Agenda (Updated) – 3rd Targeted Protein Degradation Conference in Japan

Day 1 Day 2 Day 3

29th July 2025
9:30	Registration Networking & Coffee
10:30	Opening Remarks Katsuhiro Uto, CEO, FIMECS
Morning Session, Chair: Katsuhiro Uto
10:35	Keynote Presentation Bexobrutideg(NX-5948): Leading the Way to the First CNS-Active BTK Degrader for B-Cell Malignancies and Charting a Path to Our Next Generation of Innovative Drugs Gwenn Hansen, CSO, Nurix Therapeutics, Inc. Bexobrutidegis an orally administered, CNS-penetrant, heterobifunctional small molecule degrader that acts to catalytically eliminate both wild-type and mutant BTK protein to treat B-cell malignancies. Bexobrutidegis differentiated from BTK inhibitors by its exquisite selectivity and ability to address both the enzymatic and scaffolding functions of BTK, leading to more complete pathway blockade and as well as improved control of treatment-emergent resistance mutations. Bexobrutideghas demonstrated robust clinical activity in both chronic lymphocytic leukemia (CLL) and Waldenström macroglobulinemia (WM), showing deepening responses in heavily pre-treated patient populations. Expanding ligand repertoires for both undruggable targets and E3 ligases remains a key challenge to unlocking the next generation of innovative targeted protein degrader drugs.
11:20	Targeted Degradation of TRK for Cancer Therapy and Pain Management JialiangWang, Executive VP of Operation, Cullgen, Inc. Targeted degradation of TRK overcomes resistance to kinase inhibitors TRK degrader is well tolerated in cancer patients TRK degradation exhibits significant analgesic activities in multiple preclinical pain models
11:45	Discovery and Clinical Development of Targeted Protein Degraders and Degrader- Antibody Conjugates (DACs) Koichi Ito, Senior Director Biology, Prelude Therapeutics Lessons learned from the pre-clinical discovery, translational research and development of our VHL-based IV and CRBN-based oral clinical SMARCA2 selective degraders Degrader-Antibody Conjugate (DAC) strategy to enhance drug exposure and improve the therapeutic window in pre-clinical models
12:10	Luncheon Sponsor Showcase and Coffee Break (Lunch box will be served)
Afternoon Session 1, Chair: Ian Churcher
13:20	Development of highly active PROTACs and research on expanding PROTAC molecular modalities Hidetomo Yokoo, Chief, Division of Organic Chemistry, National Institute of Health and Science (NIHS) Development of peptide-based PROTAC Development of Nanoparticle-based PROTAC in silico design of PROTAC Comparison of several E3 ligases in the developenmt of PROTAC
13:45	Advancing Degrader Discovery and Expanding the Landscape of E3 Ligase by RaPPIDS^TM platform Kanae Gamo, CSO, FIMECS, Inc. Leveraging the RaPPIDS^TM platform to accelerate degrader discovery via high-throughput synthesis and phenotypic screening Identification and characterization of proprietary ligands that engage novel E3 ligases Enabling expansion of E3 ligase usage to expand degrader space and accelerate pipeline progression
14:10	Characterization of PROTAC specificity and endogenous protein interactomes using ProtacID Suman Shrestha, Postdoctoral Researcher, Princess Margaret Cancer Centre We developed ProtacID, a flexible BioID (proximity-dependent biotinylation)-based approach to identify PROTAC-proximal proteins in living cells. ProtacID analysis of VHL- and CRBN- recruiting PROTACs targeting a number of different proteins (localized to chromatin or cellular membranes) demonstrates how this technique can be used to validate PROTAC degradation targets and identify non-productive (i.e. nondegraded) PROTAC-interacting proteins, addressing a critical need in the field of PROTAC development. We also demonstrate that ProtacID can be used to characterize native, endogenous multiprotein complexeswithout the use of antibodies, or modification of the protein of interest with epitope tags or biotin ligase tagging.
