2024年的晚餐短期課程*（僅限面對面型式）

Discovery on Target的短期課程由講師主持，以對特定領域提供詳細信息為目的，並設有問答時間。每個課程都包括針對初學者或希望深入瞭解的人的入門課程，以及關於本次會議未能充分解釋的更技術性方面闡述。講師來自工業界和學術界，其中許多人在該領域皆被認可為權威或具有指導經驗。

以下是2024年度（當前的）議題和講師。追加的課程即將公佈。

短期課程僅限面對面型式。

* 需要額外費用或單獨報名。

2024年9月30日（一） 5:00 - 7:30 pm

SC1: Protein Degraders: A Focus on PROTACs from an ADME-Tox Perspective

This course focuses on proteolysis targeting chimeras (PROTACs) and will cover topics relevant to developing them as therapeutics. Topics to be covered in this part of the course will include looking at what is known about how PROTACs are metabolized in vivo and strategies to deliver them with adequate PK/PD. The unique mechanism of action of PROTACs gives 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.

Instructors:

Prasoon Chaturvedi, PhD, Vice President & Head, DMPK, C4 Therapeutics, Inc.

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) and 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:

Prasoon Chaturvedi, PhD, Vice President & Head, DMPK, C4 Therapeutics, Inc.

Prasoon Chaturvedi, Ph.D., currently leads the DMPK efforts in the protein degrader space as Vice President, DMPK, at C4 Therapeutics in Watertown, MA. Over the last two decades, Prasoon has worked with numerous cutting-edge technologies to drive drug development endeavors in multiple therapeutic areas including infectious disease, oncology, hematology, cardiovascular, inflammation, and rare diseases leading to multiple successful IND, CTA, and NDA filings and has made key DMPK contributions for several marketed drugs including NUZYRA and ONPATTRO. Prasoon holds a Ph.D. from IIT, Roorkee (India), and did his postdoctoral training at E.K. Shriver Center of Harvard Medical School, MA.

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: Fragment-Based Drug Design: Advancing Tools and Technologies

This course aims to introduce the fundamentals of Fragment-Based Lead Discovery (FBLD) to attendees. The first section will focus on the concepts of using fragments for hit generation. Special emphasis will be placed on practical pitfalls and the many ways to advance fragments to leads and drugs. The second part of the course will discuss the variety of fragment screening methods and when they are best applied. The composition of fragment libraries will also be discussed in detail. The attendees should come away from this course with a solid understanding of what FBLD is and how to apply it.

Instructors:

Daniel A. Erlanson, PhD, Chief Innovation Officer, Innovation and Discovery, Frontier Medicines Corporation

Ben J. Davis, PhD, Research Fellow, Biology, Vernalis R&D Ltd.

Topics to be Covered:

Pros and cons of fragment-based approaches
What makes a good fragment; properties of a good fragment library
Finding, validating, and characterizing low-affinity ligands
The importance of using orthogonal screening methods
What to do with a fragment-growing, linking, and more

INSTRUCTOR BIOGRAPHIES:

Daniel A. Erlanson, PhD, Chief Innovation Officer, Innovation and Discovery, Frontier Medicines Corporation

Dr. Daniel A. Erlanson is the VP of Chemistry for Frontier Medicines, which is using covalent fragments, machine learning, and chemoproteomics to target proteins often thought undruggable. Prior to Frontier he co-founded Carmot Therapeutics, where he contributed to two clinical-stage molecules. Before Carmot, Dr. Erlanson spent a decade developing fragment-based discovery technologies and leading medicinal chemistry projects at Sunesis Pharmaceuticals. Dr. Erlanson was an NIH postdoctoral fellow with James A. Wells at Genentech, earned his PhD in chemistry from Harvard University in the laboratory of Gregory L. Verdine, and his BA in chemistry from Carleton College. He has co-edited two books on fragment-based drug discovery and is an inventor on more than a dozen issued patents and an author of more than forty scientific publications. He also runs a blog devoted to fragment-based drug discovery, Practical Fragments (http://practicalfragments.blogspot.com/).

Ben J. Davis, PhD, Research Fellow, Biology, Vernalis R&D Ltd.

Dr. Ben Davis is a Research Fellow at Vernalis Research, a biotech company based in Cambridge UK which has been at the forefront of fragment-based approaches since 1998. An NMR spectroscopist and biophysicist by training, his current research focus is the development of biophysics and FBLD methods for challenging therapeutic targets and systems. Dr Davis studied for his PhD in protein folding and molecular interactions with Professor Alan Fersht at Cambridge University, and then studied the interactions of small molecules with proteins and RNA. He has over 20 years’ experience in the drug discovery industry. He has contributed to seven books over the last decade and is an author on more than forty scientific publications. He is a frequent speaker at scientific conferences and has been running FBLD training workshops since 2007.

