The Centre for Medicines Discovery aims to catalyse the discovery and development of new medicines for patients.
24 March 2021
Saracatinib is a clinically-tested dual Src/Abl kinase inhibitor. A new paper from Ellie Williams and the Growth Factor Signalling and Ubiquitination group led by Alex Bullock shows that saracatinib is an equipotent ALK2 kinase inhibitor. The paper outlines preclinical work that supports a current phase 2 clinical trial (NCT04307953) exploring the potential of saracatinib to treat cases of fibrodysplasia ossificans progressiva (FOP) driven by gain of function ALK2 mutations.
26 February 2021
The Kessler group describes a new methodology named ABPP-HT (high-throughput-compatible activity-based protein profiling), implementing a semi-automated proteomic workflow to profile a panel of deubiquitylating enzyme (DUB) inhibitors in cells. This allows direct cellular target engagement of small molecules against cellular DUBs, thereby accelerating DUB drug discovery.
23 February 2021
The Bullock Lab at CMD Oxford were delighted to be a part of this review from LUMC Leiden on Fibrodysplasia ossificans progressiva; an ultrarare congenital disease that progresses through intermittent episodes of bone formation at ectopic sites.
Moesin & CD44 are drivers of a co-expression module correlated with pathological/cognitive measures of #Alzheimer’s disease. Developed with @PharmChemBio @EmoryMedicine @UNCPharmacy, this Target Enabling Package opens the way to modulating the CD44:Moesin interaction. #Moesin http://doi.org/10.5281/zenodo.4429216
Structure and activation mechanism of the human liver-type glutaminase GLS2.
Ferreira IM. et al, (2021), Biochimie, 185, 96 - 104
Global proteomic analysis of extracellular matrix in mouse and human brain highlights relevance to cerebrovascular disease.
Pokhilko A. et al, (2021), J Cereb Blood Flow Metab
Fragment Screening Reveals Starting Points for Rational Design of Galactokinase 1 Inhibitors to Treat Classic Galactosemia.
Mackinnon SR. et al, (2021), ACS Chem Biol