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Synthesis and use of sulfonamide-, sulfoxide-, or sulfone-containing aminoglycoside-CoA bisubstrates as mechanistic probes for aminoglycoside N-6'-acetyltransferase.
TLDR
Interestingly, the sulfonamide- linked bisubstrate, which was expected to best mimic the tetrahedral intermediate, does not show improved inhibition when compared with amide-linked bisubstrates, and most of the sulfone- and sulfoxide-containing bisUBstrates prepared are nanomolar inhibitors of AAC(6')-Ii. Expand
Inhibitors of aminoglycoside resistance activated in cells.
TLDR
This work provides a proof-of-concept for the utility of prodrug compounds activated by enzymes of the coenzyme A biosynthetic pathway, to resensitize resistant strains of bacteria to aminoglycoside antibiotics. Expand
An artificial metalloenzyme biosensor can detect ethylene gas in fruits and Arabidopsis leaves
TLDR
An artificial metalloenzyme-based ethylene probe can be used to detect ethylene in plants with improved spatiotemporal resolution and represents an example of an ArM biosensor, designed specifically for the spatial and temporal detection of a biological metabolite previously not accessible using enzyme biosensors. Expand
In Vivo Gold Complex Catalysis within Live Mice.
TLDR
A glycoalbumin-AuIII complex was designed and developed that enables organ-specific, localized propargyl ester amidation with nearby proteins within live mice, which could enable the exploitation of other metal catalysis strategies for biomedical and clinical applications. Expand
Biocompatibility and therapeutic potential of glycosylated albumin artificial metalloenzymes
The ability of natural metalloproteins to prevent inactivation of their metal cofactors by biological metabolites, such as glutathione, is an area that has been largely ignored in the field ofExpand
Geminal dialkyl derivatives of N-substituted pantothenamides: synthesis and antibacterial activity.
TLDR
A synthetic route to N-substituted pantothenamides with various alkyl substituents replacing the geminal dimethyl groups is reported, which yielded a new N- substituent of Pantothenamide which is amongst the most potent reported so far. Expand
Exploring structural motifs necessary for substrate binding in the active site of Escherichia coli pantothenate kinase.
TLDR
A study on the selectivity of pantothenate kinase, the first and rate limiting step of CoA biosynthesis, and insight for the future design of PanK substrates in the production of useful CoA analogues is provided. Expand
Understanding and overcoming aminoglycoside resistance caused by N-6'-acetyltransferase.
TLDR
Aminoglycosides-modifying enzymes (AMEs) are discussed, with a special emphasis on the efforts to comprehend and block resistance caused by aminoglycoside 6'-N-acetyltransferase (AAC(6')). Expand
2-Benzoylpyridine Ligand Complexation with Gold Critical for Propargyl Ester-Based Protein Labeling.
TLDR
Observations appear to suggest that BPy-Au-mediated, propargyl ester-based protein labeling acts via an activated ester intermediate, which contributes to the authors' understanding of this process and will aid the expansion/optimization of gold-catalyst usage in future bioconjugation applications, especially in vivo. Expand
Cellular Studies of an Aminoglycoside Potentiator Reveal a New Inhibitor of Aminoglycoside Resistance
TLDR
A new aminoglycoside resistance inhibitor is revealed, as well as the possibility that these prodrugs are transformed into more than one inhibitor in bacteria, and the onset of the potentiators is rapid. Expand
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