The MUT056399 inhibitor of FabI is a new antistaphylococcal compound.

PubWeight™: 1.21‹?› | Rank: Top 10%

🔗 View Article (PMC 3186954)

Published in Antimicrob Agents Chemother on August 08, 2011

Authors

S Escaich1, L Prouvensier, M Saccomani, L Durant, M Oxoby, V Gerusz, F Moreau, V Vongsouthi, Kirsty Maher, Ian Morrissey, C Soulama-Mouze

Author Affiliations

1: FAB Pharma, 14, avenue de l'Opéra, 75001 Paris, France. sonia.escaich@fabpharma.com

Articles citing this

Antimicrobial resistance in Neisseria gonorrhoeae in the 21st century: past, evolution, and future. Clin Microbiol Rev (2014) 2.45

Bacterial lipids: metabolism and membrane homeostasis. Prog Lipid Res (2013) 1.42

Current and future antimicrobial treatment of gonorrhoea - the rapidly evolving Neisseria gonorrhoeae continues to challenge. BMC Infect Dis (2015) 1.27

Staphylococcus aureus FabI: inhibition, substrate recognition, and potential implications for in vivo essentiality. Structure (2012) 1.22

Perturbation of Staphylococcus aureus gene expression by the enoyl-acyl carrier protein reductase inhibitor AFN-1252. Antimicrob Agents Chemother (2013) 1.06

Rational optimization of drug-target residence time: insights from inhibitor binding to the Staphylococcus aureus FabI enzyme-product complex. Biochemistry (2013) 1.05

Investigational antimicrobial agents of 2013. Clin Microbiol Rev (2013) 1.04

How bacterial pathogens eat host lipids: implications for the development of fatty acid synthesis therapeutics. J Biol Chem (2015) 0.99

Antimicrobial Resistance Expressed by Neisseria gonorrhoeae: A Major Global Public Health Problem in the 21st Century. Microbiol Spectr (2016) 0.98

Rational design of broad spectrum antibacterial activity based on a clinically relevant enoyl-acyl carrier protein (ACP) reductase inhibitor. J Biol Chem (2014) 0.92

Resistance to AFN-1252 arises from missense mutations in Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI). J Biol Chem (2013) 0.91

New agents for the treatment of drug-resistant Mycobacterium tuberculosis. Adv Drug Deliv Rev (2016) 0.90

Meleagrin, a new FabI inhibitor from Penicillium chryosogenum with at least one additional mode of action. PLoS One (2013) 0.86

Activity of AFN-1252, a novel FabI inhibitor, against Staphylococcus aureus in an in vitro pharmacodynamic model simulating human pharmacokinetics. J Chemother (2013) 0.81

FabH mutations confer resistance to FabF-directed antibiotics in Staphylococcus aureus. Antimicrob Agents Chemother (2014) 0.78

Radiosynthesis and biological evaluation of a novel enoyl-ACP reductase inhibitor for Staphylococcus aureus. Eur J Med Chem (2014) 0.78

Bacterial fatty acid metabolism in modern antibiotic discovery. Biochim Biophys Acta (2016) 0.77

Dissemination of Novel Antimicrobial Resistance Mechanisms through the Insertion Sequence Mediated Spread of Metabolic Genes. Front Microbiol (2016) 0.77

Mutations upstream of fabI in triclosan resistant Staphylococcus aureus strains are associated with elevated fabI gene expression. BMC Genomics (2015) 0.76

Environmental fatty acids enable emergence of infectious Staphylococcus aureus resistant to FASII-targeted antimicrobials. Nat Commun (2016) 0.76

Clinical Relevance of Type II Fatty Acid Synthesis Bypass in Staphylococcus aureus. Antimicrob Agents Chemother (2017) 0.75

Rationalizing the Binding Kinetics for the Inhibition of the Burkholderia pseudomallei FabI1 Enoyl-ACP Reductase. Biochemistry (2017) 0.75

