Cambridge Healthtech Institute’s Inaugural

Expanding Chemical & Druggable Space

Encoded Libraries & Macrocyclics, FBDD & Lead Generation, PROTACs

June 2-4, 2020


Progress of the past decade in encoded libraries and macrocyclic peptide synthesis are enabling new types of drug-like molecules to be created and rapidly screened, which is widening the ‘base’ from which successful drugs can be found. Moreover, the types of intracellular targets these newer chemical entities can act upon is also expanding. Disease-relevant protein-protein interactions (PPIs) and larger molecular complexes can be disrupted by these larger, yet cell-penetrable drug-like compounds. Fragment-based drug discovery (FBDD) and other biophysical screening approaches have also provided drug leads against such non-traditional, non-enzymatic drug targets. And now one of the latest innovations in drug discovery, PROTACs, special compounds designed against any part of the target so that upon binding of the PROTACs the target is destroyed, is expanding therapeutic possibilities even more. But how good are all these new approaches? Is theory meeting practice? Join fellow discovery chemistry and biology colleagues to hear case studies, discuss challenges, and share refinements that remain in the newest approaches for generating tomorrow’s orally-bioavailable medicines.

ENCODED LIBRARIES & MACROCYCLICS

Advances in DNA-Encoded Library Technologies
Thomas Kodadek, PhD, Professor of Chemistry, The Scripps Research Institute

IDO Inhibitors: Proceeding from DNA-Encoded Library Hits to Leading Drug Candidates
Bing Xia, PhD, Investigator, NCE Encoded Library Technologies, RD Medical Science & Technology, GlaxoSmithKline

Development of Macrocyclic Peptides for Intracellular Targets
David Tellers, PhD, Director, Discovery Chemistry, Merck Research Labs

mRNA Encoded Libraries for Macrocyclic Peptides
Wayne Fairbrother, PhD, Director and Senior Staff Scientist, Early Discovery Biochemistry, Genentech

FRAGMENT-BASED DRUG DESIGN & LEAD GENERATION APPROACHES

Optimizing a Fragment Hit into Undruggable Space: A Case Study
Justin Dietrich, PhD, Senior Scientist III, Fragment Based Drug Discovery, Abbvie

From Fragment to Clinical Candidate: The Role of Biophysical Methods in Protein-Protein Interaction (PPI) Inhibitor Development
Chiara Valenzano, PhD, Senior Research Associate, Molecular Sciences Group, Astex Pharmaceuticals

Next Generation Inhibitors of Bruton’s Tyrosine Kinase (BTK) and Clinical Trial Results of BIIB068, a Selective, Potent, Reversible BTK Inhibitor
Bin Ma, PhD, Senior Scientist, Medicinal Chemistry, Biogen

PROTACs & TARGETED PROTEIN DEGRADATION

Discovery of Bcl-xL Degraders: A PROTAC Strategy for Tissue Selective Targeting
Guangrong Zheng, PhD, Associate Professor, Department of Medicinal Chemistry, College of Pharmacy, University of Florida

Immunotherapeutic Approaches for Degrading Tau Pathology in Alzheimer’s Disease
Gilbert Gallardo, PhD, Assistant Professor, Hope Center for Neurological Disorders, Washington University School of Medicine