macrolides

Summary

Summary: A group of macrocyclic compounds formed by chain extension of multiple PROPIONATES and cyclized into a large (typically 12, 14, 16) membered lactone. They are often glycosylated. Many of them are ANTIBIOTICS.

Top Publications

  1. ncbi Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells
    A Yamamoto
    Department of Physiology and Liver Research Center Cell Biology, Kansai Medical University, Osaka, Japan
    Cell Struct Funct 23:33-42. 1998
  2. ncbi Does bafilomycin A1 block the fusion of autophagosomes with lysosomes?
    Daniel J Klionsky
    Autophagy 4:849-950. 2008
  3. ncbi Role of autophagy in temozolomide-induced cytotoxicity for malignant glioma cells
    T Kanzawa
    Department of Neurosurgery, The University of Texas MD Anderson Cancer Center, Houston, TX, USA
    Cell Death Differ 11:448-57. 2004
  4. ncbi Modulation of the host immune response by a transient intracellular stage of Mycobacterium ulcerans: the contribution of endogenous mycolactone toxin
    Emmanuelle Coutanceau
    Unite de Genetique Moleculaire Bacterienne, Institut Pasteur, Paris, France
    Cell Microbiol 7:1187-96. 2005
  5. pmc Development and application of real-time PCR assays for quantification of erm genes conferring resistance to macrolides-lincosamides-streptogramin B in livestock manure and manure management systems
    Jing Chen
    The MAPLE Research Initiative, Department of Animal Sciences, The Ohio State University, Columbus, OH 43210, USA
    Appl Environ Microbiol 73:4407-16. 2007
  6. pmc Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis
    Laurent Marsollier
    Unite de Genetique Moleculaire Bacterienne, Institut Pasteur, Paris, France
    PLoS Pathog 3:e62. 2007
  7. pmc Vacuolar H+-ATPase activity is required for endocytic and secretory trafficking in Arabidopsis
    Jan Dettmer
    Center for Plant Molecular Biology Plant Physiology, Universitat Tubingen, 72076 Tubingen, Germany
    Plant Cell 18:715-30. 2006
  8. ncbi Chemical genomics identifies the unfolded protein response as a target for selective cancer cell killing during glucose deprivation
    Sakae Saito
    Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, Tokyo, Japan
    Cancer Res 69:4225-34. 2009
  9. ncbi High prevalence of macrolide resistance in Mycoplasma pneumoniae isolates from adult and adolescent patients with respiratory tract infection in China
    Bin Cao
    Department of Infectious Diseases and Clinical Microbiology, Beijing Chao Yang Hospital, Capital Medical University, People s Republic of China
    Clin Infect Dis 51:189-94. 2010
  10. pmc Azithromycin blocks autophagy and may predispose cystic fibrosis patients to mycobacterial infection
    Maurizio Renna
    Department of Medical Genetics, Cambridge Institute for Medical Research, University of Cambridge, Cambridge, United Kingdom
    J Clin Invest 121:3554-63. 2011

Detail Information

Publications297 found, 100 shown here

  1. ncbi Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells
    A Yamamoto
    Department of Physiology and Liver Research Center Cell Biology, Kansai Medical University, Osaka, Japan
    Cell Struct Funct 23:33-42. 1998
    ..These results suggested that acidification of the lumenal space of autophagosomes or lysosomes by V-ATPase is important for the fusion between autophagosomes and lysosomes...
  2. ncbi Does bafilomycin A1 block the fusion of autophagosomes with lysosomes?
    Daniel J Klionsky
    Autophagy 4:849-950. 2008
    ..However, data from one of our labs noted an apparently different result in a relatively recent manuscript. Therefore, we decided to look into this more carefully...
  3. ncbi Role of autophagy in temozolomide-induced cytotoxicity for malignant glioma cells
    T Kanzawa
    Department of Neurosurgery, The University of Texas MD Anderson Cancer Center, Houston, TX, USA
    Cell Death Differ 11:448-57. 2004
    ..Application of an autophagy inhibitor that works after the association of LC3 with autophagosome membrane, such as bafilomycin A1, is expected to enhance the cytotoxicity of TMZ for malignant gliomas...
  4. ncbi Modulation of the host immune response by a transient intracellular stage of Mycobacterium ulcerans: the contribution of endogenous mycolactone toxin
    Emmanuelle Coutanceau
    Unite de Genetique Moleculaire Bacterienne, Institut Pasteur, Paris, France
    Cell Microbiol 7:1187-96. 2005
    ....
  5. pmc Development and application of real-time PCR assays for quantification of erm genes conferring resistance to macrolides-lincosamides-streptogramin B in livestock manure and manure management systems
    Jing Chen
    The MAPLE Research Initiative, Department of Animal Sciences, The Ohio State University, Columbus, OH 43210, USA
    Appl Environ Microbiol 73:4407-16. 2007
    ..six classes of erm genes (classes A through C, F, T, and X) that encode the major mechanism of resistance to macrolides-lincosamides-streptogramin B (MLS(B))...
  6. pmc Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis
    Laurent Marsollier
    Unite de Genetique Moleculaire Bacterienne, Institut Pasteur, Paris, France
    PLoS Pathog 3:e62. 2007
    ..The results of this study support a model whereby biofilm changes confer selective advantages to M. ulcerans in colonizing various ecological niches successfully, with repercussions for Buruli ulcer pathogenesis...
  7. pmc Vacuolar H+-ATPase activity is required for endocytic and secretory trafficking in Arabidopsis
    Jan Dettmer
    Center for Plant Molecular Biology Plant Physiology, Universitat Tubingen, 72076 Tubingen, Germany
    Plant Cell 18:715-30. 2006
    ..Together, our results suggest the convergence of the early endocytic and secretory trafficking pathways in the TGN...
  8. ncbi Chemical genomics identifies the unfolded protein response as a target for selective cancer cell killing during glucose deprivation
    Sakae Saito
    Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, Tokyo, Japan
    Cancer Res 69:4225-34. 2009
    ..Our findings show that disrupting the UPR during glucose deprivation could be an attractive approach for selective cancer cell killing and could provide a chemical genomic basis for developing UPR-targeting drugs against solid tumors...
  9. ncbi High prevalence of macrolide resistance in Mycoplasma pneumoniae isolates from adult and adolescent patients with respiratory tract infection in China
    Bin Cao
    Department of Infectious Diseases and Clinical Microbiology, Beijing Chao Yang Hospital, Capital Medical University, People s Republic of China
    Clin Infect Dis 51:189-94. 2010
    ..Patients infected with macrolide-resistant M. pneumoniae required significantly longer durations of antibiotic therapy and had longer time to resolution of fever...
  10. pmc Azithromycin blocks autophagy and may predispose cystic fibrosis patients to mycobacterial infection
    Maurizio Renna
    Department of Medical Genetics, Cambridge Institute for Medical Research, University of Cambridge, Cambridge, United Kingdom
    J Clin Invest 121:3554-63. 2011
    ....
  11. ncbi Macrolides beyond the conventional antimicrobials: a class of potent immunomodulators
    Evangelos J Giamarellos-Bourboulis
    4th Department of Internal Medicine, Attikon University Hospital, University of Athens, Medical School, 1 Rimini Street, 124 62 Athens, Greece
    Int J Antimicrob Agents 31:12-20. 2008
    ..of erythromycin in its treatment has focused attention of researchers on the anti-inflammatory properties of macrolides. Chronic inflammation of the airways accompanied by infiltration by neutrophils and overproduction of mucus and ..
  12. ncbi Concanamycin A, the specific inhibitor of V-ATPases, binds to the V(o) subunit c
    Markus Huss
    Universitat Osnabruck, Fachbereich Biologie chemie, Abteilung Tierphysiologie, 49069 Osnabruck, Germany
    J Biol Chem 277:40544-8. 2002
    ..Binding was also prevented by the plecomacrolides bafilomycin A(1) and B(1), respectively, but not by the benzolactone enamide salicylihalamide, a member of a novel class of V-ATPase inhibitors...
