Phenotypic screening is experiencing a Renaissance in the pharmaceutical industry, based on its successful track record in delivering first-in-class medicines stemming from novel biology. Although phenotypic screening may appear at first sight to be similar to target-based screening, there are some fundamental differences between the two approaches. This course will deliver a theoretical and practical framework for the use of phenotypic drug discovery by (1) providing a broad context of the drug discovery process, (2) comparing and contrasting molecular target driven and empirical phenotypic drug discovery strategies, (3) providing guidelines on why and when to utilize an empirical phenotypic drug discovery approach and (4) providing practical information to prosecute phenotypic programs more effectively.
Those interested in the following tracks:
Attendees will leave this course with:
Fabien Vincent, Ph.D.
Fabien Vincent, Ph.D., is an Associate Research Fellow in the Hit Discovery and Lead Profiling Group at Pfizer. His laboratory provides molecular pharmacology support for the small molecule project portfolios of the Immunology & Inflammation research unit and the Centers for Therapeutic Innovation. This work includes designing hit identification strategies and screening funnels, developing assays for high throughput screening as well as additional assays to elucidate the structure activity relationship of active compounds, understand their mechanism of action and facilitate translation to pre-clinical models. His main research interests are centered on improving the translation of discovery research to patients and specifically include phenotypic screening and atypical molecular mechanisms of action.
Fabien Vincent recently led a team of Pfizer scientists in an analysis of how best to approach phenotypic screening, and specifically how to design the optimal phenotypic assays, those which can best predict compounds and mechanisms that will be effective in patients (Sci. Trans. Med., 2015, 7, 293ps15).
Fabien Vincent received a Diplôme d’Ingénieur in organic chemistry from CPE Lyon (France) before conducting graduate research in the fields of chemical biology and enzymology in the laboratory of Pr. Harold Kohn at the University of Houston. He later became a post-doctoral fellow in chemical biology at the Genomics Institute of the Novartis Research Foundation in San Diego. He entered the field of drug discovery as both a drug discovery research project leader and molecular pharmacology-biochemistry group leader. He has authored more than 25 peer-reviewed research articles, review articles, book chapters and abstracts and has been invited to present his research at more than 15 events and conferences. He is a member of the Scientific Advisory Board of the Chemical Probes Initiative and has been a NIH study section reviewer on HTS and molecular probe identification. He was recently a guest editor for a special issue in Med. Chem. Comm. surveying progress and advances in the field of phenotypic drug discovery.
David C. Swinney, Ph.D.
David Swinney has a long interest to better understand how drugs work to provide effective, safe, therapeutically useful responses, and how these medicines and their respective mechanisms are discovered. Dave believes that better understanding of how drugs work will inform strategies to identify safer medicines, leading to an increase chance of success, and thereby increase productivity by reducing attrition. Dave’s analysis of how medicines were discovered concluded that the empiricism of phenotypic assays is important to the successful discovery of first in class medicines. This work was published in Nature Reviews Drug Discovery in 2011 and contributed to a reevaluation of the value of phenotypic assays to drug discovery.
Currently Dave works as an independent consultant and at the Institute for Rare and Neglected Diseases Drug Discovery aka iRND3, (www.irnd3.org), where he is founder and CEO. Dave has over 25 years of drug discovery experience (Roche, Syntex, iRND3) working to identify promising strategies, leads, clinical candidates and effective mechanisms of drug action that address unmet medical needs. At iRND3 Dave has established a portfolio of early stage programs using drug discovery strategies that include phenotypic and target-based. He has a PhD in medicinal chemistry from the University of Washington, Seattle, did his post doc at the Roche Institute for Molecular Biology and expertise in drug discovery, drug discovery strategies, assay development and screening, enzymology, pharmacology, biochemistry and binding kinetics.
Jonathan Lee, Ph.D.
Jonathan Lee is a Senior Research Advisor in the department of Quantitative Biology at Eli Lilly and Company. Jonathan’s pharmaceutical experience includes portfolio/research management and the evaluation, development, and deployment of new technologies for drug discovery. Recent research emphasizes the use of complex, physiologically relevant cellular systems for target validation, lead generation, SAR support, and biomarker discovery. Jonathan was an early adopter of contemporary empirical drug discovery approaches and plays an active part in the emerging phenotypic drug discovery (PDD) community through publications, presentations, initiating the PDD Special Interest group, and initiating/co-organizing the Keystone Symposium “Modern Phenotypic Drug: Defining the Path Forward”. He received his Ph.D. in chemistry from the University of California, San Diego and was a postdoctoral fellow in the laboratory of H.R. Kaback at the Roche Institute of Molecular Biology.