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European Medicinal Chemistry 2023 Agenda

This document contains the agenda for a conference on medicinal chemistry. It includes presentations on various topics such as druggability, efflux pump inhibitors, antimicrobial resistance, anticancer agents, and more. There will be keynote speeches, oral competition presentations, poster presentations, and networking events over the course of two days.

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Shubham Shahu
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0% found this document useful (0 votes)
5 views4 pages

European Medicinal Chemistry 2023 Agenda

This document contains the agenda for a conference on medicinal chemistry. It includes presentations on various topics such as druggability, efflux pump inhibitors, antimicrobial resistance, anticancer agents, and more. There will be keynote speeches, oral competition presentations, poster presentations, and networking events over the course of two days.

Uploaded by

Shubham Shahu
Copyright
© All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd

Thursday September 7, 2023

14:15 Registration
15:15 Welcome and Opening
Dr Maja BEUS (DUKE UNIVERSITY, Durham, United States)
Dr Hrvoje RIMAC (SELVITA, Zagreb, Croatia)
15:30 KL01 - Druggability Beyond the Rule of Five
Dr Sanja KOSTRUN (SELVITA, Zagreb, Croatia)

EFMC-YMCS Competition Presentation Session I


Session Chair: Dr Hrvoje RIMAC (SELVITA, Zagreb, Croatia)

16:00 OC01 - Shedding Light on L-Type Calcium Channels with Novel Far-Red Fluorescent Ligands
Winner of the young medicinal chemist meeting in Belgium (KVCV)
Mrs Carlotta BORGARELLI (KU LEUVEN, Heverlee, Belgium)
16:15 OC02 - Biophysical Screening for the Identification of Small Molecules as Lactate
Dehydrogenase (LDHS)’s Oligomeric State Disruptors
Winner of the young medicinal chemist meeting in Belgium (SRC)
Mrs Chiara BRUSTENGA (UCL/LDRI, Brussels, Belgium)
16:30 OC03 - Discovery of Allosteric Modulators of A2A Receptors
Winner of the young medicinal chemist meeting in Croatia
Ms Tana TANDARIC (RUDER BOSKOVIC INSTITUTE, Zagreb, Croatia)
16:45 OC04 - Molecular Sensing and Imaging of Carbon Dioxide Incomplex Environments
Winner of the young medicinal chemist meeting in Israel
Dr Ori GREEN (ETH ZURICH, Zürich, Switzerland)

17:00 Flash Poster Presentations (Part I)

FP01 – In Silico-Aided Optimization of Metallo Beta-Lactamase Inhibitors Active against


Clinically Relevant Carbapenemases
Dr Matteo BERSANI (UNIVERSITÀ DEGLI STUDI DI TORINO, Torino, Italy)
FP02 – Voc’s Art: Voc-Based Probes for Exploration, Detection and Monitoring of Pathologies
Ms Estelle BLOCHOUSE (IC2MP CNRS, Poitiers, France)
FP03 – Using Chemical Modification of Anticancer Drug Scaffolds to Study Efflux Mediated
Chemoresistance in Cancer Cells
Mrs Madiha CHOWDHURY (KINGS COLLEGE LONDON, London, United Kingdom)
FP04 – Semi-Synthesis of Thioglycoside Derivatives of the Natural Product Antibiotic
Fidaxomicin
Ms Isabella FERRARA (UNIVERSITY OF ZURICH, Zurich, Switzerland)
FP05 – Carbamates as Potential New Drugs in the Treatment of Alzheimer’s Disease
Dr Ana MATOSEVIC (INSTITUTE FOR MEDICAL RESEARCH AND OCCUPATIONAL HEALTH (IMI), Zagreb, Croatia)
FP06 – GPR84 Structural-Functional Selectivity Relationship (SFSR) Reveals Distinct Responses
Induced by Biased Agonists
Mr Wang PINQI (UNIVERSITY OF OXFORD, Oxford, United Kingdom)
FP07 – Design, Synthesis and in vitro Evaluation of New Peptide-Based Inhibitors Targeting Sars-
Cov-2 Main Protease, Focusing on the Exploration of Heterocyclic Systems for the S3/S4 Sub-Pockets
Dr Sara ROSSI (UNIVERSITY OF SIENA, Grosseto, Italy)
FP08 – A Multistep High-Throughput Chemistry Platform to Take Protac Synthesis and Testing to
a New Level
Ms Rebecca STEVENS (GSK/UNIVERSITY OF STRATHCLYDE, Stevenage, United Kingdom)
FP09 – Development of Dual-Functionalized Fluorophores to Monitor Antibody Delivery Systems
Ms Luu TRACEY ( MONASH UNIVERSITY, Parkville, Australia)
FP10 – Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists
Ms Alice VALENTINI ( UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark)
FP13 – Photoswitching HDAC Inhibitors for the Spatiotemporal Targeting of Cancer Cells with Light
Dr Laia JOSA CULLERE (INSTITUTE FOR ADVANCED CHEMISTRY OF CATALONIA (IQAC-CSIC), Barcelona, Spain)

