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The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases.
Troisi J, Venutolo G, Terracciano C, Carri MD, Di Micco S, Landolfi A, Fasano A. Troisi J, et al. Curr Med Chem. 2021;28(28):5788-5807. doi: 10.2174/0929867328666210104110053. Curr Med Chem. 2021. PMID: 33397225 Review.
BACKGROUND: The involvement of intercellular tight junctions and, in particular, the modulation of their competency by the zonulin pathway with a subsequent increase in epithelial and endothelial permeability, has been described in several chronic and acute inflammatory diseases. …
BACKGROUND: The involvement of intercellular tight junctions and, in particular, the modulation of their competency by the zonulin pathway w …
Targeting endothelial tight junctions to predict and protect thoracic aortic aneurysm and dissection.
Yang X, Xu C, Yao F, Ding Q, Liu H, Luo C, Wang D, Huang J, Li Z, Shen Y, Yang W, Li Z, Yu F, Fu Y, Wang L, Ma Q, Zhu J, Xu F, Cong X, Kong W. Yang X, et al. Eur Heart J. 2023 Apr 7;44(14):1248-1261. doi: 10.1093/eurheartj/ehac823. Eur Heart J. 2023. PMID: 36638776 Free article.
Furthermore, the protease-activated receptor 2 inhibitor AT-1001, which seals TJs, alleviated the BAPN-induced impairment of endothelial TJ function and expression and subsequently reduced TAAD incidence. ...Mechanistically, vascular inflammation and edema were obse …
Furthermore, the protease-activated receptor 2 inhibitor AT-1001, which seals TJs, alleviated the BAPN-induced impairment of e …
Targeting zonulin and intestinal epithelial barrier function to prevent onset of arthritis.
Tajik N, Frech M, Schulz O, Schälter F, Lucas S, Azizov V, Dürholz K, Steffen F, Omata Y, Rings A, Bertog M, Rizzo A, Iljazovic A, Basic M, Kleyer A, Culemann S, Krönke G, Luo Y, Überla K, Gaipl US, Frey B, Strowig T, Sarter K, Bischoff SC, Wirtz S, Cañete JD, Ciccia F, Schett G, Zaiss MM. Tajik N, et al. Nat Commun. 2020 Apr 24;11(1):1995. doi: 10.1038/s41467-020-15831-7. Nat Commun. 2020. PMID: 32332732 Free PMC article.
Moreover, treatment with the zonulin antagonist larazotide acetate, which specifically increases intestinal barrier integrity, effectively reduces arthritis onset. ...
Moreover, treatment with the zonulin antagonist larazotide acetate, which specifically increases intestinal barrier integrity, …
Coeliac disease and the intestinal barrier: mechanisms of disruption and strategies for restoration.
Damianos JA, Bledsoe A, Camilleri M, Murray JA. Damianos JA, et al. Gut. 2026 Mar 6;75(4):826-838. doi: 10.1136/gutjnl-2025-335373. Gut. 2026. PMID: 40579122 Review.
We also review comprehensively the therapies targeting barrier integrity and normalising intestinal permeability, including particular diets and supplements, and experimental and improved medications including larazotide acetate and IMU-856. Finally, we highlight th …
We also review comprehensively the therapies targeting barrier integrity and normalising intestinal permeability, including particular diets …
AT-1001: a high-affinity alpha3beta4 nAChR ligand with novel nicotine-suppressive pharmacology.
Cippitelli A, Wu J, Gaiolini KA, Mercatelli D, Schoch J, Gorman M, Ramirez A, Ciccocioppo R, Khroyan TV, Yasuda D, Zaveri NT, Pascual C, Xie XS, Toll L. Cippitelli A, et al. Br J Pharmacol. 2015 Apr;172(7):1834-45. doi: 10.1111/bph.13034. Epub 2015 Jan 23. Br J Pharmacol. 2015. PMID: 25440006 Free PMC article.
