Archived: 15th Winter Conference
on Medicinal & Bioorganic Chemistry

January 30th - February 3rd 2022

Steamboat Springs Resort, Colorado


Sunday, January 30th 2022

Drug Hunting

Program Chair: Scott Wolkenberg, Janssen

Kevin Freeman-Cook Pfizer

Design of PF-07104091, a CDK2 Selective Inhibitor for the Treatment of Cancer

Antonio Romero Cytokinetics

The Discovery of CK-136, a Selective Cardiac Troponin Activator

Dustin J. Mergott Lilly

Discovery and Early Clinical Development of LY3372689, an O-GlcNAcase (OGA) Enzyme Inhibitor

Sabine Hadida Vertex

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

Bryan Norman Enveda Biosciences

Opening Remarks

Sarah Reisman Caltech

A Chemical Synthesis of Ritterazine B, A Marine Natural Product with Potent Anticancer Activity

Ian Seiple UCSF

Next-generation Synthesis of Antibiotics

Ania Fryszkowska Merck

Enzymatic Routes to the Next Generation Therapeutics

Rusty Lewis Pfizer

Commercial Synthesis of APIs enabled by Enzymatic Reductive Amination

Darren Dixon University of Oxford

Catalytic Approaches for Simplifying Complex Alkaloid Total Synthesis

Nontraditional Modalities in Drug Discovery

Program Chair: Dr Lou Chupak, Bristol-Myers Squibb

Larry Burgess Vividion Therapeutics

Application of a Proteome-Wide Covalent Fragment Screening Platform: The Discovery of Potent, Selective, Allosteric JAK1 Inhibitors

Ingrid Wertz Bristol-Myers Squibb

Co-opting the Ubiquitin System for Therapeutic Benefit

Lauren Monovitch Novartis

Identification of a PCSK9-LDLR Disruptor Peptide with In Vivo Function

Thomas Tucker Merck

Cyclic peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure Based-Design

Alexander Buitrago Santanilla GlaxoSmithKline

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

Mary Matyskiela Neomorph Inc

Drugging the Undruggable with Molecular Glue

Kaspar Hollenstein Merck

Structures of Active-State Orexin Type-2 Receptor Enable Structure-Based Drug Discovery

Kathleen Farley Pfizer

Impacting Drug Design using NMR Solution Conformations

Jakob Fuhrmann Genentech

Structure and Property Guided Design of Cell Permeable Peptidic Degraders

Dave Wensel ViiV Healthcare

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

Xenia Searle AbbVie

A Synthesis-Driven Approach to Drug Discovery: CFTR Modulators

Chuck Hendrick Janssen

Direct-to-Biology Platform for High-Throughput Synthesis and Evaluation of Hetero-bifunctional Degraders

Marvin Meyers Saint Louis University

Optimization of  Triazolopyridazines towards a Novel Drug to Treat Cryptosporidiosis Reveals Striking Impact by Positioning of Fluorine

Kate Jackson C4

Discovery of a Potent and Selective BRD9 Degrader with Activity in a Preclinical Model of Synovial Sarcoma

Doug Beshore Merck

Building a Culture of Medicinal Chemistry Knowledge Sharing

Networking Session


Wednesday, February 2nd 2022

New Methodologies and Technologies to Enable Drug Synthesis

Program Chair: Darren Dixon, University of Oxford

Sophie Rousseaux University of Toronto

Synthesis and Functionalization of Cyclopropanes and Cyclobutanes

Martin Eastgate Bristol-Myers Squibb

Innovation in the Synthesis of Complex Pharmaceuticals

Andy McNally Colorado State

Selective Functionalization of Pyridines, Diazines and Pharmaceuticals via Unconventional Intermediates

Cara Brocklehurst Novartis

Tackling Synthetic Challenges and Applying Synthetic Technologies across the Novartis Drug Discovery Portfolio

Robert Paton Colorado State

Computational Predictions of Reactivity & Site-Selectivity with Quantum Machine Learning 

Chemical Biology

Program Chair: Dr Stephanie Monson, Genetech

Lyn Jones Dana-Farber Cancer Institute

Covalent Chemical Probes – Cysteine Labeling and Beyond

Marcus Bantschef Cellzome, A GSK Company

Tracking Drug Action at the Cell Surface and in the Secreted Proteome

Justin Rettenmaier Jnana Therapeutics

RAPID – a High-Throughput, Cell-Based Ligand Discovery Platform for Difficult to Drug Targets

Tamara Reyes Robles Merck

Understanding Immune Cell Interactions via Photocatalysis

Michael Lazear Scripps

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

Eric Newcomb Pfizer

Discovery of the Selective CSF1R Inhibitor ARRY-382

Julian Levell Constellation Pharmaceuticals, a MorphoSys Company

Identification and Optimization of First-in-Class Small Molecule Inhibitors for a Novel Oncology Target

Brendan Crowley Merck & Co., Inc.

Next Generation Oxazolidinone Antibiotics for the Treatment of Tuberculosis

James Taylor Gilead

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

5.00 - 6.00pm
Dr Jay Bradner Novartis

Small Molecules with Big Ambitions: Approaches to Intractable Targets

Networking Session

Conference Dinner

Media Sponsors