Anti-adhesive therapy for Crohn : mannose derivatives
AIEC can cause inflammation. Targeting bacterial adhesion of FimH-expressing bacteria appears to be a promising therapeutic approach, consisting of disarming bacteria without killing them, representing a selective strategy to suppress a potentially critical trigger of intestinal inflammation, without disrupting the gut microbiota.
A study of heptyl-mannoside (HM) anti-stick compounds that can block the attachment of invasive Escherichia coli bacteria associated with CD. HM compounds have a high affinity for FimH, which is an antagonist of FIMH, and the best compound has a Kd of 2.9 nM. HM compounds reduce AIEC levels in stool and in colonic and ileal mucosa after oral administration in animal models of CM. Signs of colitis and intestinal inflammation were also avoided. This promising therapeutic method involves "disarming" bacteria without killing them, representing a selective strategy to remove a potentially critical trigger of intestinal inflammation, without disrupting the gut microbiota.
IN VIVO - Preuve de concept
UMR 6230 - CEISAM
Equipe CORAIL Catalysis, ORganometallic chemistry And synthesIs of Ligands
EP : EP12305906 - filed on the 07-24-2012
WO - BE,BR,CA,CH,DE,FR,GB,IN,JP,KR,MX,US
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