2022 Archived Content
OVERVIEW | DOWNLOAD BROCHURE | INTERACTIVE DISCUSSIONS | SHORT COURSES | PLENARY KEYNOTES | ATTENDEES

Dinner Short Courses* (In-Person Only)

Short courses at Discovery on Target are designed to be instructional, interactive, and provide in-depth information on a specific topic with opportunities for Q&A throughout. The courses include introductions for those new to the fields and those looking to learn more, as well as explanations on more technical aspects than time allows during our main conference presentations. Instructors are drawn from industry and academics alike, and many are recognized authorities in the fields or have teaching experience.

Short courses will be offered IN-PERSON ONLY.

*Premium Pricing or separate registration required

Monday, October 17, 2022  5:00 - 7:30 pm

SC1: Protein Degraders: A Focus on PROTACs from a Beyond Rule of Five Space Perspective

Detailed Agenda
This course focuses on proteolysis targeting chimeras (PROTACs) and will cover topics relevant to developing them as oral therapeutics. Topics to be covered in this first part of the course will include their physicochemical properties and how these influence solubility and permeability and assays to determine polarity. We will also examine some aspects of transporters and how drug-PROTAC interactions may arise.
John Erve, PhD, President, Jerve Scientific Consulting

ROOM LOCATION: Back Bay A

Instructor: 

John Erve, PhD, President, Jerve Scientific Consulting


Topics to be Covered:     

  • Comparison of Rule of 5 and Beyond Rule of 5 space
  • Importance of intramolecular hydrogen bonds for solubility and permeability
  • Determining chameleonicity and its importance for PROTACs
  • Transporters and potential drug-drug interactions (DDIs) 

Who Should Attend:

Scientists in the field of proteolysis targeting chimeras (PROTACs) who would like to deepen their understanding of these molecules and the physicochemical attributes that may contribute to their success as oral drugs. ADME scientists and medicinal chemists wishing to understand PROTACs from a drug safety and metabolism perspective. Graduate students and academic scientists interested in learning more about this rapidly developing new drug modality.

INSTRUCTOR BIOGRAPHIES:

John Erve, PhD, President, Jerve Scientific Consulting

John Erve is from Chicago and studied Chemistry (BS, MS) at the University of Chicago and earned a PhD in Toxicology at Oregon State University. Following postdoctoral work at Vanderbilt (1995-1999) he joined BD-Biosciences (Woburn, MA) as a Study Director. In 2002, he joined AstraZeneca (Sweden) where he characterized reactive metabolites. In 2004 he joined Wyeth (Collegeville, PA) as a Principal Scientist responsible for metabolite identification. In 2010, John joined Novartis (Cambridge, MA) as a Lab Head in Analytical Sciences. John returned to drug metabolism at Elan Pharmaceuticals (San Francisco, CA) in 2012 and later formed Jerve Scientific Consulting, Inc to help small biotech companies in the Bay area with their drug discovery efforts. John was a certified D.A.B.T. from 2004 to 2019.

SC2: Chemical Biology for Phenotypic Screening and Target Deconvolution

Detailed Agenda
This course is designed to provide an overview and best practices in the use of chemical biology probes and assays that have been developed for applications in early drug discovery. Chemists and biologists working in lead generation, assay development, phenotypic screening, target discovery and deconvolution, target engagement and mechanism-of-action (MoA) studies will all benefit from attending this course. The instructors will share their knowledge and expertise around the use of various technologies and chemistries and there will be time for open discussion and exchange of ideas.
Paul Brennan, PhD, Professor, Nuffield Department of Medicine, University of Oxford
Brent Martin, PhD, Vice President, Chemical Biology, Scorpion Therapeutics
Andrew Zhang, PhD, Director, Chemical Biology, AstraZeneca

ROOM LOCATION: Back Bay C

Instructors:

Paul Brennan, PhD, Professor, Nuffield Department of Medicine, University of Oxford

Brent Martin, PhD, Vice President, Chemical Biology, Scorpion Therapeutics

Andrew Zhang, PhD, Director, Chemical Biology, AstraZeneca


Topics to be Covered:         

  • Chemical biology assays and probes for diverse applications
  • Chemoproteomic methods and reagents for covalent drug discovery
  • Comparison of various chemical biology approaches (mass spectrometry, affinity-bead methods, thermal profiling and more) 
  • Cysteine profiling and covalent inhibitors for target discovery
  • Case studies highlighting use of small molecules for target engagement and deconvolution​

