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Amino acid appended diphenylglycoluril-based chiral molecular receptors 2 and 3 have been prepared and their aggregation has been studied in water at various pH’s and in chloroform. The binding of several biologically relevant guests with aromatic moieties to these aggregates has been studied with UV-Vis spectroscopy in competition experiments with 4-(4-nitrophenylazo)resorcinol (Magneson) and 2-(4-hydroxyphenylazo)benzoic acid (HABA) as probes. Aggregates of chiral host 2b showed binding of catecholamines and aromatic amino acids in an aqueous environment, as well as discrimination between amino acid enantiomers, and can be considered a mimic for adrenergic receptors.

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Metal catalyst and ligand design,
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beta-Cyclodextrin (beta-CD) functionalized with diaza-18-crown-6 at primary face shows 7-10 fold greater binding constants for aromatic ammonium ions in aqueous media than the unmodified beta-CD by the cooperative binding of the aromatic group to beta-CD and ammonium group to crown ether moiety.

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Metal catalyst and ligand design,
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Amino acid appended diphenylglycoluril-based chiral molecular receptors 2 and 3 have been prepared and their aggregation has been studied in water at various pH’s and in chloroform. The binding of several biologically relevant guests with aromatic moieties to these aggregates has been studied with UV-Vis spectroscopy in competition experiments with 4-(4-nitrophenylazo)resorcinol (Magneson) and 2-(4-hydroxyphenylazo)benzoic acid (HABA) as probes. Aggregates of chiral host 2b showed binding of catecholamines and aromatic amino acids in an aqueous environment, as well as discrimination between amino acid enantiomers, and can be considered a mimic for adrenergic receptors.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Astrocytic and oligodendroglial gliomas are intrinsic brain tumours characterized by infiltrative growth and resistance to classic cancer therapies, which renders them inevitably lethal. Glioblastoma, the most common type of glioma, also exhibits neoangiogenesis and profound immunosuppressive properties. Accordingly, strategies to revert glioma-associated immunosuppression and promote tumour-directed immune responses have been extensively explored in rodent models and in large clinical trials of tumour immunotherapy. This Review describes vaccination approaches investigated for the treatment of glioma. Several strategies have reached phase III clinical trials, including vaccines targeting epidermal growth factor receptor variant III, and the use of either immunogenic peptides or tumour lysates to stimulate autologous dendritic cells. Other approaches in early phases of clinical development employ multipeptide vaccines such as IMA-950, cytomegalovirus-derived peptides, or tumour-derived peptides such as heat shock protein-96 peptide complexes and the Arg132His mutant form of isocitrate dehydrogenase. However, some preclinical trial data suggest that addition of immunomodulatory reagents such as immune checkpoint inhibitors, transforming growth factor-beta inhibitors, signal transducer and activator of transcription 3 inhibitors, or modifiers of tryptophan metabolism could augment the therapeutic activity of vaccination and overcome glioma-associated immunosuppression.

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Metal catalyst and ligand design,
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Provided herein are compounds capable of activating GPR139. Also provided are methods of increasing and decreasing the activity of GPR139. Methods of using the identified compounds to modulate GPR139 activity or conditions that may be affected by GPR139 activity are also disclosed.

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Coordination properties of 3-functionalized beta-cyclodextrins. Thermodynamic stereoselectivity of copper(II) complexes of the A,B-diamino derivative and its exploitation in LECE

The bis-amino AB derivative of beta-cyclodextrin on the secondary rim was synthesised and spectroscopically characterised by different techniques. Its binary systems both with protons and copper(II) were thermodynamically characterised by pH-metric potentiometry. In addition the ternary systems with each of the enantiomers of tryptophan and alanine were investigated. A thermodynamic stereoselectivity was observed for the tryptophan enantiomers and this was exploited to separate them by capillary electrophoresis through a ligand exchange mechanism (LEGE). LECE separation of racemates of phenylalanine and tyrosine was also obtained. The Royal Society of Chemistry 2005.