  13. pmc Mechanisms of action and clinical application of macrolides as immunomodulatory medications
    Soichiro Kanoh
    Department of Pediatrics, Virginia Commonwealth University School of Medicine, 1001 E Marshall St, Richmond, VA 23298, USA
    Clin Microbiol Rev 23:590-615. 2010
    b>Macrolides have diverse biological activities and an ability to modulate inflammation and immunity in eukaryotes without affecting homeostatic immunity...
  14. ncbi Mycobacterium ulcerans toxic macrolide, mycolactone modulates the host immune response and cellular location of M. ulcerans in vitro and in vivo
    Sarojini Adusumilli
    Microbiology Department, University of Tennessee, Knoxville, TN, USA
    Cell Microbiol 7:1295-304. 2005
    ..Neither WT M. ulcerans nor mycolactone negative strains are strong neutrophil attractants. These results suggest that mycolactone is largely responsible for the unique pathology produced by M. ulcerans...
  15. pmc Activities of new macrolides and fluoroquinolones against Mycobacterium ulcerans infection in mice
    A Bentoucha
    , , Paris, France
    Antimicrob Agents Chemother 45:3109-12. 2001
    ..The RIF+AMK combination and possibly RIF+STR warrant further study for the treatment of M. ulcerans infection in humans...
  16. ncbi Prevalence and mechanism of resistance against macrolides and lincosamides in Streptococcus suis isolates
    A Martel
    Department of Pathology, Bacteriology and Poultry Diseases, Faculty of Veterinary Medicine, Ghent University, Salisburylaan 133, B 9820, Merelbeke, Belgium
    Vet Microbiol 83:287-97. 2001
    ..suis, one S. pneumoniae and three of the S. pyogenes isolates. This study demonstrates that resistance against macrolides, lincosamides and streptogramin B is widespread in S...
  17. ncbi Inhibitors of V-ATPases: old and new players
    Markus Huss
    Department of Biology Chemistry, University of Osnabruck, 49069 Osnabruck, Germany
    J Exp Biol 212:341-6. 2009
    ....
  18. ncbi Immunosuppressive signature of cutaneous Mycobacterium ulcerans infection in the peripheral blood of patients with buruli ulcer disease
    Richard Phillips
    Komfo Anokye Teaching Hospital, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana
    J Infect Dis 200:1675-84. 2009
    ..Moreover, we identified immunological markers of BUD, which may be helpful for confirmatory diagnosis of the disease and, especially, for monitoring the response to antibiotic treatment...
  19. ncbi Mechanisms of resistance to macrolides and lincosamides: nature of the resistance elements and their clinical implications
    Roland Leclercq
    Service de Microbiologie, Hôpital Côte de Nacre, Universite de Caen, Caen 14033, France
    Clin Infect Dis 34:482-92. 2002
    Resistance to macrolides and lincosamides is increasingly reported in clinical isolates of gram-positive bacteria...
  20. pmc Mycolactone-mediated inhibition of tumor necrosis factor production by macrophages infected with Mycobacterium ulcerans has implications for the control of infection
    Egidio Torrado
    Life and Health Sciences Research Institute, School of Health Sciences, University of Minho, 4710 057 Braga, Portugal
    Infect Immun 75:3979-88. 2007
    ..ulcerans bacilli inhibits, in a dose-dependent manner, but does not abrogate, the production of macrophage inflammatory protein 2, which is consistent with the persistent inflammatory responses observed in experimentally infected mice...
  21. pmc Mycobacterium ulcerans triggers T-cell immunity followed by local and regional but not systemic immunosuppression
    Alexandra G Fraga
    Life and Health Sciences Research Institute ICVS, School of Health Sciences, Campus de Gualtar, University of Minho, 4710 057 Braga, Portugal
    Infect Immun 79:421-30. 2011
    ..These results suggest that prophylactic and/or therapeutic interventions to prevent dissemination of M. ulcerans to DLN during the early phase of infection would contribute for the maintenance of protective immunity and disease control...
  22. pmc Mycolactone impairs T cell homing by suppressing microRNA control of L-selectin expression
    Laure Guenin-Macé
    Institut Pasteur, Unité de Pathogénomique Mycobactérienne Intégrée, 75015 Paris, France
    Proc Natl Acad Sci U S A 108:12833-8. 2011
    ..Our results identify T-cell homing as a biological process targeted by mycolactone. Moreover, they reveal a mechanism of control of CD62-L expression involving the miRNA let-7b...
  23. ncbi Macrolides: from in vitro anti-inflammatory and immunomodulatory properties to clinical practice in respiratory diseases
    P Zarogoulidis
    Pulmonary Department, G Papanikolaou Hospital, Aristotle University of Thessaloniki, Thessaloniki 57010, Greece
    Eur J Clin Pharmacol 68:479-503. 2012
    b>Macrolides have long been recognised to exert immunomodulary and anti-inflammatory actions...
  24. ncbi Combined treatment with bortezomib plus bafilomycin A1 enhances the cytocidal effect and induces endoplasmic reticulum stress in U266 myeloma cells: crosstalk among proteasome, autophagy-lysosome and ER stress
    Tomohiro Kawaguchi
    Department of Biochemistry, Tokyo Medical University, Tokyo, Japan
    Int J Oncol 38:643-54. 2011
    ..Controlling these interactions and kinetics appears to have important implications for optimizing clinical cancer treatment including MM-therapy...
  25. ncbi A Dalpha6 knockout strain of Drosophila melanogaster confers a high level of resistance to spinosad
    Trent Perry
    Department of Genetics, Centre for Environmental Stress and Adaptation Research, Bio21 Institute, University of Melbourne, Parkville, Victoria, Australia
    Insect Biochem Mol Biol 37:184-8. 2007
    ..This, combined with the high degree of evolutionary conservation of nAChR subunits, suggests that mutations in Dalpha6 orthologues may underpin the spinosad resistance identified in several economically important field pests...
  26. ncbi Clinical implications of the immunomodulatory effects of macrolides
    Jun Tamaoki
    First Department of Medicine, Tokyo Women s Medical University, 8 1 Kawada cho, Shiinjuku, Tokyo, Japan
    Am J Med 117:5S-11S. 2004
    ..cause of morbidity and mortality in patients with chronic airway inflammation, is directly inhibited by macrolides and suppressed by decreased inflammation in the airway...
  27. ncbi Mutations in the extracellular domains of glutamate-gated chloride channel alpha3 and beta subunits from ivermectin-resistant Cooperia oncophora affect agonist sensitivity
    Annete I Njue
    Institute of Parasitology, McGill University, 21 111 Lakeshore Road, Ste Anne de Bellevue, Quebec, Canada H9X 3V9
    J Neurochem 89:1137-47. 2004
    ..Of the three amino acids distinguishing the IVS and IVR GluClalpha3 subunits, only one of them, L256F, accounted for the differences in response between the IVS and IVR GluClalpha3 homomeric channels...
  28. ncbi Induction of autophagic cell death in malignant glioma cells by arsenic trioxide
    Takao Kanzawa
    Department of Neurosurgery, Mount Sinai School of Medicine, New York, New York 10029, USA
    Cancer Res 63:2103-8. 2003
    ..These findings suggest that As(2)O(3) at a clinically safe concentration may be an effective chemotherapeutic agent for malignant gliomas...
  29. pmc Enhancement of biofilm formation by subinhibitory concentrations of macrolides in icaADBC-positive and -negative clinical isolates of Staphylococcus epidermidis
    Qian Wang
    Department of Pharmacy, Southwest Hospital, The Third Military Medical University, Chongqing 400038, China
    Antimicrob Agents Chemother 54:2707-11. 2010
    ..The levels of expression of the biofilm-related genes icaA, atlE, fruA, pyrR, sarA, and sigB were increased in response to erythromycin. The results likely underscore the potential clinical relevance of macrolide-induced biofilm growth...
