EFMC-ISMC 2021
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Programme

Indicated times are in CEST timezone.


Sunday August 29, 2021
EFMC-ISMC 2021 Opening
Morning Session
EFMC-ISMC 2021 Opening Ceremony

10:00Opening Address by EFMC-ISMC 2021 Chairman
Prof. Karl-Heinz ALTMANN
(ETH ZÜRICH, Zürich, Switzerland)
Address by EFMC president
Prof. Rui MOREIRA
(UNIVERSITY OF LISBON, Lisbon, Portugal)
10:15Opening Lecture
Creating the Next Generation of Therapeutics - Medicinal Chemistry Unleashed (PL001)
Dr Karin BRINER
(NOVARTIS, Cambridge, United States)

THE NAUTA PHARMACOCHEMISTRY AWARD FOR MEDICINAL CHEMISTRY AND CHEMICAL BIOLOGY
Award Ceremony
10:55Award Ceremony presided by EFMC Past-President
Dr Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
Nauta Award Presentation
Prof. Henk TIMMERMAN (VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands)
Dr Andele NAUTA (PROF. DR. W. TH NAUTA STICHTING, The Netherlands)
11:05The Nauta Pharmacochemistry Award for Medicinal Chemistry and Chemical Biology
Award Lecture
Partial Agonism in the Picture (AL001)
Prof. Ad P. IJZERMAN
(LEIDEN UNIVERSITY, Leiden, The Netherlands)
11:45End of Morning Session
EFMC-ISMC 2021 Opening
Afternoon Session
13:00THE UCB-EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY
Award Ceremony
Dr Yves P. AUBERSON (NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
Dr Adrian HALL (UCB PHARMA S.A., Braine-l'Alleud, Belgium)
13:10The UCB-Ehrlich Award for Excellence in Medicinal Chemistry
Award Lecture
Experiences & Future Direction for Medicinal Chemistry in Cardiovascular, Renal and Metabolism Diseases (AL002)
Dr Malin LEMURELL
(ASTRAZENECA, Gothenburg, Sweden)
13:50THE PROUS INSTITUTE-OVERTON AND MEYER AWARD FOR NEW TECHNOLOGIES IN DRUG DISCOVERY
Award Ceremony
Dr Yves P. AUBERSON (NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
Dr Josep Jr. PROUS (PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, Barcelona, Spain)
14:00The Prous Institute - Overton and Meyer Award for New technologies in Drug Discovery
Award Lecture
De Novo Drug Design with Machine Intelligence (AL003)
Prof. Gisbert SCHNEIDER
(ETH ZÜRICH, Zürich, Switzerland)
14:40EFMC Fellows Ceremony
Prof. Rui MOREIRA (UNIVERSITY OF LISBON, Lisbon, Portugal)
Dr Yves P. AUBERSON (NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
15:10Closing
15:15End of the Day
Monday August 30, 2021
Plenary Session
Chair
Dr Karl-Heinz BARINGHAUS
(SANOFI, Frankfurt, Germany)
09:30Medicinal Chemistry: More than Ever (PL002)
Dr Jean-Paul CLOZEL
(IDORSIA PHARMACEUTICALS LTD, Allschwil, Switzerland)
Session 1 'Chemical Biology'

Molecular Imaging Tools for Chemical Biology


Session 2 'Technologies'

Novel Strategies and Methods for Drug Discovery and Development
(CPA Session)
Session 3 'Drug Discovery Projects'

