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Larazotide acetate: a pharmacological peptide approach to tight junction regulation.
Slifer ZM, Krishnan BR, Madan J, Blikslager AT. Slifer ZM, et al. Am J Physiol Gastrointest Liver Physiol. 2021 Jun 1;320(6):G983-G989. doi: 10.1152/ajpgi.00386.2020. Epub 2021 Apr 21. Am J Physiol Gastrointest Liver Physiol. 2021. PMID: 33881350 Free PMC article. Review.
Larazotide acetate (LA) is a single-chain peptide of eight amino acids that acts as a tight junction regulator to restore intestinal barrier function. ...Small (rodent) and large (porcine) animal studies have been conducted that demonstrate the importance of LA as a …
Larazotide acetate (LA) is a single-chain peptide of eight amino acids that acts as a tight junction regulator to restore inte …
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.
Here, we identify intestinal barrier integrity as an important checkpoint in translating autoimmunity to inflammation. Zonulin family peptide (zonulin), a potent regulator for intestinal tight junctions, is highly expressed in autoimmune mice and humans and can be used to …
Here, we identify intestinal barrier integrity as an important checkpoint in translating autoimmunity to inflammation. Zonulin family pep …
Peptide Derivatives of the Zonulin Inhibitor Larazotide (AT1001) as Potential Anti SARS-CoV-2: Molecular Modelling, Synthesis and Bioactivity Evaluation.
Di Micco S, Musella S, Sala M, Scala MC, Andrei G, Snoeck R, Bifulco G, Campiglia P, Fasano A. Di Micco S, et al. Int J Mol Sci. 2021 Aug 30;22(17):9427. doi: 10.3390/ijms22179427. Int J Mol Sci. 2021. PMID: 34502335 Free PMC article.
Recently, we adopted the drug repurposing as appropriate strategy to give fast response to global COVID-19 epidemic, by demonstrating that the zonulin octapeptide inhibitor AT1001 (Larazotide acetate) binds M(pro) catalytic domain. Thus, in the present study we tried to in …
Recently, we adopted the drug repurposing as appropriate strategy to give fast response to global COVID-19 epidemic, by demonstrating that t …
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.
This review explores the evidence for increased permeability in coeliac disease and the underlying mechanisms, including the roles of zonulin, inflammatory cytokines, microbial alterations and immune responses to gliadin peptides. We also review comprehensively the therapi …
This review explores the evidence for increased permeability in coeliac disease and the underlying mechanisms, including the roles of zonuli …
Antibacterial hyaluronic acid hydrogel with sustained release of larazotide as effective colitis treatment.
Yu F, Chen Y, Ouyang S, Tong B, Jiang Z, Wang J, Ding B, Mao K, Wu W, Xu H. Yu F, et al. J Control Release. 2025 Nov 10;387:114205. doi: 10.1016/j.jconrel.2025.114205. Epub 2025 Sep 5. J Control Release. 2025. PMID: 40915363
Herein, inspired by natural gut mucus, a dual-crosslinked hydrogel (HSMP-LA) composed of thiol/maleimide-modified hyaluronic acid together with co-loading of antimicrobial epsilon-polylysine (epsilon-PL) and larazotide acetate (LA) had been developed as an injectable artif …
Herein, inspired by natural gut mucus, a dual-crosslinked hydrogel (HSMP-LA) composed of thiol/maleimide-modified hyaluronic acid together w …
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 …
Nondietary Therapies for Celiac Disease.
Serena G, Kelly CP, Fasano A. Serena G, et al. Gastroenterol Clin North Am. 2019 Mar;48(1):145-163. doi: 10.1016/j.gtc.2018.09.011. Epub 2018 Dec 13. Gastroenterol Clin North Am. 2019. PMID: 30711207 Review.
Larazotide acetate in patients with coeliac disease undergoing a gluten challenge: a randomised placebo-controlled study.
Kelly CP, Green PH, Murray JA, Dimarino A, Colatrella A, Leffler DA, Alexander T, Arsenescu R, Leon F, Jiang JG, Arterburn LA, Paterson BM, Fedorak RN; Larazotide Acetate Celiac Disease Study Group. Kelly CP, et al. Aliment Pharmacol Ther. 2013 Jan;37(2):252-62. doi: 10.1111/apt.12147. Epub 2012 Nov 19. Aliment Pharmacol Ther. 2013. PMID: 23163616 Clinical Trial.
BACKGROUND: Coeliac disease, an autoimmune disorder triggered by gluten ingestion, is managed by a gluten-free diet (GFD), which is difficult for many patients. Larazotide acetate is a first-in-class oral peptide that prevents tight junction opening, and may reduce …
BACKGROUND: Coeliac disease, an autoimmune disorder triggered by gluten ingestion, is managed by a gluten-free diet (GFD), which is difficul …
Larazotide acetate promotes tight junction assembly in epithelial cells.
Gopalakrishnan S, Tripathi A, Tamiz AP, Alkan SS, Pandey NB. Gopalakrishnan S, et al. Peptides. 2012 May;35(1):95-101. doi: 10.1016/j.peptides.2012.02.016. Epub 2012 Feb 28. Peptides. 2012. PMID: 22401910
TJ formation is dependent on E-cadherin-mediated cell-cell adhesion and actin rearrangement, and is regulated by the Rho family GTPase and aPKC signaling pathways. Larazotide acetate, an 8-mer peptide and TJ modulator, inhibits TJ disassembly and dysfunction caused …
TJ formation is dependent on E-cadherin-mediated cell-cell adhesion and actin rearrangement, and is regulated by the Rho family GTPase and a …
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. ...
PURPOSE: The standard of care for treatment of celiac disease (CD) is a stringent lifetime gluten-free diet (GFD). Larazotide acetate …
64 results