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This year's tenth anniversary of Mastering Medicinal Chemistry focuses on the challenge of finding ways to drug the undruggable, with presentations and case studies highlighting different strategies, tools and technologies to help reach tough targets with viable clinical candidates.Topics will include leveraging unique properties of macrocycles, optimizing synthetic complexity, shape and chirality and utilizing matched pairs to design better drugs; phenotypic screening and flow chemistry; novel strategies for ADCs and linker chemistry; and updates on epigenetic and PPI pipelines.

Wednesday, February 13

7:00 am Registration and Morning Coffee

 

Plenary Keynote Session 

8:00 – 9:40 am Plenary Keynote Presentation - Personalized Oncology – Fulfilling the Promise for Today's Patients

In honor of the 20th anniversary of the Molecular Medicine Tri-Conference, CHI and Cancer Commons will present a plenary panel on Personalized Oncology. Innovations such as NGS and The Cancer Genome Atlas have revealed that cancer comprises hundreds of distinct molecular diseases. Early clinical successes with targeted therapies suggest that cancer might one day be managed as a chronic disease using an evolving cocktail of drugs.Representing all five conference channels, Diagnostics, Therapeutics, Clinical, Informatics, and Cancer, a panel of experts will lead a highly interactive exploration of what it will take to realize this vision in the near future.

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9:40 Refreshment Break in the Exhibit Hall with Poster Viewing

 

Increasing Complexity, Macrocycles,
3-DStructure, Shape & Chirality 

11:00 Chairperson's Opening Remarks

Nick Terrett, Ph.D., CSO, Ensemble Therapeutics Corp.

11:10 Opening Address: Using Synthetic Chemistry to Answer the Challenge of Increasing Molecular Complexity in Small Molecule Drug Discovery

Simon Bailey, Ph.D., Senior Director, Worldwide Medicinal Chemistry Oncology, Pfizer

This presentation will provide examples of the benefits that increased molecular complexity can bring to small molecule drug discovery programs in increasing potency, selectivity and patentability. Ways in which medicinal chemists can adopt new synthetic chemistry strategies to access molecularly complex compounds will be illustrated.

11:40 Beyond the Rule of Five – Novel Strategies for Accessing Macrocyclic Chemical Space

Keith James, President, The Ferring Research Institute; Visiting Investigator, The Scripps Research Institute

Macrocycle-based drug design represents a compelling strategy for addressing challenging molecular targets, and an exciting new frontier in drug discovery. This presentation will describe both novel strategies for accessing this intriguing region of chemical space, and some unique properties of macrocyclic systems.

12:10 pm Moving in New Circles – An Introduction to Macrocycles in Drug Discovery

Nick Terrett, Ph.D., CSO, Ensemble Therapeutics Corp.

Recently there has been a rapid growth in interest in small molecules outside of Lipinski 'Rule of 5' space. Macrocycles in particular can bind to challenging protein targets and maintain good drug-like properties offering a new fertile direction for drug discovery.

12:40 Exploiting the Chemical Space of Macrolides as Promising Templates for New DrugsVesna Gabelica Markovic, Ph.D., Senior Director, Chemistry, FideltaMacrolides are stereospecific macrolactones with drug-like physicochemical properties. This will be demonstrated in the presentation with examples which describe the design and evaluation of novel classes of anti-infective and anti-inflammatory macrolides.

12:55 Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on Your Own 

1:45 20th Anniversary Cake in the Exhibit Hall with Poster Viewing

 

Next Generation Payload Linker and Conjugation Technologies 

2:15 Chairperson's Remarks

2:20 Design of Novel Linkers, Payloads and Antibody-Drug Conjugates for the Treatment of Cancer

Christopher J. O'Donnell, Ph.D., Senior Director, Oncology Medicinal Chemistry, Pfizer

Antibody drug conjugates (ADCs) are an emerging modality for the treatment of cancer. Presently, three classes of cytotoxic payloads have been successfully employed on these modalities in clinical settings, namely the auristatins, maytansines and calicheamicins. This talk will focus on Pfizer’s innovative chemistry strategy to discover and develop new linker-payload classes that will yield more efficacious and potentially better tolerated conjugates to advance this area of research.

2:50 Antibody-Drug Conjugates for the Treatment of Cancer: Novel Linker and Payload Strategies

John Flygare, Ph.D., Senior Scientist, Discovery Chemistry, Genentech

Combining the specificity of a monoclonal antibody with the cell killing ability of a cytotoxic agent is an outstanding method for treating cancer. There are three components to this strategy; the antibody, linker , and cytotoxic drug. Assembling the correct combination of these components is key to the success of this method. These variables can be used in concert to widen the therapeutic window of cytotoxic drugs. This presentation will briefly review some of the successful applications of this technology and discuss in more depth the future directions of the linkers and cytotoxic drugs used in this approach.

3:20 Using Small Molecules to Engineer and Explore Human Immunity

David A. Spiegel, Ph.D., Associate Professor of Chemistry, Yale

This talk describe recent research efforts in our laboratories toward the design, chemical synthesis, and biological characterization of small molecule antibody recruiting therapeutics against prostate cancer, Staphylococcus aureus, and the human immunodeficiency virus (HIV). These are bifunctional small molecules designed to redirect antibodies already present in the human bloodstream to the surfaces of pathogenic cells, such as cancer cells, bacteria, and virus particles. The ternary complex formed between these agents, endogenous antibodies, and target cells will lead to immune-mediated pathogen destruction. In theory, this strategy would exploit many of the advantages of biologics, while circumventing the disadvantages, by capitalizing on the chemical properties of small molecules (e.g., high oral bioavailability, facile synthesis, and low cost). It is our hope that this small molecule-based strategy will serve as starting point toward entirely novel scientific insights and therapeutic approaches relevant to a wide range of disease states.

3:50 Rationalizing Non-Standard Interactions in Ligand Design: The Duality of Halogens

Chris Williams, Ph.D., Principal Scientist, Chemical Computing GroupNon-standard intermolecular interactions are significant in ligand binding, but they are inadequately modeled using molecular mechanics.  An Extended Hückel Theory (EHT) model is proposed, which accounts for electronic effects on interaction strengths.  Model accuracy is demonstrated using case studies.

4:20 Networking Reception in the Exhibit Hall with Poster Viewing (Sponsorship Opportunities Available)

5:20 Breakout Discussions in the Exhibit Hall

Macrocycles & Exploring the Middle Space

Moderator: Nick Terrett, Ph.D., Chief Scientific Officer, Ensemble Therapeutics Corp.

Epigenetic Targets – The Way Forward

Moderator: Ed Olhava, Ph.D., Associate Director, Preclinical Development, Epizyme, Inc.

Protein-Protein Interactions

Moderator: Michelle R. Arkin, Ph.D., Associate Adjunct Professor, Pharmaceutical Chemistry, University of California San Francisco School of Pharmacy

6:20 Close of Day

 

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