第14回 HTS之生物化学筛选法
5月13日(二) ～ 14日(三)
Title to Be Announced
FUNCTIONAL ENZYMATIC ASSAYS
Discovery of Protease Inhibitor Probes by Target Class Profiling
Andrew Napper, Ph.D., Director, High-Throughput Screening, Penn Center for Molecular Discovery, University of Pennsylvania
Optimization of Enzymatic Assays for HTS: Sampling the Biochemical Space using a Parallel, Streamlined Approach
Daniele Carettoni, Ph.D., Head, Biochemistry, Axxam SpA
Title to Be Announced
Marshall Michener, Ph.D., Research Fellow, Inflammation Research, Pfizer Inc. (tentative)
Beyond Kinases: Interrogating the Purinome
Bob Lowery, Ph.D., President, CEO, Corporate, BellBrook Labs
BINDING ASSAYS
Drug Discovery in Academia: Two Examples of Novel Approaches to Biochemical Assays
Marcie Glicksman, Ph.D., Senior Director, Leads Discovery, Laboratory for Drug Discovery in Neurodegeneration, Brigham and Women’s Hospital
High-Throughput Screening for Inhibitors of p27Kip1 Proteolysis
Xuedong Liu, Ph.D., Associate Professor, Chemistry and Biochemistry, University of Colorado-Boulder
STRUCTURE-BASED ASSAYS
An Example of the Fragonomics Paradigm
Anthony Macherone, Ph.D., Senior Director, Analytical & Bioanalytical Services, ASDI Group of Companies
RECOMMENDED SHORT COURSE *Separate Registration Required
(DC1) 晚餐课程 生物化学筛选法用之工具及治疗法的开发 (5月13日 9:00am - 12:00pm)
Tutor: Daniele Carettoni, Ph.D., Head, Biochemistry, Axxam SpA Xuedong Liu, Ph.D., Associate Professor, Department of Chemistry and Biochemistry, University of Colorado-Boulder
- Functional Enzymatic Assays
- Structure-based Drug Design
- Binding Assays
Topics to be addressed for each:
- The value of the expression host for recombinant protein expression
- Protein engineering: truncations, ancillary domains, tags, etc.
- Quality criteria for assay configuration aìnd screening
- Assays and type of inhibitors (active-site, allosteric, exosite, etc.)
- Types of assays used (surrogate substrates, enzymatic cascades, reactive probes, etc.)
- What is the readout?
- Benefits and limitations of each assay
- What is the degree of throughput?
- Homogeneous (addition-only steps) assays
- How can assay and equipment be adapted for target when more complex assays are needed?
