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
… The mannose-binding pocket of FimH is … of FimH bound to α-d-mannose, and mannose
derivatives, called mannosides (37–39), were used to rationally design biphenyl FimH inhibitors …
derivatives, called mannosides (37–39), were used to rationally design biphenyl FimH inhibitors …
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 (…
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
… (39, 41, 42) Nonspecific interactions to the various mannose receptors by FimH inhibitors
would have a profound impact on these processes. We therefore determined the affinity of …
would have a profound impact on these processes. We therefore determined the affinity of …
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 …
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 …
Intervening with urinary tract infections using anti-adhesives based on the crystal structure of the FimH–oligomannose-3 complex
A Wellens, C Garofalo, H Nguyen, N Van Gerven… - PLoS one, 2008 - journals.plos.org
… We demonstrate that α-d-mannose based inhibitors of FimH not only block bacterial
adhesion on uroepithelial cells but also antagonize invasion and biofilm formation. Heptyl α-d-…
adhesion on uroepithelial cells but also antagonize invasion and biofilm formation. Heptyl α-d-…
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
… of urinary tract infections conducted with FimH antagonists. … with antibodies directed against
FimH, protected animals from … the inhibition of the initial host-pathogen interaction with FimH …
FimH, protected animals from … the inhibition of the initial host-pathogen interaction with FimH …
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
… effective FimH inhibitors. During this period, a variety of synthetic mannosides and naturally
occurring oligosaccharides isolates were further identified as inhibitors of the FimH lectin. …
occurring oligosaccharides isolates were further identified as inhibitors of the FimH lectin. …
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
… This consequently led to a new structural series of FimH inhibitors disclosed in a new
application[Citation47], with the most potent heterocyclic derivatives being thiophene urea …
application[Citation47], with the most potent heterocyclic derivatives being thiophene urea …
FimH and anti-adhesive therapeutics: a disarming strategy against uropathogens
… the uropathogens that allow the establishment of urinary tract infections (UTIs). As the antibiotic
… heterogeneities of different FimH variants, several FimH inhibitors have been developed …
… heterogeneities of different FimH variants, several FimH inhibitors have been developed …
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