  30. ncbi The non-target impact of spinosyns on beneficial arthropods
    Antonio Biondi
    French National Institute for Agricultural Research INRA, ISA, Sophia Antipolis, France
    Pest Manag Sci 68:1523-36. 2012
    ..This review will help to optimise the future use of spinosad and new spinosyns in IPM programmes and for organic farming, notably by preventing the possible side effects of spinosyns on beneficial arthropods...
  31. ncbi Diffuse panbronchiolitis
    V Poletti
    Dept of Diseases of the Thorax, GB Morgagni Hospital, Forli, Italy
    Eur Respir J 28:862-71. 2006
    ....
  32. pmc Nested PCR-linked capillary electrophoresis and single-strand conformation polymorphisms for detection of macrolide-resistant Mycoplasma pneumoniae in Beijing, China
    Changying Lin
    Beijing Center for Disease Prevention and Control, Department of Bacteriology, Capital Institute of Pediatrics, No 2 Yabao Road, Beijing 100020, People s Republic of China
    J Clin Microbiol 48:4567-72. 2010
    Mycoplasma pneumoniae is usually susceptible to macrolides, but macrolide-resistant strains have been found frequently in recent years. Mutations in domain V of the 23S rRNA gene of M...
  33. pmc Natural biocombinatorics in the polyketide synthase genes of the actinobacterium Streptomyces avermitilis
    Holger Jenke-Kodama
    Department of Molecular Ecology, Institute of Biology, Humboldt University, Berlin, Germany
    PLoS Comput Biol 2:e132. 2006
    ..Our results indicate that homologous recombination facilitated by the modularity of PKS architecture is the most important mechanism underlying polyketide diversity in bacteria...
  34. ncbi A Mycobacterium ulcerans toxin, mycolactone, induces apoptosis in primary human keratinocytes and in HaCaT cells
    Chiarella Bozzo
    Department of Clinical and Experimental Medicine, University of Piemonte Orientale A Avogadro, Via Solaroli 17, 28100 Novara, Italy
    Microbes Infect 12:1258-63. 2010
    ..In conclusion, mycolactone induces apoptosis in human keratinocytes, thus contributing to Buruli ulcer lesions development...
  35. ncbi Mechanisms of fluoroquinolone and macrolide resistance in Campylobacter spp
    Sophie Payot
    Institut National de la Recherche Agronomique, UR086 BioAgresseurs, santé, Environnement, Nouzilly, France
    Microbes Infect 8:1967-71. 2006
    ..infections is increasing worldwide, as well as the proportion of isolates resistant to fluoroquinolones and/or macrolides, the drugs of choice to treat campylobacteriosis...
  36. ncbi Resistance to spinosad in the western flower thrips, Frankliniella occidentalis (Pergande), in greenhouses of south-eastern Spain
    Pablo Bielza
    Departamento de Producción Vegetal, Universidad Politecnica de Cartagena, Paseo Alfonso XIII 48, 30203 Cartagena, Spain
    Pest Manag Sci 63:682-7. 2007
    ..These findings suggest that rotation with spinosad may be an effective resistance management strategy...
  37. pmc Synergy between efflux pump CmeABC and modifications in ribosomal proteins L4 and L22 in conferring macrolide resistance in Campylobacter jejuni and Campylobacter coli
    Cedric Cagliero
    Institut National de la Recherche Agronomique, UR1282 Infectiologie Animale et Santé Publique IASP 213, 37380 Nouzilly, France
    Antimicrob Agents Chemother 50:3893-6. 2006
    ..These mutants exhibited modifications in the ribosomal proteins L4 (G74D) and L22 (insertions at position 86 or 98). A synergy between the CmeABC efflux pump and these modifications in conferring macrolide resistance was observed...
  38. pmc Development, stability, and molecular mechanisms of macrolide resistance in Campylobacter jejuni
    Dave Bryson Caldwell
    Department of Animal Science, The University of Tennessee, Knoxville, Tennessee, USA
    Antimicrob Agents Chemother 52:3947-54. 2008
    ..jejuni, and indicate that C. jejuni utilizes complex and different mechanisms to develop Ery resistance in vitro and in vivo...
  39. ncbi Emergence of macrolide-resistant strains during an outbreak of Mycoplasma pneumoniae infections in children
    M Chironna
    Department of Biomedical Sciences and Human Oncology Hygiene Section, University of Bari, and Department of Pulmonology, Giovanni XXIII Pediatric Hospital, Piazza G Cesare 11, 70124 Bari, Italy
    J Antimicrob Chemother 66:734-7. 2011
    Mycoplasma pneumoniae is a frequent cause of human lower respiratory tract infections (LRTIs) for which macrolides are the treatment of choice. The aim of this study was to determine the rate of macrolide resistance and to subtype M...
  40. ncbi Bafilomycin A1 inhibits chloroquine-induced death of cerebellar granule neurons
    John J Shacka
    Department of Pathology, Division of Neuropathology, University of Alabama at Birmingham, SC961, 1530 3rd Ave South, Birmingham, AL 35294 0017, USA
    Mol Pharmacol 69:1125-36. 2006
    ....
  41. ncbi A novel mycolactone from a clinical isolate of Mycobacterium ulcerans provides evidence for additional toxin heterogeneity as a result of specific changes in the modular polyketide synthase
    Hui Hong
    Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
    Chembiochem 6:643-8. 2005
  42. ncbi The genome, evolution and diversity of Mycobacterium ulcerans
    Katharina Röltgen
    Swiss Tropical and Public Health Institute, Molecular Immunology, Basel, Switzerland
    Infect Genet Evol 12:522-9. 2012
    ..ulcerans are not entirely explored. However, comparative genome analysis of closely related M. ulcerans isolates is anticipated to give deeper insights into the population structure of this enigmatic mycobacterium...
  43. ncbi Therapeutic and prophylactic efficacy of milbemycin oxime (Interceptor) against Thelazia callipaeda in naturally exposed dogs
    E Ferroglio
    Dipartimento di Produzioni Animali, Epidemiologia ed Ecologia, Universita di Torino, Via L Da Vinci, 44 10095 Grugliasco TO, Italy
    Vet Parasitol 154:351-3. 2008
    ..0056). The efficacy of the prophylactic use of a monthly treatment with milbemycin oxime showed 90% efficacy in reducing T. callipaeda infection rate...
  44. ncbi Pharmacological characterization of the Haemonchus contortus GABA-gated chloride channel, Hco-UNC-49: modulation by macrocyclic lactone anthelmintics and a receptor for piperazine
    David D R Brown
    Applied Bioscience Graduate Program, Faculty of Science, University of Ontario Institute of Technology, 2000 Simcoe Street North, Oshawa, ON L1H 7K4, Canada
    Vet Parasitol 185:201-9. 2012
    ..In addition, this is the first report of the heterologous expression and subsequent characterization of a receptor for piperazine...
  45. pmc Increased macrolide resistance of Mycoplasma pneumoniae in pediatric patients with community-acquired pneumonia
    Miyuki Morozumi
    Laboratory of Molecular Epidemiology for Infectious Agents, Kitasato Institute for Life Sciences, Kitasato University, 5 9 1 Shirokane, Minatoku, Tokyo 108 8641, Japan
    Antimicrob Agents Chemother 52:348-50. 2008
    ..These resistant strains increased rapidly from April 2002 to December 2006...
  46. pmc Macrolide resistance in Mycoplasma pneumoniae, Israel, 2010
    Diana Averbuch
    Hadassah Hebrew University Medical Center, Jerusalem, Israel
    Emerg Infect Dis 17:1079-82. 2011
    ..We report the emergence of macrolide-resistant M. pneumoniae in Israel and the in vivo evolution of such resistance during the treatment of a 6-year-old boy with pneumonia...
  47. ncbi Inhibition of autophagy enhances anticancer effects of atorvastatin in digestive malignancies
    Pei Ming Yang
    Department of Pharmacology, College of Medicine, National Taiwan University, Taipei, Taiwan
    Cancer Res 70:7699-709. 2010
    ..Combinations of atorvastatin with bafilomycin A1 provide a novel and promising strategy to improve the treatment of digestive malignancies...
