Picomolar bivalent inhibitors of protein kinase CK2 active against β-coronavirus replication.

The protein casein kinase 2 (CK2) has been shown to be upregulated in SARS-CoV-2 infections. However, few inhibitors have been tested for antiviral activity against coronaviruses. In this study, highly potent and selective bivalent inhibitors targeting the protein kinase CK2 were developed.

Binding-Site Switch for Protein Kinase CK2 Inhibitors.

The serine/threonine protein kinase CK2, a tetramer composed of a regulatory dimer (CK2β) bound to two catalytic subunits CK2α, is a well-established therapeutic target for various pathologies, including cancer and viral infections. Several types of CK2 inhibitors have been developed, including inhibitors that bind to the catalytic ATP-site, bivalent inhibitors that occupy both the CK2α ATP-site and the αD pocket, and inhibitors that target the CK2α/CK2β interface. Interestingly, the bivalent inhibitor AB668 shares a similar chemical structure with the interface inhibitor CCH507.

Access to BODIPY -Glycosides as Linker-Free Nonsymmetrical BODIPY-Carbohydrate Conjugates.

Recent years have witnessed an increasing interest in the synthesis and study of BODIPY-glycoconjugates. Most of the described synthetic methods toward these derivatives involve postfunctional modifications of the BODIPY core followed by the covalent attachment of the fluorophore and the carbohydrate through a "connector". Conversely, few synthetic approaches to linker-free carbohydrate-BODIPY hybrids have been described.

Linkers in fragment-based drug design: an overview of the literature.

Introduction: In fragment-based drug design, fragment linking is a popular strategy where two fragments binding to different sub-pockets of a target are linked together. This attractive method remains challenging especially due to the design of ideal linkers.

Areas Covered: The authors review the types of linkers and chemical reactions commonly used to the synthesis of linkers, including those utilized in protein-templated fragment self-assembly, where fragments are directly linked in the presence of the protein.

Prevalence of Staphylococcus aureus and methicillin-resistant S aureus on environmental surfaces in Ohio nursing homes.

Background: Methicillin-resistant Staphylococcus aureus (MRSA) is common in medical institutions. We sought to examine the prevalence of S aureus on environmental surfaces in nursing homes and to obtain molecular information on contaminating strains.

Methods: A total of 259 environmental samples were collected from 7 different nursing homes in Northeast Ohio (NEO), from suburban, urban, and rural settings.

Prevalence and Characterization of and Methicillin-Resistant on Public Recreational Beaches in Northeast Ohio.

can cause severe life-threatening illnesses such as sepsis and endocarditis. Although has been isolated from marine water and intertidal beach sand, only a few studies have been conducted to assess prevalence of at freshwater recreational beaches. As such, we aimed to determine prevalence and molecular characteristics of in water and sand at 10 freshwater recreational beaches in Northeast Ohio, USA.

Characterization of Staphylococcus aureus in Goose Feces from State Parks in Northeast Ohio.

Staphylococcus aureus can colonize a range of species. Although numerous studies have isolated pathogenic bacteria from wild birds, very little is known regarding S. aureus and their potential to spread methicillin-resistant (MRSA) strains.

Prospective multicenter surveillance identifies Staphylococcus aureus infections caused by livestock-associated strains in an agricultural state.

We conducted a surveillance study to investigate the epidemiology of Staphylococcus aureus infections in Iowa, using a convenience sample. Diagnostic laboratories submitted 20 S. aureus isolates per month for a 20-month period between 2011 and 2013.