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Chair’s Opening Remarks

Adam Gilbert
Senior Director, Discovery Sciences, Design & Synthesis Sciences

Keynote Plenary: Accelerating Emerging Protein Degraders into the Clinic


Accelerating the PROTAC Field through Competition & Collaboration

• Boehringer-Ingelheim‘s approach to PROTAC drug discovery illustrated with examples
• There are too many E3 Ligases to go it alone – a call for pre-competitive collaboration
• Perspectives on emerging areas of PROTAC drug discovery

Darryl McConnell
Vice President and Research Site Head Austria
Boehringer Ingelheim


Industry Leaders Panel Discussion

• How TPD has changed the face of drug discovery and how to unlock its full potential as a competitive but yet collaborative community?
• Is TPD the much sought after modality to finally drug the “undruggable”?
• In the case of clinical setbacks, how would the momentum, interest and investment in the field be affected? Where to go from there?

Panel Moderator:

Frank Mercurio
Chief Scientific Officer


Randy Teel
Vice President – Corporate Development

Joshua Hansen
Director, Chemistry

Ingrid Wertz
Senior Scientist and Project Team Leader


Networking and Morning Refreshments

Target Identification & Mechanism of Action

Confirmed Chair:

Paola Castaldi, Associate Director & Head of Chemical Biology, AstraZeneca

Optimizing Emerging TPD Strategies

Confirmed Chair:

Charu Chaudhry, Senior Research Investigator, Lead Discovery and Optimization, Bristol-Myers Squibb

Innovating TPD Modalities by Uncovering Novel Biology & Disease Targeting Strategies

Improving Potency, Selectivity & Bioavailability by Rational & Scalable Drug Discovery Approaches


Utilizing a Diverse, Drug-Like, Cereblon-Directed Chemical Library to Deliver on the Therapeutic Potential of Targeted Protein Degradation

• Develop a chemical library of cereblon-directed Protein Homeostatic Modulators (PHMs™) to accelerate the therapeutic potential of targeted protein degradation
• Novel IND-track PHMs whose unique MOA distinguish their therapeutic utility from that of classical IMiDs
• The diverse PHM chemical scaffolds enable the development of innovative and clinically effective PROTACs

Frank Mercurio, Chief Scientific Officer, BioTheryx


Identification of Protein Degraders with Potential for Immuno-oncology

• Target rationale and clinical promise
• In vivo PK/PD relationship
• Lead optimization to achieve excellent potency, selectivity and bioavailability

Nan Ji, Executive Director, Head of Chemistry, Kymera Therapeutics


New Insight into Proteasome Regulation and New Opportunities for Drug Development

• Recent research has shown that proteasome function (like ubiquitin conjugates) is tightly regulated and influences rates of protein degradation
• Degradation of ubiquitinated proteins is activated upon binding of specific proteins (e.g. in muscle atrophy) and by phosphorylation (e.g. by hormones and drugs that raise cAMP)
• Enhancing proteasome function is a promising new approach to promote the clearance of misfolded proteins that cause major neurodegenerative disease

Alfred Goldberg, Professor of Cell Biology, Harvard Medical School


Discovery of Brain Penetrant PROTAC® Degrader Molecules that Target Pathologic Tau Protein Species

• Arvinas has engineered PROTAC degrader molecules that are brain penetrant
• Tau targeted PROTAC degrader molecules degrade Tau protein species
• PROTAC degrader molecules represent a new modality for the potential treatment of tauopathies

Angela Cacace, Vice President of Neuroscience and Platform Biology, Arvinas


New Modalities of Protein Degradation in the Nervous System

• Neuronal plasma membrane-bound proteasomes(NMPs) are neuroproteasomes that are distinct from canonical UPS systems
• NMPs present an entirely unexplored modality of protein degradation in the nervous system with yet undefined functions in health and disease
• We have the tools to monitor and manipulate NMPs in order to modulate their function in vitro and in vivo

Kapil Ramachandran, Junior Fellow, Harvard Society of Fellows, Harvard Medical School


Ubiquitin Mediated Small Molecule Induced Target Elimination (uSMITE) For Cancer

• Development of orally-active degraders
• Identification of novel degraders for transcriptional regulators
• Physico-chemical properties in degrader design

Michael Plewe, Vice President, Medicinal Chemistry, Cullgen


Networking Lunch

Plenary: Characterizing & Enhancing Next Generation TPD Strategies


Novel E3 Ligase Ligands for New Generation PROTACs

• Discovery of novel E3 ligase ligands using Progenra’s UbiProTM platform
• Characterization of ligands for three novel E3 ligases for building PROTACs
• Proof of concept using novel PROTACs

Suresh Kumar                                        Senior director R&D                                Progenra


Enhancing Autophagic Degradation by Small Molecules as a Strategy for Neuro-Degenerative Disorders

• Autophagy as a degradation mechanism that is important for multiple diseases
• Validation of autophagy as a disease-relevant mechanism in neuro-degenerative disorders
• Small molecule compound screening for identification of enhancers of autophagy

Robin Ketteler, Group Leader, MRC Laboratory for Molecular Cell Biology, University College London


Plenary Round Table Discussions

1. DELs: How to enable novel ligand and ligase discovery through enabling technologies such as DELs?
2. PK/PD: How to leverage the pharmacokinetic and pharmacodynamic relationship to optimize your TPD strategy for clinical development?
3. Neurodegeneration: How to expand the focus of the TPD field beyond oncology: Is TPD the next big breakthrough for neurodegenerative diseases?
4. Assays: How to establish a cellular assay platform to profile protein degraders and the (un)expected challenges with translation to in vivo models?


Charu Chaudhry
Senior Research Investigator,
Lead Discovery and Optimization
Bristol-Myers Squibb

Adam Gilbert
Senior Director, Discovery
Sciences, Design & Synthesis


Chairs Closing Remarks & End of The 2nd Annual TPD Summit 2019