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 …

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) …

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 …

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 …

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 …

Fragments as Novel Starting Points for tRNA‐Guanine Transglycosylase Inhibitors Found by Alternative Screening Strategies

E Hassaan, PO Eriksson, S Geschwindner… - …, 2020 - Wiley Online Library
Crystallography provides structural information crucial for fragment optimization, however
several criteria must be met to screen directly on protein crystals as soakable, well …

Crystallographic study of inhibitors of tRNA-guanine transglycosylase suggests a new structure-based pharmacophore for virtual screening

R Brenk, EA Meyer, K Reuter, MT Stubbs… - Journal of molecular …, 2004 - Elsevier
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 …

A new target for shigellosis: rational design and crystallographic studies of inhibitors of tRNA-guanine transglycosylase

U Grädler, HD Gerber… - Journal of Molecular …, 2001 - Elsevier
Eubacterial tRNA-guanine transglycosylase (TGT) is involved in the hyper-modification of
cognate tRNAs leading to the exchange of G34 at the wobble position in the anticodon loop …

Virtual screening for submicromolar leads of tRNA-guanine transglycosylase based on a new unexpected binding mode detected by crystal structure analysis

R Brenk, L Naerum, U Grädler, HD Gerber… - Journal of medicinal …, 2003 - ACS Publications
Eubacterial tRNA-guanine transglycosylase (TGT) is involved in the hypermodification of
cognate tRNAs, leading to the exchange of G34 by preQ1 at the wobble position in the …

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 …