Resistance Mechanisms and the Future of Bacterial Enoyl-Acyl Carrier Protein Reductase (FabI) Antibiotics. Cold Spring Harb Perspect Med (2016) 0.75

Verrulactones D and E with unprecedented skeletons, new inhibitors of Staphylococcus aureus enoyl-ACP reductase, from Penicillium verruculosum F375. J Antibiot (Tokyo) (2015) 0.75

A Pathogen-Selective Antibiotic Minimizes Disturbance to the Microbiome. Antimicrob Agents Chemother (2016) 0.75

Gonorrhea - an evolving disease of the new millennium. Microb Cell (2016) 0.75

Thiolactomycin-Based Inhibitors of Bacterial β-Ketoacyl-ACP Synthases with in Vivo Activity. J Med Chem (2016) 0.75

Structural characterisation of the fatty acid biosynthesis enzyme FabF from the pathogen Listeria monocytogenes. Sci Rep (2017) 0.75

Articles cited by this

Hospitalizations and deaths caused by methicillin-resistant Staphylococcus aureus, United States, 1999-2005. Emerg Infect Dis (2007) 6.75

Membrane lipid homeostasis in bacteria. Nat Rev Microbiol (2008) 3.88

Bacterial fatty acid biosynthesis: targets for antibacterial drug discovery. Annu Rev Microbiol (2001) 3.35

Type II fatty acid synthesis is not a suitable antibiotic target for Gram-positive pathogens. Nature (2009) 2.68

Lipid biosynthesis as a target for antibacterial agents. Prog Lipid Res (2001) 2.60

Characterization of a daptomycin-nonsusceptible vancomycin-intermediate Staphylococcus aureus strain in a patient with endocarditis. Antimicrob Agents Chemother (2007) 2.38

Reduced glycopeptide susceptibility in methicillin-resistant Staphylococcus aureus (MRSA). Int J Antimicrob Agents (2007) 2.23

Molecular basis of triclosan activity. Nature (1999) 2.18

Inhibitors of FabI, an enzyme drug target in the bacterial fatty acid biosynthesis pathway. Acc Chem Res (2008) 2.07

Inhibiting bacterial fatty acid synthesis. J Biol Chem (2006) 2.03

Inhibitors of fatty acid synthesis as antimicrobial chemotherapeutics. Appl Microbiol Biotechnol (2002) 1.96

Control and outcome of a large outbreak of colonization and infection with glycopeptide-intermediate Staphylococcus aureus in an intensive care unit. Clin Infect Dis (2005) 1.90

MRSA--the tip of the iceberg. Clin Microbiol Infect (2006) 1.81

Essentiality of FASII pathway for Staphylococcus aureus. Nature (2010) 1.77

Characterization of Streptococcus pneumoniae enoyl-(acyl-carrier protein) reductase (FabK). Biochem J (2003) 1.48

Mechanistic diversity and regulation of Type II fatty acid synthesis. Biochem Soc Trans (2002) 1.46

Bacterial fatty-acid biosynthesis: a genomics-driven target for antibacterial drug discovery. Drug Discov Today (2001) 1.43

Validation of antibacterial mechanism of action using regulated antisense RNA expression in Staphylococcus aureus. FEMS Microbiol Lett (2004) 1.32

AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity. Antimicrob Agents Chemother (2009) 1.32

Pharmacodynamics of the new des-f(6)-quinolone garenoxacin in a murine thigh infection model. Antimicrob Agents Chemother (2003) 1.30

Inhibition of the bacterial enoyl reductase FabI by triclosan: a structure-reactivity analysis of FabI inhibition by triclosan analogues. J Med Chem (2004) 1.29

Emerging options for treatment of invasive, multidrug-resistant Staphylococcus aureus infections. Pharmacotherapy (2007) 1.28

Diversity in enoyl-acyl carrier protein reductases. Cell Mol Life Sci (2009) 1.27

