During this webinar we look at Drug Discovery Beyond the Traditional: New Approaches to Biotherapeutics, including next-generation Antibody-Drug Conjugates.
Key Learning Objectives
- An appreciation of approaches in drug discovery that go beyond the targeting of protein binding sites with traditional small-molecule inhibitors; presented from the perspective of Synthetic and Medicinal Chemists.
- An appreciation of the therapeutic potential of hijacking the ubiquitin-proteasome system using PROTACs (small-molecule-based proteolysis-targeting chimeras) and an insight into an industrial drug-discovery campaign using this strategy.
- An understanding of a new approach for site specific antibody-drug conjugation that could allow access to the next-generation of Antibody-Drug Conjugates.
A novel chemoenzymatic approach for simple and fast site-specific antibody conjugation is presented. We repurposed tubulin tyrosine ligase (TTL) to attach various unnatural tyrosine derivatives as small bioorthogonal handles to nanobodies and recombinant antibodies containing a short tubulin-derived recognition sequence (Tub-tag). This novel strategy enables a broad range of chemoselective C-terminal antibody modifications. We foresee a wide field of potential applications throughout the life sciences, including next-generation Antibody-Drug Conjugates.
Historically, most bioactive small molecules have focused on blocking interactions between biomolecules to produce a therapeutic effect. This works well in many cases, but has intrinsic limitations. An alternative strategy is to introduce a drug-like compound which activates a process by localising proteins together. This talk will describe some of our group’s work on Protacs; drug-like small molecules which catalyse the degradation of target proteins by hijacking the ubiquitin-proteasome system. This approach offers the potential to target new biological pathways, and to produce a new generation of compounds to treat human disease.
Guest speakers include:
Dr Mark Rackham – GSK
Dr Jonas Helma & M.Sc. Dominik Schumacher – Tubulis Technologies
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