Archived: 15th Winter Conference
on Medicinal & Bioorganic Chemistry
January 30th - February 3rd 2022
Steamboat Springs Resort, Colorado
Agenda
Sunday, January 30th 2022
Drug Hunting
Program Chair: Scott Wolkenberg, Janssen
Design of PF-07104091, a CDK2 Selective Inhibitor for the Treatment of Cancer
The Discovery of CK-136, a Selective Cardiac Troponin Activator
Discovery and Early Clinical Development of LY3372689, an O-GlcNAcase (OGA) Enzyme Inhibitor
Discovery of CFTR Modulators for the Treatment of Cystic Fibrosis
Networking Session
Welcome Reception

Monday, January 31st 2022
Total Synthesis / Biocatalysis
Program Chair: Bryan Norman, Enveda Biosciences
Opening Remarks
A Chemical Synthesis of Ritterazine B, A Marine Natural Product with Potent Anticancer Activity
Next-generation Synthesis of Antibiotics
Enzymatic Routes to the Next Generation Therapeutics
Commercial Synthesis of APIs enabled by Enzymatic Reductive Amination
Catalytic Approaches for Simplifying Complex Alkaloid Total Synthesis
Nontraditional Modalities in Drug Discovery
Program Chair: Dr Lou Chupak, Bristol-Myers Squibb
Application of a Proteome-Wide Covalent Fragment Screening Platform: The Discovery of Potent, Selective, Allosteric JAK1 Inhibitors
Co-opting the Ubiquitin System for Therapeutic Benefit
Identification of a PCSK9-LDLR Disruptor Peptide with In Vivo Function
Cyclic peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure Based-Design
Development of a Nanoscale Chemistry Direct-to-Biology (D2B) Platform for High-Throughput PROTAC Synthesis
Tuesday, February 1st 2022
Molecular Interactions in Drug Discovery
Program Chair: Dr Payal Sheth, Bristol-Myers Squibb
Drugging the Undruggable with Molecular Glue
Structures of Active-State Orexin Type-2 Receptor Enable Structure-Based Drug Discovery
Impacting Drug Design using NMR Solution Conformations
Structure and Property Guided Design of Cell Permeable Peptidic Degraders
Structure-Function Relationship of a CD4-binding Adnectin with Anti-HIV-1 Activity
General Session: Synthesis and Med Chem
Program Chair: Dr Mike Visser, Novartis
A Synthesis-Driven Approach to Drug Discovery: CFTR Modulators
Direct-to-Biology Platform for High-Throughput Synthesis and Evaluation of Hetero-bifunctional Degraders
Optimization of Triazolopyridazines towards a Novel Drug to Treat Cryptosporidiosis Reveals Striking Impact by Positioning of Fluorine
Discovery of a Potent and Selective BRD9 Degrader with Activity in a Preclinical Model of Synovial Sarcoma
Building a Culture of Medicinal Chemistry Knowledge Sharing
Networking Session
POSTER SESSION

Wednesday, February 2nd 2022
New Methodologies and Technologies to Enable Drug Synthesis
Program Chair: Darren Dixon, University of Oxford
Synthesis and Functionalization of Cyclopropanes and Cyclobutanes
Innovation in the Synthesis of Complex Pharmaceuticals
Selective Functionalization of Pyridines, Diazines and Pharmaceuticals via Unconventional Intermediates
Tackling Synthetic Challenges and Applying Synthetic Technologies across the Novartis Drug Discovery Portfolio
Computational Predictions of Reactivity & Site-Selectivity with Quantum Machine Learning
Chemical Biology
Program Chair: Dr Stephanie Monson, Genetech
Covalent Chemical Probes – Cysteine Labeling and Beyond
Tracking Drug Action at the Cell Surface and in the Secreted Proteome
RAPID – a High-Throughput, Cell-Based Ligand Discovery Platform for Difficult to Drug Targets
Understanding Immune Cell Interactions via Photocatalysis
Function-first Proteomic Strategies for Chemical Probe Discovery in Human Cells
Thursday, February 3rd 2022
Late Breaking Stories in Drug Discovery
Program Chair: Dr Rebecca Gallego, Pfizer
Discovery of the Selective CSF1R Inhibitor ARRY-382
Identification and Optimization of First-in-Class Small Molecule Inhibitors for a Novel Oncology Target
Next Generation Oxazolidinone Antibiotics for the Treatment of Tuberculosis
Discovery and Early Clinical Development of the First-in-class TPL2 Kinase Inhibitor Tilpisertib (GS-4875) for Inflammatory Diseases
Robert M. Williams’ Memorial Keynote Lecture
Program Chair: Philippe Nantermet, Merck and Matthew Hayward, Pfizer
Small Molecules with Big Ambitions: Approaches to Intractable Targets
Networking Session
Conference Dinner

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