The application of computational methods to explore the diversity and structure of bacterial fatty acid synthase. J Lipid Res (2003) 1.27

Identification and characterization of inhibitors of bacterial enoyl-acyl carrier protein reductase. Antimicrob Agents Chemother (2004) 1.13

Mechanism and inhibition of saFabI, the enoyl reductase from Staphylococcus aureus. Biochemistry (2008) 1.13

Identification of inhibitors of bacterial enoyl-acyl carrier protein reductase. Curr Drug Targets Infect Disord (2005) 1.05

Antistaphylococcal activities of CG400549, a new bacterial enoyl-acyl carrier protein reductase (FabI) inhibitor. J Antimicrob Chemother (2007) 1.04

Antimicrobial susceptibility of Haemophilus ducreyi. Antimicrob Agents Chemother (1990) 1.03

Isolation and characterization of unsaturated fatty acid auxotrophs of Streptococcus pneumoniae and Streptococcus mutans. J Bacteriol (2007) 1.02

Crystal structure of enoyl-acyl carrier protein reductase (FabK) from Streptococcus pneumoniae reveals the binding mode of an inhibitor. Protein Sci (2008) 1.00

Vinaxanthone, a new FabI inhibitor from Penicillium sp. J Antimicrob Chemother (2009) 0.90

Pharmacology of novel heteroaromatic polycycle antibacterials. Antimicrob Agents Chemother (2003) 0.89

Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI). Bioorg Med Chem Lett (2009) 0.85

Reduced triclosan susceptibility in methicillin-resistant Staphylococcus epidermidis. Antimicrob Agents Chemother (2004) 0.84

Articles by these authors

Comparative genomics of Listeria species. Science (2001) 12.94

Malate Oxidation in Plant Mitochondria via Malic Enzyme and the Cyanide-insensitive Electron Transport Pathway. Plant Physiol (1980) 1.97

The E5 gene from human papillomavirus type 16 is an oncogene which enhances growth factor-mediated signal transduction to the nucleus. Oncogene (1992) 1.68

[Isolation and properties of external and internal membranes of plant mitochondria]. Biochimie (1972) 1.67

In vitro activities of telithromycin, linezolid, and quinupristin-dalfopristin against Streptococcus pneumoniae with macrolide resistance due to ribosomal mutations. Antimicrob Agents Chemother (2004) 1.65

Molecular epidemiology of multiresistant Streptococcus pneumoniae with both erm(B)- and mef(A)-mediated macrolide resistance. J Clin Microbiol (2004) 1.43

Regulatory T cells expressing granzyme B play a critical role in controlling lung inflammation during acute viral infection. Mucosal Immunol (2012) 1.39

Sequencing of porA from clinical isolates of Neisseria meningitidis defines a subtyping scheme and its genetic regulation. Can J Microbiol (1998) 1.29

Electron transport in the membrane of lutoids from the latex of Hevea brasiliensis. Biochim Biophys Acta (1975) 1.26

Malic enzyme activity and cyanide-insensitive electron transport in plant mitochondria. Biochem Biophys Res Commun (1979) 1.26

A novel resistance mechanism to triclosan that suggests horizontal gene transfer and demonstrates a potential selective pressure for reduced biocide susceptibility in clinical strains of Staphylococcus aureus. Int J Antimicrob Agents (2012) 1.23

Evaluation of reduced susceptibility to quaternary ammonium compounds and bisbiguanides in clinical isolates and laboratory-generated mutants of Staphylococcus aureus. Antimicrob Agents Chemother (2013) 1.20

Treatment de-escalation in HPV-positive oropharyngeal carcinoma: ongoing trials, critical issues and perspectives. Int J Cancer (2014) 1.20

Relationship of free intracellular calcium to the cytolytic activity of Entamoeba histolytica. Infect Immun (1988) 1.18

Identification in Listeria monocytogenes of MecA, a homologue of the Bacillus subtilis competence regulatory protein. J Bacteriol (2000) 1.12

