Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

This review covers the most recent advances in the development of inhibitors for the
bacterial enzyme sortase A (SrtA). Sortase A (SrtA) is a critical virulence factor, present …

Uropygial gland secretions of birds consist of host and bacteria derived compounds and
play a major sanitary and feather-protective role. Here we report on our microbiome studies …

Werner syndrome protein (WRN) is a multifunctional enzyme with helicase, ATPase, and
exonuclease activities that are necessary for numerous DNA-related transactions in the …

The prevalence of multidrug resistance (MDR) and stagnant drug-development pipelines
have led to the rapid rise of hard-to-treat antibiotic-resistant bacterial infections. These …

RNA methyltransferases (MTases) have recently become increasingly important in drug
discovery. Yet, most frequently utilized RNA MTase assays are limited in their throughput …

Targeted covalent inhibitors (TCIs) directing cysteine have historically relied on a narrow set
of electrophilic “warheads”. While Michael acceptors remain at the forefront of TCI design …

In this study, we have identified and optimized two lead structures from an in-house
screening, with promising results against the parasitic flatworm Schistosoma mansoni and …

The aim of this study was to investigate the transition from non-covalent reversible over
covalent reversible to covalent irreversible inhibition of cysteine proteases by making …

Covalent peptidomimetic protease inhibitors have gained a lot of attention in drug
development in recent years. They are designed to covalently bind the catalytically active …