2023年 ディナーショートコース* (対面式参加者のみ)
Drug Discovery Chemistryのショートコースでは、特定のトピックに関する詳細な情報に関して、質疑応答の機会とともに、指導向けのインタラクティブ講座として提供されます。このコースには、初めてこの分野に触れる人や、もっと学びたい人向けの入門編から、主要会議のプレゼンテーションでは時間が足りない、より専門的な内容の解説まで含まれています。インストラクターは業界や学界から選ばれており、その多くはその分野の権威として認められているか、指導経験があります。
ディナーショートコースは、4月10日(月)夜と4月12日(水)夜に開催され、対面式参加者が対象となります。
*プレミアム価格または別途登録が必要
2023年4月10日(月) 6:00 - 8:30 pm
SC1: Protein Degraders: A Focus on PROTACs from a Beyond Rule of Five Space Perspective
SC1:タンパク質分解誘導剤:「ルールオブファイブ(Ro5)を超えて」の視点からPROTACへフォーカス
Instructor:
John Erve, PhD, President, Jerve Scientific Consulting
- 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
SC2: Fragment-Based Drug Design: Advancing Tools and Technologies
SC2:フラグメント創薬(FBDD):ツール・技術の進化
Instructors:
Ben J. Davis, PhD, Research Fellow, Biology, Vernalis R&D Ltd.
Daniel A. Erlanson, PhD, Senior Vice President, Innovation and Discovery, Frontier Medicines Corporation
- 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:
Ben J. Davis, PhD, Research Fellow, Biology, Vernalis R&D Ltd.
Daniel A. Erlanson, PhD, Senior Vice President, Innovation and Discovery, Frontier Medicines Corporation
SC3: Chemical Biology for Phenotypic Screening and Target Deconvolution
SC3:表現型スクリーニング・標的デコンボリューション向けケミカルバイオロジー
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
INSTRUCTOR BIOGRAPHIES:
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
SC4: Generative and Predictive AI Modeling for Protein Inhibitors and Degraders
SC4:タンパク質阻害剤・分解誘導剤向け生成/予測的AIモデリング
Instructors:
Petrina Kamya, PhD, Head of AI Platforms and President of Insilico Medicine, Canada
Parthiban Srinivasan, PhD, Professor, Data Science and Engineering, Indian Institute of Science Education and Research
Topics to be covered:
- Small molecule inhibitors and degraders as target modulators
- AI methods for generating small molecules
- Chemical space exploration and exploitation
- Deep learning based predictive models
- Inhibitors and degraders design using these AI techniques
Who Should Attend:
INSTRUCTOR BIOGRAPHIES:
Petrina Kamya, PhD, Head of AI Platforms and President of Insilico Medicine, Canada
Parthiban Srinivasan, PhD, Professor, Data Science and Engineering, Indian Institute of Science Education and Research
2023年4月12日(水) 6:15 - 8:45 pm
SC5: Protein Degraders: A Focus on PROTACs from an ADME-Tox Perspective
SC5:タンパク質分解誘導剤:ADME/Toxの視点からPROTACへフォーカス
Instructors:
John Erve, PhD, President, Jerve Scientific Consulting
Matthew Hoffmann, PhD, Senior Director, Drug Metabolism & Pharmacokinetics, Bristol Myers Squibb Co.
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:
John Erve, PhD, President, Jerve Scientific Consulting
Matthew Hoffmann, PhD, Senior Director, Drug Metabolism & Pharmacokinetics, Bristol Myers Squibb Co.
SC6: Principles of Drug Design: Ligand-Receptor Interactions and More
SC6:医薬品設計の原理:リガンド-受容体相互作用など
Instructor:
Maricel Torrent, PhD, Principal Research Scientist, Computational Drug Discovery, AbbVie, Inc.
- Medicinal chemistry and structure-based drug design principles
- Interpretation of atomic-level protein X-ray and modeled structures of binding mode
- Understanding the relative amounts of potency gain from different types of interactions
- Case studies to illustrate all the design strategies
INSTRUCTOR BIOGRAPHIES:
Maricel Torrent, PhD, Principal Research Scientist, Computational Drug Discovery, AbbVie, Inc.
SC7: DNA-Encoded Libraries
SC7:DNAエンコードライブラリ(DEL)
Instructors:
Svetlana Belyanskaya, PhD, Vice President, Biology, Anagenex
Ghotas Evindar, PhD, Senior Vice President, Head of Drug Discovery, 1859 Inc.
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 a period of time
- Affinity-based selection strategy and how this could guide hit picking
- Data analysis and the decision-making logic in hit confirmation
- Introduction to one-bead, one-compound (OBOC) DNA-encoded libraries
- Additional benefits of the new platform
INSTRUCTOR BIOGRAPHIES:
Svetlana Belyanskaya, PhD, Vice President, Biology, Anagenex
Ghotas Evindar, PhD, Senior Vice President, Head of Drug Discovery, 1859 Inc.
SC8: Biophysical Tools for Membrane Proteins: Drug Discovery Applications
SC8:膜タンパク質の生物物理学ツール:創薬への応用
Instructor:
Matthew T. Eddy, PhD, Assistant Professor, Chemistry, University of Florida, Gainesville
Topics to be Covered:
- NMR spectroscopy in solutions & solids
- Fluorescence spectroscopy approaches
- Crystallography & Cryo-EM
- Membrane mimetics in structural & biophysical experiments
- Comparing methodologies strengths/weaknesses
INSTRUCTOR BIOGRAPHIES:
Matthew T. Eddy, PhD, Assistant Professor, Chemistry, University of Florida, Gainesville
* 不測の事態により、事前の予告なしにプログラムが変更される場合があります。