Chemical Tools and Drug Discovery for Neuroinflammation
(EuChemS Session)
Session 1%s%Chemical BiologySession 2%s%TechnologiesSession 3%s%DD Projects
10:15Session Chair
Dr Valle PALOMO
(CENTRO DE INVESTIGACIONES BIOLÓGICAS-CSIC, Madrid, Spain)
10:15Session Chair
Prof. Ke DING
(JINAN UNIVERSITY, Guangzhou, China)
10:15Session Chair
Dr Sonsoles MARTIN-SANTAMARIA
(CIB-CSIC, Madrid, Spain)
10:20Translational Chemical Biology (LE001)
Prof. Gonçalo BERNARDES
(UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
10:20Along the Allostery Stream: Recent Advances in Computational Methods for Allosteric Drug Discovery (LE005)
Prof. Jian ZHANG
(SHANGHAI JIAO TONG UNIVERSITY, Shanghai, China)
10:20Microglia in Neuroinflammation: an Intriguing Target towards Neuroprotection and Neuroregeneration (LE009)
Prof. Barbara MONTI
(UNIVERSITY OF BOLOGNA, Bologna, Italy)
11:00Chemical Tools to Study Redox Biology (LE002)
Prof. Pablo RIVERA FUENTES
(EPF LAUSANNE, Lausanne, Switzerland)
11:00Molecular Glue Design for Targeted Cancer Therapy (LE006)
Dr Xiangbing QI
(TSINGHUA UNIVERSITY | NATIONAL INSTITUTE OF BIOLOGICAL SCIENCE, China)
11:00Development of Fluorinated PET Tracers for Imaging of α1 Receptors in the Brain (LE010)
Prof. Bernhard WÜNSCH
(UNIVERSITY OF MÜNSTER, Münster, Germany)
11:20Sensing Enzymatic Activity with Quantum Dots in Patient-Derived Neurodegenerative Disease Models (LE003)
Dr Valle PALOMO
(CENTRO DE INVESTIGACIONES BIOLÓGICAS-CSIC, Madrid, Spain)
11:20Discovery of New SARS-COV-2 MPRO Inhibitors With Potent in vitro and In vivo Antiviral Activity (LE007)
Prof. Shengyong YANG
(SICHUAN UNIVERSITY, Sichuan, China)
11:20Boosting the Resolution of Inflammation Through Formyl Peptide Receptor 2 (FPR2) Agonists as a Novel Strategy in Neuroinflammation-associated Central Nervous System Disorders (LE011)
Prof. Enza LACIVITA
(UNIVERSITÀ DEGLI STUDI DI BARI, Bari, Italy)
11:40Pattern-generating Fluorescent Molecular Probes for Chemical Biology (LE004)
Dr Leila MOTIEI
(WEIZMANN INSTITUTE OF SCIENCE, Rehovot, Israel)
11:40Development of A New Target Identification System for Small Molecules in Trypanosoma Brucei Parasites (LE008)
Ms Suzanne Sherihan SAHRAOUI
(UNIVERSITY OF GENEVA, Geneva, Switzerland)
11:40Small Molecule Degradeers Targeting Folding Intermediates: the Prion Protein Case Study (LE012)
Dr Andrea ASTOLFI
(UNIVERSITY OF PERUGIA, Perugia, Italy)
12:00End of morning session
Company Workshop
12:30Company Workshop
Schrödinger
LiveDesign: a Collaborative Environment for Real-world Drug Discovery Workflows
13:15Poster Session 1, Exhibition & Networking
Session 4 'Chemical Biology'

Photochemistry in Drug Discovery: Photopharmacology, Phototoxicity and Synthesis
(ACSMEDI Session)
Session 5 'Technologies'

Cryo-EM as an Emerging Tool for Small-Molecule Drug Discovery


Session 6 'Drug Discovery Projects'

Next Generation Drugs for Heart Failure



Session 4%s%Chemical BiologySession 5%s%TechnologiesSession 6%s%DD Projects
15:30Session Chairs
Mr Timothy J. HENDERSON (MERCK & CO, Boston, United States)
Dr Amjad ALI (MERCK & CO. INC., Kenilworth, United States)
15:30Session Chair
Dr Jean-Paul RENAUD
(URANIA THERAPEUTICS, Ostwald, France)
15:30Session Chair
Dr Alleyn T. PLOWRIGHT
(WREN THERAPEUTICS LTD, Cambridge, United Kingdom)
15:35Photopharmacology: Towards Light-Controlled Therapy (LE013)
Dr Wiktor SZYMANSKI
(UNIVERSITY OF GRONINGEN, Groningen, The Netherlands)
15:35Cryo-EM in GPCR Structure Based Drug Discovery (LE017)
Dr Stacey SOUTHALL
(SOSEI HEPTARES, Cambridge, United Kingdom)
15:35Identification of Potent and Long Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases (LE021)
Dr Sergio MALLART
(SANOFI R&D, CHILLY MAZARIN, France)
16:15Mapping Cell-Cell Interactions in Tumor Microenvironment via Photocatalytic Proximity Labeling (LE014)
Dr Niyi FADEYI
(MERCK & CO, Cambridge, United States)
16:15Allosteric Regulation of GTP Cyclohydrolase I (LE018)
Dr Herbert NAR
(BOEHRINGER INGELHEIM, Biberach, Germany)
16:15MAP4K4 Inhibitors For The Suppression Of Cardiac Muscle Cell Death (LE023)
Dr Gary NEWTON
(THE INSTITUTE OF CANCER RESEARCH, London , United Kingdom)
16:35Azaaurones as Novel Chemotypes Against Mycobacterium Tuberculosis: SAR ADME Profiling and Photo-Switching Properties (LE015)
Mr André CAMPANICO
(I.MED.ULISBOA - FFULISBOA, Lisboa, Portugal)
16:35The Role of Cryo-EM in Fragment-Based Drug Discovery (LE019)
Dr Judith REEKS
(ASTEX PHARMACEUTICALS, Cambridge, United Kingdom)
16:35Development of Non-Coding RNA Based Next-Generation Heart Failure Therapeutics (LE024)
Dr Thomas THUM
(HANNOVER MEDICAL SCHOOL (MHH), Hannover, Germany)
16:55In vivo Adrenergic Modulation with Photopharmacology (LE016)
Dr Davia PRISCHICH
(INSTITUTE FOR BIOENGINEERING OF CATALONIA (IBEC) , Barcelona, Spain)
16:55Structure Based Drug Discovery Targeting Helicobacter Pylori, Using Cryo-EM (LE020)
Dr Eva CUNHA
(UNIVERSITY OF OSLO & OSLO UNIVERSITY HOSPITAL, OSLO, Norway)
16:55Discovery of Aficamten (CK-274): A Novel, Small Molecule, Cardiac Myosin Inhibitor for the Potential Treatment of Hypertrophic Cardiomyopathies (HCM) (LE022)
Dr Grace CHUANG
(CYTOKINETICS, South San Francisco, United States)
Session 7.1.