  48. ncbi IFN-gamma-dependent activation of macrophages during experimental infections by Mycobacterium ulcerans is impaired by the toxin mycolactone
    Egidio Torrado
    Life and Health Sciences Research Institute, School of Health Sciences, University of Minho, Braga, Portugal
    J Immunol 184:947-55. 2010
    ..Our findings suggest that the protection mediated by IFN-gamma in M. ulcerans-infected macrophages is impaired by the local buildup of mycolactone...
  49. pmc Distribution of serotypes, genotypes, and resistance determinants among macrolide-resistant Streptococcus pneumoniae isolates
    Xiaoping Xu
    Department of Laboratory Medicine, Shenzhen Second People s Hospital, Shenzhen 518035, People s Republic of China
    Antimicrob Agents Chemother 54:1152-9. 2010
    ..1. Erythromycin resistance among S. pneumoniae isolates in New South Wales is mainly due to the dissemination of multidrug-resistant S. pneumoniae strains or horizontal spread of the Tn916 family of transposons...
  50. ncbi Characterization of macrolide resistance in Mycoplasma pneumoniae isolated from children in Shanghai, China
    Yang Liu
    Institute of Antibiotics, Huashan Hospital, Fudan University, Shanghai 200040, PR China
    Diagn Microbiol Infect Dis 67:355-8. 2010
    ..Ninety-three (93%) clinical isolates were classified into the P1 gene restriction fragment length polymorphism (RFLP) type I, and 7 (7%) were type II...
  51. ncbi Genetics of spinosad resistance in Frankliniella occidentalis (Thysanoptera: Thripidae)
    P Bielza
    Departamento de Producción Vegetal, Universidad Politecnica de Cartagena, Paseo Alfonso XIII 48, 30203 Cartagena, Spain
    J Econ Entomol 100:916-20. 2007
    ..Another approach, which was based on phenotypic variances, showed that nE, or the minimum number of freely segregating genetic factors for the resistant strain, equaled 0.59...
  52. ncbi Macrolide resistance of Staphylococcus aureus and Haemophilus species associated with long-term azithromycin use in cystic fibrosis
    Sonja J Phaff
    Department of Pediatric Pulmonology and Allergology, Erasmus MC Sophia Children s Hospital, Rotterdam, The Netherlands
    J Antimicrob Chemother 57:741-6. 2006
    ..The purpose of this study was to determine the association between long-term use of azithromycin in CF patients and change over time in macrolide susceptibility of Staphylococcus aureus and Haemophilus spp...
  53. ncbi Resistance and cross-resistance to neonicotinoid insecticides and spinosad in the Colorado potato beetle, Leptinotarsa decemlineata (Say) (Coleoptera: Chrysomelidae)
    David Mota-Sanchez
    Department of Entomology, Michigan State University, East Lansing, MI 48824, USA
    Pest Manag Sci 62:30-7. 2006
    ..Rotation with spinosad also carries some risk, but it is unlikely that spinosad resistance in this case is mechanistically related to that for the neonicotinoids...
  54. ncbi Immunomodulatory effects of macrolide antibiotics in respiratory disease: therapeutic implications for asthma and cystic fibrosis
    Sanjiv Sharma
    Portex Unit, Institute of Child Health, London, UK
    Paediatr Drugs 9:107-18. 2007
    ..for a proinflammatory propensity in CF immune effector and epithelial cells and many studies indicate that macrolides modulate these inflammatory processes...
  55. pmc Global mapping of translation initiation sites in mammalian cells at single-nucleotide resolution
    Sooncheol Lee
    Division of Nutritional Sciences, Cornell University, Ithaca, NY 14853, USA
    Proc Natl Acad Sci U S A 109:E2424-32. 2012
    ..Our study establishes a practical platform for uncovering the hidden coding potential of the transcriptome and offers a greater understanding of the complexity of translation initiation...
  56. ncbi A comparative clinical study of macrolide-sensitive and macrolide-resistant Mycoplasma pneumoniae infections in pediatric patients
    Keita Matsubara
    Department of Pediatrics, National Hospital Organization Tokyo Medical Center, 2 5 1 Higashigaoka, Meguro ku, Tokyo, Japan
    J Infect Chemother 15:380-3. 2009
    ..We isolated 94 strains of M. pneumoniae, and determined the minimum inhibitory concentrations (MICs) of macrolides and other antimicrobial agents for these strains...
  57. ncbi Diffuse panbronchiolitis: role of macrolides in therapy
    Naoto Keicho
    Department of Respiratory Diseases, Research Institute, International Medical Center of Japan, Toyama, Shinjuku ku, Tokyo, Japan
    Am J Respir Med 1:119-31. 2002
    ..The bactericidal activity of macrolides, particularly erythromycin, is not a significant factor for their clinical efficacy in DPB...
  58. ncbi Transcripts of the nicotinic acetylcholine receptor subunit gene Pxylα6 with premature stop codons are associated with spinosad resistance in diamondback moth, Plutella xylostella
    Frank D Rinkevich
    Department of Entomology, Comstock Hall, Cornell University, Ithaca, NY 14853 0901, USA
    Invert Neurosci 10:25-33. 2010
    ..Thus, it appears that spinosad resistance in diamondback moth is due to a mutation(s) that results in no functional Pxylα6 being produced...
  59. ncbi Distribution of macrolides, sulfonamides, and trimethoprim in tropical waters: ubiquitous occurrence of veterinary antibiotics in the Mekong Delta
    Satoshi Managaki
    Laboratory of Organic Geochemistry, Institute of Symbiotic Science and Technology, Tokyo University of Agriculture and Technology, Fuchu, Tokyo 183 8509, Japan
    Environ Sci Technol 41:8004-10. 2007
    We investigated the distributions of 12 antibiotics (viz., sulfonamides, macrolides, and trimethoprim) in the water from the Mekong Delta, Vietnam, and compared them with those in the Tamagawa River, Japan...
  60. pmc Induction of apoptosis in human cancer cells by candidaspongiolide, a novel sponge polyketide
    Daniela Trisciuoglio
    Tumor Hypoxia Laboratory, SAIC Frederick, Inc, National Cancer Institute, Frederick, MD 21702, USA
    J Natl Cancer Inst 100:1233-46. 2008
    ..Candidaspongiolide (CAN), a novel polyketide from a marine sponge, is the active component of a mixture that was found to be potently cytotoxic in the National Cancer Institute's 60-cell-line screen...
  61. ncbi Distribution and antibacterial susceptibility of macrolide resistance genotypes in Streptococcus pneumoniae: PROTEKT Year 5 (2003-2004)
    David J Farrell
    G R Micro Ltd, 7 9 William Road, London NW1 3ER, UK
    Int J Antimicrob Agents 31:245-9. 2008
    ..Of the erm(B)+mef(A) strains, 43.5% were resistant to amoxicillin/clavulanic acid. Most ERSP isolates were susceptible to levofloxacin (98.3%) and telithromycin (99.4%)...
  62. ncbi A dichotomy in bronchiolitis obliterans syndrome after lung transplantation revealed by azithromycin therapy
    B M Vanaudenaerde
    Laboratory of Pneumology, Katholieke Universiteit Leuven, Leuven, Belgium
    Eur Respir J 32:832-43. 2008
    ....
  63. ncbi The antiparasitic moxidectin: safety, tolerability, and pharmacokinetics in humans
    Monette M Cotreau
    Experimental Medicine, Wyeth Research, 87 CambridgePark Drive, Cambridge, MA 02140, USA
    J Clin Pharmacol 43:1108-15. 2003
    ..In summary, the results from this study indicate that MOX is safe and well tolerated in humans between the doses of 3 mg and 36 mg...
