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Flannigan, K. L.

Publications and source records attributed to Flannigan, K. L..

3 recordsLinked to original sources

Mycobacterium avium subspecies paratuberculosis targets M cells in enteroid-derived monolayers through interactions with β1 integrins

Paratuberculosis is a global infectious disease caused by the bacterium, Mycobacterium avium subspecies paratuberculosis (MAP). MAP infection of ruminants triggers progressive wasting disease characterized by granulomatous lymphadenitis, enteritis, and severe intestinal pathology that often requires early culling of the animal. The resulting economic burden is significant and MAP exposure in the workplace constitutes a significant zoonotic risk. While it has been established the MAP propagates within resident intestinal immune cells, including macrophages and dendritic cells, significantly less is known about how it attaches, enters and traverses the epithelium. The current paradigm suggests MAP infects the small intestinal epithelium by targeting both enterocytes and M cells, with a potential tropism for the latter. In the current study, we employed emerging enteroid technology to identify the target cells for MAPs entry into the small intestinal epithelium. We generated mouse enteroid-derived monolayers with functional M cells capable of transcytosis. Upon exposure to MAP, the bacteria were detected within both enterocytes and M cells. Following quantification, it was apparent that MAP exhibited tropism for M cells. Complementary studies using the Caco-2/Raji-B co-culture system provided similar results, wherein MAP was found primarily in cells expressing functional M cell markers. Since other mycobacteria have been shown to initiate cell attachment and entry by using a fibronectin-bridging process, we tested whether these interactions were involved in MAPs targeting of M cells. We found that MAPs M cell tropism was significantly enhanced in the presence of fibronectin and that this effect was abolished when monolayers were pretreated with an integrin-blocking peptide. Taken together, our data indicate the MAP preferentially targets M cells and that this process involves a fibronectin-bridging process. Furthermore, our data suggest that targeting M cell-associated integrins could provide a mechanism to reduce MAP infection and transmission within livestock herds. Author SummaryIn the current study, we sought to determine the target cell for Mycobacterium avium subspecies paratuberculosis (MAP), which is the causative agent of Johnes disease (JD, also termed paratuberculosis) in ruminants. While MAP primarily infects domestic ruminants including cattle, sheep, goats, and deer, it has also been shown to infect wildlife throughout the world, including cats, rabbits, badgers, and wood mice. Given the significant economic burden of MAP infections in livestock, its role in the pathogenesis of JD has been the focus of much research. However, the broad diversity of MAP-susceptible hosts and reservoirs observed calls into question the true scope of MAP infection and transmission and the true number of susceptible hosts. Furthermore, MAP constitutes a zoonotic threat that some have linked to intestinal pathologies, including Crohns disease. To date, it is still not known exactly how MAP attaches, enters and traverses the small intestinal epithelium to eventually propagate within resident macrophages and dendritic cells to cause eventual disease. To address this question, we developed a model of the small intestinal epithelium, from mouse enteroids, that contained functional M cells. We found that MAP selectivity enters M cells and that this involves fibronectin-bridging process that targets M cell-associated {beta}1-integrins.

cell biology↗

Targeting the Pregnane X Receptor Using Microbial Metabolite Mimicry

The human pregnane X receptor (PXR), a master regulator of drug metabolism, has important roles in intestinal homeostasis and abrogating inflammation. Existing PXR ligands have substantial off-target toxicity. Based on prior work that established microbial (indole) metabolites as PXR ligands, we proposed microbial metabolite mimicry as a novel strategy for drug discovery that allows to exploit previously unexplored parts of chemical space. Here we report functionalized indole-derivatives as first-in-class non-cytotoxic PXR agonists, as a proof-of-concept for microbial metabolite mimicry. The lead compound, FKK6, binds directly to PXR protein in solution, induces PXR specific target gene expression in, cells, human organoids, and mice. FKK6 significantly represses pro-inflammatory cytokine production cells and abrogates inflammation in mice expressing the human PXR gene. The development of FKK6 demonstrates for the first time that microbial metabolite mimicry is a viable strategy for drug discovery and opens the door to mine underexploited regions of chemical space.

biochemistry↗

Vancomycin Relieves Mycophenolate Mofetil-Induced Gastrointestinal Toxicity by Eliminating Gut Bacterial β-Glucuronidase Activity

Mycophenolate mofetil (MMF) is commonly prescribed after transplantation and has proven advantages over other immunosuppressive drugs but gastrointestinal (GI) side effects frequently limit its use. The pathways involved in the metabolism of the prodrug MMF and the bioactive derivative mycophenolic acid (MPA) are well characterized but the mechanism responsible for toxicity is unknown. Here we extend our previous observation that an intact gut microbiome is required for MMF-induced toxicity and demonstrate that gut bacterial metabolism is responsible for the GI inflammation and weight loss associated with MMF exposure. In mice consuming MMF, the introduction of vancomycin alone was sufficient to prevent or reverse MMF-induced weight loss and colonic inflammation. MMF induced the expansion of bacteria expressing {beta}-glucuronidase (GUS) in the cecum and proximal colon. GUS activity, which is responsible for the catabolism of glucuronidated MPA (MPAG) to free MPA, was increased in the presence of MMF and eliminated by vancomycin. Vancomycin eliminated multiple Bacteroides spp. that flourished in the presence of MMF and prevented the breakdown of MPAG without negatively affecting serum MPA levels. Human data suggests that increased stool GUS activity can be associated with MMF-related toxicity. Our work provides a mechanism for the GI toxicity associated with MMF and a future direction for the development of therapeutics.

microbiology↗