INSTRUCTOR BIOGRAPHIES:

Paul Brennan, PhD, Professor, Nuffield Department of Medicine, University of Oxford

Paul Brennan received his PhD in organic chemistry from UC Berkeley. Following post-doctoral research at Cambridge University, Paul spent eight years working in the pharmaceutical industry at Amgen and Pfizer. In 2011, Paul joined the Structural Genomics Consortium at the University of Oxford. Over the course of his career, Paul has worked on most major drug classes of drug targets: kinases, GPCRs, ion-channels, metabolic enzymes, and epigenetic proteins. Paul is currently Professor of Medicinal Chemistry and CSO of the Alzheimer’s Research UK Oxford Drug Discovery Institute in the Centre for Medicines Discovery at the University of Oxford. His research is focused on finding new treatments for dementia.

Brent Martin, PhD, Vice President, Chemical Biology, Scorpion Therapeutics

Brent Martin received his Ph.D. in Pharmacology at the University of California in San Diego developing new chemical strategies for correlated fluorescence and electron microscopy. He then carried out postdoctoral studies at the Scripps Research Institute developing new strategies for activity-based profiling, high-throughput screening, and chemical proteomics. As faculty member at the University of Michigan in Ann Arbor, he continued expanding the scope of activity-based profiling methods, while also establishing new bioconjugation reactions to detect and profile protein lipidation, redox modifications, and cysteine occupancy. Brent is the recipient of the NCI Howard Temin K99/R00 award in Cancer Research, the NIH Director’s New Innovator Award, and the NIGMS MIRA Established Investigator Award. He then moved to industry to lead the Chemical Biology at Janssen and is currently Vice President and Head of Chemical Biology at Scorpion Therapeutics.

Andrew Zhang, PhD, Director, Chemical Biology, AstraZeneca

Andrew Zhang is a Team Leader in the Chemical Biology Department at AstraZeneca. He joined AstraZeneca in 2013 with research interests in target deconvolution, particularly using chemical proteomics and orthogonal methods for identifying target engagement events and profiling selectivity. He is now leading the proteomics efforts around profiling the selectivity and mechanism of small molecule protein degraders. Andrew trained at the interface of chemistry and molecular and cell biology, obtaining a B.S. in Chemistry and a B.A. in Molecular and Cell Biology from the University of California, Berkeley, followed by Ph.D. studies with Professor David Spiegel at Yale University around small molecule immunomodulators. Prior to joining AstraZeneca, Andrew carried out postdoctoral trainings with the Drug Discovery Group at the Ontario Institute for Cancer Research (Toronto, Canada) with Dr. Rima Al-awar.

SC3: Best Practices for Targeting GPCRs, Ion Channels, and Transporters with Monoclonal Antibodies

Detailed Agenda
Complex membrane proteins are important therapeutic targets and together represent the majority of protein classes addressed by therapeutic drugs. Significant opportunities exist for targeting complex membrane proteins with antibodies, but it has been challenging to discover therapeutic antibodies against them. This course will examine emerging technologies and strategies for enabling the isolation of specific and functional antibodies against GPCRs, ion channels, and transporters, and highlight progress via case studies.
Joseph Rucker, PhD, Vice President, Research and Development, Integral Molecular, Inc.

ROOM LOCATION: Back Bay B

Instructor:

Joseph Rucker, PhD, Vice President, Research and Development, Integral Molecular, Inc.

Topics to be Covered: 
  • Overview of different classes of membrane proteins, including structure, mechanism, and their role in disease
  • Membrane protein biochemistry and antigen preparation strategies
  • Use of mRNA and DNA for eliciting immune responses against membrane proteins
  • Antibody discovery and methods to enable isolation of functional antibodies
  • Review of mechanisms relevant to complex membrane proteins (GPCRs, ion channels, transporters) in vitro assays for measuring the detailed binding and function of antibodies
  • Review of promising membrane protein targets and antibodies in development

INSTRUCTOR BIOGRAPHIES:

Joseph Rucker, PhD, Vice President, Research and Development, Integral Molecular, Inc.

Joe Rucker is the Vice President of Research & Development, a co-founder of Integral Molecular and an inventor of Integral Molecular’s founding Lipoparticle technology. Since joining the company, he has led the development of new applications for Lipoparticle technology, including its use in generating novel antibodies against membrane proteins. Dr. Rucker earned his PhD from the University of California, Berkeley and completed postdoctoral studies at the University of Pennsylvania.