  64. ncbi Effectiveness and safety of macrolides in cystic fibrosis patients: a meta-analysis and systematic review
    Yun Cai
    Department of Clinical Pharmacology, PLA General Hospital, Beijing, People s Republic of China
    J Antimicrob Chemother 66:968-78. 2011
    To evaluate the efficacy and safety of macrolides in cystic fibrosis (CF).
  65. ncbi Is there a role for inhaled corticosteroids and macrolide therapy in bronchiectasis?
    Paul King
    Monash University, Department of Medicine, Monash Medical Centre, Melbourne, Victoria, Australia
    Drugs 67:965-74. 2007
    ..Two potentially useful therapies are inhaled corticosteroids (ICS) and macrolides. The clinical trials that have been performed in bronchiectasis with these two medications can be considered to ..
  66. ncbi Chemistry. The renaissance of natural products as drug candidates
    Ian Paterson
    Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
    Science 310:451-3. 2005
  67. pmc Mycolactone diffuses into the peripheral blood of Buruli ulcer patients--implications for diagnosis and disease monitoring
    Fred S Sarfo
    Komfo Anokye Teaching Hospital, Kumasi, Ghana
    PLoS Negl Trop Dis 5:e1237. 2011
    ..Whether mycolactone diffuses from ulcerated lesions in clinically accessible samples and is modulated by antibiotic therapy remained to be established...
  68. pmc Heat shock protein 90 homeostasis controls stage differentiation in Leishmania donovani
    M Wiesgigl
    Bernhard Nocht Institute for Tropical Medicine, D-20359 Hamburg, Germany
    Mol Biol Cell 12:3307-16. 2001
    ..Our results are consistent with Hsp90 homeostasis serving as cellular thermometer for these primitive eukaryotes, controlling both the heat shock response and morphological differentiation...
  69. ncbi Mycolactone inhibits monocyte cytokine production by a posttranscriptional mechanism
    Rachel E Simmonds
    Cytokine and Signal Transduction Laboratory, Kennedy Institute of Rheumatology Division, London, United Kingdom
    J Immunol 182:2194-202. 2009
    ..The current findings also suggest that monocyte-derived cytokine transcript and protein levels may not correlate in Buruli ulcer lesions, and urge caution in the interpretation of RT-PCR data obtained from patient biopsy samples...
  70. ncbi Macrolide-resistant Mycoplasma pneumoniae: characteristics of isolates and clinical aspects of community-acquired pneumonia
    Miyuki Morozumi
    Laboratory of Molecular Epidemiology for Infectious Agents, Graduate School of Infection Control Sciences, Kitasato Institute for Life Sciences, Kitasato University, 5 9 1 Shirokane, Minatoku, Tokyo, 108 8641, Japan
    J Infect Chemother 16:78-86. 2010
    ..pneumoniae for many years. In 2000, however, M. pneumoniae showing resistance to macrolides was isolated from clinical samples obtained from Japanese pediatric patients with community-acquired pneumonia (..
  71. ncbi Mycolactone suppresses T cell responsiveness by altering both early signaling and posttranslational events
    Sheerazed Boulkroun
    Unité Postulante Pathogénomique Mycobactérienne Intégrée, Institut Pasteur, Paris, France
    J Immunol 184:1436-44. 2010
    ..Mycolactone thus constitutes a novel type of T cell immunosuppressive agent, the potent activity of which may explain the defective cellular responses in Buruli ulcer patients...
  72. ncbi Uptake and cellular actions of mycolactone, a virulence determinant for Mycobacterium ulcerans
    D Scott Snyder
    Rocky Mountain Laboratories, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Hamilton, MT 59840, USA
    Microb Pathog 34:91-101. 2003
    ..Mitochondrial polarization is maintained in treated cells for up to 3 days arguing that the rise in intracellular calcium levels may be a result of cytoskeletal remodeling...
  73. ncbi Combination antibiotic therapy with macrolides improves survival in intubated patients with community-acquired pneumonia
    I Martin-Loeches
    Critical Care Department, Mater Misericordiae University Hospital, Dublin, Ireland
    Intensive Care Med 36:612-20. 2010
    To assess the effect on survival of macrolides or fluoroquinolones in intubated patients admitted to the intensive care unit (ICU) with severe community-acquired pneumonia (severe CAP).
  74. ncbi A spinosyn-sensitive Drosophila melanogaster nicotinic acetylcholine receptor identified through chemically induced target site resistance, resistance gene identification, and heterologous expression
    Gerald B Watson
    Dow AgroSciences LLC, Discovery Research, 9330 Zionsville Road, Indianapolis, IN 46268, USA
    Insect Biochem Mol Biol 40:376-84. 2010
    ....
  75. pmc Heterogeneity of mycolactones produced by clinical isolates of Mycobacterium ulcerans: implications for virulence
    Armand Mve-Obiang
    Institute of Tropical Medicine, B 2000 Antwerp, Belgium
    Infect Immun 71:774-83. 2003
    ..A cytopathic assay of the core lactone showed that this molecule is sufficient for cytotoxicity, although it is much less potent than the complete mycolactone...
  76. pmc Antibiotic selection pressure and macrolide resistance in nasopharyngeal Streptococcus pneumoniae: a cluster-randomized clinical trial
    Alison H Skalet
    Francis I Proctor Foundation for Research in Opthalmology, University of California, San Francisco, San Francisco, California, United States of America
    PLoS Med 7:e1000377. 2010
    ..In this study, we used a randomized clinical trial design to assess whether macrolide resistance was higher in communities treated with mass azithromycin for trachoma, compared to untreated control communities...
  77. pmc Mycolactone diffuses from Mycobacterium ulcerans-infected tissues and targets mononuclear cells in peripheral blood and lymphoid organs
    Hui Hong
    University of Cambridge, Department of Biochemistry, Cambridge, United Kingdom
    PLoS Negl Trop Dis 2:e325. 2008
    ..The defective inflammatory responses in BU lesions reflect these biological properties of the toxin. However, whether mycolactone diffuses from infected tissues and suppresses IFN-gamma responses in BU patients remains unclear...
  78. ncbi Inhibition of macroautophagy by bafilomycin A1 lowers proliferation and induces apoptosis in colon cancer cells
    Ya Chun Wu
    Department of Gastroenterology, The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, PR China
    Biochem Biophys Res Commun 382:451-6. 2009
    ..Our results not only indicate that inhibitors of macroautophagy may be used therapeutically to inhibit cancer growth, but also delineate the relationship between macroautophagy and apoptosis...
  79. ncbi The chemistry and biology of the bryostatin antitumour macrolides
    Karl J Hale
    Christopher Ingold Laboratories, Department of Chemistry, University College London, 20 Gordon Street, London, UK WC1H 0AJ
    Nat Prod Rep 19:413-53. 2002
    ..This review summarises the main developments that have occurred in bryostatin chemistry over the period 1982 to 2001 and has 117 references...
  80. ncbi Effects of orally administered spinosad (Comfortis) in dogs on adult and immature stages of the cat flea (Ctenocephalides felis)
    Byron L Blagburn
    Auburn University, Auburn, AL, USA
    Vet Parasitol 168:312-7. 2010
    ....
  81. ncbi Macrolide-ketolide inhibition of MLS-resistant ribosomes is improved by alternative drug interaction with domain II of 23S rRNA
    S Douthwaite
    Department of Molecular Biology, Odense University, DK 5230 Odense M, Denmark
    Mol Microbiol 36:183-93. 2000
    ....
  82. ncbi Mutations in subunit C of the vacuolar ATPase confer resistance to bafilomycin and identify a conserved antibiotic binding site
    Barry J Bowman
    Department of Molecular, University of California, Santa Cruz, California 95064, USA
    J Biol Chem 277:3965-72. 2002
    ....
  83. ncbi Eukaryotic initiation factor 2alpha-independent pathway of stress granule induction by the natural product pateamine A
    Yongjun Dang
    Department of Pharmacology and Molecular Sciences, Solomon H Snyder Department of Neuroscience, and Department of Oncology, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA
    J Biol Chem 281:32870-8. 2006
    ....
