De Novo Design, Synthesis, and In Vitro Evaluation of Inhibitors for Prokaryotic tRNA‐Guanine Transglycosylase: A Dramatic Sulfur Effect on Binding Affinity
EA Meyer, R Brenk, RK Castellano, M Furler… - …, 2002 - Wiley Online Library
Shigellosis (bacillary dysentary) is a bacterial disease that results in more than one million
deaths each year.[1] Enteric infections caused by the Shigella organisms have traditionally …
deaths each year.[1] Enteric infections caused by the Shigella organisms have traditionally …
From Hit to Lead: De Novo Design Based on Virtual Screening Hits of Inhibitors of tRNA‐Guanine Transglycosylase, a Putative Target of Shigellosis Therapy
R Brenk, HD Gerber, JD Kittendorf… - Helvetica chimica …, 2003 - Wiley Online Library
Shigellosis, a bacterial disease, causes the death of more than one million people per year.
Extensive studies of Shigella flexneri have recognized tRNA‐guanine transglycosylase …
Extensive studies of Shigella flexneri have recognized tRNA‐guanine transglycosylase …
Crystallographic study of inhibitors of tRNA-guanine transglycosylase suggests a new structure-based pharmacophore for virtual screening
The enzyme tRNA-guanine transglycosylase (TGT) is involved in the pathogenicity of
Shigellae. As the crystal structure of this protein is known, it is a putative target for the …
Shigellae. As the crystal structure of this protein is known, it is a putative target for the …
Synthesis, Biological Evaluation, and Crystallographic Studies of Extended Guanine‐Based (lin‐Benzoguanine) Inhibitors for tRNA‐Guanine Transglycosylase (TGT)
EA Meyer, N Donati, M Guillot… - Helvetica chimica …, 2006 - Wiley Online Library
This paper describes the rational design, synthesis, and biological evaluation of a new
generation of inhibitors of the bacterial enzyme tRNA‐guanine transglycosylase (TGT) …
generation of inhibitors of the bacterial enzyme tRNA‐guanine transglycosylase (TGT) …
High‐Affinity Inhibitors of tRNA‐Guanine Transglycosylase Replacing the Function of a Structural Water Cluster
PC Kohler, T Ritschel, WB Schweizer… - … A European Journal, 2009 - Wiley Online Library
The tRNA‐modifying enzyme tRNA–guanine transglycosylase (TGT) is essential for the
pathogenic mechanism of Shigella flexneri, the causing agent of the bacterial diarrheal …
pathogenic mechanism of Shigella flexneri, the causing agent of the bacterial diarrheal …
Synthesis and In Vitro Evaluation of 2‐Aminoquinazolin‐4(3H)‐one‐Based Inhibitors for tRNA‐Guanine Transglycosylase (TGT)
EA Meyer, M Furler, F Diederich, R Brenk… - Helvetica chimica …, 2004 - Wiley Online Library
Abstract tRNA‐Guanine transglycosylase (TGT) plays a key role in the post‐transcriptional
modification of tRNA. It has been linked with the pathogenicity of shigellae, the causative …
modification of tRNA. It has been linked with the pathogenicity of shigellae, the causative …
From lin‐Benzoguanines to lin‐Benzohypoxanthines as Ligands for Zymomonas mobilis tRNA–Guanine Transglycosylase: Replacement of Protein–Ligand …
LJ Barandun, F Immekus, PC Kohler… - … A European Journal, 2012 - Wiley Online Library
The foodborne illness shigellosis is caused by Shigella bacteria that secrete the highly
cytotoxic Shiga toxin, which is also formed by the closely related enterohemorrhagic …
cytotoxic Shiga toxin, which is also formed by the closely related enterohemorrhagic …
High-affinity inhibitors of Zymomonas mobilis tRNA–guanine transglycosylase through convergent optimization
LJ Barandun, F Immekus, PC Kohler… - … Section D: Biological …, 2013 - journals.iucr.org
The tRNA-modifying enzyme tRNA–guanine transglycosylase (TGT) has been recognized
as a drug target for the treatment of the foodborne illness shigellosis. The active site of TGT …
as a drug target for the treatment of the foodborne illness shigellosis. The active site of TGT …
How to Replace the Residual Solvation Shell of Polar Active Site Residues to Achieve Nanomolar Inhibition of tRNA‐Guanine Transglycosylase
T Ritschel, PC Kohler, G Neudert, A Heine… - …, 2009 - Wiley Online Library
In a computational and structural study, we investigated a series of 4‐substituted lin‐
benzoguanines that are potent inhibitors of tRNA‐guanine transglycosylase (TGT), a …
benzoguanines that are potent inhibitors of tRNA‐guanine transglycosylase (TGT), a …
Crystal Structure Analysis and in Silico pKa Calculations Suggest Strong pKa Shifts of Ligands as Driving Force for High‐Affinity Binding to TGT
T Ritschel, S Hoertner, A Heine, F Diederich… - …, 2009 - Wiley Online Library
Expanded lin‐benzoguanines exhibit binding affinities to tRNA‐guanine transglycosylase
(TGT) in the low‐nanomolar range. A significant pKa shift is observed for the inhibitors …
(TGT) in the low‐nanomolar range. A significant pKa shift is observed for the inhibitors …
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