ACSMEDI-EFMC Medicinal Chemistry Frontiers 2023

Scientific Program

Saturday 10/06/2023
15:00Registration
Opening Session
17:30Opening of the Symposium and Welcome address
Prof. Daniel HARKI
(UNIVERSITY OF MINNESOTA, Minneapolis, MN, United States)
17:45PL01- Medicinal Chemistry of the Future: Trends, Targets and Technologies
Dr Klaus URBAHNS
(EMD SERONO, Billerican, MA, United States)
18:30Welcome Reception
Sunday 11/06/2023
08:00Registration
Session 1 - Chemical Modulation of RNA
Session chair
Dr Darby SCHMIDT
(SONATA THERAPEUTICS, Cambridge, MA, United States)
09:00IL01 - Modulating the Conformation and Function of Disease-Relevant RNA with Small Molecules
Prof. Amanda HARGROVE
(DUKE UNIVERSITY, Durham, NC, United States)
09:30IL02 - Targeting Non-Coding RNAs Using Synthetic Small Molecules: Original Targets for Innovative Therapies
Dr Maria DUCA
(UNIVERSITY OF CÔTE D'AZUR, Nice, France)
10:00IL03 - Discovery and Development of Selective Splicing Modifiers as Therapeutics
Dr Matthew WOLL
(PTC THERAPEUTICS, South Plainfield, NJ, United States)
10:15IL04 - Small Molecules Targeting RNA - a Safety Perspective
Dr Helen Louise LIGHTFOOT
(F. HOFFMANN-LA ROCHE AG, BASEL, Switzerland)
10:30Coffee break & Exhibition
Session 2 - Advances in Targeted Protein Degradation
Session chair
Prof. Terry MOORE
(UNIVERSITY OF ILLINOIS, Chicago, IL, United States)
11:00IL05 - Ligand Directed Degradation: from Proof-of-Concept Degradation to Clinical Studies
Dr Deborah MORTENSEN
(BRISTOL MYERS SQUIBB, San Diego, CA, United States)
11:30IL06 - Chemical Approaches to Edit Post-Translational Modification In Cells
Prof. Christina WOO
(HARVARD UNIVERSITY, Cambridge, MA, United States)
12:00OC01 - Treatment of Pediatric AML Via Protac-Mediated Degration of CDK9
Ms Alexandria CHAN
(UNIVERSITY OF MARYLAND SCHOOL OF PHARMACY, Baltimore, United States)
12:15OC02 - Targeting Progerin Degradation as a New Therapeutic Approach for Treating Progeria
Prof. Silvia ORTEGA-GUTIERREZ
(COMPLUTENSE UNIVERSITY, Madrid, Spain)
12:30Lunch & Exhibition
12:45Company Workshop by Pelago Bioscience: CETSA® Enabled Drug Discovery: An Applied Workshop on Target Identification/Validation and Target Engagement-Driven Lead Generation and Optimization
Dr Fredrik RAHM (PELAGO BIOSCIENCE, Solna, Sweden)
Dr Stina LUNDGREN (PELAGO BIOSCIENCE, Solna, Sweden)
Session 3 - Proximity-inducing Molecules and their Therapeutic Applications
Session chair
Dr Amit CHOUDHARY
(THE BROAD INSTITUTE, Cambridge, MA, United States)
14:00IL07 -Chemoproteomic-Enabled Development of Proximity-Inducing Molecules
Dr Christopher PARKER
(THE SCRIPPS RESEARCH INSTITUTE, La Jolla, CA, United States)
14:30IL08 - An Intramolecular Bivalent Degrader Glues an Intrinsic BRD4-DCAF16 Interaction
Prof. Alessio CIULLI
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom)
15:00OC03 - Discovery of MRT-2359, an Orally Bioavailable GSPT1 Molecular Glue Degrader, for MYC-Driven Cancers
Dr Bernhard FASCHING
(MONTE ROSA THERAPEUTICS, Basel, Switzerland)
15:15OC04 - Integrated Platform Approach for Molecular Degrader Discovery in Proxidrugs
Dr Johanna HUCHTING
(FRAUNHOFER INSTITUTE FOR TRANSLATIONAL MEDICINE AND PHARMACOLOGY, Hamburg, Germany)
15:30Coffee break & Exhibition
16:00PL02 - RIPTACs: A New ‘Hold and Kill’-based Therapeutic Modality
Prof. Craig CREWS
