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YOU'RE INVITED!

OCTOBER 7TH 2020

15:00 - 16:00 (GMT)

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LIVE WEBINAR : OCTOBER 7TH 2020 - 3PM GMT

'INTRODUCTION TO PROTAC TECHNOLOGY FOR NOVEL DRUG DISCOVERY'

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PROTAC has opened up a new path to drug the ‘undruggable ‘ protein candidates and has taken drug discovery for small molecules to an extraordinary level. The challenge is to find ways to expedite the drug discovery process by overcoming the bottlenecks with the workflow.


Guest Presenters:

Dr. Emelyne Diers - University of Dundee

Cyrille S. Kounde BSc - Imperial College London

Dr. Induka Abeysena - SP Genevac


On October 7th, 2020 at 3pm GMT, Biopharma Group & SP Genevac, will host a 1 hour live webinar that aims to provide an introduction to PROTAC & how a better understanding of the ternary complex between the PROTAC, the POI & an E3 ubiquitin ligase can lead to rationally designed degraders. Additionally, we will also discuss activation & delivery control strategies in a cellular environment & key points for eliminating evaporation bottlenecks during the synthesis & purification stages of PROTAC research.

OUR PRESENTERS

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Cyrille S. Kounde MSc

Research Scientist at

Imperial College London


Cyrille completed his B.Sc. degree in biochemistry at Paris Diderot University and his M.Sc. in organic chemistry at Paris Descartes University. In 2006, he started his career in industry in the United Kingdom as a drug discovery scientist at Evotec Ltd then joined Novartis Horsham in 2010.


Subsequently, he moved to Singapore in 2011 and worked at the Novartis Institute for Tropical diseases (NITD) on various medicinal chemistry projects related to neglected infectious diseases.


Having returned to the UK in 2017, he is currently pursuing a PhD in the group of Prof. Ed Tate at Imperial College London. His research focuses on the conditional activation of bifunctional degraders also known as PROTACs.

Dr. Emerlyne Diers

Project Lead Scientist & Medicinal Chemist

University of Dundee


Emelyne is working within a multi-disciplinary team at the School of Life Sciences, University of Dundee, involved in a collaboration between Alessio Ciulli and Boehringer Ingelheim, aiming at advancing PROTAC drug discovery.


After a degree in chemical engineering and a PhD in synthetic methodologies development she has been involved in a variety of medicinal chemistry projects. She is responsible for the design and synthesis of PROTACs and is working to develop the translation of this exciting modality into new molecular therapeutics.


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Dr. Induka Abeysena

Product Manager at

SP Genevac


Induka has been dedicated for over 15 years to the development of applications and technologies to support the broad range of industry sectors represented by the Genevac family of users. Her work has helped to move the field of centrifugal evaporation from 'concept' thinking to instruments that the global scientific community has come to rely upon.

PRESENTATIONS AGENDA

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THE PRESENTATION ABSTRACTS

Cyrille S. Kounde MSc


Title: Multifunctional PROTACs: expanding the horizon of targeted protein degradation



Abstract:

Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has recently emerged as a powerful strategy to reduce cellular protein levels and is currently being investigated as a new therapeutic modality in drug discovery. With the intent of expanding the breadth of PROTAC-mediated applications, our group has been exploring different strategies to control the activation and delivery of PROTACs in a cellular environment. Our presentation will showcase the use of light as a triggering switch to regulate PROTAC cellular activity in a spatiotemporal manner1 and will also highlight how the conjugation of PROTACs with antibodies can achieve exquisite tissue-selective degradation.2 We anticipate that those novel multifunctional PROTACs will enrich the arsenal of tools available in the field of targeted protein degradation and will create additional opportunities in chemical biology and drug discovery.


Dr. Emerlyne Diers


Title: Understanding the ternary complex: on the road to better degraders



Abstract: 

Proteolysis Targeting Chimeras (PROTACs) are emerging as a powerful new therapeutic modality. PROTACs offer the potential to degrade a wide scope of disease-causing proteins. Their catalytic mode of action and improved selectivity for the target open an opportunity to translate this modality into efficacious and safer therapeutics against diseases with unmet medical needs.

Degradation of the protein of interest (POI) via the ubiquitin proteasome system is consequent to the formation of an essential intermediate species: the ternary complex between the PROTAC, the POI and an E3 ubiquitin ligase. Biophysical assays and ternary crystal structures are enabling a better understanding of the ternary complex formation and how its cooperativity, stability and kinetic lifetimes may be used as optimization parameters. This is significantly helping us move medicinal chemistry design from the synthesis of large libraries to rationally designed degraders.

This presentation will highlight some of the recent progress made in this field.



Dr. Induka Abeysena


Title: Drug discovery workflow for PROTAC with a focus on eliminating bottlenecks in evaporation


Abstract: 

An emerging modality of therapeutics called Proteolysis Targeting Chimers (PROTACs) could enable the design of new drugs targeting ‘undruggable’’ proteins which make up to 85% of the proteome. Their novel mode of action allows them to hijack a cells natural function and initiate degradation of the target protein for a particular disease. This development has led to great interest in the pharmaceutical and biotechnology industries. However, synthesis of PROTACs require numerous evaporation steps and use of a range of solvents, causing bottlenecks in their production and slowing the drug development process. Here we discuss the typical workflow within this process and the most appropriate equipment and the use of its features to overcome obstacles.


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