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On-demand webinar

Biophysics in kinase drug discovery: FBS to PROTAC® ternary complex characterisation

Watch this webinar to learn how biophysics can be used in different cascade strategies where the goal is to identify and characterise fragments, compounds or active degraders targeting PIM3 kinase.

Kinase inhibitor discovery is a dynamic field where scientists are taking a deep dive into the design of immune-modulatory compounds tackling chronic diseases or cancer treatment. In recent years, the proteolysis targeting chimera (PROTAC®) approach has revolutionised this work.

In this webinar, we present how biophysical approaches can be integrated into different cascade strategies aiming at the identification and characterisation of fragments, compounds or active degraders targeting PIM3 kinase.

Person using scientific equipment

Overview

We will outline how our experts can help advance drug discovery projects using state-of-the-art technology, which maximises on complementary approaches and revolutionary throughput. We will illustrate these innovative techniques by sharing:

  • A fragment-based campaign, from screening to MoA, including the identification of non-competitive ATP fragments.
  • A PROTAC® characterisation study using SPR, Spectral Shift and TSA, as well as binary and ternary complex characterisation with the determination of the cooperativity factor (α).

Results & further applications

With high-throughput equipment (Dianthus), we were able to quickly and efficiency screen a set of fragments from Eurofins library. In addition, we were able to identify fragments with µM-range affinity values (KD) for PIM3 and provide valuable information regarding their mechanisms of action (ATP competitors).

We found that Biophysics provides sensitive and robust assays for the characterisation of PIM3 PROTAC®: CRBN ternary complex, helping further understand and predict the target ubiquitination efficiency and ultimately the in vivo degradation process.

Register to join this biophysics webinar discussion for free

Key takeaways

  • Explore the use of new biophysics methods to gain valuable insight into the characterisation of your molecule.
  • Understand how by combining biophysical assays (MST, TSA and SPR), it is possible to identify PIM3 binders, distinguish between stabilisers and destabilisers, as well as their classification according to their binding site (ATP competitors).
  • Learn how PROTAC® ternary complex characterisation using biophysics can generate promising candidates.
  • Gain valuable information as how these techniques are a time-saving solution which can head off long and expensive in vivo studies down the road.
  • Ask our biophysics experts questions and benefit from their knowledge and guidance.

OUR SPEAKERS

Vanessa Porkolab, PhD, Biophysics Director – Eurofins Cerep

Dr. Porkolab manages the Biophysics Platform for drug discovery projects at Eurofins Cerep. Prior to joining as Biophysics Director in 2022, she was Team leader, Senior Scientist in Biophysics in another European CRO and Biotech working on fragments, small-molecules, antibodies and aptamer-based drug discovery programs. With her scientific team, she is involved in integrated projects spanning target validation, high-throughput screening campaigns and hit-to-lead to lead optimisation. She completed her PhD at the Institut de Biologie Structurale (IBS) in Grenoble, France where she worked on multidisciplinary drug design projects targeting carbohydrate-based proteins involved in the immune response. She then moved to Brandeis University near Boston, USA where her postdoctoral studies were focused on RNA display and biophysical characterisation of glycopeptides for anti-HIV Abs.

 

Maud Sigoillot, PhD, Biophysics Research Scientist – Eurofins Cerep

Dr Sigoillot is a Project Leader for Biophysics Projects. She works closely with clients to define the most effective biophysical strategy and is responsible for the integrity of the scientific data of the project.
DSigoillot obtained her PhD [at the University of Burgundy in 2011, specialising in the perception of sweet and umami tastes mediated by G-Protein Coupled Receptors (GPCRs). Subsequently, she deepened her knowledge of GPCR biochemistry during a first postdoctoral experience at Tsinghua University (China). Back in Europe, she focused on engineering nanobodies to treat cystic fibrosis at the University of Brussels (ULB, Belgium) and had the opportunity to join Chromacure biotech as a Research Scientist to develop complementary biophysical assays targeting orphan nuclear receptors in the context of drug discovery programs in oncology.

FAQs

Is the webinar free?
Yes – there is no charge to watch the webinar, either live or on-demand.

When will the webinar take place?
The webinar will take place live on 6 December at 16:00 UK Time

I’m busy. Can I watch it later?
The webinar will become available to watch on-demand shortly after the live webinar takes place.

What are the benefits of attending live?
During the live webinar, you’ll be able to ask the speakers your questions, which will then be answered during the live Q&A session towards the end of the webinar.

How long will the webinar be?
This webinar will last for up to one hour.

What do I need to watch this webinar?
All you need is a computer with an internet connection. Be sure to use headphones if in an office environment.

Do I receive a certificate?
Yes, you will receive a certificate if you attend the webinar live. The certificate will be sent with your on-demand video link.

ABOUT US

Eurofins Discovery can optimise your discovery process – whether you need complete, end-to-end services, help with one or more stages, or the products for discovery work.

With over 600 scientists around the world, 50 patents, and 30 billion data points screened, you can rely on Eurofins Discovery to provide you with the deep resources needed for your success.

Standalone Services. Offering the ability to support your projects on an as-needed basis across the drug discovery workflow, Eurofins Discovery offers you services for Medicinal Chemistry, Synthetic Chemistry, In Vitro Pharmacology, Safety & Efficacy, ADME & Toxicology, and Phenotypic Assays. In Vivo services are available through our partner lab, Pharmacology Discovery Services.

Integrated Drug Discovery. The DiscoveryOne™ integrated drug discovery team works hand-in-hand as partners with you, integrating all Eurofins Discovery capabilities to accelerate delivery of preclinical candidates by utilising our in-house project management and deep scientific expertise.

Products for Drug Discovery. Eurofins DiscoverX, a Eurofins Discovery company, is the trusted product solutions provider that can accelerate your programs with confidence with qualified reagents, cell lines, and assays ready to run today. Eurofins DiscoverX develops and manufactures cutting-edge assays, stable cell lines, membrane preps, enzymes, and reagents for drug discovery and development.