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Cell envelope proteases and peptidases of Pseudomonas aeruginosa: multiple roles, multiple mechanisms.

Published in FEMS microbiology reviews

Pseudomonas aeruginosa is a Gram-negative bacterium that is commonly isolated from damp environments. It is also a major opportunistic pathogen, causing a wide range of problematic infections. The cell envelope of P. aeruginosa, comprising the cytoplasmic membrane, periplasmic space, peptidoglycan layer and outer membrane, is critical to the bacter...

Structure Guided Development of Potent Piperazine-Derived Hydroxamic Acid Inhibitors Targeting Falcilysin.

Published in Bioorganic & medicinal chemistry letters

The protozoan parasite Plasmodium falciparum causes the most severe form of human malaria and is estimated to kill 400,000 people a year. The parasite infects and replicates in host red blood cells (RBCs), where it expresses an array of proteases to carry out multiple essential processes. We are investigating the function of falcilysin (FLN), a pro...

Controlled Inhibition of Apoptosis by Photoactivatable Caspase Inhibitors

Caspases control regulated cell death (apoptosis), a process that is crucial in the development of multicellular organisms as well as in various diseases. In order to spatiotemporally study apoptosis, we here develop photoactivatable caspase inhibitors. These are based on cysteine-reactive acyloxymethyl ketone electrophiles connected to a peptide t...

Identification of a C2-symmetric diol based human immunodeficiency virus protease inhibitor targeting Zika virus NS2B-NS...

Published in Journal of biomolecular structure & dynamics

Zika virus (ZIKV) is an emerging mosquito-borne flavivirus and infection by ZIKV Asian lineage is known to cause fetal brain anomalies and Guillain-Barrés syndrome. The WHO declared ZIKV a global public health emergency in 2016. However, currently neither vaccines nor antiviral prophylaxis/treatments are available. In this study, we report the iden...

Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2

Published in ACS Medicinal Chemistry Letters

A consensus virtual screening protocol has been applied to ca. 2000 approved drugs to seek inhibitors of the main protease (Mpro) of SARS-CoV-2, the virus responsible for COVID-19. 42 drugs emerged as top candidates, and after visual analyses of the predicted structures of their complexes with Mpro, 17 were chosen for evaluation in a kinetic assay ...

Toward Disentangling the Multiple Nutritional Constraints Imposed by Planktothrix : The Significance of Harmful Secondar...

Published in Frontiers in Microbiology

The harmful bloom-forming cyanobacterium Planktothrix is commonly considered to be nutritionally inadequate for zooplankton grazers, resulting in limited top-down control. However, interactions between Planktothrix and zooplankton grazers are poorly understood. The food quality of Planktothrix is potentially constrained by morphological properties ...

Treatment outcomes of integrase inhibitors, boosted protease inhibitors and nonnucleoside reverse transcriptase inhibito...

Published in HIV medicine

Although outcomes of antiretroviral therapy (ART) have been evaluated in randomized controlled trials, experiences from subpopulations defined by age, CD4 count or viral load (VL) in heterogeneous real-world settings are limited. The study design was an international multicohort collaboration. Logistic regression was used to compare virological and...

Antiviral Drug Discovery To Address the COVID-19 Pandemic.

The magnitude of the morbidity and mortality inflicted upon the global population in less than 1 year has driven the inescapable conclusion that the discovery and development of effective antiviral drugs for COVID-19 are urgent and should be prioritized. The antiviral drug discovery programs that emerged for HIV and hepatitis C virus have enabled t...