  84. ncbi Antimicrobial treatment guidelines for acute bacterial rhinosinusitis
    Jack B Anon
    University of Pittsburgh, School of Medicine, USA
    Otolaryngol Head Neck Surg 130:1-45. 2004
  85. ncbi Macrolide resistance in Campylobacter jejuni and Campylobacter coli
    Amera Gibreel
    Department of Medical Microbiology and Immunology, University of Alberta Edmonton, Alberta, Canada
    J Antimicrob Chemother 58:243-55. 2006
    ..However, erythromycin-resistant Campylobacter have emerged during therapy with macrolides. Moreover, the widespread use of macrolides, including erythromycin, in veterinary medicine has accelerated this ..
  86. ncbi Colonization of the salivary glands of Naucoris cimicoides by Mycobacterium ulcerans requires host plasmatocytes and a macrolide toxin, mycolactone
    Laurent Marsollier
    Unite de Genetique Moleculaire Bacterienne, Institut Pasteur, Paris, France
    Cell Microbiol 7:935-43. 2005
    ..ulcerans isolates are able to invade the salivary glands, a site where they proliferate. Later, the raptorial legs of Naucoris are covered by M. ulcerans-containing material that displays features of biofilms...
  87. pmc Mycolactones: immunosuppressive and cytotoxic polyketides produced by aquatic mycobacteria
    Hui Hong
    Department of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge, CB2 1GA, UK
    Nat Prod Rep 25:447-54. 2008
    ..This Highlight summarizes recent progress in understanding the structural diversity of the mycolactones, their biological activity and mode of action in mammalian cells, and the genetics, evolution, and enzymology of their biosynthesis...
  88. ncbi The membrane potential of the intraerythrocytic malaria parasite Plasmodium falciparum
    Richard J W Allen
    School of Biochemistry and Molecular Biology, Faculty of Science, Australian National University, Canberra, Australian Capital Territory 0200, Australia
    J Biol Chem 279:11264-72. 2004
    ..The current associated with the efflux of H(+) is countered, in part, by the influx of K(+) via Ba(2+)- and Cs(+)-sensitive K(+) channels in the parasite plasma membrane...
  89. ncbi Desensitizing and non-desensitizing subtypes of alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors in cockroach neurons
    Vincent L Salgado
    Bayer CropScience AG, Global Biology Insecticides, Alfred Nobel Strasse 50, D 40789 Monheim am Rhein, Germany
    J Insect Physiol 50:867-79. 2004
    ..Spinosyn A weakly antagonizes nAChD receptors -23% at 10 microM. The roles of the two nAChR subtypes in insecticide poisoning are discussed...
  90. ncbi Phase II study of eribulin mesylate, a halichondrin B analog, in patients with metastatic breast cancer previously treated with an anthracycline and a taxane
    Linda T Vahdat
    Weill Medical College of Cornell University, Division of Hematology Oncology, New York, NY 10021, USA
    J Clin Oncol 27:2954-61. 2009
    ..This open-label, single-arm, phase II study evaluated efficacy and tolerability of eribulin in heavily pretreated patients with metastatic breast cancer (MBC)...
  91. pmc Distribution of genes encoding resistance to macrolides, lincosamides, and streptogramins among staphylococci
    G Lina
    Faculte de Medecine, Laboratoire de Bacteriologie, Centre national de référence des toxémies à staphylocoques, EA 1655, 69372 Lyon Cedex 08, France
    Antimicrob Agents Chemother 43:1062-6. 1999
    The relative frequency of 10 determinants of resistance to macrolides, lincosamides, and streptogramins was investigated by PCR in a series of 294 macrolide-, lincosamide-, and/or streptogramin-resistant clinical isolates of ..
  92. ncbi Storage and release of ATP from astrocytes in culture
    Silvia Coco
    Consiglio Nazionale delle Ricerche Institute of Neuroscience, Cellular and Molecular Pharmacology, Department of Medical Pharmacology, University of Milano, Italy
    J Biol Chem 278:1354-62. 2003
    ..They also suggest that ATP-storing vesicles may be distinct from glutamate-containing vesicles, thus opening up the possibility that their exocytosis is regulated differently...
  93. ncbi Resistance among Streptococcus pneumoniae: Implications for drug selection
    Peter C Appelbaum
    Departments of Pathology and Clinical Microbiology, Milton S Hershey Medical Center, Pennsylvania State University College of Medicine, Hershey, PA, 17033, USA
    Clin Infect Dis 34:1613-20. 2002
    ..Efforts should be made to prevent pneumococcal infections in high-risk patients through vaccination...
  94. ncbi Pathogenetic mechanisms of the intracellular parasite Mycobacterium ulcerans leading to Buruli ulcer
    Manuel T Silva
    IBMC Instituto de Biologia Molecular e Celular, Universidade do Porto, Rua do Campo Alegre 823, Porto 4150 180, Portugal
    Lancet Infect Dis 9:699-710. 2009
    ....
  95. ncbi Macrolide antibiotics as immunomodulatory medications: proposed mechanisms of action
    Masaharu Shinkai
    Ministry of Defense and National Defense Medical College, Japan
    Pharmacol Ther 117:393-405. 2008
    ..b>Macrolides initially decrease, then increase, and have finally a sustained suppression of cytokine secretions from normal ..
  96. ncbi The mechanism of action of macrolides, lincosamides and streptogramin B reveals the nascent peptide exit path in the ribosome
    Tanel Tenson
    Institute of Technology, Tartu University, Riia 23, Tartu 51010, Estonia
    J Mol Biol 330:1005-14. 2003
    ..We have studied the mechanisms of action of four macrolides (erythromycin, josamycin, spiramycin and telithromycin), one lincosamide (clindamycin) and one streptogramin B (..
  97. ncbi Mode of action of long-term low-dose macrolide therapy for chronic sinusitis in the light of neutrophil recruitment
    Hideaki Suzuki
    Department of Otolaryngology, Sendai National Hospital, Sendai, Japan
    Curr Drug Targets Inflamm Allergy 1:117-26. 2002
    ..In the 1990's it was also shown to be an effective treatment for chronic sinusitis. The inhibitory effect of macrolides on neutrophil infiltration in inflammatory sites has been well documented in these diseases...
  98. ncbi Macrolide-resistant Streptococcus pyogenes in the United States, 2002-2003
    Sandra S Richter
    Department of Pathology, University of Iowa Carver College of Medicine, Iowa City, IA 52242 1009, USA
    Clin Infect Dis 41:599-608. 2005
    ..pyogenes isolates from throughout the United States and to elucidate the mechanisms of resistance and genetic relatedness of macrolide-resistant isolates...
  99. ncbi A double-blind, randomized, placebo-controlled trial of macrolide in the treatment of chronic rhinosinusitis
    Ben Wallwork
    School of Biomolecular and Biomedical Science, Griffith University, and Princess Alexandria Hospital, Brisbane, Australia
    Laryngoscope 116:189-93. 2006
    ..Several studies have suggested that long-term, low-dose macrolides may be efficacious in the treatment of chronic rhinosinusitis; however, these studies have lacked a control ..
  100. pmc Toll-like receptor-mediated activation of neutrophils by influenza A virus
    Jennifer P Wang
    Department of Medicine, University of Massachusetts Medical School, Worcester, MA 01605, USA
    Blood 112:2028-34. 2008
    ..These studies demonstrate neutrophil activation by influenza virus and highlight the importance of TLR7 and TLR8 in that response...
  101. pmc Ligand-regulated transport of the Menkes copper P-type ATPase efflux pump from the Golgi apparatus to the plasma membrane: a novel mechanism of regulated trafficking
    M J Petris
    Department of Genetics, University of Melbourne, Parkville, Victoria, Australia
    EMBO J 15:6084-95. 1996
    ....

Research Grants64

  1. Novel Macrolide Th17 Inhibitors
    Jay K Kolls; Fiscal Year: 2012
    ..CyA, FK- 506, and rapamycin suppressed both Th1 and Th17 cells and thus were non-selective. However macrolides, specifically Azithromycin showed dose dependent suppression of Th17 development with an ED50 of approximately ..
