In the last couple of decades, affinity-based selection methods have emerged to enable de novo screening of novel entities with therapeutic potential. Display technologies, including phage display, mRNA display and DNA-encoded libraries (DELs), are now broadly used to identify biologics or small molecules with desired activity and function. In all of these platforms, the displayed collection of molecules (proteins, peptides or small molecules) are physically linked to an encoding gene. This allows for their identification from a complex library collection in a one-pot mixture following their affinity-based selection against the drug target of interest. These molecular evolution platforms are helping to expand and expedite the drug discovery process. While there is a common theme between the display platforms, each has unique features that determine their design, application and technical challenges. In the following course, the authors will cover some the most recent advances in these platforms.

Topics to be Covered:

Affinity-Based Screening Methods for Peptides and Biologics (45 minutes)

Jonas Schaefer, PhD, Novartis Pharma AG

  • Phage, yeast, ribosome and mRNA display
  • Overview and comparison of different selection challenges

DNA-Encoded Libraries (DEL) (60 minutes)

Svetlana Belyanskaya, PhD, GSK Boston

  • An overview and comparison of different DEL platforms
  • A step-by-step overview of Encoded Library Technology (ELT) platform at GSK

DEL Chemistry (45 minutes)

Ghotas Evindar, PhD, Exo Therapeutics

  • Examples of chemistry used for library synthesis
  • Basics of chemistry follow-up for DEL hits


Belyanskaya_SvetlanaSvetlana Belyanskaya, PhD, Encoded Library Technologies, R&D Platform Technology & Science, GSK Boston

Svetlana Belyanskaya is Scientific Leader at Encoded Library Technology (ELT) group at GlaxoSmithKline. Svetlana has been involved in the development of DNA-encoded technology at Praecis Pharmaceutical and significantly contributed in designing and adapting the DNA tagging strategies for DNA- Encoded Libraries. She led biochemistry and affinity based selection effort for several targets, partnered between GSK and Praecis Pharmaceutical. This effort resulted in the discovery of a series of potent and selective inhibitors, one of which is currently undergoing clinical trials. Post GSK acquisition, Svetlana led a team of scientists in the ELT Lead Discovery group and was responsible for ELT selections against multiple targets. Her team discovered multiple target specific small molecules with different MOAs, several of which were the first known small molecule inhibitors for novel targets.

Evindar_GGhotas Evindar, PhD, Senior Director of Drug Discovery, Exo Therapeutics

Ghotas is a senior director of drug discovery at Exo therapeutics in Cambridge, MA. He has authored well over 50 publications and patents in the area of drug discovery and is committed to education surrounding DNA encoded library (DEL) technology, leading a number of DEL roundtable discussions and courses over the last several years. He was born and raised in the Kurdish mountains before migrating to Canada. He completed his undergraduate and MSc degrees at the University of Waterloo, concentrating on synthesis and structure-activity studies of aureobasidins. He then joined Vertex Pharmaceuticals, in Cambridge, as a medicinal chemist. While at Vertex, he was instrumental in the success of P38 MAP Kinase (first and second generation), ICE-1 inhibitors (second generation), and early ZAP-70 programs. After four years at Vertex, and four clinical candidates, he moved to the University of Toronto to pursue a PhD degree in organic chemistry with focus on “Novel Approaches to Synthesis of Nitrogen Containing Heterocycles”. After completing his PhD with Dr. Robert Batey, he moved back to the Boston area to join Praecis Pharmaceuticals as a staff scientist. There he lead the medicinal chemistry sphingosine-1- phosphate (S1P) receptor agonist discovery program and contributed to the inception of the novel DEL platform. Praecis was acquired by GlaxoSmithKline in 2007 and Ghotas began a 12 year journey with DNA encoded library technology (ELT) platforms, including portfolio, library and selection design, data analysis and post-selection chemistry. In early 2019, Ghotas moved to Exo Therapeutics where he continues his adventures in small molecule drug discovery.

Schaefer_JonasJonas Schaefer, PhD, Laboratory Head, Encoded Library Technologies, Novartis Institutes for Biomedical Research, Chemical Biology & Therapeutics (CBT), Novartis Pharma AG

Dr. Schaefer is heading an R&D laboratory supporting Novartis’ lead finding through the utilization of Encoded Library Technologies, using various screening methods to select low-molecular-weight compounds against a broad variety of protein targets. Prior to this assignment, Jonas did establish and headed the High-Throughput Binder Selection Facility at the University of Zurich for many years, using automated Ribosome Display and various High-Throughput screenings to develop specific proteinaceous affinity reagents called DARPins. For over a decade, Jonas focused on the development of new methodologies and technologies enabling the improved generation, screening and validation of various affinity compounds, which were used in applications ranging from basic research to diagnostic usage and medical applications.

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