14:35	Networking & Coffee Break
Afternoon Session 2, Chair: Suman Shrestha
15:20	Protein Knockdown Mediated by Auxin-Inducible Degron (AID) Technology Masato Kanemaki, Professor, Department of Chromosome Science, National Institute of Genetics Overview and history of auxin-inducible degron (AID) technology AID2-mediated protein knockdown in cell culture and animals Single-chain antibody AID2 (scAb-AID2) for degrading endogenous proteins without degron tag
15:45	Linker free PROTACs Hai Rao, Professor, Southern University of Science and Technology A set of miniPROTACs with short and interchangeable degrons 19 amino acids can be adapted possibly without the need of linkers 6 ubiquitin E3 enzymes may be employed Excellent oral bioavailability
16:10	Induction of lysosomal degradation by IAP-based PROTACs, SNIPERs Mikihiko Naito, Professor, Graduate School of Pharmaceutical Sciences, University of Tokyo SNIPERs recruit IAP ubiquitin ligases for protein degradation Identification of a target protein degraded exclusively by lysosome, not by proteasome, upon SNIPER treatment Mechanism of the lysosomal degradation induced by SNIPERs
16:35	Partner’s Presentation: WuXi AppTec In vitro Platform to Facilitate Target Protein Degrader Discovery and Approaches to Optimize its ADME Properties
17:05	Short Break
17:30	Reception Party at the Venue (Open to All Participants)
19:00	Venue Closing

30th July 2025
9:00	Registration Networking & Coffee
Morning Session 1, Chair: Kanae Gamo
9:30	A Molecular Glue Degrader of HuRto Treat Cancer and Cancer-induced Cachexia Yong Cang, CSO and Co-founder, Degron Therapeutics Human antigen R (HuR), encoded by Elavl1, is an RNA binding protein driving tumor development and metastasis but undruggable by traditional approaches; Molecular glue degraders of HuRwas identified from customized chemical library of DegronTxand exhibited superb activity against BRAF-mutant tumors. Genetic and pharmacological depletion of HuRrescued cancer-induced cachexia in mice. FDA has cleared DEG6498, an oral HuRdegrader, for clinical development to treat solid tumors including hepatocellular carconomaand BRAF-mutant colorectal tumor.
9:55	Oral Therapies for Immunology: Degrading IRF5, a Highly Credentialed, Historically Undrugged Transcription Factor Veronica Campbell, Senior Director, Immunology, Kymera Therapeutics Building a pipeline of oral therapies for well validated targets in immunology Biology of IRF5 and drugging the undrugged KT-579, a potent, selective, oral IRF5 degrader, preclinical profile in human primary cells, patient derived cells, and in vivo disease models
10:20	Broad-Spectrum Efficacy of CEACAM6-Targeted ADC with BET Protein Degrader in Solid Cancer Models Hiroyuki Kogai, Scientist, Eisai Co., Ltd. Developing a novel ADC targeting CEACAM6 with BET protein degrader Demonstrating potent and broad spectrum efficacy in pancreatic cancer, colorectal cancer, breast cancer , and lung cancer models Discussing combination therapy effects with immune checkpoint inhibitors
10:45	Coffee Break
Morning Session 2, Chair: Masato Kanemaki
11:05	Bifunctional Molecules to Break Antimicrobial Resistance Emilia Taylor, PhD Researcher, The University of Oxford Antimicrobial resistance (AMR) represents a critical global health challenge, necessitating innovative therapeutic strategies with novel mechanisms of action. Identification of resistance enzymes in bacteria that are susceptible to targeted protein degradation via recruitment or activation of bacterial proteases, alongside the development of biochemical assays to quantify degradation potency. Evaluation of active and inactive BacPROTACs, demonstrating selective degradation of bacterial resistance enzymes in vitro
11:30	Development of anti-virulence therapy against bacterial infections. Minsoo Kim, Associate Professor, Kyoto University Pathogenic bacteria utilize conserved bacterial ubiquitin ligases to degrade host proteins and evade immune responses. We developed a novel anti-virulence drug using PROTAC technology to selectively degrade bacterial virulence factors. Our PROTAC effectively inhibited bacterial growth and reduced host cell death in Salmonella-infected cells. This approach offers a new therapeutic modality that disables bacterial virulence with long-lasting effects, fewer side effects, and reducing resistance pressure.