Wednesday, October 19, 2022  6:30 - 9:00 pm

SC4: Protein Degraders: A Focus on PROTACs from an ADME-Tox Perspective

Detailed Agenda
This course focuses on proteolysis targeting chimeras (PROTACs) and will cover topics relevant to developing them as oral therapeutics. Topics to be covered in this second part of the course will include an examination of the assays used to determine ADME properties and the challenges that PROTACs pose. We will also look at the metabolism of PROTACs including how the linker affects stability and pharmacokinetics. The unique mechanism of action of PROTACs give rise to some drug safety issues not seen in small molecules, which will be discussed. Finally, we will explore the possible relevance of circadian rhythm to protein degradation and PROTACs.
Matthew Hoffmann, PhD, Senior Director, Drug Metabolism & Pharmacokinetics, Bristol Myers Squibb Co.
John Erve, PhD, President, Jerve Scientific Consulting

ROOM LOCATION: Back Bay C

Instructors:

Matthew Hoffmann, PhD, Senior Director, Drug Metabolism & Pharmacokinetics, Bristol Myers Squibb Co.

John Erve, PhD, President, Jerve Scientific Consulting


Topics to be Covered:     

  • Measuring ADME properties in vitro and in vivo and specific challenges
  • Metabolism of PROTACs and influence of linker length on stability
  • Case study of optimizing a PROTAC
  • Safety issues unique to PROTACs
  • Circadian rhythm considerations

Who Should Attend:

Scientists in the field of proteolysis targeting chimeras (PROTACs) who would like to deepen their understanding of these molecules and the physicochemical attributes that may contribute to their success as oral drugs. ADME scientists and medicinal chemists wishing to understand PROTACS from a drug safety and metabolism perspective. Graduate students and academic scientists interested in learning more about this rapidly developing new drug modality.

INSTRUCTOR BIOGRAPHIES:

Matthew Hoffmann, PhD, Senior Director, Drug Metabolism & Pharmacokinetics, Bristol Myers Squibb Co.

Matt Hoffmann is from the Northeast, earning an undergraduate degree from Cornell University and a PhD in Toxicology from Rutgers University. After completing his graduate work in 2000, Matt joined Wyeth (Collegeville, PA) as a Senior Research Scientist in the drug metabolism department. In 2009, he moved to Celgene (Summit, NJ) as a Senior Principal Scientist, overseeing the biotransformation laboratories. Matt currently works as a Senior Director at Bristol Myers Squibb (Lawrenceville, NJ), and is responsible for coordinating all nonclinical drug metabolism activities for the developmental small molecule pipeline. During his 20+ year career in the pharmaceutical industry, Matt has worked to achieve marketing approval for multiple programs including tigecycline, desvenlafaxine, apremilast and pomalidomide.

John Erve, PhD, President, Jerve Scientific Consulting

John Erve is from Chicago and studied Chemistry (BS, MS) at the University of Chicago and earned a PhD in Toxicology at Oregon State University. Following postdoctoral work at Vanderbilt (1995-1999) he joined BD-Biosciences (Woburn, MA) as a Study Director. In 2002, he joined AstraZeneca (Sweden) where he characterized reactive metabolites. In 2004 he joined Wyeth (Collegeville, PA) as a Principal Scientist responsible for metabolite identification. In 2010, John joined Novartis (Cambridge, MA) as a Lab Head in Analytical Sciences. John returned to drug metabolism at Elan Pharmaceuticals (San Francisco, CA) in 2012 and later formed Jerve Scientific Consulting, Inc to help small biotech companies in the Bay area with their drug discovery efforts. John was a certified D.A.B.T. from 2004 to 2019.

SC5: Biophysical Tools for Membrane Proteins: Drug Discovery Applications

Detailed Agenda
This course will cover NMR screening methods for membrane proteins, especially GPCRs; LCP (liquid cubic phase) crystallization applications with a few GPCR examples; and advances in Cryo-EM and nanodiscs. All these biophysical techniques will be discussed in the context of their impact on membrane-protein targeted drug discovery​.
Matthew T. Eddy, PhD, Assistant Professor, Chemistry, University of Florida, Gainesville

Back Bay A

Instructor:

Matthew T. Eddy, PhD, Assistant Professor, Chemistry, University of Florida, Gainesville

INSTRUCTOR BIOGRAPHIES:

Matthew T. Eddy, PhD, Assistant Professor, Chemistry, University of Florida, Gainesville

