SC8: Practical Phenotypic Screening
WEDNESDAY, JUNE 19 | 6:15-9:15pm (DINNER PROVIDED)

ABOUT THIS COURSE:

Phenotypic drug discovery is experiencing a renaissance in the pharmaceutical industry, based on its successful track record in delivering first-in-class medicines. This approach offers the promise of delivering both novel targets & chemical matter modulating a disease phenotype of interest. Although phenotypic screening may appear at first sight to be similar to target-based screening, there are some significant differences between the two approaches. These need to be properly considered and addressed to ensure the greatest likelihood of success for phenotypic drug discovery programs. This presentation will cover a range of relevant topics with a goal of providing practical information to help prosecute such programs more effectively.

WHAT YOU WILL LEARN:

  • What is the rationale for conducting phenotypic screening?
  • When does phenotypic screening provide the most value? What may be the best indications for this strategy?
  • Not all phenotypic assays are created equal: what are the characteristics of the best assays?
  • Which libraries should be screened and why?
  • What are key considerations and strategies for phenotypic screening hit triage and validation?
  • What are key considerations and strategies for target/mechanism identification and validation?
  • What are key considerations and strategies for safety derisking and phenotypic program progression?

INSTRUCTOR BIOGRAPHIES:

Fabien_VincentFabien Vincent, PhD, Associate Research Fellow, Discovery Sciences, Pfizer Inc.

Fabien Vincent, PhD, 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.

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 30 peer-reviewed research articles, review articles and book chapters and has been invited to present his research at more than 30 conferences and other events. 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 as well as a meeting co-organizer for the Keystone symposium Phenotypic Drug Discovery: Recent Advances and Insights from Chemical and Systems Biology in March 2019.

Rockwell_KristinKristin Rockwell, Senior Scientist, Discovery Sciences, Pfizer Inc.

Kristin Rockwell is a Senior Scientist in the Discovery Sciences department at Pfizer. She has worked in the pharmaceutical industry for over 15 years and is a technical expert in assay development and screening. Among her successes, Kristin developed an HTS assay utilizing primary human T cells aimed at identifying allosteric JAK3 inhibitors, and more recently, in support of a platform that was seeking novel targets, she developed and executed siRNA and CRISPR screens in primary human CD4+ T cells. Kristin was the lead author on a recent book chapter on GPCR allosterism (Rockwell and Alt, Positive Allosteric Modulators of Opioid Receptors, RSC, 2016). Additionally, she presented her functional genomics work as an invited speaker at SLAS2018 (Phenotypic Screening SIG 2018) and was selected for a podium presentation at the Keystone Symposium on Phenotypic Drug Discovery (March 2019).

Kristin obtained her Bachelor’s degree from Southern CT State University and her Masters from Brown University. Formerly at Neurogen in Branford, Kristin began her Pfizer career in 2007 as part of the High Throughput Screening Group. From 2012-2015 Kristin spent 3 years at Bristol-Myers Squibb in Wallingford where she gained significant experience in rare diseases and GPCRs. She returned to Pfizer in 2015 to focus on building phenotypic screening platforms in PPG. She has a passion for phenotypic screening and will be presenting the rationale for designing and assessing the most optimal and physiologically relevant phenotypic assays.