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Home>Mission Therapeutics’ Scientists Highlight Significance of Deubiquitylating Enzymes (DUBs) as Key Drug Targets

Mission Therapeutics’ Scientists Highlight Significance of Deubiquitylating Enzymes (DUBs) as Key Drug Targets

Mission Therapeutics’ Scientists Highlight Significance of Deubiquitylating Enzymes (DUBs) as Key Drug Targets

10/02/2017

Mission Therapeutics’ Scientists Highlight Significance of Deubiquitylating Enzymes (DUBs) as Key Drug Targets

Keynote Nature article reviews drug discovery opportunities in multiple disease areas of unmet need

An article entitled “Deubiquitylating enzymes (DUBs) and drug discovery: emerging opportunities,” written by the drug discovery team at Mission Therapeutics was published online today in the scientific journal Nature Reviews Drug Discovery.

The peer-reviewed article outlines how understanding the physiological and pathophysiological roles of human DUBs has accelerated over the past decade. It also highlights how elucidating the biological complexities of this enzyme family is providing opportunities for the development of potentially transformative therapies for a range of clinical indications.

The article is authored by Company co-founders and scientists, including Dr Jeanine A. Harrigan and Professor Steve Jackson FRS.

DUBs comprise a group of some 100 proteins that are known to play important roles in regulating ubiquitylation, the process whereby ubiquitin – a small protein so called because it is present in all complex organisms and virtually all cells in the body – controls protein homeostasis, protein activity, intracellular location, and sub-cellular turnover or degradation.

The clinical development of DUB inhibitors initially proved challenging, in large part due to issues linked to specificity and selectivity. However, recent progress in DUB enzymology, biology and technological developments, described in the review, has confirmed that DUBs are druggable, novel therapeutic targets. As a result, first-generation inhibitors are now moving into, or are on the threshold of entering, patient trials in a number of clinical settings.

Professor Steve Jackson, Co-Founder and CSO, Mission Therapeutics, and senior author on the paper, commented: “This article in Nature Reviews Drug Discovery covers seminal advances that have yielded critical insights into DUB target biology and chemistry over the past decade. A strong foundation in DUB research has been fundamental to Mission Therapeutics’ novel target validation and drug discovery platforms. To date, the platform has demonstrated the diverse clinical potential of novel chemistries selectively targeting different members of the DUB enzyme class.”

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