CONFERENCE DAY ONE | WEDNESDAY APRIL 2, 2025

7:20 am Check In & Morning Coffee

8:10 am Chair’s Opening Remarks

  • Cameron Pye Chief Executive Officer, Unnatural Products

Reflecting on the State of Play & Future Directions of the Peptide Drug Space

8:20 am Peptide Industry Leaders’ Panel Discussion – Is 2025 the Goldilocks Year for Peptide-Based Therapeutics?

  • Cameron Pye Chief Executive Officer, Unnatural Products
  • Tomi Sawyer Chief Drug Hunter & President, Maestro Therapeutics
  • Pete Gough Chief Scientific Officer, Nimble Therapeutics
  • Abbas Walji Senior Director, Discovery Chemistry, Merck

Synopsis

This panel will discuss the key breakthroughs that have happened this year, the key challenges that have been overcome, and where the biggest excitement remains:

  • Taking stock of the strengths, weaknesses, opportunities and threats (SWOT) for peptide-based therapeutics
  • How do you perceive the peptide therapeutics space? How has this changed in the past 12 months?
  • What are the scientific bottlenecks that are slowing peptide-based drug discovery into translation and into the clinic?
  • How are peptide-based therapies going to be positioned against standards of care, compete against other drugs and take market share away from small molecules, antibody drug conjugates and other biologics?

Pioneering Cutting-Edge Computational Approaches & Blended Platforms in Peptide Discovery to Design for Function

8:50 am Integrating Molecular Dynamics Simulation & Machine Learning for Cyclic Peptide Structure Prediction

  • Yu-Shan Lin Professor and Department Chair of Chemistry, Tufts University

Synopsis

  • A significant obstacle preventing the rational or structure-based design of cyclic peptides is that little solution structural information is available for these molecules, since most cyclic peptides adopt multiple conformations in solution, existing as structural ensembles
  • Developing the StrEAMM (Structural Ensembles Achieved by Molecular dynamics and Machine learning) platform for cyclic peptides by combining molecular dynamics simulation and machine learning to provide efficient, high-quality cyclic peptide structure predictions
  • Rapidly predicting cyclic peptide structures to enable researchers to understand the structural basis for the diverse properties of cyclic peptides and accelerate the development of this unique class of molecules

9:20 am Development of Orally Bioavailable Peptides Targeting an Intracellular Protein

  • Yoshihisa Murata Head of Advanced Computational Chemistry Group, Chugai Pharmaceutical Co

Synopsis

  • Validating of a new methodology to create oral drugs beyond the rule of 5 for intracellular tough targets
  • Developing LUNA18: from a hit to a clinical KRAS inhibitor
  • Discussing computational chemistry and structure-based molecular design for cyclic peptide drug discovery platform development

9:50 am Using Stapled Peptide Helicons TM as Protein Degraders

  • Markus Haeberlein Executive Vice President - Discovery Science, Parabilis Medicines

Synopsis

  • Optimizing Helicons for intracellular targeting of difficult-to-drug targets
  • Exploring the use of Helicons for targeted protein degradation
  • Exemplifying learnings with case-studies

10:320am Structured Speed Networking

Synopsis

This informal session provides the perfect opportunity to connect with industry pioneers and key opinion leaders in the peptide-based therapeutics field. Establish meaningful connections to build upon at the rest of the conference and gain exclusive first-hand insights into the latest research and developments driving progress in the space.

11:00am Morning Coffee Break

11:20 am Green Approaches to Peptide Manufacturing: From Minimal Protection Strategies in API Synthesis to Macrocyclization & Peptide-Oligonucleotide Conjugation in Eco-Friendly Solvents

Synopsis

Further details to be announced

11:30 am Computationally Guided Design & Testing Of De Novo Miniproteins

Synopsis

  • Evaluating computational design strategies, high throughput characterization, and rational optimization of 45-60 amino acid miniproteins
  • Reviewing computationally guided libraries for efficient affinity maturation
  • Exploring computationally guided miniprotein engineering for multivalency and sitespecific conjugation

