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LATEST NEWS

Saracatinib is an efficacious clinical candidate for fibrodysplasia ossificans progressiva

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

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

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

MSN: A TEP for Alzheimer’s Disease