Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0022104 (
irritable bowel syndrome
)
8,033
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The serotonin receptor 4b (5-
HTR
4b
) is expressed throughout the gastrointestinal tract, and its agonists are used in the treatment of
irritable bowel syndrome
with constipation (IBS-C). Today, there are no rapid assays for the identification of 5-
HTR
4b
agonists. Here, we developed a luciferase-based 5-
HTR
4b
assay capable of assessing one compound per second with a 38-fold dynamic range and nM limit of detection for serotonin. We used the assay to screen more than 1000 natural products and anti-infection agents and identified five new 5-
HTR
4b
ligands: hordenine, halofuginone, proflavine, ethacridine, and revaprazan. We demonstrate that hordenine (antibiofilm), halofuginone (antiparasitic), and revaprazan (gastric acid reducer) activate 5-
HTR
4b
in human colon epithelial cells, leading to increased cell motility or wound healing. The 5-
HTR
4b
assay can be used to screen larger pharmaceutical libraries to identify novel treatments for
IBS
-C. This work shows that antimicrobials interact not only with the gut microbiota, but also with the human host.
...
PMID:Identification of Three Antimicrobials Activating Serotonin Receptor 4 in Colon Cells. 3171 51
