mardi 26 mai 2015

13-Deoxytetrodecamycin, a new tetronate ring-containing antibiotic that is active against multidrug-resistant Staphylococcus aureus

13-Deoxytetrodecamycin, a new tetronate ring-containing antibiotic that is active against multidrug-resistant Staphylococcus aureus

The Journal of Antibiotics advance online publication, May 27 2015. doi:10.1038/ja.2015.60

Authors: Tomas Gverzdys, Michael Kamin Hart, Sheila Pimentel-Elardo, Geoffrey Tranmer & Justin R Nodwell



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First total synthesis of (+)-epogymnolactam, a novel autophagy inducer

First total synthesis of (+)-epogymnolactam, a novel autophagy inducer

The Journal of Antibiotics advance online publication, May 27 2015. doi:10.1038/ja.2015.63

Authors: Yuji Okado, Kengo Shigetomi, Shinya Mitsuhashi & Makoto Ubukata



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mercredi 20 mai 2015

Classification of group B streptococci with reduced {beta}-lactam susceptibility (GBS-RBS) based on the amino acid substitutions in PBPs

All clinical isolates of group B Streptococcus (GBS; Streptococcus agalactiae) are considered uniformly susceptible to β-lactams, including penicillins. However, GBS with reduced penicillin susceptibility (PRGBS) were first identified by our group in Japan and have also been reported from North America. PRGBS are non-susceptible to penicillin because of acquisition of amino acid substitutions near the conserved active-site motifs in PBP2X. In particular, V405A and Q557E are considered the key amino acid substitutions responsible for penicillin non-susceptibility. We revealed that in addition to the substitutions in PBP2X, an amino acid substitution in PBP1A confers high-level cephalosporin resistance in GBS. As the number of publications on GBS with reduced β-lactam susceptibility (GBS-RBS), especially PRGBS, and concomitantly the need for a systematic classification of GBS-RBS is increasing, we propose here a classification of GBS-RBS based on the amino acid substitutions in their PBPs.



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Antibiotic research and development: business as usual?

The global burden of antibiotic resistance is tremendous and, without new anti-infective strategies, will continue to increase in the coming decades. Despite the growing need for new antibiotics, few pharmaceutical companies today retain active antibacterial drug discovery programmes. One reason is that it is scientifically challenging to discover new antibiotics that are active against the antibiotic-resistant bacteria of current clinical concern. However, the main hurdle is diminishing economic incentives. Increased global calls to minimize the overuse of antibiotics, the cost of meeting regulatory requirements and the low prices of currently marketed antibiotics are strong deterrents to antibacterial drug development programmes. New economic models that create incentives for the discovery of new antibiotics and yet reconcile these incentives with responsible antibiotic use are long overdue. DRIVE-AB is a 9.4 million public–private consortium, funded by the EU Innovative Medicines Initiative, that aims to define a standard for the responsible use of antibiotics and to develop, test and recommend new economic models to incentivize investment in producing new anti-infective agents.



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Chloroquine analogues in drug discovery: new directions of uses, mechanisms of actions and toxic manifestations from malaria to multifarious diseases

Antimalarial drugs (e.g. chloroquine and its close structural analogues) were developed primarily to treat malaria; however, they are beneficial for many dermatological, immunological, rheumatological and severe infectious diseases, for which they are used mostly today. Chloroquine and hydroxychloroquine, two of the most fascinating drugs developed in the last 50 years, are increasingly recognized for their effectiveness in myriad non-malarial diseases. In advanced research, chloroquine and hydroxychloroquine have been shown to have various immunomodulatory and immunosuppressive effects, and currently have established roles in the management of rheumatic diseases, lupus erythematosus (different forms) and skin diseases, and in the treatment of different forms of cancer. Recently, chloroquine analogues have also been found to have metabolic, cardiovascular, antithrombotic and antineoplastic effects. This review is concerned with the lysosomotropic, anti-inflammatory and immunomodulatory mechanisms of chloroquine, hydroxychloroquine, quinacrine and related analogues, and the current evidence for both their beneficial effects and potential adverse manifestations in various diseases.



