15:30 - 18:15 pm 3月9日
Protein Degraders: Getting Beyond the Lab
( 蛋白质分解诱导药：研究阶段以后的进展 )
About the course:
This course is designed as an extension to the topics discussed at the PROTACs and Beyond conference. It brings together experts in the ubiquitin field to discuss the cellular pathways governing protein degradation and explore existing chemistries that can be utilized for designing efficient and specific protein degrader molecules. There will also be discussion around optimizing the degraders to predict their in vivo activity and ultimately, their success in the clinic. This course offers an additional opportunity for attendees to share ideas and best practices in this rapidly evolving field.
Topics to be Discussed:
- Understanding the underlying biology to best harness protein degradation
- How to access many different degradation machineries
- Avoiding artefacts and developing reliable methods for high-throughput PROTAC discovery
- Tools for exploring new E3 ligases:
(i) Crystallography for new E3 ligases
(ii) Defining substrate degrons for assays and crystallography
- Building the right assays and platforms for protein degradation
- Applications beyond protein degradation
Laura Itzhaki, FRSC, Professor of Structural Pharmacology, Department of Pharmacology, University of Cambridge and CSO, PolyProx Therapeutics
Dr. Laura Itzhaki has over 20 years’ experience leading academic research in the field of protein engineering. She has a BA in Chemistry (Oxford) and PhD in Biochemistry (Cambridge). From 2003 to 2011 her group was located at the MRC Cancer Cell Unit in Cambridge UK, and she is currently a Professor in the Department of Pharmacology at the University of Cambridge. In 2019, she secured seed finance for PolyProx Therapeutics to develop biotherapeutics harnessing the cell’s quality-control machinery to destroy disease-associated proteins that cannot be targeted by conventional drug modalities.
Tauseef R. Butt, PhD, President and CEO, Progenra Inc.
Dr. Butt obtained a Ph.D. degree in Molecular Biology from The University of Glasgow, Scotland, He was a Staff Fellow at the National Institutes of Health, Bethesda, MD, before joining SmithKline Beckman (now GSK) Pharmaceuticals. He also served as an Adjunct Professor Biochemistry and Biophysics, University of Pennsylvania Medical School, Philadelphia. Dr. Butt has published more than 100 papers in life sciences research, raised several million dollars of capital, and launched highly innovative and profitable biotechnology companies.
Alex Bullock, PhD, Associate Professor, Nuffield Department of Medicine, University of Oxford and Principal Investigator at the Structural Genomics Consortium (SGC)
Alex Bullock is an Associate Professor at the Nuffield Department of Medicine, University of Oxford and Principal Investigator at the Structural Genomics Consortium (SGC), an international public-private partnership that aims to catalyse the discovery of new medicines through open access collaborative science. Alex trained in biochemistry at the University of Cambridge where he completed his PhD with Sir Alan Fersht. He subsequently held a Wellcome Fellowship for positions with David Baker at the University of Washington, Seattle and later with Sir Peter Ratcliffe at the University of Oxford. In his current post he has gained more than 15 years of experience working on proteins mediating phosphorylation and ubiquitylation. His work has revealed a Jekyll and Hyde behaviour of BMP signalling that drives different cancers and developmental diseases. He is now working with patient groups to develop BMP pathway inhibitors for clinical investigation and plans a phase II study in FOP in early 2020.
Nikki Carter, PhD, Associate Director, Discovery Biology, AstraZeneca
Nikki Carter has worked in early drug discovery in Pharmaceutical, CRO and Commercial settings for 17 years. She joined AstraZeneca’s Discovery Sciences’ function in 2009. During this time, Nikki has led novel technology developments for mechanistic enzymology and helped pioneer HT-mechanistic kinase profiling to support multiple projects. Nikki now leads the cellular assay development group in the UK. She has been heavily involved in the recent Protacs build at AstraZeneca.
Gopal Sapkota, PhD, Programme Leader, MRC Protein Phosphorylation & Ubiquitylation Unit, Sir James Black Centre, School of Life Sciences, University of Dundee
Gopal is a tenured programme leader at the MRC Protein Phosphorylation and Ubiquitylation Unit at Dundee University. Originally from Nepal, Gopal obtained a Masters in Biochemistry degree from University of Bath in 1999 and Ph.D. in Biochemistry from University of Dundee in 2003. He received the prestigious Damon Runyon Cancer Research Fellowship to undertake postdoctoral research in Joan Massagué’s laboratory at Memorial Sloan-Kettering Cancer Center in New York. His research group studies the molecular mechanisms that underpin cellular signal transduction pathways, in particular through reversible protein ubiquitylation and phosphorylation processes, and their interplay, in human cells and diseases. His lab is involved in developing innovative technologies that harness the ubiquitin proteasome system to enable targeted protein degradation in cells that allow one to interrogate fundamental research questions and help expedite drug discovery.