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Research ArticleArticle

Discovery of a Quorum-Sensing Inhibitor of Drug-Resistant Staphylococcal Infections by Structure-Based Virtual Screening

Madanahally D. Kiran, Nallini Vijayarangan Adikesavan, Oscar Cirioni, Andrea Giacometti, Carmela Silvestri, Giorgio Scalise, Roberto Ghiselli, Vittorio Saba, Fiorenza Orlando, Menachem Shoham and Naomi Balaban
Molecular Pharmacology May 2008, 73 (5) 1578-1586; DOI: https://doi.org/10.1124/mol.107.044164
Madanahally D. Kiran
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Nallini Vijayarangan Adikesavan
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Oscar Cirioni
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Andrea Giacometti
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Carmela Silvestri
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Giorgio Scalise
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Roberto Ghiselli
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Vittorio Saba
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Fiorenza Orlando
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Menachem Shoham
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Naomi Balaban
Department of Biomedical Sciences, Cummings School of Veterinary Medicine, Tufts University, North Grafton, Massachusetts (M.D.K., N.B.); Department of Biochemistry, Case Western Reserve University, Cleveland, Ohio (N.V.A., M.S.); Institute of Infectious Diseases and Public Health, University of Ancona, Ancona, Italy (O.C., A.G., C.S., G.S.); Department of General Surgery, Instituto Nazionale Riposo e Cura Anziani/Instituto de Ricovero e Cura a Carattere Scientifico (INRCA IRRCS), University of Ancona, Ancona, Italy (R.G., V.S.); and Experimental Animal Models for Aging Units, Research Department, INRCA IRRCS, Ancona, Italy (F.O.)
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Abstract

Staphylococci are a major health threat because of increasing resistance to antibiotics. An alternative to antibiotic treatment is preventing virulence by inhibition of bacterial cell-to-cell communication using the quorum-sensing inhibitor RNAIII-inhibiting peptide (RIP). In this work, we identified 2′,5-di-O-galloyl-d-hamamelose (hamamelitannin) as a nonpeptide analog of RIP by virtual screening of a RIP-based pharmacophore against a database of commercially available small-molecule compounds. Hamamelitannin is a natural product found in the bark of Hamamelis virginiana (witch hazel), and it has no effect on staphylococcal growth in vitro; but like RIP, it does inhibit the quorum-sensing regulator RNAIII. In a rat graft model, hamamelitannin prevented device-associated infections in vivo, including infections caused by methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis strains. These findings suggest that hamamelitannin may be used as a suppressor to staphylococcal infections.

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Molecular Pharmacology: 73 (5)
Molecular Pharmacology
Vol. 73, Issue 5
1 May 2008
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Research ArticleArticle

Discovery of a Quorum-Sensing Inhibitor of Drug-Resistant Staphylococcal Infections by Structure-Based Virtual Screening

Madanahally D. Kiran, Nallini Vijayarangan Adikesavan, Oscar Cirioni, Andrea Giacometti, Carmela Silvestri, Giorgio Scalise, Roberto Ghiselli, Vittorio Saba, Fiorenza Orlando, Menachem Shoham and Naomi Balaban
Molecular Pharmacology May 1, 2008, 73 (5) 1578-1586; DOI: https://doi.org/10.1124/mol.107.044164

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Research ArticleArticle

Discovery of a Quorum-Sensing Inhibitor of Drug-Resistant Staphylococcal Infections by Structure-Based Virtual Screening

Madanahally D. Kiran, Nallini Vijayarangan Adikesavan, Oscar Cirioni, Andrea Giacometti, Carmela Silvestri, Giorgio Scalise, Roberto Ghiselli, Vittorio Saba, Fiorenza Orlando, Menachem Shoham and Naomi Balaban
Molecular Pharmacology May 1, 2008, 73 (5) 1578-1586; DOI: https://doi.org/10.1124/mol.107.044164
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