First Time Disclosures (Part I)
Session Chair
Dr Cornelia ZUMBRUNN
(IDORSIA PHARMACEUTICALS LTD., Allschwil, Switzerland)
17:15Design and Preclinical Characterization Program Towards BAY 2433334, an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic Disorders (LE025)
Dr Susanne ROEHRIG
(BAYER HEALTHCARE, Wuppertal, Germany)
17:45First Time Disclosure of BI 1265162, an ENaC Inhibitor for the Treatment of Cystic Fibrosis (LE026)
Dr Jörg KLEY
(BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach an der Riss, Germany)
18:15Discovery of the Clinical Candidate AZD4604, a Potent and Selective Janus Kinase 1 Inhibitor, as an Inhaled Treatment for Respiratory Disease (LE027)
Dr Magnus NILSSON
(ASTRAZENECA, Mölndal, Sweden)
18:45End of the Day
Tuesday August 31, 2021
EFMC Prize Ceremony & Lectures 2020
09:30Prize Ceremony
09:35The 2020 EFMC Prize for a Young Medicinal Chemist in Industry
Discovery of Potent Selective GABAA Alpha5 Positive Allosteric Modulators (PAMs) for the treatment of neurological disorders (PR001)
Dr Giuseppe CECERE
(F. HOFFMANN-LA ROCHE, Basel, Switzerland)
09:55The 2020 EFMC Prize for a Young Medicinal Chemist in Academia
Within Our Control? Illuminating How Ephemeral Electrophiles Rewire Cell Decision-Making Processes (PR002)
Prof. Yimon AYE
(EPFL, Lausanne, Switzerland)
Session 8 'Chemical Biology'

Chemical Probes for Target Discovery and Validation

Session 9 'Technologies'

Innovative Synthesis for Medicinal Chemistry


Session 10 'Drug Discovery Projects'