SC3: DNA-Encoded Libraries

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.

Instructors:

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

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

Topics to be Covered:

Introduction to DNA-encoded libraries
Pros and cons of using DNA-encoded chemical libraries
Structure of the DNA coding region and how it has evolved over time
Affinity-based selection strategy and how it guides hit-picking
Data analysis and the decision-making logic in hit confirmation
Introduction to and benefits of one-bead, one-compound (OBOC) DNA-encoded libraries

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.

SC4: Best Practices for Targeting GPCRs, Ion Channels, and Transporters with Monoclonal Antibodies

Complex membrane proteins 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. This course will examine emerging technologies and strategies for enabling the successful isolation of specific and functional antibodies against GPCRs, ion channels, and transporters, and highlight progress via case studies.

Instructors:

Ross Chambers, PhD, Vice President, Antibody Discovery, Integral Molecular, Inc.

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:

Ross Chambers, PhD, Vice President, Antibody Discovery, Integral Molecular, Inc.

Ross Chambers is the Vice President of Antibody Discovery at Integral Molecular. He pioneered the use of DNA immunization for antibody production and developed Integral Molecular’s MPS system for isolating antibodies. Dr. Chambers earned his PhD from the University of Otago, New Zealand, and did post-doctoral studies at UC Davis and Berkeley. Before joining Integral Molecular, he was the Director of R&D at SDIX and directed the discovery of thousands of commercial antibodies.

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.

SC5: Developing Physiologically Relevant 3D Models

With the passing of the FDA Modernization Act 2.0, there is a greater interest in the drug discovery community to develop and use physiologically relevant in vitro models for drug candidate testing and IND filings. This course will help attendees understand what it takes to design and develop relevant 3D organoid/spheroid models through the various stages of assay development, automation compatibility and data analysis. The utility of these models in answering specific biological questions and the importance of developing a robust, scalable 3D model-based assay for preclinical decision-making will also be demonstrated through case studies.

Instructor:

Madhu Lal Nag, PhD, CSO, InSphero

INSTRUCTOR BIOGRAPHIES:

Madhu Lal Nag, PhD, CSO, InSphero

Dr. Nag is a scientific and executive leader with a profound expertise in developing preclinical MPS (MicroPhysiological Systems) and 3D models, targeted therapies, biomarker discovery, and the application of cutting-edge technologies across various domains including toxicology, safety pharmacology, oncology, functional genomics, and stem cell research. She currently serves as the Chief Scientific Officer at InSphero AG. Madhu holds a Doctor of Philosophy (PhD) in Molecular and Cellular Oncology from George Washington University and a master’s degree in Bioscience Business from Keck Graduate Institute. Her primary goal is to unify the academic and translational facets of pioneering science in oncology, metabolic diseases, and investigative toxicology. Leveraging insights from contemporary therapeutic regimens, Madhu creatively translates state-of-the-art research to promptly address patient requirements.

2024年10月2日（三） 6:00 - 8:30 pm

SC6: Protein Degraders: A Focus on PROTACs from a Beyond Rule of Five Space Perspective

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 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 ADME topics focusing on in vitro assays including stability assays, transporters, drug-drug interactions (DDIs), Cytochrome P450 (CYP450) inhibition, etc.

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

SC7: Chemical Biology for Covalent Discovery, Phenotypic Screening, and Target Deconvolution

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.

Instructors:

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

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

Aarti Kawatkar, Associate Principal Scientist, Chemical Biology & Proteomics, AstraZeneca R&D

Topics to be Covered:

Chemical biology assays and probes for target engagement and mechanistic understanding
Chemoproteomic methods and reagents for covalent ligand drug discovery
Comparison of various chemical biology approaches (mass spectrometry, affinity-bead methods, thermal profiling, and more)
Use of quantitative mass spectrometry-based proteomics and global proteomics
Cysteine profiling and covalent inhibitors for target discovery and occupancy
Design and screening of chemogenomics libraries for target identification
Case studies highlighting use of proteomics 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.

