We are pleased to present the next instalment of our live webinar series, titled Drug Discovery Beyond the Traditional: New Approaches to Biotherapeutics. The free webinar aims to offer a Medicinal Chemists guide to the nuances of Biotherapeutics and Bioconjugation.
DATE: Wednesday April 12th 2017 | TIME: 4pm GMT, 11am (EST)
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|
“Protacs: Medicinal Chemistry Beyond Inhibitors”
| Jonas Helma & M.Sc. Dominik SchumacherTubulis Technologies|
“Novel chemoenzymatic approach for simple and fast site-specific antibody conjugation”
Missed our previous webinars?
Catch up with any in the current series so far, where we’ve hosted live discussions from some of the most highly respected individuals from academia and industry. Covering many important and current topics of chemistry, along with answering questions from our live global audience, here. For further information on our webinar series and to keep up to date on news on future sessions, please visit our Twitter page.