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Cyclic Lipopeptide

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141. Daptomycin is more efficacious than vancomycin against a methicillin-susceptible Staphylococcus aureus in experimental meningitis. (PubMed)

Daptomycin is more efficacious than vancomycin against a methicillin-susceptible Staphylococcus aureus in experimental meningitis. To test the efficacy of daptomycin, a cyclic lipopeptide antibiotic, against a methicillin-susceptible Staphylococcus aureus strain in experimental rabbit meningitis and to determine its penetration into non-inflamed and inflamed meningesOver a treatment period of 8 h, daptomycin (15 mg/kg) was significantly superior to the comparator regimen vancomycin (-4.54

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2006 Journal of Antimicrobial Chemotherapy

142. The importance of the development of antibiotic resistance in Staphylococcus aureus. (PubMed)

proportion of cases in the near future. New classes of antibiotic are urgently needed to treat infections with this growing population of multidrug-resistant S. aureus, and the recently introduced oxazolidinone linezolid and the cyclic lipopeptide daptomycin are welcome additions to the ever-narrowing range of therapies effective against this pathogen.

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2006 Clinical Microbiology and Infection

143. The efficacy and safety of daptomycin: first in a new class of antibiotics for Gram-positive bacteria. (PubMed)

The efficacy and safety of daptomycin: first in a new class of antibiotics for Gram-positive bacteria. In the face of increasing resistance to currently available antibiotics, there is a continued interest in the development of new drugs to treat Gram-positive infections. One such agent is the cyclic lipopeptide daptomycin-licensed in the USA for treatment of Gram-positive complicated skin and skin structure infections (cSSSIs) in 2003 and currently awaiting European approval for a similar

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2006 Clinical Microbiology and Infection

144. Trichosporon Asahii. Blood-stream Infection in a non-cancer patient receiving Combination Antifungal Therapy (PubMed)

Webb C H CH Bedi A A eng Case Reports Journal Article Northern Ireland Ulster Med J 0417367 0041-6193 0 Antifungal Agents 0 Echinocandins 0 Lipopeptides 0 Peptides, Cyclic 7XU7A7DROE Amphotericin B F0XDI6ZL63 Caspofungin IM Accidents, Occupational Aged Agriculture Amphotericin B pharmacology therapeutic use Antifungal Agents therapeutic use Caspofungin Drug Therapy, Combination Echinocandins Fatal Outcome Humans Lipopeptides Male Multiple Organ Failure microbiology Mycoses drug therapy microbiology (...) Peptides, Cyclic pharmacology therapeutic use Sepsis microbiology Species Specificity Trichosporon drug effects isolation & purification 2006 9 13 9 0 2006 11 3 9 0 2006 9 13 9 0 ppublish 16964817 PMC1891755 J Clin Microbiol. 2003 Feb;41(2):911 12574315 J Clin Microbiol. 2004 May;42(5):2341-4 15131229 Scand J Infect Dis. 2004;36(8):564-9 15370667 J Clin Microbiol. 1998 Oct;36(10):2950-6 9738049 Eur J Clin Microbiol Infect Dis. 2002 Dec;21(12):892-6 12525928 South Med J. 2005 Sep;98(9):954-5 16217998

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2006 The Ulster medical journal

145. Deferasirox, an Iron-Chelating Agent, as Salvage Therapy for Rhinocerebral Mucormycosis (PubMed)

NIAID NIH HHS United States R01 AI063382 AI NIAID NIH HHS United States R01 AI019990 AI NIAID NIH HHS United States Case Reports Letter 2006 09 25 United States Antimicrob Agents Chemother 0315061 0066-4804 0 Antifungal Agents 0 Benzoates 0 Echinocandins 0 Iron Chelating Agents 0 Lipopeptides 0 Peptides, Cyclic 0 Triazoles 7XU7A7DROE Amphotericin B F0XDI6ZL63 Caspofungin V8G4MOF2V9 Deferasirox IM Adult Amphotericin B therapeutic use Antifungal Agents therapeutic use Benzoates pharmacology Brain Stem (...) microbiology pathology Caspofungin Cavernous Sinus microbiology pathology Central Nervous System Fungal Infections drug therapy microbiology pathology Deferasirox Diabetic Ketoacidosis complications Drug Therapy, Combination Echinocandins Humans Iron Chelating Agents therapeutic use Lipopeptides Magnetic Resonance Imaging Male Mucormycosis drug therapy microbiology pathology Nose Diseases drug therapy microbiology Peptides, Cyclic therapeutic use Salvage Therapy Triazoles pharmacology 2006 9 27 9 0 2006 12