(YALE UNIVERSITY, New Haven, CT, United States)
16:45Poster session 1 (odd numbers)
18:00End of the scientific programme
18:10City Tour
Monday 12/06/2023
08:00ACMEDI-YMCC | EFMC-YSN Programme for Early Career Researchers
Chair
Dr Melissa GRENIER-DAVIES
(GLAXOSMITHKLINE, Cambridge, MA, United States)
08:00Panel Discussion - "Landing a Job in Industry"
Dr Chris DE GRAAF (SOSEI HEPTARES, Cambridge, United Kingdom)
Dr Abdellatif EL MARROUNI (MERCK & CO., West Point, United States)
 (SANOFI-AVENTIS DEUTSCHLAND GMBH)
Dr Malin LEMURELL (ASTRAZENECA, Gothenburg, Sweden)
Dr Darby SCHMIDT (SONATA THERAPEUTICS, Cambridge, MA, United States)
Session 4 - Drug Targets in GPCR Signaling
Session chair
Prof. György KESERU
(HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary)
09:00IL09 - New Hot Targets? Medicinal Chemistry of G Protein-Coupled Receptors Involved in Immunity and Cancer
Prof. Christa MÜLLER
(UNIVERSITY OF BONN, Bonn, Germany)
09:30IL10 - Frontier SBDD across the Orthosteric and Allosteric GPCRome
Dr Chris DE GRAAF
(SOSEI HEPTARES, Cambridge, United Kingdom)
10:00OC05 - Best-In-Class Orally Bioavailable CXCR4 Antagonists to Treat Renal Cell Carcinoma
Dr Eric MILLER
(EMORY UNIVERSITY SCHOOL OF MEDICINE, Atlanta, United States)
10:15OC06 - Targeting Sodium Binding Pocket in Mu Opioid Receptor to Design Safer Analgesics
Dr Susruta MAJUMDAR
(UHSP & WASHINGTON UNIVERSITY, Saint Louis, United States)
10:30Coffee break & Exhibition
Session 5 - Organic Synthesis Impacting Medicinal Chemistry & Chemical Biology
Session chair
Prof. Rui MOREIRA
(UNIVERSITY OF LISBON, Lisbon, Portugal)
11:00IL11 - Photocatalysis in the Pharmaceutical Industry: Synthesis under a New Light
Dr Giulia BERGONZINI
(ASTRAZENECA, Gothenburg, Sweden)
11:30IL12 - HTE Chemistry to Accelerate Medicinal Chemistry Programs
Dr Fabio LIMA
(NOVARTIS, Basel, Switzerland)
12:00OC07 - New Precision Anti-TB Agents by Allosteric Inhibition of Glutamate-5-Kinase Enzyme
Prof. Concepcion GONZALEZ-BELLO
(UNIVERSIDADE DE SANTIAGO DE COMPOSTELA - CIQUS, santiago de compostela, Spain)
12:15OC08 - Impact of gem-Difluoromethylene Group on Physicochemical Properties in Medchem-Relevant Building Blocks
Dr Sergey RYABUKHIN
(ENAMINE LTD, Kyiv, Ukraine)
12:30Lunch & Exhibition
12:45Company Workshop by Schrödinger: Augmenting Medicinal Chemistry with Digital Chemistry: A Lead Optimization Design Challenge for D-Amino Acid Oxidase Inhibitors
Mr Wade MILLER
(SCHRÖDINGER, Cambridge, United States)
Session 6 - Enabling Chemistries for Chemical Biology Research
Session chair
Prof. Daniel HARKI
(UNIVERSITY OF MINNESOTA, Minneapolis, MN, United States)
14:00IL13 - Chemical Probes Enabling Drug Target Discovery and Validation
Prof. Edward TATE
(IMPERIAL COLLEGE LONDON, London, United Kingdom)
14:30IL14 - Generating Stem-Like T Cells with Small-Molecule Modulators for Cancer Immunotherapy
Prof. Peng WU
(THE SCRIPPS RESEARCH INSTITUTE, La Jolla, CA, United States)
15:00OC09 - Targeting Receptor Complexes with Therapeutic Peptides
Prof. Kristian STROMGAARD
(UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark)
15:15OC10 - Azetidin-2-Ones as Quenched Activity-Based Probes to Profile Human Neutrophil Elastase in Proteomes
Ms Rita FÉLIX
(IMED.ULISBOA - RESEARCH INSTITUTE FOR MEDICINES, Lisbon, Portugal)
15:30Coffee break & Exhibition
