Search Results - "McKinney, David C."
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Novel Rapidly Diversifiable Antimicrobial RNA Polymerase Switch Region Inhibitors with Confirmed Mode of Action in Haemophilus influenzae
Published in Journal of Bacteriology (01-10-2012)“…A series of inhibitors with a squaramide core was synthesized following its discovery in a high-throughput screen for novel inhibitors of a…”
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Pyrazolopyrimidines Establish MurC as a Vulnerable Target in Pseudomonas aeruginosa and Escherichia coli
Published in ACS chemical biology (17-10-2014)“…The bacterial peptidoglycan biosynthesis pathway provides multiple targets for antibacterials, as proven by the clinical success of β-lactam and glycopeptide…”
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3
Molecular basis for substrate recruitment to the PRMT5 methylosome
Published in Molecular cell (02-09-2021)“…PRMT5 is an essential arginine methyltransferase and a therapeutic target in MTAP-null cancers. PRMT5 uses adaptor proteins for substrate recruitment through a…”
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Discovery of a First-in-Class Inhibitor of the PRMT5–Substrate Adaptor Interaction
Published in Journal of medicinal chemistry (12-08-2021)“…PRMT5 and its substrate adaptor proteins (SAPs), pICln and Riok1, are synthetic lethal dependencies in MTAP-deleted cancer cells. SAPs share a conserved PRMT5…”
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X‑ray Crystal Structures of Escherichia coli RNA Polymerase with Switch Region Binding Inhibitors Enable Rational Design of Squaramides with an Improved Fraction Unbound to Human Plasma Protein
Published in Journal of medicinal chemistry (09-04-2015)“…Squaramides constitute a novel class of RNA polymerase inhibitors of which genetic evidence and computational modeling previously have suggested an inhibitory…”
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Selective inhibitors of bacterial t-RNA-(N(1)G37) methyltransferase (TrmD) that demonstrate novel ordering of the lid domain
Published in Journal of medicinal chemistry (26-09-2013)“…The tRNA-(N(1)G37) methyltransferase (TrmD) is essential for growth and highly conserved in both Gram-positive and Gram-negative bacterial pathogens…”
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Time-dependent, reversible, oxaborole inhibition of Escherichia coli leucyl-tRNA synthetase measured with a continuous fluorescence assay
Published in Analytical biochemistry (01-12-2012)“…Enzyme assays for the catalytic activity of aminoacyl-tRNA synthetases generally measure the incorporation of radioactive amino acids into tRNA. Such assays…”
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Selective Inhibitors of Bacterial t‑RNA-(N1G37) Methyltransferase (TrmD) That Demonstrate Novel Ordering of the Lid Domain
Published in Journal of medicinal chemistry (26-09-2013)“…The tRNA-(N1G37) methyltransferase (TrmD) is essential for growth and highly conserved in both Gram-positive and Gram-negative bacterial pathogens…”
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The Role of a Novel Auxiliary Pocket in Bacterial Phenylalanyl-tRNA Synthetase Druggability
Published in The Journal of biological chemistry (01-08-2014)“…The antimicrobial activity of phenyl-thiazolylurea-sulfonamides against Staphylococcus aureus PheRS are dependent upon phenylalanine levels in the…”
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Antibacterial FabH Inhibitors with Mode of Action Validated in Haemophilus influenzae by in Vitro Resistance Mutation Mapping
Published in ACS infectious diseases (08-07-2016)“…Fatty acid biosynthesis is essential to bacterial growth in Gram-negative pathogens. Several small molecules identified through a combination of…”
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Novel broad-spectrum inhibitors of bacterial methionine aminopeptidase
Published in Bioorganic & medicinal chemistry letters (15-08-2015)“…With increasing emergence of multi-drug resistant infections, there is a dire need for new classes of compounds that act through unique mechanisms. In this…”
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Structural Insights Lead to a Negamycin Analogue with Improved Antimicrobial Activity against Gram-Negative Pathogens
Published in ACS medicinal chemistry letters (13-08-2015)“…Negamycin is a natural product with antibacterial activity against a broad range of Gram-negative pathogens. Recent revelation of its ribosomal binding site…”
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Synthesis of Amine- and Thiol-Modified Nucleoside Phosphoramidites for Site-Specific Introduction of Biophysical Probes into RNA
Published in Journal of organic chemistry (27-05-2005)“…For studies of RNA structure, folding, and catalysis, site-specific modifications are typically introduced by solid-phase synthesis of RNA oligonucleotides…”
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4,5-Disubstituted 6‑Aryloxy-1,3-dihydrobenzo[c][1,2]oxaboroles Are Broad-Spectrum Serine β‑Lactamase Inhibitors
Published in ACS infectious diseases (10-07-2015)“…Bacterially expressed β-lactamases are rapidly eroding the clinical utility of the important β-lactam class of antibacterials, significantly impairing our…”
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Illicit Transport via Dipeptide Transporter Dpp is Irrelevant to the Efficacy of Negamycin in Mouse Thigh Models of Escherichia coli Infection
Published in ACS infectious diseases (08-05-2015)“…Negamycin is a hydrophilic antimicrobial translation inhibitor that crosses the lipophilic inner membrane of Escherichia coli via at least two transport routes…”
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