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2006 Antimicrobial Agents and Chemotherapy

146. Daptomycin in the treatment of patients with infective endocarditis: experience from a registry. (PubMed)

Daptomycin in the treatment of patients with infective endocarditis: experience from a registry. Daptomycin (Cubicin; Cubist Pharmaceuticals, Inc., Lexington, MA) is a first-in-its-class cyclic lipopeptide approved for the treatment of patients with complicated skin and skin-structure infections due to susceptible gram-positive pathogens and recently approved for Staphylococcus aureus bloodstream infections including right-sided infective endocarditis. The clinical experience of patients

2007 American Journal of Medicine

147. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. (PubMed)

Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. LY146032, a cyclic lipopeptide antibiotic, is an inhibitor of cell wall peptidoglycan biosynthesis in gram-positive bacteria. Although LY146032 at relatively high concentrations inhibited the in vitro polymerization of UDP-linked sugar precursors, inhibition of cell wall formation in intact Staphylococcus aureus and Bacillus megaterium cells did not lead to the accumulation of UDP-N-acetyl-muramyl (MurNAc)-peptide(s

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1987 Antimicrobial Agents and Chemotherapy

148. New model of oropharyngeal and gastrointestinal colonization by Candida albicans in CD4+ T-cell-deficient mice for evaluation of antifungal agents. (PubMed)

isolates. Mice were challenged by gavage and swabbing their oral mucosae with a pure culture of C. albicans. Gentamicin was withdrawn 3 days postchallenge, and antifungal compounds were administered via the drinking water ad libitum at concentrations ranging from 25 to 400 micrograms/ml. L-693989, a water-soluble phosphorylated cyclic lipopeptide prodrug of pneumocandin Bo, and L-733560, a semisynthetic derivative of pneumocandin Bo, are inhibitors of 1,3-beta-D-glucan synthesis that exhibit potent

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1996 Antimicrobial Agents and Chemotherapy

149. Photoaffinity Analog of the Semisynthetic Echinocandin LY303366: Identification of Echinocandin Targets in Candida albicans (PubMed)

Photoaffinity Analog of the Semisynthetic Echinocandin LY303366: Identification of Echinocandin Targets in Candida albicans The echinocandins are a family of cyclic lipopeptides with potent antifungal activity. These compounds inhibit the synthesis of BETA-1,3-glucan in fungi. The new semisynthetic echinocandin LY303366 was derivatized to produce a photoactivatable cross-linking echinocandin analog with antifungal activity. This analog was radioiodinated and used as a probe in microsomal

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1998 Antimicrobial Agents and Chemotherapy

150. Use of beta-1,3-glucan-specific antibody to study the cyst wall of Pneumocystis carinii and effects of pneumocandin B0 analog L-733,560. (PubMed)

Use of beta-1,3-glucan-specific antibody to study the cyst wall of Pneumocystis carinii and effects of pneumocandin B0 analog L-733,560. A new class of promising antipneumocystis agents, cyclic lipopeptide pneumocandin analogs, has been shown to effectively prevent Pneumocystis carinii cyst development in murine models. These compounds are believed to inhibit the biosynthesis of beta-1,3-glucan, a major constituent of the cell walls of various pathogenic fungi. However, all evidence

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1994 Antimicrobial Agents and Chemotherapy

151. Gene yerP, Involved in Surfactin Self-Resistance in Bacillus subtilis (PubMed)

Gene yerP, Involved in Surfactin Self-Resistance in Bacillus subtilis Surfactin is a cyclic lipopeptide biosurfactant. Transposon mutagenesis was performed in Bacillus subtilis strain 168, and a surfactin-susceptible mutant, strain 801, was isolated. Analysis of the region of insertion revealed that yerP was the determinant of surfactin self-resistance. YerP had homology with the resistance, nodulation, and cell division (RND) family proton motive force-dependent efflux pumps only characterized

