A2 - Advanced methods to accelerate drug discovery

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Anton Simeonov (National Center for Advancing Translational Sciences, National Institutes of Health, USA) and Rebecka Isaksson (Chair of SIG New Generation of Pharmaceutical Scientists, Department of Chemistry UCL, UK)


Recent advances in screening and disease modeling are poised to yield unprecedented opportunities for drug discovery and design. These advances include improved processes for small molecule library design and management, broadly-enabling advances in mass spectrometry, as well as three-dimensional (3D) human cell-based systems capable of recapitulating complex human physiology and disease. In addition, approaches based on the control of target protein degradation, e.g. PROTAC, represent an exciting opportunity to modulate targets in a way that is independent of functional activity.  As such, they present a powerful tool to expand the landscape of ‘druggable’ proteins. This session focuses on most recent advances in the fields of high-throughput screening technologies and the design and validation of complex disease modeling platforms.


Targeted Degradation of BTK: a PROTAC case study
Matt Calabrese (Pfizer, USA)

DNA-encoded libraries
Timothy Foley (Pfizer, USA)

HTS in a non-profit environment: The EU perspective
Sheraz Gul (Fraunhofer Institute for Molecular Biology and Applied Ecology, Germany)

Organs-on-Chips: A platform for drug development and disease modeling
Daniel Levner (Emulate, USA)




Learning Objectives

1) identify most recent trends in drug discovery technologies;

2) translate more efficiently the latest discoveries in human biology to tangible interventions to improve human health;

3) advocate for novel public-private partnerships;

4) formulate the best ways to use advanced informatics approaches to drug discovery.