Pre-Conference Focus Day
Tuesday 12th December 2023
8:15 am Registration Opens & Welcome Coffee
8:50 am Chair’s Opening Remarks
Optimizing Screening Technologies to Validate RNA Targets for Accelerated Hit to Lead
9:00 am Applying Biophysical Screening to Determine RNA Structure & Validate Targets
Synopsis
- Understanding the importance of biophysical screening in progressing in a rational way
- Understanding how compounds interact with RNA
- Optimizing compounds to validate RNA Targets for small molecules – do the RNA-small molecule interactions have an effect?
9:30 am Comprehensive Interactome Profiling of RNA Library vs Compound Library Identifies Selective RNA Binders
Synopsis
- A highly structured RNA library that includes RNA structures identified through in-cell probing
- In vitro interactome of ~30,000 drug-like compounds vs ~1,000 RNA structures extracted from naturally occurring RNA
- Quantitative profiling of selectivity between RNA structures and small molecules
- Simultaneous analysis of binding modes at the single-nucleotide resolution
10:00 am Roundtable Discussion: Investigating the Dynamic Interactions Between RNA & Small Molecules to Determine Targetable RNA Regions
Synopsis
- Fundamental understanding of the RNA structures being inhibited by small molecules
- Exploring the current database to understand the different confirmations of RNA to identify targets
- What are the approaches to narrow down potential candidates for drug targets that bind small molecules and elicit a response?
11:00 am Morning Networking Break
12:00 pm Structural Biology of mRNA Driving Drug Design
Synopsis
- Identification of relevant mRNA isoforms and druggable regions
- Selection of accurate and fast screening methods
- Cellular assays for hit confirmation and optimization
Successfully Develop an Effective Toolbox to Fast-Track RNA Target Discovery
12:30 pm Panel Discussion: What Makes a ‘Good’ RNA Target?
Synopsis
- Understanding how to find the best RNA target to drug the undruggable
- Which RNA structures would make suitable targets?
- How to achieve successful proof-of-concept with validated targets?
- Deciphering different validation levels
1:30 pm Lunch & Networking Break
Analyzing Screening Techniques to Determine Biological Effect & Improve Drug Affinity
2:30 pm Roundtable Session: Ensuring On-Target Effects when Using Phenotypic Screening & Fragment-Based Screening to Select Functional RNA Targets
Synopsis
- Identifying targets that have a biologically functional effect
- Leveraging the toxic side-effects of using phenotypic screening
- Developing phenotypic screens to validate RNA targets that successfully bind the small molecule
- Understanding how to generate fragment maps to get better predictability of targetable RNA
- Screening large numbers of targets to synthesize RNA libraries
3:30 pm Successfully Identifying RNA Binding Pockets for Improved RNA-Small Molecule Interactions & Functional Response
Synopsis
- How the understanding of RNA structure helps to describe RNA pockets for selective drug binding
- Which RNA elements and characteristics elicit a biological effect and how to modify in silico screens to obtain defined targetable RNA regions?
- Exploiting the possibilities of interactions with RNA outside the binding pockets to increase and diversify interactions which can improve drug affinity and specificity
- Discussing how to ensure sufficient interactions between small molecules and RNA targets to improve affinity