16:00PL03 -Carbohydrates in Health and Disease
Prof. Laura KIESSLING
(MIT, Cambridge, MA, United States)
16:45Poster session 2 (even numbers)
18:00End of the scientific programme
20:00Banquet (optional)
Tuesday 13/06/2023
Session 7 - A Focus on Early Career Investigators
Session chair
Dr Melissa GRENIER-DAVIES
(GLAXOSMITHKLINE, Cambridge, MA, United States)
09:00IL15 - E3 Ligase Ligand Discovery for TPD
Dr Benika PINCH
(NOVARTIS, Cambridge, MA, United States)
09:15IL16 - Chemical Approaches to Enhance Cellular Immunotherapies
Dr Mark P. FARRELL
(UNIVERSITY OF KANSAS, Lawrence, KS, United States)
09:30IL17 - Machine Learning Tools to Accelerate Chemical Biology Studies
Dr Tiago RODRIGUES
(UNIVERSITY OF LISBON, Lisbon, Portugal)
09:45OC11 - Chemical Probes for RHO GEF/GTPase Complexes
Ms Mia CALLENS
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
10:00OC12 - Potent Targeted Activator of Cell Kill Molecules Selectively Eliminate HIV Infected Cells
Dr Abdellatif EL MARROUNI
(MERCK & CO., West Point, United States)
10:15OC13 - Borrowing Transcriptional Kinases to Activate Apoptosis Using Chemically Induced Proximity
Dr Roman SAROTT
(STANFORD UNIVERSITY, Menlo Park, United States)
10:30Coffee break & Exhibition
Session 8 - Approaches to Identify and Target Cryptic and Allosteric Pocket
Session chair
Dr Malin LEMURELL
(ASTRAZENECA, Gothenburg, Sweden)
11:00IL18 - A Computation-First Approach to Drug Challenging Disease Targets
Dr Woody SHERMAN
(PSIVANT THERAPEUTICS, Boston, MA, United States)
11:30IL19 - X-ray Crystallographic Fragment Screening for the Identification of Allosteric Binding Sites
Dr Andrew WOODHEAD
(ASTEX THERAPEUTICS, Cambridge , United Kingdom)
12:00IL20 - Exploiting Allostery for Computer-Aided Drug Design of Oncogenes
Dr Zoe COURNIA
(BIOMEDICAL RESEARCH FOUNDATION ACADEMY OF ATHENS, Athens, Greece)
12:30OC14 - Structure-Based Drug Discovery and Umbrella Sampling Simulations Identify Novel Potent Troponin Calcium Sensitizers and Elucidate their Function
Prof. Steffen LINDERT
(OSU, Columbus, United States)
12:45Lunch & Exhibition
13:00Company Workshop by CAS: The Evolution of Science at CAS: Connections Between Multi-disciplinary Data and Capabilities
Mrs Vee LINDSAY (CAS, Columbus, United States)
Dr Angela ZHOU (CAS, Columbus, United States)
Session 9 - Getting Out of the Starting Block: New Hit Finding and Chemotype Advancement Methods
Session chair
Dr Carolyn DZIERBA
(BRISTOL-MYERS SQUIBB, Cambridge, MA, United States)
14:00IL21 - RAPID – a Next-Generation Chemoproteomics Technology Enabling the Discovery of Reversible Binders to Pre-specified Targets in Living Cells
Dr Justin RETTENMAIER
(JNANA THERAPEUTICS, Boston, MA, United States)
14:30IL22 - Covalent Fragment-Based Drug Discovery
Dr Daniel ERLANSON
(FRONTIER MEDICINES, South San Francisco, CA, United States)
15:00IL23 - Large-scale in Silico Fragment Screening of ~200 Million Fragments Based on Absolute Free Energy Perturbation
Dr Eric THERRIEN
(SCHRODINGER, New York, NY, United States)
15:15OC15 - Small Molecule Drug Discovery with Peptide-Encoded Libraries
Dr Nathalie GROB
(MASSACHUSETTS INSTITUTE OF TECHNOLOGY, Cambridge, United States)
16:00Closing Ceremony & Poster Prizes Ceremony
16:30End of the Symposium
19:10Boston Red Sox's game (optional)

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