Literature DB >> 15043388

Fatty acid biosynthesis as a target for novel antibacterials.

Richard J Heath1, Charles O Rock.   

Abstract

The bacterial fatty acid synthesis pathway has significant potential as a target for the development of novel antibacterials. The pathway has been extensively studied in Escherichia coli, the crystal structures of the compounds involved are known and homologous genes are readily identified in the genomes of important pathogens. The currently used drugs triclosan and isoniazid are known to target one step in the pathway. Other experimental compounds such as thiolactomycin and cerulenin effectively inhibit other steps. These known pathway inhibitors are reviewed and the areas for potential future developments are explored.

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Year:  2004        PMID: 15043388      PMCID: PMC1618763     

Source DB:  PubMed          Journal:  Curr Opin Investig Drugs        ISSN: 1472-4472


  73 in total

1.  Overproduction of beta-ketoacyl-acyl carrier protein synthase I imparts thiolactomycin resistance to Escherichia coli K-12.

Authors:  J T Tsay; C O Rock; S Jackowski
Journal:  J Bacteriol       Date:  1992-01       Impact factor: 3.490

2.  Isolation and characterization of the beta-ketoacyl-acyl carrier protein synthase III gene (fabH) from Escherichia coli K-12.

Authors:  J T Tsay; W Oh; T J Larson; S Jackowski; C O Rock
Journal:  J Biol Chem       Date:  1992-04-05       Impact factor: 5.157

3.  Preparation and antibacterial activities of new 1,2,3-diazaborine derivatives and analogues.

Authors:  M A Grassberger; F Turnowsky; J Hildebrandt
Journal:  J Med Chem       Date:  1984-08       Impact factor: 7.446

4.  Thiolactomycin, a new antibiotic. I. Taxonomy of the producing organism, fermentation and biological properties.

Authors:  H Oishi; T Noto; H Sasaki; K Suzuki; T Hayashi; H Okazaki; K Ando; M Sawada
Journal:  J Antibiot (Tokyo)       Date:  1982-04       Impact factor: 2.649

5.  Thiolactomycin, a new antibiotic. IV. Biological properties and chemotherapeutic activity in mice.

Authors:  S Miyakawa; K Suzuki; T Noto; Y Harada; H Okazaki
Journal:  J Antibiot (Tokyo)       Date:  1982-04       Impact factor: 2.649

6.  Thiolactomycin, a new antibiotic. III. In vitro antibacterial activity.

Authors:  T Noto; S Miyakawa; H Oishi; H Endo; H Okazaki
Journal:  J Antibiot (Tokyo)       Date:  1982-04       Impact factor: 2.649

7.  Effect of a diazaborine derivative (Sa 84.474) on the virulence of Escherichia coli.

Authors:  C Lam; F Turnowsky; G Högenauer; E Schütze
Journal:  J Antimicrob Chemother       Date:  1987-07       Impact factor: 5.790

8.  Acetoacetyl-acyl carrier protein synthase, a potential regulator of fatty acid biosynthesis in bacteria.

Authors:  S Jackowski; C O Rock
Journal:  J Biol Chem       Date:  1987-06-05       Impact factor: 5.157

9.  Mechanism of action of the antibiotic thiolactomycin inhibition of fatty acid synthesis of Escherichia coli.

Authors:  T Hayashi; O Yamamoto; H Sasaki; A Kawaguchi; H Okazaki
Journal:  Biochem Biophys Res Commun       Date:  1983-09-30       Impact factor: 3.575

10.  envM genes of Salmonella typhimurium and Escherichia coli.

Authors:  F Turnowsky; K Fuchs; C Jeschek; G Högenauer
Journal:  J Bacteriol       Date:  1989-12       Impact factor: 3.490

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  43 in total

1.  Structure-activity relationships at the 5-position of thiolactomycin: an intact (5R)-isoprene unit is required for activity against the condensing enzymes from Mycobacterium tuberculosis and Escherichia coli.