Addressing Neglected and Emerging Viral Diseases with Small Molecules
(AFMC Session)
Session 8%s%Chemical BiologySession 9%s%TechnologiesSession 10%s%DD Projects
10:15Session Chair
Prof. Gyorgy KESERU
(HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary)
10:15Session Chair
Prof. Cristina NEVADO
(UNIVERSITY OF ZURICH, Zurich, Switzerland)
10:15Session Chair
Prof. Esin AKI-YALCIN
(ANKARA UNIVERSITY, Ankara, Turkey)
10:20Chemical Probes to Explore Cancer Biology and Validate Drug Targets (LE028)
Prof. Paul WORKMAN
(INSTITUTE OF CANCER RESEARCH, London, United Kingdom)
10:20Recent Developments in Strategies and Tactics Towards Complex Secondary Metabolites (LE032)
Prof. Erick M. CARREIRA
(ETH ZÜRICH, Zürich, Switzerland)
10:20Discovery of a Novel Class of Small Molecule Dengue Virus Inhibitors (LE036)
Dr Tim JONCKERS
(JANSSEN, Beerse, Belgium)
11:00Chemical Probes to Study Lipid Signaling (LE029)
Dr Mario VAN DER STELT
(LEIDEN UNIVERSITY, Leiden, The Netherlands)
11:00Innovative DNA-based Asymmetric Catalysis (LE033)
Dr Stellios ARSENIYADIS
(QUEEN MARY UNIVERSITY OF LONDON, London, United Kingdom)
11:00Antivirals Against Chikungunya Virus: Analyzing the Current Situation to Identify New Opportunities (LE037)
Prof. Maria-Jesus PÉREZ-PÉREZ
(INSTITUTO DE QUÍMICA MÉDICA, Madrid, Spain)
11:20Discovery of MRK-740, a First-in-class, Potent, Selective and Cell Active PRDM9 Chemical Probe (LE030)
Dr Christian FISCHER
(MERCK, SHARP & DOHME, Boston, United States)
11:20Scaffold-Assisted Peptide Cyclizations: Towards Protein Mimics (LE034)
Prof. Jan VAN MAARSEVEEN
(UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands)
11:20Artificial Intelligence for Emerging and Neglected Diseases Drug Discovery (LE038)
Prof. Carolina H. ANDRADE
(FEDERAL UNIVERSITY OF GOIAS , Goiânia, Brazil)
11:40Quenched Activity-based Probes as New Chemical Tools to Analyse Resistance to Antibiotics (LE031)
Ms Rita FÉLIX
(IMED.ULISBOA - INSTITUTO DE INVESTIGAÇÃO DO MEDICAMENTO, Lisboa, Portugal)
11:40Synthesis of New Building Blocks from the Chemical Universe Database GDB (LE035)
Ms Aline CARREL
(UNIVERSITY OF BERN, Bern, Switzerland)
11:40Innovative Dihydroorotate Dehydrogenase Clinical Ready Inhibitors as Pan-Coronavirus Antivirals: Targeting the Unexpected with Innovation (LE039)
Dr Marco LOLLI
(UNIVERSITY OF TURIN, Torino, Italy)
12:00End of morning session
Company Workshop 1Company Workshop 2
Chemical%s%Computing GroupWuXi AppTec
12:30Chemical Computing Group: Designing Molecules in the Binding Site
12:30WuXi AppTec: DEL Screening Technology as an Enabling Tool for Medicinal Chemists
13:15Poster Session 2, Exhibition & Networking
Session 11 'Chemical Biology'

Chemical Approaches to Stem Cell Differentiation
(ICBS Session)
Session 12 'Technologies'

Expanding Chemical Space through AI - Linking Synthesis Prediction and Automation

Session 13 'Drug Discovery Projects'

Breathing Life into Inhaled Drug Discovery: Challenges and Breakthroughs to the Clinic
(ACSMEDI Session)
Session 11%s%Chemical BiologySession 12%s%TechnologiesSession 13%s%DD Projects
15:30Session Chair
Prof. Colin POUTON
(MONASH UNIVERSITY, Clayton, Australia)
15:30Session Chair
Dr Ola ENGKVIST
(ASTRAZENECA, Mölndal, Sweden)
15:30Session Chair
Dr Nicole GOODWIN
(GSK, King of Prussia, United States)
15:35A Chemical Approach to Controlling Cell Fate (LE040)
Dr Sheng DING
(UNIVERSITY OF CALIFORNIA SAN FRANCISCO, San Francisco, United States)
15:35AI Assisted and Automated Chemical Synthesis (LE044)
Prof. Klavs F. JENSEN
(MASSACHUSETTS INSTITUTE OF TECHNOLOGY, Cambridge, United States)
15:35Inhaled New Modalities in Respiratory Disease: Past, Present, Future (LE048)
Dr Werngard CZECHTIZKY
(ASTRAZENECA, Mölndal, Sweden)
16:15Discovery of Small Molecules to Manipulate Cell Fate in vivo: Towards New Therapies for Degenerative Diseases (LE041)
Prof. Angela RUSSELL
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
16:15Universal Synthesis Machines and Chemputation (LE045)
Prof. Leroy CRONIN
(UNIVERSITY OF GLASGOW, Glasgow, United Kingdom)
16:15Discovery of Novel Inhaled PI3Kd Inhibitor by Lung Retention Optimisation (LE049)
Dr Montse ERRA SOLA
(ALMIRALL, S.A., Barcelona, Spain)
16:35Probing Embryonic Mesodermal Differentiation Enables Identification of Small Molecule Bone Morphogenetic Protein Activators (LE042)
Prof. Dennis SCHADE
(CHRISTIAN-ALBRECHTS-UNIVERSITY OF KIEL, Kiel, Germany)
16:35AI in the Lab: Automating Chemical Synthesis. Where Next From Here? (LE046)
Dr Teodoro LAINO
(IBM RESEARCH EUROPE, Rueschlikon, Switzerland)
16:35Introduction to Preclinical Inhaled Drug Dosing and its Application to Measure the Therapeutic Index of Inhaled Steroids (LE050)
Dr Jonathan PHILLIPS
(AMGEN, Newbury Park, United States)
16:55Potential of Stem Cell Technology in Discovery of Drugs for Neurodegenerative Diseases (LE043)
Prof. Colin POUTON
(MONASH UNIVERSITY, Clayton, Australia)
16:55Progress and Limitations in Exploring the Chemical Space with AI (LE047)
Dr Ola ENGKVIST
(ASTRAZENECA, Mölndal, Sweden)
16:55Design and Development of Inhaled Molecules to Target the Pulmonary Vasculature (LE051)
Dr Duncan SHAW
(NOVARTIS, Cambridge, United States)
Session 7.2.

