The synthesis and structural elucidation, by 1D and 2D NMR and X-ray diffraction techniques, of novel E/Z 16-azolylmethylene-17-oxoandrostanes 2–9 prepared from the Vilsmeier–Hack reaction product 17-chloro-16-formylandrosta-5,16-dien-3β-yl acetate 1 is reported. The reaction proceeds with py...
Mono(indolyl)-4-trifluoromethylpyridines and bis(indolyl)-4-trifluoromethylpyridines were synthesized using Suzuki cross-coupling reaction between 2-chloro-4-trifluoromethylpyridine 9, 2,6-dichloro-4-trifluoromethylpyridine 6 or 2,6-dichloro-3-cyano-4-trifluoromethylpyridine 23 and N-tosyl-3-ind...
A number of studies suggested that anaerobic digestion processes can be enhanced by inserting electrodes in anaerobic digesters, however a thorough work with relation to the bacterial shifts, especially with regards to acetogenesis, is lacking. In our work we investigated the performance and the...
l-Amino acid ligase catalyzes dipeptide synthesis from unprotected l-amino acids in an ATP-dependent manner. We recently identified a new member of l-amino acid ligase, the plu1440 protein, from Photorhabdus luminescens subsp. laumondii TT01 by in silico analysis. This protein was found to synth...
Bacillus velezensis CC09, which was isolated from healthy leaves of Cinnamomum camphora and previously identified as Bacillus amyloliquefaciens CC09, shows great potential as a new biocontrol agent, in control of many phytopathogenic diseases. To extend our understanding of the potential antifun...
Bacillus subtilis QST713 is extensively used as a biological control agent in agricultural fields including in the button mushroom culture, Agaricus bisporus. This last use exploits its inhibitory activity against microbial pathogens such as Trichoderma aggressivum f. europaeum, the main button ...
SummaryRhizocticins are phosphonate oligopeptide antibiotics containing the C-terminal nonproteinogenic amino acid (Z)-l-2-amino-5-phosphono-3-pentenoic acid (APPA). Here we report the identification and characterization of the rhizocticin biosynthetic gene cluster (rhi) in Bacillus subtilis ATC...
Rhizocticins and Plumbemycins are natural phosphonate antibiotics produced by the bacterial strains Bacillus subtilis ATCC 6633 and Streptomyces plumbeus, respectively. Up to now, these potential threonine synthase inhibitors have only been synthesized under enzymatic catalysis. Here we report t...
The syntheses of novel N-aminoalkyl proline-derived spacers (X′) in polycationic (R–X′–R)-motif cell-penetrating α–ω–α-peptides are described as improved molecular transporters and their structural features studied by CD. FACS analysis shows enhanced cellular uptake and confocal microsc...
The effects of a potent serine protease inhibitor, Boc-D-Phe-Pro-Arg-H, on the secretion and content of ACTH and β-endorphin-like immunoreactivities of cultured rat anterior pituitary cells were studied. Basal release of the hormones was not affected by the drug but secretion in response to sta...
The effect of Boc-DPhe-Phe-Lysinal (Boc-DPPL) on the 45Ca2+ uptake of rat anterior pituitary monolayer cultures was investigated. The compound decreased the basal Ca2+ uptake at 3 × 10−4 mol/l. The 45Ca2+ uptake stimulated by potassium-induced depolarization was more sensitive to Boc-DPPL inhib...
A quantitative reversed-phase high-performance liquid chromatographic procedure was developed to facilitate the preclinical development of a new Acyl-CoA:cholesterol acyltransferase inhibitor, CI-976 (I). This procedure has a lower quantitation limit of 0.06 μg/ml and a quantitation range of 0....
2,2-Dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide (I, CI-976) has been determined in rat mesenteric lymph and plasma using a rapid and sensitive high-performance liquid chromatographic method. The samples prepared from plasma and lymph by liquid—liquid extraction were analysed on a reversed-p...
IntroductionL’endométriose est une maladie fréquente et invalidante, définie par la présence de tissu endométrial en dehors de l’utérus. La prévalence chez les femmes en âge de procréer est estimée à 10 %. Voici le cas d’une femme âgée de 31 ans, atteinte d’endométriose profonde ...
In patients undergoing somatostatin receptor scintigraphy, treatment with octreotide (Sandostatin®) is usually discontinued 24–48 h before and after injection with the radioligand 111In-pentetreotide ([111In-DTPAo]octreotide) (Octreoscan®) because octreotide competes with radioligand for the sa...
Somatostatin and its analogues bind to somatostatin receptors (sst) 1 through 5 that are overexpressed in neuroendocrine neoplasms such as gastroenteropancreatic (GEP) malignancies. After ligand-receptor binding, a fraction of the ligand-receptor complexes internalize. This internalization proce...
Bronchial carcinoid tumors are an uncommon cause of recurrent pneumonia in young patients. Diagnosis is determined from imaging studies, bronchoscopy, and histological confirmation, and treatment is generally surgical. Two cases are reviewed in order to examine the value of 111In-DTPA-Phe-octreo...
Carcinoid is a neuroendocrine neoplasm derived from primitive stem cells, occurring most frequently in the alimentary tract. Somatostatin-receptor scintigraphy with indium-111 pentetreotide is a sensitive and noninvasive technique for imaging carcinoid and its metastatic spread. However, nontumo...
IntroductionSince Pall-Gelman stopped manufacturing ITLC-SG, it has become necessary to validate alternative stationary phases.
Rationale and ObjectivesHybrid single photon-emission computed tomographic (SPECT) and computed tomographic (CT) imaging for the investigation of neuroendocrine tumors allows the fusion of functional and anatomic information in a rapid and efficient method. The aim of this study was to assess th...
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