Matthew Eddy received his PhD in physical chemistry from the Massachusetts Institute of Technology in the laboratory of Professor Robert Griffin. During his PhD, Dr. Eddy developed new approaches for using nuclear magnetic resonance (NMR) in the solid state to determine structures of membrane proteins in cellular-like environments. Following his PhD, Dr. Eddy joined the laboratories of Professors Raymond Stevens and Kurt Wüthrich at The Scripps Research Institute as an American Cancer Society Postdoctoral Fellow, applying an integrative structural biology approach to study human G protein-coupled receptors (GPCRs) and focusing on applications of nuclear magnetic resonance to improve our understanding of GPCR allosteric functions. Dr. Eddy is currently an assistant professor in the Department of Chemistry at the University of Florida and affiliated faculty of the National High Magnetic Field Laboratory. His group continues to study human GPCRs to understand the role of the cellular environment in regulating GPCR dynamics, structure, and function.

SC6: DNA-Encoded Libraries

Detailed Agenda
This course provides an overview of DNA-Encoded Library (DEL) screening platforms, discusses common selection strategies for identifying novel hits from DEL campaigns and delves into parameters for building a library collection. The instructors will also cover strategic considerations in using DEL selection data to accelerate hit-to-lead steps in drug discovery.
Svetlana Belyanskaya, PhD, former Vice President, Biology, Anagenex
Ghotas Evindar, PhD, Drug Discovery Consultant, Former DEL Platform Senior Manager and Group Leader at GlaxoSmithKline

Back Bay B

Instructors: Svetlana Belyanskaya and Ghotas Evindar

Svetlana Belyanskaya, PhD, former Vice President, Biology, Anagenex

Ghotas Evindar, PhD, Drug Discovery Consultant, Former DEL Platform Senior Manager and Group Leader at GlaxoSmithKline

INSTRUCTOR BIOGRAPHIES:

Svetlana Belyanskaya, PhD, former Vice President, Biology, Anagenex

Dr. Belyanskaya is accomplished scientific leader in the field of small molecule drug discovery and an expert in DNA encoded library platform. She was involved in the development of DEL platform for 20 years. Svetlana has made significant contributions to the design and development of the DEL technology at Praecis Pharmaceuticals and, later, at GlaxoSmithKline. She was instrumental in discovering first DEL-sourced molecule to progress into clinical trials, a potent and selective inhibitor for enzyme soluble epoxide hydrolase (hsEH). At GSK, Svetlana successfully led team of scientists on multiple scientific programs. Svetlana has deep expertise in biochemistry, molecular biology, cell biology and very passionate about future development of DEL technology with goal to find novel quality leads that bring value for the treatment of diseases with unmet medical needs

Ghotas Evindar, PhD, Drug Discovery Consultant, Former DEL Platform Senior Manager and Group Leader at GlaxoSmithKline

Before recently joining 1859 Inc, Ghotas was VP and head of drug discovery at Exo Therapeutics in Watertown, MA. He has authored well over 50 publications and patents in the area of drug discovery and is committed to education surrounding DNA-encoded library (DEL) technology, leading a number of DEL roundtable discussions and courses over the last several years. He was born and raised in the Kurdish mountains before migrating to Canada. He completed his undergraduate and MSc degrees at the University of Waterloo, concentrating on synthesis and structure-activity studies of aureobasidins. He then joined Vertex Pharmaceuticals, in Cambridge, as a medicinal chemist. While at Vertex, he was instrumental in the success of P38 MAP Kinase (first and second generation), ICE-1 inhibitors (second generation), and early ZAP-70 programs. After four years at Vertex, and four clinical candidates, he moved to the University of Toronto to pursue a PhD degree in organic chemistry with focus on “Novel Approaches to Synthesis of Nitrogen Containing Heterocycles”. After completing his PhD with Dr. Robert Batey, he moved back to the Boston area to join Praecis Pharmaceuticals as a staff scientist. There he led the medicinal chemistry sphingosine-1-phosphate (S1P) receptor agonist discovery program and contributed to the inception of the novel DEL platform. Praecis was acquired by GlaxoSmithKline in 2007 and Ghotas began a 12-year journey with DNA-encoded library technology (ELT) platforms, including portfolio, library and selection design, data analysis, Hit ID, and H2L medicinal chemistry. In early 2019, Ghotas moved to Exo Therapeutics where he continues his adventures in small molecule drug discovery.