FimH and anti-adhesive therapeutics: a disarming strategy against uropathogens

M Sarshar, P Behzadi, C Ambrosi, C Zagaglia… - Antibiotics, 2020 - mdpi.com
Chaperone-usher fimbrial adhesins are powerful weapons against the uropathogens that
allow the establishment of urinary tract infections (UTIs). As the antibiotic therapeutic …

Antiadhesion Therapy for Urinary Tract Infections A Balanced PK/PD Profile Proved To Be Key for Success

X Jiang, D Abgottspon, S Kleeb… - Journal of medicinal …, 2012 - ACS Publications
The initial step for the successful establishment of urinary tract infections (UTIs),
predominantly caused by uropathogenic Escherichia coli, is the adhesion of bacteria to …

FimH Antagonists: Structure–Activity and Structure–Property Relationships for Biphenyl α‐D‐Mannopyranosides

L Pang, S Kleeb, K Lemme, S Rabbani… - …, 2012 - Wiley Online Library
Urinary tract infections (UTIs) are caused primarily by uropathogenic Escherichia coli
(UPEC), which encode filamentous surface‐adhesive organelles called type 1 pili. FimH is …

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
ABSTRACT Introduction: The bacterial adhesin FimH is a virulence factor and an attractive
therapeutic target for urinary tract infection (UTI) and Crohn's Disease (CD). Located on type …

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
Background Escherichia coli strains adhere to the normally sterile human uroepithelium
using type 1 pili, that are long, hairy surface organelles exposing a mannose-binding FimH …

FimH antagonists: bioisosteres to improve the in vitro and in vivo PK/PD profile

S Kleeb, L Pang, K Mayer, D Eris, A Sigl, RC Preston… - 2015 - ACS Publications
Urinary tract infections (UTIs), predominantly caused by uropathogenic Escherichia coli
(UPEC), belong to the most prevalent infectious diseases worldwide. The attachment of …

The tyrosine gate as a potential entropic lever in the receptor-binding site of the bacterial adhesin FimH

A Wellens, M Lahmann, M Touaibia, J Vaucher… - Biochemistry, 2012 - ACS Publications
Uropathogenic Escherichia coli (UPEC) are the major causative agents of urinary tract
infections. During infection, UPEC adhere to mannosylated glycoreceptors on the urothelium …

Structure-based drug design and optimization of mannoside bacterial FimH antagonists

Z Han, JS Pinkner, B Ford, R Obermann… - Journal of medicinal …, 2010 - ACS Publications
FimH-mediated cellular adhesion to mannosylated proteins is critical in the ability of
uropathogenic E. coli (UPEC) to colonize and invade the bladder epithelium during urinary …

Binding of the bacterial adhesin FimH to its natural, multivalent high-mannose type glycan targets

MM Sauer, RP Jakob, T Luber… - Journal of the …, 2018 - ACS Publications
Multivalent carbohydrate–lectin interactions at host–pathogen interfaces play a crucial role
in the establishment of infections. Although competitive antagonists that prevent pathogen …

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
Introduction: Type 1 pili are utilized by Gram-negative bacteria to adhere to host tissue and
thus are a key virulence factor in urinary tract infections (UTIs) and Crohn's disease (CD) …