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2001 Antimicrobial Agents and Chemotherapy

152. Daptomycin: a lipopeptide antibiotic for the treatment of serious Gram-positive infections. (PubMed)

Daptomycin: a lipopeptide antibiotic for the treatment of serious Gram-positive infections. Infections caused by drug-resistant pathogens are on the rise. Daptomycin, a cyclic lipopeptide with activity against most Gram-positive pathogens, including vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus, is a newly US-FDA approved antimicrobial for complicated skin and skin structure infections (cSSSI). Daptomycin has a unique mechanism of action that results

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2005 Journal of Antimicrobial Chemotherapy

153. Sequencing and analysis of the biosynthetic gene cluster of the lipopeptide antibiotic Friulimicin in Actinoplanes friuliensis. (PubMed)

Sequencing and analysis of the biosynthetic gene cluster of the lipopeptide antibiotic Friulimicin in Actinoplanes friuliensis. Actinoplanes friuliensis produces the lipopeptide antibiotic friulimicin, which is a cyclic peptide with one exocyclic amino acid linked to a branched-chain fatty acid acyl residue. The structural relationship to daptomycin and the excellent antibacterial performance of friulimicin make the antibiotic an attractive drug candidate. The complete friulimicin biosynthetic

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2007 Antimicrobial Agents and Chemotherapy

154. Lipopeptide Production in Pseudomonas sp. Strain DSS73 Is Regulated by Components of Sugar Beet Seed Exudate via the Gac Two-Component Regulatory System (PubMed)

Lipopeptide Production in Pseudomonas sp. Strain DSS73 Is Regulated by Components of Sugar Beet Seed Exudate via the Gac Two-Component Regulatory System Pseudomonas sp. strain DSS73 isolated from the sugar beet rhizosphere produces the cyclic lipopeptide amphisin, which inhibits the growth of plant-pathogenic fungi. By Tn5::luxAB mutagenesis, we obtained two nonproducing mutant strains, DSS73-15C2 and DSS73-12H8. The gene interrupted by the transposon in strain DSS73-15C2 (amsY) encoded

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2002 Applied and environmental microbiology

155. Lipopeptides are effective stimulators of tyrosine phosphorylation in human myeloid cells. (PubMed)

Lipopeptides are effective stimulators of tyrosine phosphorylation in human myeloid cells. Synthetic lipopeptide analogues of the N-terminus of bacterial lipoprotein are effective activators of macrophages, neutrophils and lymphocytes. We studied the effect of the lipopeptide N-palmitoyl-S-[2,3-bis(palmitoyloxy)-(2RS)-propyl]- (R)-cysteinyl-(S)-seryl-(S)-lysyl-(S)-lysyl-(S)-lysyl-(S)-lysine [Pam3Cys-Ser-(Lys)4] on tyrosine phosphorylation in dibutyryl-cyclic-AMP-differentiated HL-60 cells (...) -palmitoyloxy heptanoyl-Ser-(Lys)4 [Pam3Ahh-Ser-(Lys)4] was as potent as Pam3Cys-Ser(Lys)4, whereas (2S,6S)-2-palmitoylamino-6,7-bis(palmitoyloxy)heptanoyl++ +-Ser-(Lys)4 [Pam3Adh-Ser-(Lys)4] and Pam3Cys-Ser-Gly did not induce tyrosine phosphorylation. Lipopeptide-induced tyrosine phosphorylation was not affected by treatment of cells with pertussis toxin. Neither phorbol 12-myristate 13-acetate nor A23187 induced tyrosine phosphorylation in dibutyryl-cyclic-AMP-differentiated HL-60 cells. In HL-60

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1992 Biochemical Journal

156. Production of Cyclic Lipopeptides by Pseudomonas fluorescens Strains in Bulk Soil and in the Sugar Beet Rhizosphere (PubMed)

Production of Cyclic Lipopeptides by Pseudomonas fluorescens Strains in Bulk Soil and in the Sugar Beet Rhizosphere The production of cyclic lipopeptides (CLPs) with antifungal and biosurfactant properties by Pseudomonas fluorescens strains was investigated in bulk soil and in the sugar beet rhizosphere. Purified CLPs (viscosinamide, tensin, and amphisin) were first shown to remain highly stable and extractable (90%) when applied (ca. 5 microg g(-1)) to sterile soil, whereas all three compounds