12:00 pm Next Generation Orally Available Macrocycles for Challenging Targets

Synopsis

  • Providing an overview of the Orbis high-throughput macrocycle discovery platform
  • Building an understanding of macrocycle permeability & oral availability
  • Sharing a case study: Application of the Orbis platform for identification and optimization of a macrocyclic GPCR agonist

12:30 pm Therapeutically Relevant & Novel Amino Acids from Biocatalysis

  • Tina Boville Chief Executive Officer & Co-Founder, Aralez Bio

Synopsis

  • Exploring the opportunities and challenges for noncanonical amino acids in peptide therapeutics
  • Applying biocatalysis as a tool for efficient and sustainable noncanonical amino acid synthesis at all scales

12:40 pm Development of Oral Peptides for Immune-Mediated Disease

Synopsis

  • Nimble’s proprietary, light-mediated parallel synthesis platform allows for peptide therapeutic discovery and optimization at the million-peptide scale
  • Enabling rapid optimization of properties critical for oral therapeutic delivery
  • Leveraging this platform to generate a pipeline of oral, peptidic therapeutics for immunemediated diseases

1:10pm Lunch & Networking Break

Pinpointing Fundamental Mechanisms to Achieve Cell Permeability with Peptide-Based Drugs & Unlock Access to Intracellular Targets

2:00 pm Mechanism and Rational Design of Cell-Permeable Peptide Therapeutics

  • Dehua Pei Professor of Chemistry & Biochemistry, Ohio State University

Synopsis

  • Discussing the molecular mechanisms by which peptides and proteins cross the plasma and endosomal membranes
  • Applying this mechanistic understanding to guide rational design of cell-permeable peptides and proteins
  • Showcasing examples of cell-permeable macrocyclic peptides as PPI inhibitors and protein degraders 

Building mRNA Display & DNA-Encoded Chemical Libraries Biased Towards Peptide Drug Discovery with Enhanced Therapeutic Functionality

2:30 pm Identification of Oral Macrocyclic Peptide Inhibitors Against IL-17 for the Treatment of Psoriasis

Synopsis

  • Designing mRNA display libraries with diverse chemical properties and scaffolds
  • Combining assay and computational approaches for initial peptide hit identification and selection, with high affinity and specificity for targets
  • Further constraining or optimizing peptides to become viable, orally available therapeutics

3:00 pm Strategies for Finding Macrocyclic Peptide Leads From an mRNA Display Platform

  • Emel Adaligil Principal Scientific Manager, Macrocycle Discovery Group, Genentech

Synopsis

  • Discussing the selection criteria for intracellular and extracellular targets
  • Further details to be announced

3:30pm Afternoon Networking Break & Scientific Poster Session

Synopsis

Want to share your work but not ready for the big stage just yet? The Scientific Poster Session is your prime time to share your work with peers from various backgrounds, all focused on developing cutting-edge peptide therapeutics. Gain feedback on how you can accelerate the progression of your discovery drug pipelines and build connections for potential collaborations to take your therapeutic from concept to clinic.

4:00 pm Peptidic Macrocyclic Molecular Glues for Interrogating Hard to Drug Intercellular Targets

  • Rick Ewing Vice President & Head of Chemistry, Rapafusyn Pharmaceuticals

Synopsis

  • Exploring the principles of constructing DEL libraries with topological diversity as a key driver for broadly unlocking target classes
  • Showcasing the performance platform against several target classes
  • Describing SAR studies directed at optimizing lead molecules against a target

4:30 Breakout Roundtable Discussions

Uncover the story behind leaps and setbacks from the movers and shakers of peptide drug discovery and development. Each roundtable will be hosted by a leader in the space who will share a challenge, question or case study to discuss:

Scaling Up Peptide Synthesis Efficiency of Complex Peptides From R&D Towards the Clinic Through Innovative Automated Technologies

Ranganath Gopalakrishnan

Director, New Modalities Medicinal Chemistry, Early CVRM, AstraZeneca

Using Green Chemistry to Propel Peptide Drug Manufacturing Forward Sustainably

Speaker to be Announced

Translatable Oral Delivery Systems to Maximize Peptide Therapeutic Bioavailability

David J. Brayden

Professor of Advanced Drug Delivery, University College Dublin

5:00 pm Chair’s Closing Remarks

  • Cameron Pye Chief Executive Officer, Unnatural Products