First Time Disclosures (Part II)
17:15Session Chair
Dr Antonia F. STEPAN
(F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland)
17:15Discovery of an Oral, RO5 Compliant, Interleukin 17a Protein-Protein Interaction Modulator for the Treatment of Psoriasis and other Inflammatory Diseases (LE052)
Mr Kevin DACK
(LEO PHARMA, Ballerup, Denmark)
17:45Insights to the Discovery and Design of Ataxia Telangiectasia Mutated (ATM) Kinase inhibitors M3541 and M4076 with Strong Anti-tumor Efficacy in Combination Therapy Approaches (LE053)
Dr Thomas FUCHSS
(MERCK KGAA, Darmstadt, Germany)
18:15Discovery of JDQ443 a Structurally Unique, Highly Potent, Selective and Orally Bioavailable KRASG12C Covalent Inhibitor (LE054)
Dr Simona COTESTA
(NOVARTIS, Basel, Switzerland)
18:45End of the Day
Wednesday September 1, 2021
EFMC Prize Ceremony & Lectures 2021
09:30Prize Ceremony
09:35The 2021 EFMC Prize for a Young Medicinal Chemist in Industry
Integrin Antagonists for the Treatment of Idiopathic Pulmonary Fibrosis (PR003)
Dr Niall ANDERSON
(GLAXOSMITHKLINE, Hertfordshire, United Kingdom)
09:55The 2021 EFMC Prize for a Young Medicinal Chemist in Academia
COVID Moonshot – Crowdsourcing a Covid-19 Cure (PR004)
Dr Nir LONDON
(THE WEIZMANN INSTITUTE OF SCIENCE, Rehovot, Israel)
Session 14 'Chemical Biology'

Carbohydrate Recognition and Drug Design

Session 15 'Technologies'

Application of Artificial Intelligence in Drug Discovery Projects
Session 16 'Drug Discovery Projects'

New Strategies and Agents for Targeting Gram-Negative Pathogens
Session 14%s%Chemical BiologySession 15%s%TechnologiesSession 16%s%DD Projects
10:15Session Chair
Dr Alexander TITZ
(HELMHOLTZ INSTITUTE FOR PHARMACEUTICAL SCIENCES, Saarbrücken, Germany)
10:15Session Chair
Dr Christopher SWAIN
(CAMBRIDGE MEDCHEM CONSULTING, Duxford, United Kingdom)
10:15Session Chair
Dr Vicky STEADMAN
(SAI LIFE SCIENCES LTD, Essex, United Kingdom)
10:20C-type Lectin Receptors as Drug Targets (LE055)
Dr Christoph RADEMACHER
(UNIVERSITY OF VIENNA, Vienna, Austria)
10:20Artificial Intelligence in Chemical Biology and Drug Discovery - Data, Applications, and Illusions (LE059)
Prof. Andreas BENDER
(UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
10:20Therapies for Gram-Negative Bacterial Infections: New Approaches and Further Generations of Existing Series (LE063)
Dr Mike DAWSON
(MIKE DAWSON ANTIMICROBIAL RESEARCH CONSULTANCY LTD., Stevenage, United Kingdom)
11:00Design, Synthesis, and Development of Lectin Ligand Mimetics (LE056)
Prof. Ulf NILSSON
(LUND UNIVERSITY, Lund, Sweden)
11:00Augmenting Drug Hunters with Generative Chemistry Models (LE060)
Dr Nadine SCHNEIDER
(NOVARTIS, Basel, Switzerland)
11:00Tethered Macrocyclic Peptides, a Novel Antibiotic Class Targeting Acinetobacter Baumannii (LE064)
Dr Patrizio MATTEI
(ROCHE INNOVATION CENTER BASEL, Basel, Switzerland)
11:20Lectins from Pathogens: From Structural Glycobiology to Antiadhesive Strategies (LE057)
Dr Anne IMBERTY
(CNRS/CERMAV, Grenoble, France)
11:20Navigating Chemical Space by Artificial Intelligence (LE061)
Dr Gerhard HESSLER
(SANOFI-AVENTIS DEUTSCHLAND, Frankfurt am Main, Germany)
11:20Discovery of Submicromolar Inhibitors of the Virulence Factor LASB from Pseudomonas Aeruginosa Using Rational Design (LE065)
Prof. Anna K. H. HIRSCH
(HELMHOLTZ INSTITUTE FOR PHARMACEUTICAL RESEARCH SAARLAND, Saarbrücken, Germany)
11:40Development of Glycomimetic Collectin-11 Antagonists to Reduce Complement-Mediated Ischemia-Reperfusion Injuries (LE058)
Dr Rachel HEVEY
(UNIVERSITÄT BASEL, Basel, Switzerland)
11:40Generative Recurrent Neural Networks (RNN) for de novo Drug Design (LE062)
Dr Pooja DESHMUKH
(SAI LIFESCIENCES PVT LIMITED, Hyderabad, India)
11:40DOTAM-based Sideromycins to Visualize and Treat MDR Bacterial Pathogens in vivo and in vitro (LE066)
Mr Carsten PEUKERT
(HELMHOLTZ CENTRE FOR INFECTION RESEARCH, Braunschweig, Germany)
12:00End of morning sesssion
Company Workshops 1Company Workshops 2
Charles River%s%workshopNovAliX%s%workshop
12:30Charles River: Developing Inhaled Drugs for Respiratory Diseases: A Medicinal Chemistry Perspective
12:30NovAliX: DNA-Encoded Library Technology: Strengths and Development Opportunities
13:15Poster Session 3, Exhibition & Networking
Session 17 'Chemical Biology'

