CONFERENCE DAY TWO
7:15 am Check-in & Morning Coffee
8:15 am Chair’s Opening Remarks
Advancing Bifunctionals Towards the First Approval with Clinical Data from Leaders in Clinic
8:30 am Initial Clinical Data From the Ongoing Clinical Trial of CFT1946
Synopsis
NEW DATA
- Well-tolerated at all dose levels; no dose-limiting toxicities
- Dose proportional pharmacokinetic exposure; successfully degrades BRAF V600 mutant protein
- Early evidence of CFT1946 monotherapy anti-tumor activity in patients who have progressed on or after BRAF inhibitor therapies
- Preclinical data demonstrating blood-brain barrier permeability
9:00 am Clinical Activity of NX-5948 in CLL & NHL: A First-in-Class BTK Degrader
9:30 am Enabling Insights into Molecular Glue MoA Toward Design of Potent & Selective CK1a Degraders
10:00 am Teaching CRBN New Tricks
10:30 am Morning Break & Networking
Novel Target & Pathway Identification & Selection to Unearth
New Molecular Glues
Chair: Leo Fu, Co-Founder & Chief Technology Officer, GluBio Therapeutics
11:30am: Novel Molecular Glue Targets
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Gregory Michaud, Director, Novartis
12:00pm: First-in-Class Molecular Glue Degrader of an RNA-Binding Protein to Treat BRAF-Mutant Tumor
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Yong Cang, Director of Assay & DEL Screening, Wuxi Apptec
12:00pm: Presentation Brought to You by WuXi Apptec
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Zhifeng Yu, Chief Scientific Officer & Co-Founder, Degron Therapeutics
12:50pm: Fast-Tracking MDM2: Efficient Expression & Purification of active E3 Ubiquitin Ligase for Target Protein Degradation
- Securing adequate supply of functional recombinant E3 ligases is essential for advancing drug discovery. The eProtein Discovery System transforms cell-free protein production, enabling researchers to obtain high-quality proteins in just 2 days.
- Demonstrating a streamlined process for rapid expression and purification screening, which helps define the optimal conditions for producing MDM2 at high yields
- Functional validation with an autoubiquitination activity assay helps identify the best truncation for MDM2, allowing selection of construct for scale up production to accelerate drug discovery efforts
Michael Chen, Chief Executive Officer, Nuclera
1:00pm: Networking Lunch Break
Unravelling MOA & Optimizing Binding of Selective Degraders
2:00pm: Discovery of Novel Monovalent Degraders of SMARCA2/4
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Joachim Rudolph, Senior Fellow, Genentech
2:30pm: Degrading Hard to Drug Disease Causing Extracellular Proteins
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Shyra Gardai, Chief Scientific Officer, EpiBiologics
3:00pm: Afternoon Networking Break
CLOSING KEYNOTE PLENARY SESSION
3:30 pm Structural, Biochemical, Biophysical, & Computational Characterization of KT-474
Synopsis
- Heterobifunctional degrader KT-474 induces ternary complex formation, ubiquitination, and degradation of IRAK4
- Ternary complex structure shows novel protein-protein interactions important for ternary complex formation and stability
- Structural explanations for cooperativity and selectivity will be discussed
Preparing for the Future: Accelerating Strategy, Partnering & Investment for TPD & Beyond
4:00 pm A review of the TPD Deals & Companies Landscape
Synopsis
- An overview of the commercial landscape
- The 2024 deals & companies landscape
- Investment into novel degrader technologies
4:10 pm Panel Discussion: Lessons Learned from a Major Strategic Partnership Deal for a Platform
4:45 pm Introduction: A Review of the Current Trends in Asset Deals
Synopsis
- 10-minute high level overview of the past and recent deals for early stage and later stage assets in TPD & Induced Proximity, for PROTACs, Molecular Glues, and beyond