Comparative activity of carbapenem testing: the COMPACT study. J Antimicrob Chemother (2011) 1.11

BiaCore analysis of leptin-leptin receptor interaction: evidence for 1:1 stoichiometry. Anal Biochem (2004) 1.07

Stable expression of functional mitochondrial uncoupling protein in Chinese hamster ovary cells. Proc Natl Acad Sci U S A (1990) 1.06

Prevalence and molecular analysis of macrolide and fluoroquinolone resistance among isolates of Streptococcus pneumoniae collected during the 2000-2001 PROTEKT US Study. J Clin Microbiol (2004) 1.05

Discovery of new Gram-negative antivirulence drugs: structure and properties of novel E. coli WaaC inhibitors. Bioorg Med Chem Lett (2008) 0.99

Lack of evidence for reduced fitness of clinical Staphylococcus aureus isolates with reduced susceptibility to triclosan. Antimicrob Agents Chemother (2012) 0.97

Evaluation of humoral response and protective efficacy of two inactivated vaccines against bluetongue virus after vaccination of goats. Vaccine (2011) 0.95

Quinupristin-dalfopristin resistance in Streptococcus pneumoniae: novel L22 ribosomal protein mutation in two clinical isolates from the SENTRY antimicrobial surveillance program. Antimicrob Agents Chemother (2003) 0.95

Development of Sulfate Uptake Capacity and ATP-Sulfurylase Activity during Root Elongation in Maize. Plant Physiol (1977) 0.94

Non-susceptibility trends among Haemophilus influenzae and Moraxella catarrhalis from community-acquired respiratory tract infections in the UK and Ireland, 1999-2007. J Antimicrob Chemother (2008) 0.92

Combined pancreatic islet-lung transplantation: a novel approach to the treatment of end-stage cystic fibrosis. Am J Transplant (2010) 0.92

In vitro and in vivo interaction between trophozoites of Entamoeba histolytica and gerbil lymphoid cells. Infect Immun (1985) 0.91

The use of machine learning methodologies to analyse antibiotic and biocide susceptibility in Staphylococcus aureus. PLoS One (2013) 0.89

Non-susceptibility trends and serotype distributions among Streptococcus pneumoniae from community-acquired respiratory tract infections and from bacteraemias in the UK and Ireland, 1999 to 2007. J Antimicrob Chemother (2008) 0.88

[Prolonged treatment of severe hypoglycemia with diazoxide]. Sem Hop (1974) 0.88

Subtyping of Neisseria meningitidis strains isolated in Quebec, Canada: correlation between deduced amino acid sequences and serosubtyping techniques. Can J Microbiol (1997) 0.88

Mutational analysis of the promoter region of the porA gene of Neisseria meningitidis. Gene (1999) 0.87

Comparative activity of ceftobiprole against Gram-positive and Gram-negative isolates from Europe and the Middle East: the CLASS study. J Antimicrob Chemother (2011) 0.85

Microspectrofluorometry of the protonation state of ellipticine, an antitumor alkaloid, in single cells. Biophys J (1993) 0.85

[Colonic Crohn's disease and oral contraceptive (author's transl)]. Sem Hop (1980) 0.84

Evidence for humoral rejection of a pancreatic islet graft and rescue with rituximab and IV immunoglobulin therapy. Am J Transplant (2009) 0.84

Liver preservation below 0 degrees C with UW solution and 2,3-butanediol. Cryobiology (1996) 0.83

Consequences of omega -6-oleate desaturase deficiency on lipid dynamics and functional properties of mitochondrial membranes of Arabidopsis thaliana. J Biol Chem (2000) 0.83

Entamoeba histolytica: chemoattractant activity for gerbil neutrophils in vivo and in vitro. Exp Parasitol (1987) 0.83

Variations in energization parameters and proton conductance induced by cold adaptation and essential fatty acid deficiency in mitochondria of brown adipose tissue in the rat. Biochim Biophys Acta (1990) 0.83

