The Centre for Medicines Discovery aims to catalyse the discovery and development of new medicines for patients.
LATEST NEWS
Chemogenomics for drug discovery: clinical molecules from open access chemical probes
12 April 2021
A key focus of the CMD is the development of small molecule chemical probes to investigate the biology of interesting, disease-relevant protein targets. An often touted benefit of probes is that they accelerate the drug discovery process by providing a starting point for small molecule drugs, but is this really the case? This review seeks to answer that question by describing a number of probes that have gone on to inspire a variety of clinical molecules, and will hopefully encourage drug discoverers to turn to chemical probes for inspiration.
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.
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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Thymosin β4 protects against aortic aneurysm via endocytic regulation of growth factor signaling.
Journal article
Munshaw S. et al, (2021), J Clin Invest
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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