17:25 Coffee Break & Exhibition

EFMC-YMCS Competition Presentation Session II


Session Chair: Dr Michele MARI (UNIVERSITY OF URBINO, Urbino, Italy)

17:45 OC05 - Optimization of a Pyridylpiperazine Series as a Novel Class of Efflux Pump Inhibitors in
E. Coli to Fight Antimicrobial Resistance
Winner of the young medicinal chemist meeting in France (SCT)
Ms Nina COMPAGNE (UNIVERSITY OF LILLE, DRUGS AND MOLECULES FOR LIVING SYSTEMS, Lille, France)

18:00 OC06 - Ga(III) Siderophore Complexes - A Metallo-Trojan Horse Strategy to Tackle Antimicrobial
Resistance
Winner of the young medicinal chemist meeting in Ireland
Mr Lewis MORE O’FERRALL (ROYAL COLLEGE OF SURGEONS, Dublin, Ireland)

18:15 OC07 - Discovery of Isoquinoline Sulfonamides as Gyrase Inhibitors Active against


Fluoroquinolone-Resistant Bacteria
Winner of the young medicinal chemist meeting in The Netherlands
Dr Alexander BAKKER (LEIDEN UNIVERSITY, ‘s-Gravenhage, The Netherlands)

18:30 OC08 - Design Principles for Cyclin K Molecular Glue Degraders


Winner of the 2023 EFMC-YSN PhD Prize
Mrs Zuzanna KOZICKA (FRIEDRICH MIESCHER INSTITUTE FOR BIOMEDICAL RESEARCH, Basel, Switzerland)

18:45 EFMC-YSN Soft Skills Training (1) - Reaxys Workshop: A Tandem Tour to Unveil the Profile of an
Active Molecule
Dr Giulia MONCELSI (ELSEVIER LIFE SCIENCES, Amsterdam, The Netherlands)

19:30 EFMC-YMCS Poster Presentation Session 1

20:45 EFMC-YSN Networking Event

22:00 End of the Day


Friday September 8, 2023
08:30 EFMC-YSN Soft Skills Training (2) - Career Panel Discussion
Dr Kristina GONCHARENKO (ZIFO RND SOLUTIONS, Basel, Switzerland)
Dr Chiara BORSARI (UNIVERSITY OF MILAN, Milan, Italy)
Dr Sanja KOSTRUN (SELVITA LTD., Zagreb, Croatia)
Mr Patrik NIKOLIC (OPTIBRIUM, Cambridge, United Kingdom)
Dr David PERALTA (CHEMMEDCHEM/CHEMISTRY EUROPE, Weinheim, Germany)
Dr Minh Thao TRAN (JANSSEN PHARMACEUTICA, Beerse, Belgium)

EFMC-YMCS Competition Presentation Session III


Session Chair: Ms Floriane ESHAK (UNIVERSITY PARIS CITÉ, Paris, France)

09:30 KL02 - Leveraging Natural Products to Afford New Therapeutic Leads that Can Target Resistant Tumors
Prof. Thomas POULSEN (AARHUS UNIVERSITY, Aarhus C, Denmark)

10:00 OC09 - Synthesis of Quinazoline Derivatives as Anticancer Agents


Winner of the young medicinal chemist meeting in Greece
Dr Eleftheria GEORGIOU (NKUA, Athens, Greece)

10:15 OC10 - Synthesis and Cytotoxic Activity of Novel Sclareol Derivatives


Winner of the young medicinal chemist meeting in Serbia
Mr Pavle A. STOJKOVIC (UNIVERSITY OF BELGRADE, Beograd, Serbia)

