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Son T Nguyen et al.
Bioorganic & medicinal chemistry, 23(9), 2024-2034 (2015-03-31)
Recently we described a novel pyranopyridine inhibitor (MBX2319) of RND-type efflux pumps of the Enterobacteriaceae. MBX2319 (3,3-dimethyl-5-cyano-8-morpholino-6-(phenethylthio)-3,4-dihydro-1H-pyrano[3,4-c]pyridine) is structurally distinct from other known Gram-negative efflux pump inhibitors (EPIs), such as 1-(1-naphthylmethyl)-piperazine (NMP), phenylalanylarginine-β-naphthylamide (PAβN), D13-9001, and the pyridopyrimidine derivatives. Here
Samuel W Cramer et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 35(14), 5664-5679 (2015-04-10)
The Ca(2+) channelopathies caused by mutations of the CACNA1A gene that encodes the pore-forming subunit of the human Cav2.1 (P/Q-type) voltage-gated Ca(2+) channel include episodic ataxia type 2 (EA2). Although, in EA2 the emphasis has been on cerebellar dysfunction, patients
Catalin Chimerel et al.
Chemphyschem : a European journal of chemical physics and physical chemistry, 14(2), 417-423 (2013-01-11)
Indole is an important biological signalling molecule produced by many Gram positive and Gram negative bacterial species, including Escherichia coli. Here we study the effect of indole on the electrical properties of lipid membranes. Using electrophysiology, we show that two
C Baes et al.
Animal : an international journal of animal bioscience, 7(5), 714-720 (2012-12-06)
Genetically reducing boar taint using low-taint lines is considered the most sustainable and economic long-term alternative to surgical castration of male pigs. Owing to the high heritability of the main boar taint components (androstenone, skatole and indole), breeding is an
Benjamin Hidalgo-Romano et al.
Microbiology (Reading, England), 160(Pt 11), 2464-2473 (2014-08-29)
The LuxI/R quorum-sensing system and its associated N-acylated homoserine lactone (AHL) signal is widespread among Gram-negative bacteria. Although inhibition by indole of AHL quorum signalling in Pseudomonas aeruginosa and Acinetobacter oleivorans has been reported previously, it has not been documented
Total synthesis of the tremorgenic indole diterpene paspalinine.
Masaru Enomoto et al.
Angewandte Chemie (International ed. in English), 51(51), 12833-12836 (2012-11-09)
Mohammed Almuhayawi et al.
Journal of clinical microbiology, 52(9), 3230-3236 (2014-06-22)
In this study, we investigated the performance of the FilmArray and matrix-assisted laser desorption ionization-time of flight mass spectrometry (MALDI-TOF MS) in identifying microorganisms from blood culture (BC) bottles prior to positivity. First, we used simulated BacT/Alert FA Plus BC
Thomas B Parsons et al.
Chemical communications (Cambridge, England), 49(23), 2296-2298 (2013-02-12)
The first synthesis of kottamide E, a marine natural product containing a 5,6-dibromoindole linked via a (Z)-enamide to an unusual 1,2-dithiolane-containing amino acid, is reported.
Rui Wang et al.
Bioorganic & medicinal chemistry letters, 23(6), 1760-1762 (2013-02-14)
A series of novel indole-imidazole derivatives have been prepared and evaluated in vitro on the aromatase inhibitory activities. The results suggested that proton or a small electron-withdrawing group at para-position of the phenyl ring would enhance the inhibitory activities and
Jin-Hyung Lee et al.
FEMS microbiology reviews, 34(4), 426-444 (2010-01-15)
Bacteria can utilize signal molecules to coordinate their behavior to survive in dynamic multispecies communities. Indole is widespread in the natural environment, as a variety of both Gram-positive and Gram-negative bacteria (to date, 85 species) produce large quantities of indole.
Ricardo Valladares et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 27(4), 1711-1720 (2013-01-11)
In our previous work, we found that feeding Lactobacillus johnsonii to BioBreeding diabetes-prone (BBDP) rats decreased the incidence of diabetes development. The aim of this study was to investigate host pathways affected by L. johnsonii, with specific focus on the
Facile access to 3-acylindoles through palladium-catalyzed addition of indoles to nitriles: the one-pot synthesis of indenoindolones.
Yuanhong Ma et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 19(4), 1189-1193 (2012-12-15)
Zsolt Székelyhidi et al.
Bioorganic & medicinal chemistry letters, 15(13), 3241-3246 (2005-06-01)
SR protein-specific kinase-1 (SRPK-1) has been identified as a validated target for hepatitis B virus (HBV). A series of novel tricyclic quinoxaline derivatives was designed and synthesised as potential kinase inhibitory antiviral agents and was found to be active and
C Zscheppank et al.
Analytical and bioanalytical chemistry, 406(26), 6617-6628 (2014-08-26)
A new method for the growth-dependent headspace analysis of bacterial cultures by needle trap (NT)-gas chromatography-mass spectrometry (GC-MS) was established. NTs were used for the first time as enrichment technique for volatile organic compounds (VOCs) in the headspace of laboratory
Brenda Borbón et al.
Environmental science and pollution research international, 21(14), 8573-8584 (2014-03-29)
Dairy wastewater is characterized by a high content of hardly biodegradable dissolved, colloidal, and suspended organic matter. This work firstly investigates the performance of two individual electrochemical treatments, namely electrocoagulation (EC) and electro-oxidation (EO), in order to finally assess the
Dimitri Niks et al.