Aarti Kawatkar, Associate Principal Scientist, Chemical Biology & Proteomics, AstraZeneca R&D

I am an Associate Principal Scientist at AstraZeneca in the Chemical Biology and Proteomics Group of Discovery Sciences since 2013. Before that I was a lead chemist in the fragment-based lead generation group and medicinal chemist in Oncology at AstraZeneca. During this time, I contributed to several drug discovery projects making it to the clinic, and developed assays such as CEllular Thermal Shift Assay (CETSA) and in-cell Chemoproteomics to measure cellular target engagement and target validation for multipass transmembrane protein receptors. In 2017, AstraZeneca awarded me a prestigious award as Breakthrough Scientist for "Innovative techniques for profiling target engagement and selectivity for multipass transmembarne proteins.” Multipass transmembrane receptors have been challenging to study because of complexities in isolation and detection. These assays have worked successfully for multipass transmembrane receptor proteins which are not readily amenable to traditional biophysical methods. At AstraZeneca, we are using these assays successfully on multiple drug discovery projects at different stages like hit identification to lead optimization and to clinical candidates. We have published our work in ACS Chemical Biology https://www.ncbi.nlm.nih.gov/pubmed/31329413. I am a module leader for Proteomics course at Cold Spring Harbor Labs where participants get in-depth knowledge about chemoproteomics techniques routinely used in industry, with class lecture followed by lab work and deep dive into data analysis. Before joining AstraZeneca I worked at Vertex Pharmaceuticals as a medicinal chemist.

SC8: Biophysical Approaches for GPCRs

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.

Instructor:

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

Topics to be Covered:

Overview of GPCR structure and biology
GPCR expression and purification technologies for structure-function investigations
Biophysical methods for small molecule screening and characterization
GPCR dynamics - examining conformational changes associated with ligand binding and activation
Emerging technologies - introduction to cutting edge biophysical technologies including single-molecule imaging, NMR, and computational approaches

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 Wuthrich 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.

SC9: Fundamentals of Generative AI for Drug Discovery

Deep generative modeling is rapidly transforming de novo drug discovery, streamlining the entire process. This course aims to explain the potential of AI, machine learning, and generative AI models in creating tailored molecules with specific properties. It explores the fundamentals of Variational Autoencoders, Generative Adversarial Networks, Transformers, Large Language Models (LLMs), BERT, and GPT models in the context of drug discovery, highlighting their crucial role in reshaping the pharmaceutical landscape. Along the way, we'll dissect three pivotal techniques for biopharma specific LLMs: prompt engineering, retrieval augmented generation (RAG), and fine-tuning. This course is designed for medicinal chemists, molecular modeling users, and project managers seeking to harness the capabilities of modern Generative AI concepts and integrate them into their work.

Instructors:

Parthiban Srinivasan, PhD, Professor, Data Science and Engineering, Indian Institute of Science Education and Research, Bhopal

Petrina Kamya, PhD, Global Head of AI Platforms, Vice President Insilico Medicine; President, Insilico Medicine Canada, Insilico

Topics to be Covered:

Demystifying generative AI concepts and key terminologies
How predictive and generative AI works in de novo molecular design
Overview of large language models (LLMs)
Prompt engineering, RAG, and fine-tuning for biopharma-specific LLMs
Leveraging language models in drug discovery research with case studies

Who Should Attend:

This course is designed for medicinal chemists, molecular modeling users, and project managers seeking to harness the capabilities of modern generative AI concepts and integrate them into their work.

INSTRUCTOR BIOGRAPHIES:

Parthiban Srinivasan, PhD, Professor, Data Science and Engineering, Indian Institute of Science Education and Research, Bhopal

Parthiban Srinivasan, an experienced data scientist, earned his PhD from Indian Institute of Science, specializing in Computational Chemistry. After his PhD, he continued the research at NASA Ames Research Center (USA) and Weizmann Institute of Science (Israel). Then he worked at AstraZeneca in the area of Computer Aided Drug Design for Tuberculosis. Later, he headed informatics business units in Jubilant Biosys and then in GvkBio before he floated the company, Parthys Reverse Informatics and later an AI consultancy, Vingyani. Currently, he is a Professor at Indian Institute of Science Education and Research (IISER) Bhopal, teaching Data Science.

Petrina Kamya, PhD, Global Head of AI Platforms, Vice President Insilico Medicine; President, Insilico Medicine Canada, Insilico

Petrina Kamya, PhD, is the Head of AI Platforms and President of Insilico Medicine, Canada an end-to-end artificial intelligence-driven drug discovery company. Before joining Insilico, Dr. Kamya spent eight years in various roles at Chemical Computing Group that involved scientific and business-related aspects of preclinical drug discovery. In addition to establishing the corporate strategy for the sales and business development of molecular modeling software for academia, she also played an active role as an application scientist working on real-world discovery projects and finally in a senior role in strategy and business development for pharma and biotech companies. Following her time at CCG, Petrina moved to Certara as a Market Access Manager, where she learned first-hand the challenges of getting drugs to market. Petrina has been with Insilico Medicine since August 2020. She holds a PhD in Chemistry (specializing in computational chemistry) from Concordia University.

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