Chemical fragments (and a little cryo EM) for drug discovery Professor Martin Noble (Newcastle University) introduces his work on chemical fragments for drug discovery. Hosted by Dr Jamie Blaza.

Seminar
This event has now finished.
  • Date and time: Friday 6 October 2023, 1pm to 2pm
  • Location: Dianna Bowles Lecture Theatre, B/K/018, Biology Building, Campus West, University of York (Map)
  • Audience: Open to alumni, staff, students (postgraduate researchers, taught postgraduates, undergraduates)
  • Admission: Free admission, booking not required

Event details

Abstract

Anticancer drug discovery depends on understanding the enzyme activities and macromolecular interactions that drive some segment of the disease. Selectively inhibiting those activities and interactions begins with identifying hit matter that binds to functionally significant sites on a target, and developing that hit matter efficiently to on-scale inhibitory potency.  We are developing structure-based techniques that facilitate the identification of functionally important sites on a cancer-relevant targets, screening to find developable hit matter, and selection-based development of that hit matter for use as chemical probes and starting points for drug discovery. In this talk, I will present results relating to the use of crystallographic fragment screening for target-characterisation and hit-finding, and examples of those hits can be rapidly optimised by using DNA-encoded library methods.  I will also present some new cryo-EM-solved structures that illustrate how this exciting technique is starting to impact the early stages of drug discovery.

About the speaker

Professor Martin Noble

Martin is a Professor of Biomolecular Structure and Anticancer Drug Design at Newcastle University, initially in the Northern Institute for Cancer Research and now in the Newcastle University Translational and Clinical Research Institute. His group is pursuing structure-function studies of protein complexes involved in regulating transcription and progression through the eukaryotic cell cycle. His main interest is in understanding the molecular recognition events that drive cellular signalling processes, and in exploiting that understanding to produce new chemical probes and potential leads for drug discovery. This interest has also lead Martin into the field of bionanotechnology, where protein structures can be recycled as building blocks for novel materials