11:55	Partner’s Presentation: FUJIFILM Liposome Technology for TPD: Improved Blood Retention Expected to Lead to Increased Tumor Exposure and Reduced Administration Frequency
12:05	Luncheon Sponsor Showcase and Coffee Break (Lunch box will be served)
Afternoon Session 1, Chair: Jo Hyunsun
13:15	Unleashing E3 ligases for targeted protein degradation using DNA encoded libraries and Artificial intelligence (DEL-AI) Jose Santos, Vice President, NurixTherapeutics Overview of DEL screening platform focusing on the discovery of proprietary ligase binders ready for derivatization into heterobifunctional degraders and molecular glues. Implementation of proprietary SAR analysis tools to prioritize analogs with optimal properties to guide hit-to-lead efforts on DEL identified ligase binders. Application of proprietary DEL-AI Platform to accelerate DEL hit identification by eliminating the requirement for wet lab screening of target proteins.
13:40	MicDrop-Cellular DEL Screen in Droplets for TPD and beyond Ken Yamada, Associate Director, Novartis Biomedical Research Background on CRBN glue discovery Overview of cellular DEL in droplets Validation screen with CRBN glues for cellular IKZF3 degradation Screen with VHL glues for CDO1 degraders and CDO1-VHL glues
14:05	New approaches to PROTACs and Molecular Glues discovery combining AI, automated synthesis and innovative biology platform Yann Gaston-Mathé, CEO and Co-Founder, Iktos Acceleration of the DMTA (Design–Make–Test–Analyze) cycle through the integration of AI-driven molecular design and robotics-enabled synthesis and screening. MT-Bench: a patented, automated in-cellular imaging platform for high-throughput screening of modulators targeting protein–protein interactions (PPIs). Case studies illustrating the discovery of PROTACs and molecular glues enabled by MT-Bench technology. Iktos’sstrategy for discovering novel targeted protein degraders by combining MT-Bench with 3D GenAI technologies for AI-driven drug design.
14:30	Coffee Break
Afternoon Session2, Chair: Ken Yamada
14:50	High-throughput proteomic screening to identify and validate novel degrader molecules and targets Henrik Daub, Founder and CSO, NEOsphereBiotechnologies High-throughput proteomics rapidly screens entire libraries to identify innovative degrader compounds and disease-relevant targets at scale Unbiased SAR analysis and proteome-wide assessment of degrader selectivity, potency, kinetics, and efficacy support lead optimization Global ubiquitinomicsand high-throughput proximity labeling provide insights into compound-induced ubiquitination and ternary complex formation The neoVERSEdata analysis suite offers comprehensive analysis of large-scale proteomics data, transforming them into actionable insights for drug discovery
15:15	Generative AI in Target Protein Degradation: What It Can Do Now and Its Future Perspective Tasuku Ishida, Lead Scientist, Elix, Inc. Overview of how AI is contributing to accelerate drug discovery The potential of generative AI in developing molecular glue degraders PROTACs and generative AI: how AI can drive PROTAC research
15:40	Partner’s Presentation: CellFreeSciences Application of MAZiQ array® Technology to TPD Drug Discovery
15:50	Networking & Coffee Break
Evening Session, Chair: Gwenn Hansen
16:30	Strategies for non-clinical toxicity assessment of targeted protein degraders and their challenges Masako Imaoka, Senior Director, Daiichi Sankyo Co., Ltd. TPDs demonstrate powerful and sustained pharmacological effects; however, there are concerns regarding the potential for unintended protein degradation, which could lead to prolonged toxicities. Off-target protein degradation poses a significant risk because it may go undetected in animal studies. Establishing evaluation methods is a major challenge. The presentation discusses the current state of preclinical safety evaluation for TPDs and the challenges faced in strategic planning, comparing them to traditional small molecules.
