FimH antagonists for the oral treatment of urinary tract infections: from design and synthesis to in vitro and in vivo evaluation
T Klein, D Abgottspon, M Wittwer… - Journal of medicinal …, 2010 - ACS Publications
… In all cases, the FimH antagonists were directly instilled into the … FimH antagonists exhibiting
appropriate pharmacokinetic properties for iv and oral treatment of urinary tract infections…
appropriate pharmacokinetic properties for iv and oral treatment of urinary tract infections…
In vivo Evaluation of FimH Antagonists–A Novel Class of Antimicrobials for the Treatment of Urinary Tract Infection
D Abgottspon, B Ernst - Chimia, 2012 - ojs.chimia.ch
… FimH antagonists for both prevention and treatment of UTIs in vivo. In addition, FimH
antagonists … Whereas in the initial treatment experiments[7,8] bacteria/antagonist mixtures were …
antagonists … Whereas in the initial treatment experiments[7,8] bacteria/antagonist mixtures were …
Rational design strategies for FimH antagonists: new drugs on the horizon for urinary tract infection and Crohn's disease
LK Mydock-McGrane, TJ Hannan… - Expert opinion on drug …, 2017 - Taylor & Francis
… FimH protein, containing only the carbohydrate recognition domain. FimH is immobilized and
FimH antagonists … that were infected ex vivo with LF82, with or without FimH antagonists. In …
FimH antagonists … that were infected ex vivo with LF82, with or without FimH antagonists. In …
Mannose-derived FimH antagonists: A promising anti-virulence therapeutic strategy for urinary tract infections and Crohn's disease
LK Mydock-McGrane, ZT Cusumano… - Expert opinion on …, 2016 - Taylor & Francis
… FimH antagonists disclosed in the patent literature. X-ray crystallographic binding studies of
D-mannose and early FimH antagonists … orally bioavailable FimH antagonists with promising …
D-mannose and early FimH antagonists … orally bioavailable FimH antagonists with promising …
Treatment and prevention of urinary tract infection with orally active FimH inhibitors
CK Cusumano, JS Pinkner, Z Han, SE Greene… - Science translational …, 2011 - science.org
… of orally active small-molecule FimH antagonists and demonstrate their potential for treating
… a resistant bacterial infection. Our mannoside compounds block the FimH-mediated binding …
… a resistant bacterial infection. Our mannoside compounds block the FimH-mediated binding …
Urinary tract infection: Which conformation of the bacterial lectin FimH is therapeutically relevant?
K Mayer, D Eris, O Schwardt, CP Sager… - Journal of medicinal …, 2017 - ACS Publications
… in binding affinity of FimH antagonists with FimH FL and FimH LD , respectively, we studied
the binding thermodynamics of the FimH antagonists 1 and 3p for both FimH proteins by …
the binding thermodynamics of the FimH antagonists 1 and 3p for both FimH proteins by …
Target selectivity of FimH antagonists
M Scharenberg, O Schwardt, S Rabbani… - Journal of medicinal …, 2012 - ACS Publications
… Mannose-based FimH antagonists are considered new therapeutics for the treatment of
urinary tract infections (UTIs). They prevent the adhesion of uropathogenic Escherichia coli (…
urinary tract infections (UTIs). They prevent the adhesion of uropathogenic Escherichia coli (…
Positively selected FimH residues enhance virulence during urinary tract infection by altering FimH conformation
DJ Schwartz, V Kalas, JS Pinkner… - Proceedings of the …, 2013 - National Acad Sciences
… We hypothesized that the fitness advantage of expressing FimH::A62/V163 over FimH::S62/A163
throughout infection was due to differences in the ability to bind mannosylated epitopes …
throughout infection was due to differences in the ability to bind mannosylated epitopes …
A FimH Inhibitor Prevents Acute Bladder Infection and Treats Chronic Cystitis Caused by Multidrug-Resistant Uropathogenic Escherichia coli ST131
… Escherichia coli ST131 causes acute urinary tract infection in female C3H/HeN mice. Scatter
plots of E. coli EC958 titers (colony-forming units [CFU]/organ) in bladders (A) and kidneys (…
plots of E. coli EC958 titers (colony-forming units [CFU]/organ) in bladders (A) and kidneys (…
Selective depletion of uropathogenic E. coli from the gut by a FimH antagonist
CN Spaulding, RD Klein, S Ruer, AL Kau, HL Schreiber… - Nature, 2017 - nature.com
Urinary tract infections (UTIs) caused by uropathogenic Escherichia coli (UPEC) affect 150
million people annually 1 , 2 . Despite effective antibiotic therapy, 30–50% of patients …
million people annually 1 , 2 . Despite effective antibiotic therapy, 30–50% of patients …
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