The Centre for Medicines Discovery aims to catalyse the discovery and development of new medicines for patients.
LATEST NEWS
Saracatinib is an efficacious clinical candidate for fibrodysplasia ossificans progressiva
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.
Deubiquitinase (DUB) profiling goes high-throughput
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.
Challenges and Opportunities for Drug Repositioning in Fibrodysplasia Ossificans Progressiva
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.
Highlight
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
LATEST PUBLICATIONS
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Structure and activation mechanism of the human liver-type glutaminase GLS2.
Journal article
Ferreira IM. et al, (2021), Biochimie, 185, 96 - 104
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Global proteomic analysis of extracellular matrix in mouse and human brain highlights relevance to cerebrovascular disease.
Journal article
Pokhilko A. et al, (2021), J Cereb Blood Flow Metab
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Fragment Screening Reveals Starting Points for Rational Design of Galactokinase 1 Inhibitors to Treat Classic Galactosemia.
Journal article
Mackinnon SR. et al, (2021), ACS Chem Biol