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MRSA carrying mecC in captive mara

Wide dissemination of linezolid-resistant Staphylococcus epidermidis in Greece is associated with a linezolid-dependent ST22 clone

Linezolid resistance in clinical isolates of Staphylococcus epidermidis from German hospitals and characterization of two cfr-carrying plasmids

CTX-M-27- and CTX-M-14-producing, ciprofloxacin-resistant Escherichia coli of the H30 subclonal group within ST131 drive a Japanese regional ESBL epidemic

Selection and molecular characterization of ceftazidime/avibactam-resistant mutants in Pseudomonas aeruginosa strains containing derepressed AmpC

Systematic analysis of the role of bacterial Hfq-interacting sRNAs in the response to antibiotics

Multicentre evaluation of the Check-Direct CPE(R) assay for direct screening of carbapenemase-producing Enterobacteriaceae from rectal swabs

NICTABA and UDA, two GlcNAc-binding lectins with unique antiviral activity profiles

Small molecule inhibitors of the annexin A2 heterotetramer prevent human papillomavirus type 16 infection

Tetrahydroisoquinolines affect the whole-cell phenotype of Mycobacterium tuberculosis by inhibiting the ATP-dependent MurE ligase

In vitro activity of gentamicin, vancomycin or amikacin combined with EDTA or L-arginine as lock therapy against a wide spectrum of biofilm-forming clinical strains isolated from catheter-related infections

Modulation of the activity of moxifloxacin and solithromycin in an in vitro pharmacodynamic model of Streptococcus pneumoniae naive and induced biofilms

Novel synthetic bis-indolic derivatives with antistaphylococcal activity, including against MRSA and VISA strains

{beta}-Lactam combinations with daptomycin provide synergy against vancomycin-resistant Enterococcus faecalis and Enterococcus faecium

Surveillance of antibiotic susceptibility of urinary tract pathogens for a population of 5.6 million over 4 years

In vitro susceptibility of Clostridium difficile to SMT19969 and comparators, as well as the killing kinetics and post-antibiotic effects of SMT19969 and comparators against C. difficile

SMT19969 for Clostridium difficile infection (CDI): in vivo efficacy compared with fidaxomicin and vancomycin in the hamster model of CDI

A novel chimeric phage lysin with high in vitro and in vivo bactericidal activity against Streptococcus pneumoniae

Synergy of chemotherapy and immunotherapy revealed by a genome-scale analysis of murine tuberculosis

Anti-CD81 but not anti-SR-BI blocks Plasmodium falciparum liver infection in a humanized mouse model

Aryl hydantoin Ro 13-3978, a broad-spectrum antischistosomal

Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol

Extracorporeal clearance of colistin methanesulphonate and formed colistin in end-stage renal disease patients receiving intermittent haemodialysis: implications for dosing

A Phase I study to assess the safety, tolerability and pharmacokinetic profile of boceprevir and sildenafil when dosed separately and together, in healthy male volunteers

Increased systemic immune activation and inflammatory profile of long-term HIV-infected ART-controlled patients is related to personal factors, but not to markers of HIV infection severity

Circulating fibroblast growth factor 23 (FGF23) levels are associated with metabolic disturbances and fat distribution but not cardiovascular risk in HIV-infected patients

Safety and immunogenicity of a modified vaccinia Ankara-based HIV-1 vaccine (MVA-B) in HIV-1-infected patients alone or in combination with a drug to reactivate latent HIV-1

mardi 19 mai 2015

Identification of small-molecule inhibitors against SecA by structure-based virtual ligand screening

Identification of small-molecule inhibitors against SecA by structure-based virtual ligand screening

The Journal of Antibiotics advance online publication, May 20 2015. doi:10.1038/ja.2015.53

Authors: Evelien De Waelheyns, Kenneth Segers, Marios Frantzeskos Sardis, Jozef Anné, Gerry A F Nicolaes & Anastassios Economou



from The Journal of Antibiotics - AOP - nature.com science feeds http://ift.tt/1R2nLRH

Inhibitory activities of the marine streptomycete-derived compound SF2446A2 against Chlamydia trachomatis and Schistosoma mansoni

Inhibitory activities of the marine streptomycete-derived compound SF2446A2 against Chlamydia trachomatis and Schistosoma mansoni