  2. Functional Consequence of Macrolide Resistance Mutations in T. pallidum
    Sheila A Lukehart; Fiscal Year: 2012
    ..the rabbit syphilis model demonstrated the effectiveness of azithromycin, an oral azalide antibiotic related to macrolides, for treating syphilis caused by the Nichols strain of T. pallidum...
  3. Effect of Macrolide Treatment on a Novel Pathway of Neutrophilic Inflammation in
    J Edwin Blalock; Fiscal Year: 2010
    ..COPD patients, both taking azithromycin and controls, thereby providing a scientific basis for the activity of macrolides in COPD...
  4. 2012 New Antibacterial Drug Discovery and Development Gordon Research Conference
    Shahriar Mobashery; Fiscal Year: 2012
    ..Other effective agents, such as macrolides, have resistance rates on the order of 40%...
  5. Azithromycin to prevent BPD in Ureaplasma-infected Preterms: Single Dose PK study
    Rose Viscardi; Fiscal Year: 2009
    ..The new 14-membered macrolides and the related 15-member azalides have immunomodulatory effects, including effects on neutrophil function and ..
  6. 2010 New Antimicrobial Drug Discovery and Development Gordon Research Conference
    GEORGE LOUIS DRUSANO; Fiscal Year: 2010
    ..Other effective agents, such as macrolides, have resistance rates on the order of 40%...
  7. Emerging Macrolide Resistance in Mycoplasma Pneumoniae
    THOMAS PRESCOTT ATKINSON; Fiscal Year: 2010
    ..At present three classes of drugs are used to treat M. pneumoniae infections: macrolides, tetracyclines, and fluoroquinolones...
  8. A New Approach for Engineering Polyketides by Cytochrome P450 C-H Oxidation
    ROBERT VINCENT O'BRIEN; Fiscal Year: 2013
    ..their biologically activity, and cytochrome P450 monooxygenases often act to site-selectively oxidize polyketide macrolides following their biosynthesis...
  9. GONOCOCCI: GENETICS OF RESISTANCE TO PMN PROTEINS
    WILLIAM MAURICE SHAFER; Fiscal Year: 2013
    ..our work has shown that the MtrC-MtrD-MtrE efflux pump participates in gonococcal resistance to penicillin and macrolides. This efflux pump also recognizes host antimicrobials, such as antimicrobial peptides and progesterone...
  10. Mechanism of Induction of erm Genes By Ketolide Antibiotics
    Nora Vazquez Laslop; Fiscal Year: 2010
    ..The expression of many of the erm genes, including ermC, is inducible by macrolides. The proposed mechanism of induction is based on the programmed ribosome stalling at the regulatory cistron, ..
  11. NUCLEIC ACID PROBES OF RIBOSOMAL STRUCTURE AND FUNCTION
    BARRY COOPERMAN; Fiscal Year: 2003
    ..Many antibiotics in current clinical use, such as tetracycline, erythromycin and other macrolides, neomycin and other aminoglycosides, and chloramphenicol target ribosomes as their sites of action...
  12. Macrolide Accumulation by Host Cells in the Gingiva
    John D Walters; Fiscal Year: 2010
    ..We hypothesize that gingival fibroblasts, epithelial cells and PMNs possess active transporters that accumulate macrolides. These transporters play a beneficial role by enhancing macrolide levels in the soft tissue wall of the ..
  13. Hygromycin A: Activity, Biosynthesis, Export, Resistance and Regulation
    Kevin A Reynolds; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): Many clinically important classes of antibiotics, including macrolides (azithromycin, telithromycin), tetracyclines, aminoglycosides (gentamycin), and more recently oxazolidinones (linezolid) target ..
  14. Molecular bssis of mef-mediated antibiotic resistance in Streptococcus pneumoniae
    David S Stephens; Fiscal Year: 2010
    ..are both required for macrolide resistance, work in concert, are coordinately regulated, and are inducible by macrolides. Mega element homologs have now been found in Tn1207.1, Tn1207.3, Tn2009 in S...
  15. Diversity-Oriented Synthesis of Natural Product-based Libraries for the MLSMR
    Derek S Tan; Fiscal Year: 2012
    ..1) aliphatic and benzannulated spiroketals, (2) complex polyketides and peptide-polyketide hybrids, (3) macrolides and related macrocycles, (4) polycyclic alkaloid/terpenoid-like molecules...
  16. Impact of Unapproved Drug Initiative on Colchicine Use
    Eswar Krishnan; Fiscal Year: 2013
    ..evidence of significant interactions between colchicine and other commonly used medications such as statins and macrolides. In 2009 the FDA provided approval and market exclusivity for a single agent colchicine preparation (Colcrys(R)) ..
  17. Novel antibacterials targeting the 50S ribosomal subunit
    Joyce Sutcliffe; Fiscal Year: 2005
    ..Looking ahead, this agent would cover strains that have resistance to macrolides, quinolones, vancomycin, ¿-lactams, Synercid(r), and Linezolid...
  18. Effect of macrolides as immunomodulators in patients with sepsis and pneumonia
    Marcos I Restrepo; Fiscal Year: 2013
    ..The approach is innovative, because it utilizes macrolides as immunomodulators for an indication other than community-acquired pneumonia in order to improve outcomes in ..
  19. Molecular mechanisms of action of macrolide antibiotics
    Nora Vazquez-Laslop; Fiscal Year: 2013
    ..macrolide action, our preliminary studies showed that treatment of Gram-positive and Gram-negative bacteria with macrolides allows for continued translation of a defined subset of proteins...
  20. M AVIUM IMMUNE RESPONSES--IMPLICATIONS FOR THERAPY
    W Boom; Fiscal Year: 1999
    ..Concern for emergence of MAC resistance to macrolides, inability to determine who is at risk for disseminated MAC disease, and whether potent anti-retroviral therapy ..
  21. Stringent control of virulence gene expression in Pseudomonas aeruginosa
    Martin Schuster; Fiscal Year: 2009
    ..Our proposed research will provide important insights into the function of macrolides as anti-quorum sensing drugs. It will help elucidate the molecular components necessary for P...
  22. MACROLIDE TOTAL SYNTHESIS
    AMOS SMITH; Fiscal Year: 1990
    ..The latrunculins (A and B) represent a new class of highly potent macrolides that specifically bind to cytoskeletal proteins and thereby disrupt microfilament organization in cultured cells ..
  23. Strategies to Prevent COPD Exacerbation
    Fernando Martinez; Fiscal Year: 2007
    ..It is likely that infection is an important trigger of airway inflammation in COPD. The 14 and 15 membered macrolides have been demonstrated to exhibit important, anti-inflammatory effects...
  24. Target for Mefloquine in Mycobacteria
    Luiz Bermudez; Fiscal Year: 2002
    ..avium activity in humans, such as the new macrolides, treatment or prolonged prophylaxis of disseminated disease selects resistant mutants after a course of ..
  25. APPLICATIONS OF IRON COMPLEXES TO ORGANIC SYNTHESIS
    William Donaldson; Fiscal Year: 2001
    ..This new methodology will be useful for the preparation of polyene macrolides and for the preparation of cyclopropane containing natural products...
  26. GLOBAL REGULATORS OF SECONDARY METABOLISM
    Andrew Reeves; Fiscal Year: 2000
    ..An important class of antibiotics which have been in increasing demand are the macrolides. Erythromycin is the most extensively produced of the macrolides, and the producer of erythromycin, ..
  27. COMBINATORIAL BIOSYNTHESIS OF MACROLIDE ANTIBIOTICS
    CHARLES SIH; Fiscal Year: 2001
    ..of the deoxysugar biosynthesis genes, explore the possibility of making new analogs of erythromycin and related macrolides and of novel erythronolide B analogs prepared at Kosan Biosciences...