Biochemistry, 52(37), 6396-6411 (2013-08-21)
The allosteric regulation of substrate channeling in tryptophan synthase involves ligand-mediated allosteric signaling that switches the α- and β-subunits between open (low activity) and closed (high activity) conformations. This switching prevents the escape of the common intermediate, indole, and synchronizes
Fitsum Dulo et al.
PloS one, 10(11), e0142905-e0142905 (2015-11-13)
Toxigenic Escherichia coli (E. coli) are an important cause of gastroenteritis in developing countries. In Ethiopia, gastroenteritis due to food-borne disease is a leading cause of death. Yet, there is no surveillance for E. coli O157 and little is known
Huijun Dong et al.
Chemical communications (Cambridge, England), 48(95), 11644-11646 (2012-10-26)
A highly efficient macrocyclization reaction has been developed via the palladium-catalyzed C-H arylation of the side-chains of tryptophan with halophenyl-containing amino acids. This method allows for direct access to 15- to 25-membered biaryl macrocycles in 40-75% yield, at moderate concentration
Janice L Hyatt et al.
Journal of medicinal chemistry, 50(8), 1876-1885 (2007-03-24)
Carboxylesterases (CE) are ubiquitous enzymes thought to be responsible for the metabolism and detoxification of xenobiotics. Numerous clinically used drugs including Demerol, lidocaine, capecitabine, and CPT-11 are hydrolyzed by these enzymes. Hence, the identification and application of selective CE inhibitors
Mattia Mori et al.
ChemMedChem, 8(3), 484-496 (2013-02-26)
Pim-1 is a serine/threonine kinase critically involved in the initiation and progression of various types of cancer, especially leukemia, lymphomas and solid tumors such as prostate, pancreas and colon, and is considered a potential drug target against these malignancies. In
Alison Burklund et al.
Biosensors & bioelectronics, 128, 97-103 (2019-01-15)
We present a QR code paper microfluidic colorimetric assay that can exploit the hardware and software on mobile devices, and circumvent sample preparation by directly targeting volatile biomarkers. Our platform is a printable microarray of well-defined reaction regions, which outputs
Benjamin Suenkel et al.
Bioorganic & medicinal chemistry letters, 23(1), 143-146 (2012-12-01)
Sirtuins are NAD(+) consuming protein deacylases involved in many cellular processes from DNA-repair to metabolism. Their contribution to age-related and metabolic diseases makes them attractive pharmaceutical targets. Few pharmacological inhibitors have been reported yet for human Sirt5 since substrates and
Thomas Lindel et al.
Topics in current chemistry, 309, 67-129 (2011-09-15)
Important biologically active indole alkaloids are decorated with prenyl (3,3-dimethylallyl) and tert-prenyl (1,1-dimethylallyl) groups. Covering the literature until the end of 2010, this review article comprehensively summarises and discusses the currently available technologies of prenylation and tert-prenylation of indoles, which
Kyung Hwa Won et al.
Antonie van Leeuwenhoek, 107(2), 565-573 (2014-12-19)
An ivory white, rod-shaped, non-motile, non-spore forming, Gram-staining-negative, and aerobic bacterium designated THG-G118T, was isolated from a soil sample collected in a bamboo plantation in Seoul, Republic of Korea. The 16S rRNA gene sequence analysis revealed a clear affiliation of
Anastasiya Lapytsko et al.
BMC bioinformatics, 16, 392-392 (2015-11-22)
The number of γH2AX foci per nucleus is an accepted measure of the number of DNA double-strand breaks in single cells. One of the experimental techniques for γH2AX detection in cultured cells is immunofluorescent labelling of γH2AX and nuclei followed
Shengnan Shi et al.
Applied biochemistry and biotechnology, 169(4), 1088-1097 (2013-01-12)
Biotransformation of indole to indigo in liquid-liquid biphasic systems was performed in Escherichia coli cells expressing phenol hydroxylase. It was suggested that indole could inhibit the cell growth even at low concentration of 0.1 g/L. The critical Log P for strain
C J van der Horst
Cytobios, 45(181), 85-95 (1986-01-01)
Both in the male and in the female reproductive tract glucose can be converted via either the pentose pathway or the sorbitol pathway. It is shown that a disturbed carbohydrate metabolism can lead to infertility, i.e. in the cow and
Xiaoqing Tang et al.
PloS one, 9(9), e102963-e102963 (2014-09-27)
Isatis indigotica, the source of the traditional Chinese medicine Radix isatidis (Ban-Lan-Gen), is an extremely important economical crop in China. To facilitate biological, biochemical and molecular research on the medicinal chemicals in I. indigotica, here we report the first I.
Formation of enehydrazine intermediates through coupling of phenylhydrazines with vinyl halides: entry into the Fischer indole synthesis.
Fuxu Zhan et al.
Angewandte Chemie (International ed. in English), 52(4), 1266-1269 (2012-12-12)
Matthias Erb et al.
Nature communications, 6, 6273-6273 (2015-02-17)
Herbivore-induced volatile organic compounds prime non-attacked plant tissues to respond more strongly to subsequent attacks. However, the key volatiles that trigger this primed state remain largely unidentified. In maize, the release of the aromatic compound indole is herbivore-specific and occurs
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