Obstructive sleep apnoea in people with Type 1 diabetes: prevalence and association with micro- and macrovascular complications. Diabet Med (2014) 0.83

Sculpting sandcastles grain by grain: self-assembled sand towers. Phys Rev E Stat Nonlin Soft Matter Phys (2012) 0.83

Protonophoric activity of eutypine, a toxin from Eutypa lata, in plant mitochondria. Arch Biochem Biophys (1996) 0.82

Comparative Activity of Carbapenem Testing (COMPACT) study in Germany. Int J Antimicrob Agents (2012) 0.82

An injectable cellulose-based hydrogel for the transfer of autologous nasal chondrocytes in articular cartilage defects. Biotechnol Bioeng (2009) 0.81

Influence of rapamycin on rat macrophage viability and chemotaxis toward allogenic pancreatic islet supernates. Transplant Proc (2008) 0.81

Upregulation of CD38 gene expression in leukemic B cells by interferon types I and II. J Interferon Cytokine Res (1999) 0.79

Epidemiology and antimicrobial susceptibility of Gram-negative aerobic bacteria causing intra-abdominal infections during 2010-2011. J Chemother (2014) 0.79

Expression of the human papillomavirus E7 oncogene during cell transformation is sufficient to induce susceptibility to lysis by activated macrophages. J Immunol (1991) 0.78

Significant Differences Characterise the Correlation Coefficients between Biocide and Antibiotic Susceptibility Profiles in Staphylococcus aureus. Curr Pharm Des (2015) 0.78

Integrative Advanced Oxidation and Biofiltration for Treating Pharmaceuticals in Wastewater. Water Environ Res (2016) 0.77

Protonophoric activity of ellipticine and isomers across the energy-transducing membrane of mitochondria. J Biol Chem (1995) 0.77

Successful -4 degrees C liver preservation in rats with University of Wisconsin solution and 2-3-butanediol. Transplant Proc (1995) 0.77

Combined pancreatic islets-lung transplantation in cystic fibrosis-related diabetes: case reports. Transplant Proc (2010) 0.77

[Crush injury of the lower limbs. Use of anti-shock trousers]. Ann Fr Anesth Reanim (1988) 0.77

ME1036, a novel carbapenem, with enhanced activity against clinical isolates causing bacteraemic community-acquired pneumonia. J Antimicrob Chemother (2009) 0.77

The principal artery of the psoas major muscle. Surg Radiol Anat (1989) 0.77

Epidemiology and mechanisms of resistance among respiratory tract pathogens. Clin Microbiol Infect (1998) 0.77

[Aseptic osteonecrosis in renal transplantation ; apropos of 29 cases]. Rev Rhum Mal Osteoartic (1975) 0.77

Indication of electron neutrino appearance from an accelerator-produced off-axis muon neutrino beam. Phys Rev Lett (2011) 0.77

[Diffuse uptake of brown fat on computed-tomography coupled positron emission tomoscintigraphy (PET-CT) for the exploration of extra-adrenal pheochromocytoma]. Ann Endocrinol (Paris) (2006) 0.76

Factitious self-manipulation of the external insulin pump in adolescents with Type 1 diabetes. Diabet Med (2011) 0.76

[Echocardiography in anorexia nervosa]. Presse Med (1989) 0.76

Evidence of Coulomb blockade behavior in a quasi-zero-dimensional quantum well on TiO2 surface. Proc Natl Acad Sci U S A (2010) 0.75

[Neuropathy long before Waldenström's disease: effect of prolonged treatment with melphalan]. J Med Bord (1967) 0.75

[Complete atrio-ventricular block through section of the bundle of His secondary to closed theoracic trauma]. Arch Mal Coeur Vaiss (1974) 0.75

[Implementing a community surveillance network to monitor antimicrobial resistance: the Labville network]. Med Mal Infect (2008) 0.75