  28. MOLECULAR ANALYSIS OF POLYKETIDE SYNTHASE GENES
    David Hopwood; Fiscal Year: 1990
    ..polyketide family of antibiotics includes such medically important compounds as tetracyclines, anthracyclines, macrolides and others...
  29. NEW ANTIMICROTUBULE AGENTS FROM MARINE ORGANISMS
    Bradley Davidson; Fiscal Year: 2001
    ..Utah State University and the Cancer Research Center of Hawaii, we have discovered that the sponge- derived macrolides laulimalide and isolaulimalide are potent cytotoxins with paclitaxel-like anti-microtubule-stabilizing activity...
  30. Novel Macrolide and Ketolide Antibiotic Intermediates
    J Weber; Fiscal Year: 2003
    ..b>Macrolides are effective in the treatment of respirtory infections...
  31. Mechanisms of macrolide resistance in mycobacteria
    Kevin A Nash; Fiscal Year: 2010
    ..cornerstones of prophylaxis and treatment of infections caused by non-tuberculosis mycobacteria (NTM) are the macrolides, clarithromycin and azithromycin...
  32. Mycolactone-Mediated Virulence in M. ulcerans
    Pamela Small; Fiscal Year: 2005
    ..A polyketide-derived macrolide toxin designated mycolactone has been identified in M ulcerans. Macrolides are produced as secondary metabolites by soil bacteria and fungi...
  33. novel macrolides as anti-infective drugs
    Charles Hutchinson; Fiscal Year: 2007
    ..which differ from erythromycins solely via an additional sugar attached at C6 of the macrolide) were the first macrolides to display notable antiviral and antiparasitic activities...
  34. SYNTHESES OF MACROLIDES AND RELATED NATURAL PRODUCTS
    FREDERICK ZIEGLER; Fiscal Year: 1992
    ..All of these projects are currently under investigation...
  35. SYNTHESIS OF STEROID HORMONES AND ACYCLIC SYSTEMS
    Masato Koreeda; Fiscal Year: 1991
    ..and other natural 1,3,5- trimethylated carbon chains which can be used as building blocks of the antibiotic macrolides, (4) use of [2,3]-Wittig and [3,3-Claisen rearrangements for the stereocontrolled synthesis of the 1,3,5- ..
  36. SYNTHESIS OF BIOACTIVE MACROLIDES
    James White; Fiscal Year: 2002
    ..structures towards which this synthetic effort is directed are naturally occurring macrocyclic lactones (macrolides), all of which possess striking biological properties of potential chemotherapeutic value...
  37. SYNTHESIS OF THE ANTITUMOR MACROLIDE SPONGISTATIN 1
    ANATOLY PINCHUK; Fiscal Year: 2001
    ..The first representative of this class of macrolides, spongistatin 1, is claimed to be the most extraordinary potent substance presently known against a subset of ..
  38. Versatile diversity-oriented small molecule libraries for Chemogenetics
    Stuart Schreiber; Fiscal Year: 2007
    ..The selected libraries are based on a) macrolides of varying ring size, b) natural product-like spirooxoindol core structures and c) a dihydropyran carboxamide ..
  39. SYNTHESIS OF MACROLIDE ANTIBIOTICS
    James White; Fiscal Year: 1992
    ..Synthetic pathways to five macrolides will be investigated, each of which seeks to elaborate, in a stereo- controlled fashion, the complete molecular ..
  40. SALICYLIHALAMIDES--CHEMISTRY AND BIOLOGY
    Gunda Georg; Fiscal Year: 2000
    ..They are structurally novel 12-membered salicylate macrolides, carrying an unusual unsaturated enamide side chain at C15...
  41. NOVEL ANTIBIOTICS FROM CYTOSPORA
    ROBERT RONALD; Fiscal Year: 1980
    ..Although there are certain structural similarities with Erythromycin and other macrolides our chemical structure studies have shown that the novel Grahamimycins are a unique new class of macrodiolide ..
  42. Combinatorial Macrolide GPCR Screening Library
    Brian Metcalf; Fiscal Year: 2001
    ..This proposal is thus directed towards the synthesis of a library of macrolides using high-speed parallel synthesis...
  43. Natural feedstocks for diversity oriented synthesis
    Dennis Wright; Fiscal Year: 2004
    ..The main focus will relate to the synthesis of a new class of macrolides known as the nonactolides...
  44. GENETIC DESIGNS FOR HIGH-EFFICIENCY MACROLIDE PRODUCTION
    J Weber; Fiscal Year: 1993
    The macrolides are microbial natural products with many uses in clinical and veterinary medicine. Erythromycin is the best studied example of a macrolide antibiotic; rapamycin and FK506 are promising new immunosuppressant macrolides...
  45. Macrolide Discovery through Glycosylation
    Alex Romero; Fiscal Year: 2004
    ..of the 16-membered macrolide, which are active against the MLS8 resistant phenotype, into a the15-membered macrolides (for example, introducing a disaccharide at the 5-OH position of a 15-membered macrolide), could result in ..
  46. A Direct Aldol Strategy toward B-Type Amphidinolides
    Brandon Turunen; Fiscal Year: 2006
    DESCRIPTION (provided by applicant): The amphidinolides are a family of complex macrolides exhibiting potent and unique antitumor activity. The B-type amphidinolides represent promising leads in the search for new chemotherapeutic agents...
  47. ANTITUMOR, ANTIVIRAL AGENTS IN MICROALGAE
    Yuzuru Shimizu; Fiscal Year: 1993
    ..Anticipated compounds include polyethers, macrolides, and other polyoxygenated compounds...
  48. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  49. Fermentation initiated antibiotic synthesis
    STEPHEN BERGMEIER; Fiscal Year: 2005
    ..approach stands is the assumption that the sugar mimetics that we will use will provide biologically active new macrolides. This Phase I STTR project is focused on demonstrating the first 2 steps of our program: Preparation of small ..
  50. SYNTHETIC STUDIES RELATED TO CANCER RESEARCH/TREATMENT
    Paul Wender; Fiscal Year: 2005
    ..Overall, this research program is expected to be of significant value in chemistry, biology, and medicine. ..
  51. SYNTHETIC STUDIES ON THE POLYENE MACROLIDE ANTIBIOTICS
    GLENN MC GARVEY; Fiscal Year: 1991
    ..As synthetic methodology is developed, access to increasingly diverse analogs to the natural polyene macrolides becomes available to test the structural features of these compounds that lead to selective binding with certain ..
  52. Improving Glycosyltransferase by RACHITT Gene Shuffling
    Yongquan Xue; Fiscal Year: 2001
    ..to provide glycosyltransferase enzymes that can catalyze the biosynthesis of 12-, 14-, and 16-membered ring macrolides. Moreover, we expect to generate a recombinant DesVII that has a higher enzymatic activity toward the 14-..
  53. Nanoscale-Natural Products Chemistry
    TADEUSZ MOLINSKI; Fiscal Year: 2009
    ..g. caylobolide A). Aim 2 will exploit CD methods for stereochemical elucidation of chlorocyclopropane-containing macrolides, such as that found in callipeltosides A-C and the new analogs, phorbasides A-E, at sub-nanomole levels...
  54. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  55. TOTAL SYNTHESIS OF MACROLIDES
    K Nicolaou; Fiscal Year: 1992
    ..These compounds exhibit potent antifungal (nystatin) and antitumor activities (nystatin and halichondrin B)...
  56. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  57. Macrolide Discovery through Glycosylation
    Alex Romero; Fiscal Year: 2006
    ..resistance development and the potential for cross-resistance between our lead compounds and other leading macrolides/ketolides, an important criteria for assessing a compound's future marketability...
  58. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  59. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  60. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  61. Synthesis of the Anti-tumor Marcrolide Amphidinolide C
    JOHN SHOTWELL; Fiscal Year: 2004
    ..The amphidinolides, a structurally diverse group of over 30 macrolides, exhibit potent and selective anti-tumor profiles...
  62. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
  63. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
    ..abstract_text> ..
  64. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
    ....