceuticals
Prof. Jukka WESTERMARCK
LE082 - Protein Phosphatase 2A, a Druggable Tumor Suppressor for Cancer Therapy
Dr Birgit WILDING
LE048 - 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
LE055 - Discovery and Optimisation of Potent, Slow-dissociating Inhaled PI4KB Inhibitors
Dr Kenneth GRANBERG
LE028 - Discovery of AZD5462, an Oral Agonist of the Relaxin Family Peptide Receptor 1 (RXFP1) for the Treatment of Cardiorenal Disease
Dr Uwe GRETHER
LE054 - First Disclosure of Cannabinoid Receptor Type 2 Agonist Rg7774 – An Innovative Oral Treatment for Diabetic Retinopathy
Dr Peter HAEBEL
LE027 - 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
LE053 - mPGES1 Inhibitors: First Time Disclosure of Clinical Candidate BI01029539 / GS-248
Dr Kai SCHIEMANN
LE026 - 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
Dr Mikhail ZIBINSKY
LE103 - Discovery of a Selective Oral CCR4 Antagonist RPT193 for Treatment of Atopic Dermatitis and other Allergic Disorders

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