10:30 OC11 - From Pan to Pi3Kα-Selective Inhibitors: A Covalent Strategy to Fine-Tune Isoform-Specific Targeting
Winner of the young medicinal chemist meeting in Italy
Dr Chiara BORSARI (UNIVERSITY OF MILAN, Milan, Italy)

10:45 OC12 - Heterobifunctional E3 Ligase Recruiters Enable Pan-Degradation of Inhibitor of


Apoptosis Proteins
Winner of the young medicinal chemist meeting in Slovenia
Mrs Alesa BRICELJ (UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia)

11:00 Flash Poster Presentations (Part II)

FP11 – Design and Synthesis of Novel RNA Ligands as Inhibitors of Oncogenic Micrornas Production
Mr Jihed AZZOUZ (INSTITUT DE CHIMIE DE NICE-ICN, Nice, France)
FP12 – Synthesis Optimization of the First in Class 3CLPRO Inhibitor Nirmatrelvir
Mrs Anastasia FERRARO (UNIVERSITÀ DEGLI STUDI DI NAPOLI FEDERICO II, Napoli, Italy)
FP15 – Aminoacrylamides with Potential Anti-Breast Cancer Activity Act Through 14-3-3σ/Er-Αa PPI
Stabilization
Dr Paulo PITASSE SANTOS (UNIVERSITY OF LEICESTER, Leicester, United Kingdom)
FP16 – Development of First-In-Class Dual LSD1-PRMT5 Inhibitors for the Treatment of Acute
Myeloid Leukemia
Ms Alessia RAUCCI (SAPIENZA UNIVERSITY OF ROME, Rome, Italy)
FP17 – Design, Development and Evaluation of Novel Anticancer Drugs Targeting Protein Kinase D2 (Pkd2)
Ms Lauren VOETS (KU LEUVEN RESEARCH AND DEVELOPMENT, Leuven, Belgium)
FP18 – Novel Activators of Slack Potassium Channels for the Treatment of Histamine-
Independent and Chronic Itch
Mr Wenxin Felix ZHU (GOETHE UNIVERSITY, Frankfurt, Germany)
FP19 – Synthesis, Photochemistry and Biological Activity of Novel Bodipy Photochages as
Potential Anticancer Phototherapeutics
Ms Katarina ZLATIC (RUDER BOSKOVIC INSTITUTE, Zagreb, Croatia)

11:25 Coffee Break & Exhibition


EFMC-YMCS Competition Presentation Session IV
Session Chair: Dr Isabella ROMEO (MAGNA GRÆCIA UNIVERSITY, Catanzaro, Italy)

11:45 OC13 - Peroxide-Cleavable Linkers for Antibody-Drug Conjugates


Winner of the young medicinal chemist meeting in United Kingdom
Mrs Nicola ASHMAN (UNIVERSITY OF CAMBRIDGE, Cambridge , United Kingdom)

12:00 OC14 - Accelerating Mechanistic Deconvolution Using Chemical Biological Tools


Winner of the young medicinal chemist meeting in Denmark
Mr Esben BJERREGAARD SVENNINGSEN (AARHUS UNIVERSITY, Aarhus C, Denmark)

12:15 OC15 - Novel 5-Ht6 Receptor Inverse Agonists and Neutral Antagonists Derived from
2-Arylpyrrole: Sustainable Synthesis and Pharmacological Profiling
Winner of the young medicinal chemist meeting in Poland
Dr Marcin DROP (JAGIELLONIAN UNIVERSITY MEDICAL COLLEGE, Krakow, Poland)

12:30 OC16 - Styrylbenzothiazole Photoswitches for Spatiotemporal Control over Microtubule-


Dependent Biology
Winner of the young medicinal chemist meeting in Germany
Mr Li GAO (ROCHE, Penzberg, Germany)

12:45 Lunch, Networking & Exhibition

13:30 EFMC-YMCS Poster Presentation Session 2

EFMC-YMCS Competition Presentation Session V


Session Chair: Dr Kristina GONCHARENKO (ZIFO RND SOLUTIONS, Basel, Switzerland)

14:45 OC17 - Antimicrobial Photodynamic Therapy Combined with Antimicrobials: an Alternative


Approach for Eradication of Gram-Negative Bacteria
Winner of the young medicinal chemist meeting in Portugal
Mr Rafael AROSO (UNIVERSIDADE DE COIMBRA, Coimbra, Portugal)

