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A New Resistance Gene, linB, Conferring Resistance to Lincosamides by Nucleotidylation in Enterococcus faecium HM1025
ABSTRACT Resistance to lincomycin and clindamycin in the clinical isolateEnterococcus faecium HM1025 is due to a ribosomal methylase encoded by an ermAM-like gene and the plasmid-mediated…
Discovery, production, and biological assay of an unusual flavenoid cofactor involved in lincomycin biosynthesis.
In a genetic study of Streptomyces lincolnensis, a riboflavin auxotroph, NTG-3, was obtained which was also a lincomycin non-producer under standard antibiotic production conditions. The addition of…
Development of a system to evaluate compound identity, purity, and concentration in a single experiment and its application in quality assessment of combinatorial libraries and screening hits.
A new assay system for the simultaneous determination of identity, purity, and concentration of sample components from combinatorial libraries produced by parallel synthesis are described, allowing the optimization of library synthetic procedures.
Isolation and identification of 7,8-didemethyl-8-hydroxy-5-deazariboflavin, an unusual cosynthetic factor in streptomycetes, from Streptomyces lincolnensis.
Isolation and identification of a major metabolite of PNU-107859, an MMP inhibitor from the biliary fluid of rats.
- M. Kuo, D. Yurek, S. Mizsak, M. Prairie, S. Mattern, T. Dekoning
- Biology, ChemistryJournal of pharmaceutical sciences
- 1 July 1999
PNU-107859, an important representative structure in a novel class of matrix metalloproteinases (MMP) inhibitors known as thiadiazoles, was found to be quickly eliminated from rats. A major…
Structure elucidation of ficellomycin.
The structure of ficellomycin, an antibiotic previously discovered by Argoudelis et al., is elucidated as valyl-2-[4-guanidyl-1-azabicyclo[3.1.0]hexan-2-yl]glycine (1) by NMR, MS, and derivatization…
Isolation and identification of 3-propylidene-delta 1-pyrroline-5-carboxylic acid, a biosynthetic precursor of lincomycin.
- M. Kuo, D. Yurek, J. Coats, S. Chung, G. Li
- Chemistry, BiologyThe Journal of antibiotics
- 25 November 1992
Based on the structure of this newly found intermediate, a biosynthetic pathway for propylproline is proposed as tyrosine-->L-3-hydroxytyrosine (Dopa), which is shown to be 3-propylidene-delta 1-pyrroline-5-carboxylic acid, or 1, 2, 3, 6-tetradehydro-Propyl Proline.
Imidazopyridine and Pyrazolopiperidine Derivatives as Novel Inhibitors of Serine Palmitoyl Transferase.
- M. Genin, Isabel C Gonzalez Valcarcel, J. Brozinick
- Biology, ChemistryJournal of medicinal chemistry
- 6 June 2016
To develop novel treatments for type 2 diabetes and dyslipidemia, we pursued inhibitors of serine palmitoyl transferase (SPT). To this end compounds 1 and 2 were developed as potent SPT inhibitors in…
Development and pharmacological characterization of a model of sleep disruption‐induced hypersensitivity in the rat
Sleep disturbance is a commonly reported co‐morbidity in chronic pain patients, and conversely, disruption of sleep can cause acute and long‐lasting hypersensitivity to painful stimuli. The…