Chad S. Hewitt
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View article: Structure-activity relationship studies for inhibitors for vancomycin-resistant <i>Enterococcus</i> and human carbonic anhydrases
Structure-activity relationship studies for inhibitors for vancomycin-resistant <i>Enterococcus</i> and human carbonic anhydrases Open
Vancomycin-resistant enterococci (VRE), consisting of pathogenic Enterococcus faecalis and E. faecium, is a leading cause of hospital-acquired infections (HAIs). We recently repurposed the FDA-approved human carbonic anhydrase (CA) inhibit…
View article: Inhibition studies of bacterial α-carbonic anhydrases with phenols
Inhibition studies of bacterial α-carbonic anhydrases with phenols Open
The α-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogens Neisseria gonorrhoeae (NgCAα) and Vibrio cholerae (VchCAα) were investigated for their inhibition by a panel of phenols and phenolic acids. Mono-, di- and tri-s…
View article: Coumarins effectively inhibit bacterial α-carbonic anhydrases
Coumarins effectively inhibit bacterial α-carbonic anhydrases Open
Coumarins are known to act as prodrug inhibitors of mammalian α-carbonic anhydrases (CAs, EC 4.2.1.1) but they were not yet investigated for the inhibition of bacterial α-CAs. Here we demonstrate that such enzymes from the bacterial pathog…
View article: Rational Development and Characterization of a Ubiquitin Variant with Selectivity for Ubiquitin C-Terminal Hydrolase L3
Rational Development and Characterization of a Ubiquitin Variant with Selectivity for Ubiquitin C-Terminal Hydrolase L3 Open
There is currently a lack of reliable methods and strategies to probe the deubiquitinating enzyme UCHL3. Current small molecules reported for this purpose display reduced potency and selectivity in cellular assays. To bridge this gap and p…
View article: Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of <i>Neisseria gonorrhoeae</i>
Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of <i>Neisseria gonorrhoeae</i> Open
Neisseria gonorrhoeae is a high-priority pathogen of concern due to the growing prevalence of resistance development against approved antibiotics. Herein, we report the anti-gonococcal activity of ethoxzolamide, the FDA-approved human carb…
View article: Dithiocarbamates effectively inhibit the α-carbonic anhydrase from <i>Neisseria gonorrhoeae</i>
Dithiocarbamates effectively inhibit the α-carbonic anhydrase from <i>Neisseria gonorrhoeae</i> Open
Recently, inorganic anions and sulphonamides, two of the main classes of zinc-binding carbonic anhydrase inhibitors (CAIs), were investigated for inhibition of the α-class carbonic anhydrase (CA, EC 4.2.1.1) from Neisseria gonorrhoeae, NgC…
View article: Structure–Activity Relationship Studies of Acetazolamide-Based Carbonic Anhydrase Inhibitors with Activity against <i>Neisseria gonorrhoeae</i>
Structure–Activity Relationship Studies of Acetazolamide-Based Carbonic Anhydrase Inhibitors with Activity against <i>Neisseria gonorrhoeae</i> Open
Neisseria gonorrhoeae is an urgent threat to public health in the United States and around the world. Many of the current classes of antibiotics to treat N. gonorrhoeae infection are quickly becoming obsolete due to increased rates of resi…
View article: Optimization and Anti-Cancer Properties of Fluoromethylketones as Covalent Inhibitors for Ubiquitin C-Terminal Hydrolase L1
Optimization and Anti-Cancer Properties of Fluoromethylketones as Covalent Inhibitors for Ubiquitin C-Terminal Hydrolase L1 Open
The deubiquitinating enzyme (DUB) UCHL1 is implicated in various disease states including neurodegenerative disease and cancer. However, there is a lack of quality probe molecules to gain a better understanding on UCHL1 biology. To this en…
View article: Insights into Ubiquitin Product Release in Hydrolysis Catalyzed by the Bacterial Deubiquitinase SdeA
Insights into Ubiquitin Product Release in Hydrolysis Catalyzed by the Bacterial Deubiquitinase SdeA Open
We report the co-crystal structure of the (catalytic Cys)-to-Ala mutant of the deubiquitinase domain of the Legionella pneumophila effector SdeA (SdeADUB) with its ubiquitin (Ub) product. Most of the intermolecular interactions are preserv…
View article: Anion inhibition studies of the α-carbonic anhydrases from <i>Neisseria gonorrhoeae</i>
Anion inhibition studies of the α-carbonic anhydrases from <i>Neisseria gonorrhoeae</i> Open
The bacterial pathogen Neisseria gonorrhoeae encodes for an α-class carbonic anhydrase (CA, EC 4.2.1.1), NgCA, which was investigated for its inhibition with a series of inorganic and organic anions. Perchlorate and hexafluorophosphate did…