Small Molecules Targeting RNA Function and Processing
Session 18

Highlights of Medicinal Chemistry

Session 19 'Drug Discovery Projects'

Tissue and Cell Specific Drug Delivery
(EUFEPS Session)
Session 17%s%Chemical BiologySession 18Session 19%s%DD Projects
15:30Session Chair
Dr Maria DUCA
(UNIVERSITY OF CÔTE D'AZUR, Nice, France)
15:30Session Chair
Prof. Koen AUGUSTYNS
(UNIVERSITY OF ANTWERP, Antwerp, Belgium)
15:30Session Chair
Prof. Sebastien PAPOT
(SCT & UNIVERSITY OF POITIERS, Poitiers, France)
15:35Targeting RNA With Drug-Like Small Molecules (LE067)
Dr Jennifer PETTER
(ARRAKIS THERAPEUTICS, Waltham, United States)
15:35Discovery and Development of a Mkk-4 Inhibitors to Increase Liver Regeneration (LE071)
Prof. Stefan LAUFER
(UNIVERSITY OF TÜBINGEN, Tübingen, Germany)
15:35Antibody-Drug Conjugates (ADC) and Small Molecule-Drug Conjugates (SMDC): a Comparative Evaluation (LE075)
Prof. Dario NERI
(ETH ZÜRICH, Zürich, Switzerland)
16:15Drugging RNA Modifying Enzymes - METTL3 Inhibitors (LE068)
Dr David HARDICK
(STORM THERAPEUTICS LTD, Cambridge, United Kingdom)
15:55Targeting Oncogenic BRAF Using a Novel Allosteric Site (LE072)
Prof. Evripidis GAVATHIOTIS
(ALBERT EINSTEIN COLLEGE OF MEDICINE, New York, United States)
16:15Nucleic Acids as Household Medicine: Living in The World of RNA Therapeutics (LE076)
Dr Muthiah MANOHARAN
(ALNYLAM PHARMACEUTICALS, Cambridge, United States)
16:35Modulating Viral RNAS with Amiloride Small Molecules (LE070)
Prof. Amanda HARGROVE
(DUKE UNIVERSITY, Durham, United States)
16:15Furan-Oxidation Mediated Technology: from in vitro Analysis of Protein-Protein Interactions to GPCR-Ligand Interactions on Live Cells (LE073)
Dr Laia MIRET CASALS
(GHENT UNIVERSITY, Gent, Belgium)
16:35Omics-Based Development of Nanomedicines for Safe and Effective Drug Delivery in Cancer (LE077)
Prof. Erem BILENSOY
(HACETTEPE UNIVERSITY, Ankara, Turkey)
16:55Splice-Switching Small Molecules as Inducers of Apoptosis (LE069)
Ms Emma CAMPBELL
(UNIVERSITY OF STRATHCLYDE, Glasgow, United Kingdom)
16:35LNP023: Discovery and Synthesis of a First-In-Class, Oral Factor B Inhibitor for Treatment of Rare Renal and Hematological Diseases (LE074)
Dr Stefanie FLOHR
(NOVARTIS, Basel, Switzerland)
16:55Targeting the Specificities of the Tumor Microenvironment for Cancer Therapy and Diagnosis (LE078)
Prof. Sebastien PAPOT
(SCT & UNIVERSITY OF POITIERS, Poitiers, France)
16:55The IUPAC-Richter Prize Lecture
The Discovery of Relpax® and Nurtec ODT® - Two Different Treatments for Migraine Headaches (PR005)
Dr John E. MACOR
(SANOFI, Waltham, United States)
Plenary Session
17:15Session chair
Prof. Marko ANDERLUH
(UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia)
17:15Translational Chemistry (PL003)
Prof. Phil BARAN
(THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States)
18:00End of the Day
Thursday September 2, 2021
Plenary Session
Chair
Dr Luc VAN HIJFTE
(SYMERES, Nijmegen, The Netherlands)
09:30Targeting Protein Scaffolding Function in Kinases (PL004)
Prof. Stefan KNAPP
(GOETHE UNIVERSITY FRANKFURT, Frankfurt am Main, Germany)
Session 20