The Journal of Antibiotics advance online publication, May 20 2015. doi:10.1038/ja.2015.54

Authors: Anastasija Reimer, Ariane Blohm, Thomas Quack, Christoph G Grevelding, Vera Kozjak-Pavlovic, Thomas Rudel, Ute Hentschel & Usama Ramadan Abdelmohsen



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Synthesis and antibacterial activity of 4″ or 6″-alkanoylamino derivatives of arbekacin

Synthesis and antibacterial activity of 4″ or 6″-alkanoylamino derivatives of arbekacin

The Journal of Antibiotics advance online publication, May 20 2015. doi:10.1038/ja.2015.61

Authors: Kazushige Sasaki, Yoshihiko Kobayashi, Takashi Kurihara, Yohei Yamashita, Yoshiaki Takahashi, Toshiaki Miyake & Yuzuru Akamatsu



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Evaporative light scattering quantification of natural products possessing a carbon–phosphorus bond

Evaporative light scattering quantification of natural products possessing a carbon–phosphorus bond

The Journal of Antibiotics advance online publication, May 20 2015. doi:10.1038/ja.2015.62

Authors: Matthew C Chi & Geoff P Horsman



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mardi 12 mai 2015

Botryoisocoumarin A, a new COX-2 inhibitor from the mangrove Kandelia candel endophytic fungus Botryosphaeria sp. KcF6

Botryoisocoumarin A, a new COX-2 inhibitor from the mangrove Kandelia candel endophytic fungus Botryosphaeria sp. KcF6

The Journal of Antibiotics advance online publication, May 13 2015. doi:10.1038/ja.2015.46

Authors: Zhiran Ju, Xiuping Lin, Xin Lu, Zhengchao Tu, Junfeng Wang, Kumaravel Kaliyaperumal, Juan Liu, Yongqi Tian, Shihai Xu & Yonghong Liu



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Better visualization and photodocumentation of zone of inhibition by staining cells and background agar differently

Better visualization and photodocumentation of zone of inhibition by staining cells and background agar differently

The Journal of Antibiotics advance online publication, May 13 2015. doi:10.1038/ja.2015.49

Author: Mrinal K Bhattacharjee



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Cycloexpansamines A and B: spiroindolinone alkaloids from a marine isolate of Penicillium sp. (SF-5292)

Cycloexpansamines A and B: spiroindolinone alkaloids from a marine isolate of Penicillium sp. (SF-5292)

The Journal of Antibiotics advance online publication, May 13 2015. doi:10.1038/ja.2015.56

Authors: Chiwook Lee, Jae Hak Sohn, Jae-Hyuk Jang, Jong Seog Ahn, Hyuncheol Oh, Jonas Baltrusaitis, In Hyun Hwang & James B Gloer



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Micromonospora endophytica sp. nov., an endophytic actinobacteria of Thai upland rice (Oryza sativa)

Micromonospora endophytica sp. nov., an endophytic actinobacteria of Thai upland rice (Oryza sativa)

The Journal of Antibiotics advance online publication, May 13 2015. doi:10.1038/ja.2015.57

Authors: Dusanee Thanaboripat, Chitti Thawai, Chokchai Kittiwongwattana, Chamroon Laosinwattana, Prommart Koohakan & Nonglak Parinthawong



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Structure–activity relationships of the plasminogen modulator SMTP with respect to the inhibition of soluble epoxide hydrolase

Structure–activity relationships of the plasminogen modulator SMTP with respect to the inhibition of soluble epoxide hydrolase

The Journal of Antibiotics advance online publication, May 13 2015. doi:10.1038/ja.2015.58

Authors: Naoki Matsumoto, Eriko Suzuki, Kota Tsujihara, Yuuichi Nishimura & Keiji Hasumi



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Discovery of secondary metabolites in an extractive liquid-surface immobilization system and its application to high-throughput interfacial screening of antibiotic-producing fungi

Discovery of secondary metabolites in an extractive liquid-surface immobilization system and its application to high-throughput interfacial screening of antibiotic-producing fungi

The Journal of Antibiotics advance online publication, May 13 2015. doi:10.1038/ja.2015.59