16:55	Ten years of therapeutic TPD. What have we learnt and where next? Ian Churcher, Chief Executive Officer, Janus Drug Discovery Consulting Ltd Provide a perspective on global progress in the TPD field since 2015 from discovery to clinical studies Reflect on where TPD has made the biggest impact, what has been achieved and what we have learnt Assess how TPD concepts have allowed the expansion of the wider Induced-Proximity field Looking ahead as to what we can expect the next generations of TPD & induced-proximity approaches to deliver
17:20	Panel Discussion Advancing TPD and Molecular Glue Therapies: From Platform Innovation to Clinical Translation Panelists: Rohan Beckwith, Gwenn Hansen, Ian Churcher and Ken Yamada
18:05	End of Day 2

31st July 2025
9:30	Registration Networking & Coffee
Morning Session 1, Chair: Jose Santos
9:30	MrTAC opens enables induced lysosomal proteolysis of the cytosolic proteome Lauren Veronica Albercht, Assistant Professor, University of California Irvine Arginine methylation is an endogenous degradative modification for lysosomal proteolysis during growth factor signaling. Here, we develop MrTAC (methylarginine targeting chimera), a small molecule that induces proximity of target proteins with methyltransferases for targeted lyososmal proteolysis. We confirm proof-of-concept using a dual covalent molecule of protein arginine methyltransferase 1 (PRMT1) and glycogen synthase kinase 3 (GSK3). Lysosomal proteolysis was induced rapdily, within 60 minutes, and could be sustained over multiple days. Mechanistically, we validate specificity to the lysosome and confirm that methylation is required for degradation. Our latest work validates MrTAC with endogenous neo-substrate degradation. Together, MrTAC is a potent degrader modality that exploits an entirely novel proteolytic pathway.
9:55	Combining The Power of Protein Degraders With the Precision of Antibodies for Synergistic Potential Using Degrader-Antibody Conjugates (DACs) Sang Hyun Lee, Vice President, Orum Therapeutics Delving into the mechanism and design of an antibody degrader conjugate Evaluating anti-tumor activity in preclinical models Discussing the rationale for the chosen format and value proposition over traditional approaches
10:20	Targeting ‘Undruggable’ targets: pioneering novel applications of heterobifunctional degraders Chinatsu Sakata-Sakurai, Head of Oncology Research, Astellas Pharma How Astellas identified, and is executing, a long-term innovation strategy in Targeted Protein Degradation Learnings from the discovery and development of ASP3082 Accelerating our progress through an integrated approach to in-house R&D, translational research and innovation partnering
10:45	Networking & Coffee Break
Morning Session 2, Chair: Jialiang Wang
11:15	Brain-penetrant molecular glue degraders targeting ALK via a novel degron: A potential therapeutic approach for ALK-positive NSCLC Zheng Wang, Principal Scientist, Bristol Myers Squibb Molecular glue degraders for ALK identified Novel non-loop degron distal to ATP-binding pocket Degraders effective on all ALK fusions and TKI-resistant ALK mutants Improved brain penetration of ALK degrader to treat brain metastasis
11:40	Innovative drug discovery using protein degrader Hyunsun Jo, Founder and CEO, Pin Therapeutics Clinical development strategy with CK1α highly-selective MGD in oncology DAC payload strategy to minimize hematologic toxicity
12:05	Expanding the Druggable Genome with Molecular Glues Rohan Beckwith, SVP Chemistry, Neomorph Molecular glues can be utilized to target proteins lacking ligandable sites Neomorph have developed proprietary approaches towards rational, prospective design of molecular glues beyond CRBN Neomorph has discovered unique binders to new E3 ligases and leveraged these systems against novel neosubstrates with glue optimization through rational design Proprietary novel degrons drives expansion of the druggable genome
12:30	Closing Remark Kanae Gamo, CSO, FIMECS