Emerging Topics

Session 21 'Technologies'

Prodrug Strategies in Drug Design and Discovery
Session 22 'Drug Discovery Projects'

Targeting Fibrotic Diseases with Small Molecules
Session 20Session 21%s%TechnologiesSession 22%s%DD Projects
10:15Session Chair
Prof. Beatriz DE PASCUAL-TERESA
(CEU SAN PABLO UNIVERSITY, Madrid, Spain)
10:15Session Chairs
Prof. Bernd CLEMENT (UNIVERSITY OF KIEL, Kiel, Germany)
Prof. Jarkko RAUTIO (UNIVERSITY OF EASTERN FINLAND, Kuopio, Finland)
10:15Session Chair
Dr Christian KUTTRUFF
(BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach, Germany)
10:20Toward a New Therapy for Immune-mediated Tissue Injury (LE079)
Dr Julie SPICER
(THE UNIVERSITY OF AUCKLAND, Auckland, New Zealand)
10:20Prodrug Strategies in Medicinal Chemistry (LE084)
Prof. Jarkko RAUTIO
(UNIVERSITY OF EASTERN FINLAND, Kuopio, Finland)
10:20Novel Molecular Targets for the Treatment of Fibrosis (LE088)
Prof. Joerg DISTLER
(UNIVERSITY OF ERLANGEN–NUREMBERG, Erlangen, Germany)
10:40A Phenotypic Screen Identifies a Small Molecule that Induces Differentiation of AML Cells in vitro and Shows Anti-Tumour Effects in vivo (LE080)
Dr Laia JOSA CULLERE
(INSTITUTE FOR ADVANCED CHEMISTRY OF CATALONIA (IQAC-CSIC), Barcelona, Spain)
11:00New Examples for N-Hydroxyamidine Prodrugs (LE085)
Prof. Bernd CLEMENT
(UNIVERSITY OF KIEL, Kiel, Germany)
11:00Discovery of GLPG1205, a First in Class GPR84 Antagonist in Phase II Clinical Trial (LE089)
Dr Romain GOSMINI
(GALAPAGOS, Romainville, France)
11:00Isoform-selective TAU Tubuline Kinase 1 Inhibitors Reduce TDP-43 Hyperphosphorylation: a New Hope in the Treatment of TDP-43 Proteinopathies (LE081)
Ms Vanesa NOZAL GARCIA
(CIB - CSIC, Madrid, Spain)
11:20Neladenoson Bialanate Hydrochloride: a Prodrug Exploration of a Partial Adenosine A1 Agonist (LE086)
Dr Daniel MEIBOM
(BAYER PHARMA, Wuppertal, Germany)
11:20Investigating the Chameleonic Properties of RGD Integrin Antagonists for the Treatment of Idiopathic Pulmonary Fibrosis (LE090)
Dr James THOMPSON
(GLAXOSMITHKLINE, Stevenage, United Kingdom)
11:20Target-Templated de novo Design of Drug-like Cyclic Peptides: PD-1/PD-L1 Inhibitors (LE082)
Mr Salvador GUARDIOLA
(ONA THERAPEUTICS, Barcelona, Spain)
11:40Targeted (Pro)Drugs for Improved Treatment of Brain Tumors (LE087)
Dr Kristiina HUTTUNEN
(UNIVERSITY OF EASTERN FINLAND, Kuopio, Finland)
11:40Discovery of the Highly Potent and Selective S1P2 Antagonist GLPG2938, a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis (LE091)
Dr Adeline PALISSE
(GALAPAGOS NV, Mechelen, Belgium)
11:40Discovery of LAS200019, a Novel Topical Jak Inhibitor for the Treatment of Inflammatory Skin Diseases (LE083)
Dr Elena GOMEZ
(ALMIRALL, BARCELONA, Spain)
12:00End of morning session
13:15Poster Session 4, Exhibition & Networking
Session 23 'Chemical Biology'

