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Expert Opinion on Drug Discovery Volume 12, 2017 - Issue 7
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Review

Rational design strategies for FimH antagonists: new drugs on the horizon for urinary tract infection and Crohn’s disease

Laurel K. Mydock-McGraneFimbrion Therapeutics, Inc., Saint Louis, MO, USAView further author information
,
Thomas J. HannanFimbrion Therapeutics, Inc., Saint Louis, MO, USAView further author information
&
James W. JanetkaDepartment of Biochemistry and Molecular Biophysics, Washington University School of Medicine, Saint Louis, MO, USACorrespondence[email protected]
View further author information
Pages 711-731 | Received 07 Mar 2017, Accepted 12 May 2017, Published online: 02 Jun 2017

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Parker R M Kenee, Alana L Christie & Philippe E Zimmern. (2022) Cranberry Supplement, D-Mannose, and Other OTC Modalities for Prevention of Recurrent UTI in Women Post-Electrofulguration. International Journal of Women's Health 14, pages 643-653.
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Vishnu C. Damalanka, Amarendar Reddy Maddirala & James W. Janetka. (2021) Novel approaches to glycomimetic design: development of small molecular weight lectin antagonists. Expert Opinion on Drug Discovery 16:5, pages 513-536.
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Wael Elhenawy, Alexander Oberc & Brian K. Coombes. (2018) A polymicrobial view of disease potential in Crohn's-associated adherent-invasive E. coli. Gut Microbes 9:2, pages 166-174.
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Meysam Sarshar, Payam Behzadi, Cecilia Ambrosi, Carlo Zagaglia, Anna Teresa Palamara & Daniela Scribano. (2020) FimH and Anti-Adhesive Therapeutics: A Disarming Strategy Against Uropathogens. Antibiotics 9:7, pages 397.
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Hongjin Chen, Haixia Xu, Lijiao Luo, Lichao Qiao, Yaohui Wang, Minmin Xu, Youran Li, Ping Zhu & Bolin Yang. (2019) Thalidomide Prevented and Ameliorated Pathogenesis of Crohn’s Disease in Mice via Regulation of Inflammatory Response and Fibrosis. Frontiers in Pharmacology 10.
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Joscha Meiers, Eike Siebs, Eva Zahorska & Alexander Titz. (2019) Lectin antagonists in infection, immunity, and inflammation. Current Opinion in Chemical Biology 53, pages 51-67.
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Shabnam Sarshar Beydokhti, Christoph Stork, Ulrich Dobrindt & Andreas Hensel. (2019) Orthosipon stamineus extract exerts inhibition of bacterial adhesion and chaperon-usher system of uropathogenic Escherichia coli—a transcriptomic study. Applied Microbiology and Biotechnology 103:20, pages 8571-8584.
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Kevin S. Currie, Leena Patel & Kassandra F. Sedillo. (2019) Small-molecule agents for the treatment of inflammatory bowel disease. Bioorganic & Medicinal Chemistry Letters 29:16, pages 2034-2041.
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Colin W. Russell, Rashmi Sukumaran, Lu Ting Liow, Balamurugan Periaswamy, Shazmina Rafee, Yuemin C. Chee & Swaine L. Chen. (2019) Comprehensive Identification of Fim-Mediated Inversions in Uropathogenic Escherichia coli with Structural Variation Detection Using Relative Entropy. mSphere 4:2.
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Rosana Ribić, Tomislav Meštrović, Marijana Neuberg & Goran Kozina. (2019) Proposed dual antagonist approach for the prevention and treatment of urinary tract infections caused by uropathogenic Escherichia coli. Medical Hypotheses 124, pages 17-20.
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Kaylen O’Rourke & Peter A. Cadieux. 2019. The Role of Bacteria in Urology. The Role of Bacteria in Urology 23 39 .
Néha Sihra, Anna Goodman, Rhana Zakri, Arun Sahai & Sachin Malde. (2018) Nonantibiotic prevention and management of recurrent urinary tract infection. Nature Reviews Urology 15:12, pages 750-776.
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Matthew B Calvert, Varsha R Jumde & Alexander Titz. (2018) Pathoblockers or antivirulence drugs as a new option for the treatment of bacterial infections. Beilstein Journal of Organic Chemistry 14, pages 2607-2617.
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Crossref
Patrick Di Martino. (2018) Bacterial adherence: much more than a bond. AIMS Microbiology 4:3, pages 563-566.
Crossref

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