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2003 Applied and environmental microbiology

157. Biochemical, Genetic, and Zoosporicidal Properties of Cyclic Lipopeptide Surfactants Produced by Pseudomonas fluorescens (PubMed)

Biochemical, Genetic, and Zoosporicidal Properties of Cyclic Lipopeptide Surfactants Produced by Pseudomonas fluorescens Zoospores play an important role in the infection of plant and animal hosts by oomycetes and other zoosporic fungi. In this study, six fluorescent Pseudomonas isolates with zoosporicidal activities were obtained from the wheat rhizosphere. Zoospores of multiple oomycetes, including Pythium species, Albugo candida, and Phytophthora infestans, were rendered immotile within 30 s (...) of zoospores. Mass spectrometry and nuclear magnetic resonance analyses allowed the identification of the main constituent as a cyclic lipopeptide (1,139 Da) containing nine amino acids and a 10-carbon hydroxy fatty acid. The other four zoosporicidal fractions were closely related to the main constituent, with molecular massesranging from 1,111 to 1,169 Da.

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2003 Applied and environmental microbiology

158. Assessment of mosquito larvicidal potency of cyclic lipopeptides produced by Bacillus subtilis strains. (PubMed)

Assessment of mosquito larvicidal potency of cyclic lipopeptides produced by Bacillus subtilis strains. In this study, mosquito larvicidal potency of cyclic lipopeptides (CLPs) secreted by two Bacillus subtilis strains were determined. LC50 of the crude CLPs secreted by B. subtilis DM-03 and DM-04 strains against third instar larvae of Culex quinquefasciatus was 120.0+/-5.0 and 300.0+/-8.0mg/l respectively post 24 h of treatment. Physico-chemical factors such as pH of water, incubation (...) temperature, heating and exposure to sunlight hardly influenced the larvicidal potency of these CLPs. Present study provided the evidence that B. subtilis lipopeptides were safe to Indian major carp Labeo rohita, a non-target aquatic organism. These properties of B. subtilis CLPs can be exploited for the formulation of a safer, novel biopesticide for effective control of mosquito larvae.

2006 Acta Tropica

159. Lipopeptides activate Gi-proteins in dibutyryl cyclic AMP-differentiated HL-60 cells. (PubMed)

Lipopeptides activate Gi-proteins in dibutyryl cyclic AMP-differentiated HL-60 cells. Synthetic lipopeptides activate superoxide-anion (O2-) formation in human neutrophils in a pertussis-toxin (PTX)-sensitive manner, suggesting the involvement of G-proteins of the Gi family in the signal-transduction pathway. We compared G-protein activation by lipopeptides and the chemotactic peptide N-formylmethionyl-leucyl-phenylalanine (fMLP) in dibutyryl-cyclic-AMP-differentiated HL-60 cells (...) . The lipopeptide (2S)-2-palmitoylamino-6-palmitoyloxymethyl-7-palmitoyloxy heptanoyl-SK4 (Pam3AhhSK4) and fMLP activated high-affinity GTPase, i.e. the enzymic activity of G-protein alpha-subunits, in HL-60 membranes in a time- and protein-dependent manner, but they had no effect on Mg(2+)-ATPase and Na+/K(+)-ATPase. Pam3AhhSK4 and fMLP increased Vmax. of GTP hydrolysis. Pam3AhhSK4 activated GTP hydrolysis with half-maximal and maximal effects at about 2 microM and 10 microM respectively. Other lipopeptides

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1993 Biochemical Journal

160. In vitro activity and mechanism of action of A21978C1, a novel cyclic lipopeptide antibiotic. (PubMed)

In vitro activity and mechanism of action of A21978C1, a novel cyclic lipopeptide antibiotic. The in vitro activity of A21978C1, a novel cyclic polypeptide antibiotic, was compared with those of vancomycin, teichomycin, and several beta-lactam antibiotics against gram-positive bacteria. The new drug was at least as active as vancomycin against all species of streptococci and staphylococci tested, including methicillin-resistant Staphylococcus aureus and penicillin-resistant pneumococci

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1985 Antimicrobial Agents and Chemotherapy

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