Authors:  Pilho Kim; Yong-Mei Zhang; Gautham Shenoy; Quynh-Anh Nguyen; Helena I Boshoff; Ujjini H Manjunatha; Michael B Goodwin; John Lonsdale; Allen C Price; Darcie J Miller; Ken Duncan; Stephen W White; Charles O Rock; Clifton E Barry; Cynthia S Dowd
Journal:  J Med Chem       Date:  2006-01-12       Impact factor: 7.446

Review 2.  The reductase steps of the type II fatty acid synthase as antimicrobial targets.

Authors:  Yong-Mei Zhang; Ying-Jie Lu; Charles O Rock
Journal:  Lipids       Date:  2004-11       Impact factor: 1.880

3.  Discovery of FabH/FabF inhibitors from natural products.

Authors:  Katherine Young; Hiranthi Jayasuriya; John G Ondeyka; Kithsiri Herath; Chaowei Zhang; Srinivas Kodali; Andrew Galgoci; Ronald Painter; Vickie Brown-Driver; Robert Yamamoto; Lynn L Silver; Yingcong Zheng; Judith I Ventura; Janet Sigmund; Sookhee Ha; Angela Basilio; Francisca Vicente; José Rubén Tormo; Fernando Pelaez; Phil Youngman; Doris Cully; John F Barrett; Dennis Schmatz; Sheo B Singh; Jun Wang
Journal:  Antimicrob Agents Chemother       Date:  2006-02       Impact factor: 5.191

Review 4.  Recent advances in the chemistry and biology of naturally occurring antibiotics.

Authors:  K C Nicolaou; Jason S Chen; David J Edmonds; Anthony A Estrada
Journal:  Angew Chem Int Ed Engl       Date:  2009       Impact factor: 15.336

5.  Molecular dynamics and docking simulations as a proof of high flexibility in E. coli FabH and its relevance for accurate inhibitor modeling.

Authors:  Yunierkis Pérez-Castillo; Matheus Froeyen; Miguel Angel Cabrera-Pérez; Ann Nowé
Journal:  J Comput Aided Mol Des       Date:  2011-04-23       Impact factor: 3.686

6.  Toward the computer-aided discovery of FabH inhibitors. Do predictive QSAR models ensure high quality virtual screening performance?

Authors:  Yunierkis Pérez-Castillo; Maykel Cruz-Monteagudo; Cosmin Lazar; Jonatan Taminau; Mathy Froeyen; Miguel Angel Cabrera-Pérez; Ann Nowé
Journal:  Mol Divers       Date:  2014-03-27       Impact factor: 2.943

7.  Slow onset inhibition of bacterial beta-ketoacyl-acyl carrier protein synthases by thiolactomycin.

Authors:  Carl A Machutta; Gopal R Bommineni; Sylvia R Luckner; Kanishk Kapilashrami; Bela Ruzsicska; Carlos Simmerling; Caroline Kisker; Peter J Tonge
Journal:  J Biol Chem       Date:  2009-12-16       Impact factor: 5.157

8.  Elucidating the structural basis of diphenyl ether derivatives as highly potent enoyl-ACP reductase inhibitors through molecular dynamics simulations and 3D-QSAR study.

Authors:  Pharit Kamsri; Auradee Punkvang; Patchareenart Saparpakorn; Supa Hannongbua; Stephan Irle; Pornpan Pungpo
Journal:  J Mol Model       Date:  2014-06-17       Impact factor: 1.810

9.  Mechanism and inhibition of the FabV enoyl-ACP reductase from Burkholderia mallei.

Authors:  Hao Lu; Peter J Tonge
Journal:  Biochemistry       Date:  2010-02-16       Impact factor: 3.162

10.  Selectivity of Pyridone- and Diphenyl Ether-Based Inhibitors for the Yersinia pestis FabV Enoyl-ACP Reductase.

Authors:  Carla Neckles; Annica Pschibul; Cheng-Tsung Lai; Maria Hirschbeck; Jochen Kuper; Shabnam Davoodi; Junjie Zou; Nina Liu; Pan Pan; Sonam Shah; Fereidoon Daryaee; Gopal R Bommineni; Cristina Lai; Carlos Simmerling; Caroline Kisker; Peter J Tonge
Journal:  Biochemistry       Date:  2016-05-17       Impact factor: 3.162

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