15:00 OC18 - Hitting a New Combination of Biological Targets to Cope with Alzheimer’s Disease
Winner of the young medicinal chemist meeting in Spain
Ms Noemí MARTÍNEZ CONDE (UNIVERSITY OF BARCELONA, Barcelona, Spain)

15:15 OC19 - Cyclic Tetrapeptides: Novel Remedy for Lead Poisoning


Winner of the young medicinal chemist meeting in Switzerland
Mrs Tagwa MOHAMMED (UNIVERSITY OF ZURICH, Zurich, Switzerland)

15:30 OC20 - Redox Probes and Bioreductive Prodrugs


Winner of the 2023 Symeres PhD Prize for Excellence in Chemistry in Life Sciences Research
Dr Jan G. FELBER (UNIVERSITÄT MÜNCHEN, München, Germany)

15:45 Voting Break

16:00 KL03 - Trends in Medicinal Chemistry and Chemical Biology


Dr Yves P. AUBERSON (NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)

16:30 Closing and Award Ceremony

16:50 End of the Symposium

Common questions

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The development of styrylbenzothiazole photoswitches is significant for microtubule-dependent cellular processes because they offer precise spatial and temporal control over microtubule dynamics, enabling researchers to modulate cellular functions with light. This can lead to innovative therapeutic approaches where cellular processes are directed with high precision, reducing potential side effects and enhancing the specificity of treatment methodologies .

The structural-functional selectivity relationship (SFSR) of GPR84 influences responses to biased agonists by revealing distinct signaling outcomes based on specific agonist binding. This means that while classical agonists might activate a broad range of downstream effects, biased agonists can selectively modulate particular pathways, possibly reducing side effects and improving therapeutic efficacy for certain conditions .

Bioreductive prodrugs and redox probes offer new avenues for targeting disease environments by exploiting the redox imbalances characteristic of diseased tissues, such as the hypoxic and reductive conditions in tumors. These compounds can remain inactive until they reach their target site, where they are activated by redox reactions, allowing for targeted therapeutic effects with reduced systemic toxicity .

Heterobifunctional E3 ligase recruiters contribute to the degradation of inhibitor of apoptosis proteins by facilitating the ubiquitination process, marking these proteins for degradation by the proteasome. By harnessing the cell's own protein degradation pathways, these compounds can effectively remove proteins that inhibit apoptosis, promoting cell death in cancer cells and offering a targeted therapeutic approach .

Peroxide-cleavable linkers in antibody-drug conjugates offer advantages for targeted cancer therapy by providing a mechanism for controlled drug release within the cancer cell environment, characterized by higher levels of reactive oxygen species. This can enhance the selective delivery and cytotoxic activity of the drug, minimizing off-target effects and potentially improving the therapeutic index .

The benefits of using Ga(III) siderophore complexes in antimicrobial resistance strategies include their ability to mimic iron, a crucial element for bacterial growth, thereby acting as a 'Trojan Horse' to deliver antimicrobial agents inside bacterial cells effectively. However, challenges include ensuring specificity to avoid disrupting essential iron metabolism in host cells and overcoming bacterial mechanisms that may reduce siderophore recognition or import .

Novel activators of slack potassium channels represent a therapeutic approach for treating chronic itch by modulating channel activity to restore normal neuronal signaling pathways that are disrupted in conditions of chronic itch. By targeting a specific channel involved in sensory perception, these activators can provide relief from symptoms without affecting the broader nervous system activities .

The unique challenges presented by the synthesis of quinazoline derivatives as anticancer agents include achieving high specificity and potency against cancer cells while minimizing toxicity to healthy cells. Additionally, the complexity of quinazoline structures can result in synthetic difficulties, requiring careful optimization of reaction conditions to ensure efficient production and the desired pharmacokinetic properties .

The dual inhibition of LSD1 and PRMT5 might serve as a treatment strategy for acute myeloid leukemia by disrupting the epigenetic regulation of genes involved in leukemia cell survival and proliferation. Combining these inhibitory activities can potentiate antileukemic effects through the simultaneous alteration of multiple regulatory pathways, possibly overcoming resistance mechanisms seen with single-target therapies .

Exploring the druggability beyond the Rule of Five is significant because it challenges traditional constraints of drug design, allowing for the development of compounds that may not fit conventional drug-like properties but are effective against targets that require different physical and chemical characteristics. This approach can expand the therapeutic landscape by targeting previously considered 'undruggable' proteins and thus can lead to novel treatments for complex diseases .

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