The aim of this study was to investigate the mechanism of action underlying the nicotine-suppressive effects of AT-1001. EXPERIMENTAL APPROACH: Effects of AT-1001 were determined using in vitro assays and rat models of nicotine addiction, and compared …
The aim of this study was to investigate the mechanism of action underlying the nicotine-suppressive effects of AT-1001. EXPER …
Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials.
Hoilat GJ, Altowairqi AK, Ayas MF, Alhaddab NT, Alnujaidi RA, Alharbi HA, Alyahyawi N, Kamal A, Alhabeeb H, Albazee E, Almustanyir S, Abu-Zaid A. Hoilat GJ, et al. Clin Res Hepatol Gastroenterol. 2022 Jan;46(1):101782. doi: 10.1016/j.clinre.2021.101782. Epub 2021 Jul 31. Clin Res Hepatol Gastroenterol. 2022. PMID: 34339872
PURPOSE: The standard of care for treatment of celiac disease (CD) is a stringent lifetime gluten-free diet (GFD). Larazotide acetate (AT-1001) is an anti-zonulin which functions as a gut permeability regulator for treatment of CD. ...Other AEs were co …
PURPOSE: The standard of care for treatment of celiac disease (CD) is a stringent lifetime gluten-free diet (GFD). Larazotide acet …
AT-1001 Is a Partial Agonist with High Affinity and Selectivity at Human and Rat alpha3beta4 Nicotinic Cholinergic Receptors.
Tuan EW, Horti AG, Olson TT, Gao Y, Stockmeier CA, Al-Muhtasib N, Bowman Dalley C, Lewin AE, Wolfe BB, Sahibzada N, Xiao Y, Kellar KJ. Tuan EW, et al. Mol Pharmacol. 2015 Oct;88(4):640-9. doi: 10.1124/mol.115.099978. Epub 2015 Jul 10. Mol Pharmacol. 2015. PMID: 26162864 Free PMC article.
In patch-clamp electrophysiology studies, AT-1001 was a potent partial agonist with 65-70% efficacy at both human and rat alpha3beta4 nAChRs. ...Both alpha3beta4 and alpha4beta2 nAChRs are upregulated by exposure of cells to AT-1001 for 3 days. Similar …
In patch-clamp electrophysiology studies, AT-1001 was a potent partial agonist with 65-70% efficacy at both human and rat alph …
Functional characterization of AT-1001, an alpha3beta4 nicotinic acetylcholine receptor ligand, at human alpha3beta4 and alpha4beta2 nAChR.
Zaveri NT, Bertrand S, Yasuda D, Bertrand D. Zaveri NT, et al. Nicotine Tob Res. 2015 Mar;17(3):361-7. doi: 10.1093/ntr/ntu170. Epub 2014 Sep 1. Nicotine Tob Res. 2015. PMID: 25180076 Free PMC article.
METHODS: Two-electrode voltage clamp was used for functional characterization of AT-1001 at recombinant human alpha3beta4 and alpha4beta2 nAChR expressed in Xenopus oocytes. ...Pre- and co-application of various concentrations of AT-1001 with 50 …
METHODS: Two-electrode voltage clamp was used for functional characterization of AT-1001 at recombinant human alpha3bet …
New Therapeutic Challenges in Pediatric Gastroenterology: A Narrative Review.
Dipasquale V, Romano C. Dipasquale V, et al. Healthcare (Basel). 2025 Apr 17;13(8):923. doi: 10.3390/healthcare13080923. Healthcare (Basel). 2025. PMID: 40281872 Free PMC article. Review.
For CeD, therapies like gluten-degrading enzymes (latiglutenase, Kuma030) and zonulin inhibitors (larazotide acetate) show promise, though clinical outcomes are inconsistent. Immunotherapy and microbiota modulation, including probiotics and fecal microbiota transpla …
For CeD, therapies like gluten-degrading enzymes (latiglutenase, Kuma030) and zonulin inhibitors (larazotide acetate) show pro …
74 results