Authors: Shinobu Oda, Arisa Kameda, Masanori Okanan, Yusuke Sakakibara & Shinichi Ohashi



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mercredi 6 mai 2015

Induced sclerotium formation exposes new bioactive metabolites from Aspergillus sclerotiicarbonarius

Induced sclerotium formation exposes new bioactive metabolites from Aspergillus sclerotiicarbonarius

The Journal of Antibiotics advance online publication, May 6 2015. doi:10.1038/ja.2015.40

Authors: Lene M Petersen, Jens C Frisvad, Peter B Knudsen, Marko Rohlfs, Charlotte H Gotfredsen & Thomas O Larsen



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Ascosteroside C, a new mitochondrial respiration inhibitor discovered by pesticidal screening using recombinant Saccharomyces cerevisiae

Ascosteroside C, a new mitochondrial respiration inhibitor discovered by pesticidal screening using recombinant Saccharomyces cerevisiae

The Journal of Antibiotics advance online publication, May 6 2015. doi:10.1038/ja.2015.43

Authors: Takuya Suga, Yukihiro Asami, Shohei Hashimoto, Kenichi Nonaka, Masato Iwatsuki, Takuji Nakashima, Ryohei Sugahara, Takahiro Shiotsuki, Takenori Yamamoto, Yasuo Shinohara, Naoya Ichimaru, Masatoshi Murai, Hideto Miyoshi, Satoshi Ōmura & Kazuro Shiomi



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Dibenzocyclooctadiene lignans from Schisandra spp. selectively inhibit the growth of the intracellular bacteria Chlamydia pneumoniae and Chlamydia trachomatis

Dibenzocyclooctadiene lignans from Schisandra spp. selectively inhibit the growth of the intracellular bacteria Chlamydia pneumoniae and Chlamydia trachomatis

The Journal of Antibiotics advance online publication, May 6 2015. doi:10.1038/ja.2015.48

Authors: Elina Hakala, Leena Hanski, Hanna Uvell, Teijo Yrjönen, Heikki Vuorela, Mikael Elofsson & Pia Maarit Vuorela



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Avellanin C, an inhibitor of quorum-sensing signaling in Staphylococcus aureus, from Hamigera ingelheimensis

Avellanin C, an inhibitor of quorum-sensing signaling in Staphylococcus aureus, from Hamigera ingelheimensis

The Journal of Antibiotics advance online publication, May 6 2015. doi:10.1038/ja.2015.50

Authors: Yasuhiro Igarashi, Fumiya Gohda, Taito Kadoshima, Takao Fukuda, Tomoaki Hanafusa, Akane Shojima, Jiro Nakayama, Gerald F Bills & Stephen Peterson



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Evaluation of agar dilution and broth microdilution methods to determine the disinfectant susceptibility

Evaluation of agar dilution and broth microdilution methods to determine the disinfectant susceptibility

The Journal of Antibiotics advance online publication, May 6 2015. doi:10.1038/ja.2015.51

Authors: Guoyan Wu, Qianru Yang, Mei Long, Lijuan Guo, Bei Li, Yue Meng, Anyun Zhang, Hongning Wang, Shuliang Liu & Likou Zou



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Activity of lipophilic and hydrophilic drugs against dormant and replicating Mycobacterium tuberculosis

Activity of lipophilic and hydrophilic drugs against dormant and replicating Mycobacterium tuberculosis

The Journal of Antibiotics advance online publication, May 6 2015. doi:10.1038/ja.2015.52

Authors: Giovanni Piccaro, Giovanna Poce, Mariangela Biava, Federico Giannoni & Lanfranco Fattorini



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Sydoxanthone C and acremolin B produced by deep-sea-derived fungus Aspergillus sp. SCSIO Ind09F01

Sydoxanthone C and acremolin B produced by deep-sea-derived fungus Aspergillus sp. SCSIO Ind09F01

The Journal of Antibiotics advance online publication, May 6 2015. doi:10.1038/ja.2015.55

Authors: Yongqi Tian, Xiaochu Qin, Xiuping Lin, Kumaravel Kaliyaperumal, Xuefeng Zhou, Juan Liu, Zhiran Ju, Zhengchao Tu & Yonghong Liu



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