Target Deconvolution Strategies in Drug Discovery
Session 24 'Technologies'

Biocatalysis & Late Stage Functionalisation

Session 25 'Drug Discovery Projects'

Recent Advances in Anticancer Drug Discovery
Session 23%s%Chemical BiologySession 24%s%TechnologiesSession 25%s%DD Projects
15:30Session Chair
Prof. Paul BRENNAN
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
15:30Session Chair
Dr Radka SNAJDROVA
(NOVARTIS PHARMA AG, Basel, Switzerland)
15:30Session Chair
Prof. Roberto DI SANTO
(SAPIENZA UNIVERSITY OF ROME, Rome, Italy)
15:35Mechanistic Insights of a CDK9 Inhibitor via Orthogonal Proteomics Methods (LE092)
Dr Paola CASTALDI
(LIFEMINE THERAPEUTICS, Cambridge, United States)
15:35Reprogramming Nonribosomal Peptide Biosynthesis (LE096)
Prof. Donald HILVERT
(ETH ZURICH, ZURICH, Switzerland)
15:35Targeting Cancer (LE100)
Prof. Daniel RAUH
(TU DORTMUND, Dortmund, Germany)
16:15Proteomes in 3D (LE093)
Prof. Paola PICOTTI
(ETH ZÜRICH, Zürich, Switzerland)
16:15Flavoenzyme Biocatalysis in Bioorganic and Medicinal Chemistry - Challenges and Opportunities (LE097)
Prof. Marko D. MIHOVILOVIC
(TU WIEN, Vienna, Austria)
16:15Structure-Based Optimization and Synthesis of M3258, a Potent and Selective Inhibitor of the Immunoproteasome Subunit LMP7 (beta5i) Demonstrating Strong Efficacy in Multiple Myeloma Models (LE101)
Dr Markus KLEIN
(MERCK KGAA, Darmstadt, Germany)
16:35A Novel Bacterial Three-Hybrid System for Target Identification in Bacteria (LE094)
Ms Radhia EL PHIL
(UNIGE, Geneva , Switzerland)
16:35Utilization of Fe/α-Ketoglutarate-Dependent Enzymes for Stereocontrolled Functionalization (LE098)
Prof. Rebecca BULLER
(ZHAW SCHOOL OF LIFE SCIENCES AND FACILITY MANAGEMENT, Wädenswil, Switzerland)
16:35Magic in the Moonlight: Our Contribution to the Development of IDO1 Inhibitors for Cancer Immunotherapy (LE102)
Prof. Tracey PIRALI
(UNIVERSITÀ DEL PIEMONTE ORIENTALE, Novara, Italy)
16:55EFMC-YMCS Presentation Prize
Design and Synthesis of Chemical Tools to Probe the Function of TRIM33 (LE095)
Ms Jessica REYNOLDS
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
16:55Integration of Biocatalysis into Medicinal Chemistry Programs for Late-Stage Oxidised Derivatives using Polycyps Enzymes (LE099)
Mr Frank SCHEFFLER
(HYPHA DISCOVERY LTD, Abingdon, United Kingdom)
16:55Design and Optimization of a First-in-class NACK Inhibitor: A Novel Path to Notch Inhibition (LE103)
Dr Tanya KELLEY
(UNIVERSITY OF MIAMI, Miami, United States)
THE KLAUS GROHE AWARD 2020
Award Ceremony
17:15Laudatio
Prof. Daniel RAUH
(TU DORTMUND, Dortmund, Germany)
17:15Award Ceremony - GDCh President
Prof. Peter R. SCHREINER
(JUSTUS-LIEBIG UNIVERSITY, D-35392 Giessen, Germany)
17:25The Klaus Grohe Award Lecture
Chemical-Proteomic Strategies to Fight Multiresistant Bacteria (AL004)
Prof. Stephan A. SIEBER
(TECHNICAL UNIVERSITY MUNICH, Garching, Germany)
EFMC-ISMC Closing Ceremony
18:05Closing Remarks, Poster Prizes and Welcome to EFMC-ISMC 2022

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