Hydroxyl groups in synthetic and natural-product-derived therapeutics: a perspective on a common functional group

J Cramer, CP Sager, B Ernst - Journal of medicinal chemistry, 2019 - ACS Publications
By forming extended hydrogen-bond networks, the contribution of hydroxyl groups to affinity
can reach several orders of magnitude. However, because of the high directionality of their …

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 …

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 …

Antivirulence C-Mannosides as Antibiotic-Sparing, Oral Therapeutics for Urinary Tract Infections

L Mydock-McGrane, Z Cusumano, Z Han… - Journal of medicinal …, 2016 - ACS Publications
Gram-negative uropathogenic Escherichia coli (UPEC) bacteria are a causative pathogen of
urinary tract infections (UTIs). Previously developed antivirulence inhibitors of the type 1 …

[HTML][HTML] Pathoblockers or antivirulence drugs as a new option for the treatment of bacterial infections

MB Calvert, VR Jumde, A Titz - Beilstein journal of organic …, 2018 - beilstein-journals.org
The rapid development of antimicrobial resistance is threatening mankind to such an extent
that the World Health Organization expects more deaths from infections than from cancer in …

Small carbohydrate derivatives as potent antibiofilm agents

K Singh, SS Kulkarni - Journal of Medicinal Chemistry, 2022 - ACS Publications
Biofilm formation by most pathogenic bacteria is considered as one of the key mechanisms
associated with virulence and antibiotic resistance. Biofilm-forming bacteria adhere to the …

Antivirulence isoquinolone mannosides: optimization of the biaryl aglycone for FimH lectin binding affinity and efficacy in the treatment of chronic UTI

C Jarvis, Z Han, V Kalas, R Klein, JS Pinkner… - …, 2016 - Wiley Online Library
Uropathogenic E. coli (UPEC) employ the mannose‐binding adhesin FimH to colonize the
bladder epithelium during urinary tract infection (UTI). Previously reported FimH antagonists …

Structural and functional characterization of the FimH adhesin of uropathogenic Escherichia coli and its novel applications

N Foroogh, M Rezvan, K Ahmad, S Mahmood - Microbial pathogenesis, 2021 - Elsevier
Type 1 fimbriae are responsible for bacterial pathogenicity and biofilm production, which are
important virulence factors in uropathogenic Escherichia coli strains. Many articles are …

Glycoconjugates and glycomimetics as microbial anti-adhesives

S Sattin, A Bernardi - Trends in Biotechnology, 2016 - cell.com
Microbial adhesion is an essential step in infection and is mediated primarily by protein–
carbohydrate interactions. Antagonists of such interactions have become a promising target …

[HTML][HTML] Applying molecular modeling to predict Novel FmlH-binding glycomimetics with improved pharmacokinetic properties for the prevention of urinary tract …

P Samanta, RJ Doerksen - Applied Sciences, 2024 - mdpi.com
Urinary tract infections (UTIs) affect nearly 50% of women in their lifetime. Uropathogenic
Escherichia coli (UPEC) expresses F9/Fml pili tipped with the protein FmlH that specifically …