[Thyroid angiography (clinical, isotopic, anatomo-pathologic and radiologic comparisons in 46 cases)]. J Med Bord (1967) 0.75

[Persistence of ductus arteriosus into the 6th decade of life. Discussion of its surgical treatment]. Ann Cardiol Angeiol (Paris) (1973) 0.75

[Association of monoclonal gammapathy and epithelial cancer]. Nouv Presse Med (1980) 0.75

[Persistent splenomegaly after recovery from bacterial endocarditis]. Nouv Presse Med (1973) 0.75

[Mickulicz syndrome due to hemopathy]. Bull Soc Ophtalmol Fr (1974) 0.75

How technology has changed diabetes management and what it has failed to achieve. Diabetes Metab (2011) 0.75

Viral glycoproteins synthesis in Friend cell lines producing polycythemic (FV-P) and anemic (FV-A) Friend viruses. Biochem Biophys Res Commun (1980) 0.75

Substitution of insulin by exenatide in bad controlled type 2 diabetic patients: efficacy and predictive factors. Minerva Endocrinol (2014) 0.75

[Subacute polyarthritis in sarcoidosis. 1 cases with latent neuromuscular involvement]. Sem Hop (1978) 0.75

Variations in serum vanadium levels during the treatment of mental depression. Biol Psychiatry (1986) 0.75

[Pulmonary involvement in chronic lymphocytic leukemia. Diagnostic value of trans-bronchial biopsy (author's transl)]. Sem Hop (1982) 0.75

Glycemic management of diabetes by insulin therapy. Minerva Endocrinol (2013) 0.75

Activity of iclaprim against Legionella pneumophila. J Antimicrob Chemother (2007) 0.75

Association of malignant insulinoma and type 2 diabetes mellitus: a case report. Ann Endocrinol (Paris) (2008) 0.75

[On-line method for measuring extravascular lung water with heavy water (author's transl)]. Bull Eur Physiopathol Respir (1979) 0.75

[Characteristics of infants hospitalized in intensive care for severe bronchiolitis]. Arch Pediatr (2011) 0.75

[Current aspects of clinical hematology]. J Med Bord (1966) 0.75

[Metabolism of hemoglobin A1. No effect of an acute glucose load on the hemoglobin A1 titer in normal subjects]. Nouv Presse Med (1980) 0.75

[Determination of the acetylcholinesterase activities of the amniotic fluid on a centrifugal analyzer]. Pathol Biol (Paris) (1983) 0.75

[Acetylcholinesterase titers in the amniotic fluid. Value of screening dysraphia of the central nervous system]. Rev Fr Gynecol Obstet (1987) 0.75

Lung capillaries permeability to small molecules. Bibl Anat (1975) 0.75

Does vanadium play a role in depressive states? Biol Psychiatry (1986) 0.75

[Disaster on the highway]. Soins Chir Gen Spec (1982) 0.75

Type 1 diabetes and idiopathic retroperitoneal fibrosis: case report. Ann Endocrinol (Paris) (2008) 0.75

[Sleep apnea syndrome in the elderly]. Rev Mal Respir (2004) 0.75

[Biselective thyroid angiography]. Bord Med (1972) 0.75

Lung water and capillary permeability in pulmonary sarcoid-like granulomatosis. Ann N Y Acad Sci (1976) 0.75

[Difficulties in the diagnosis of bacterial endocarditis. Its border states]. Bord Med (1972) 0.75

[Thrombopenic purpura and Gougerot-Sjögren syndrome in a woman patient treated by quinidine and beta-blockaders]. Nouv Presse Med (1978) 0.75

Angiotensin-converting enzyme in sarcoidosis and other pulmonary diseases: a comparison of two methods of determination. Lung (1979) 0.75

Combining ability estimates of sulfate uptake efficiency in maize. Theor Appl Genet (1982) 0.75

[Arsenism: a case-report (author's transl)]. Sem Hop (1982) 0.75