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Metal catalyst and ligand design,
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Poly(styrene-4-sulfonate)-protected copper nanoclusters as a fluorometric probe for sequential detection of cytochrome c and trypsin

Stable copper nanoclusters (CuNCs) were prepared by utilizing D-penicillamine as both the stabilizer and reductant. The emission of the CuNCs (with excitation/emission peaks at 390/645 nm) is largely stabilized by coating with poly(sodium-p-styrenesulfonate) (PSS). Cytochrome c (Cyt c) quenches the fluorescence of the PSS-coated CuNCs, and this effect was exploited to design a quenchometric fluorometric assay for Cyt c. If trypsin is added to the loaded CuNCs, it will hydrolyze Cyt c to form peptide fragments, and fluorescence is gradually restored. A highly sensitive and fluorometric turn-off-on assay was constructed for sequential detection of Cyt c and trypsin. The linear ranges for Cyt c and trypsin are from 8.0 nM to 680 nM, and from 0.1 to 6.0 mug mL?1, and the lower detection limits are 0.83 nM and 20 ng mL?1 for Cyt c and trypsin, respectively. [Figure not available: see fulltext.].

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Metal catalyst and ligand design,
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High resolution vibronic spectra of the amino acids tryptophan and tyrosine in 0.38 K cold helium droplets

High resolution vibronic absorption spectra are reported for the amino acids tryptophan and tyrosine embedded in large (N ? 103 – 104) helium droplets. The spectra exhibit a large number of sharp (deltanu?0.5 cm-1) 000 band origins which are attributed to different conformers. The significant differences to previous spectra of the isolated molecules from seeded beam expansions are interpreted in terms of the lower temperatures and the suppression of certain conformers in the liquid helium environment.

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Metal catalyst and ligand design,
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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 153-94-6, molcular formula is C11H12N2O2, introducing its new discovery. Recommanded Product: 153-94-6

Biochemical investigations of two 6-DMATS enzymes from streptomyces reveal new features of l -tryptophan prenyltransferases

Two putative prenyltransferase genes, SAML0654 and Strvi8510, were identified in Streptomyces ambofaciens and Streptomyces violaceusniger, respectively. Their deduced products share 63-?% sequence identity. Biochemical investigations with recombinant proteins demonstrated that L-tryptophan and derivatives, including D-tryptophan, 4-, 5-, 6- and 7-methyl-dl-tryptophan, were well accepted by both enzymes in the presence of DMAPP. Structural elucidation of the isolated products revealed regiospecific prenylation at C-6 of the indole ring and proved unequivocally the identification of two very similar 6-dimethylallyltryptophan synthases (6-DMATS). Detailed biochemical investigations with SAML0654 proved L-tryptophan to be the best substrate (Km 18 mum, turnover 0.3 s-1). Incubation with different prenyl donors showed that they also accepted GPP and catalyzed the same specific prenylation. Utilizing GPP as a prenyl donor has not been reported for tryptophan prenyltransferases previously. Both enzymes also catalyzed prenylation of some hydroxynaphthalenes; this has not previously been described for bacterial indole prenyltransferases. Interestingly, SAML0654 transferred prenyl moieties onto the unsubstituted ring of hydroxynaphthalenes. They can do more: L-Tryptophan (1-?a) and derivatives as well as hydroxynaphthalenes like 2,3-dihydroxynaphthalene (10-?a) were accepted by 6-DMATSSa and 6-DMATSSv from Streptomyces strains, in the presence of DMAPP and GPP. C6-prenylated indole derivatives and dihydroxynaphthalenes with prenylation at the unsubstituted ring were identified as enzyme products of 6-DMATSSa.

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Metal catalyst and ligand design,
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Purification and characterization of tryptophan dioxygenase from Streptomyces parvulus.

Tryptophan dioxygenase, derived from Streptomyces parvulus, was purified to near homogeneity and shown to have a native Mr of 88,000. Kinetic parameters of the enzyme were determined and evidence suggesting that it is a hemoprotein was obtained. Tryptophan dioxygenase has a high specificity toward L-tryptophan with an apparent Km of 0.3 mM. L-3-Hydroxykynurenine was a competitive inhibitor with respect to L-tryptophan with a Ki of 0.16 mM. In vitro, the enzyme displayed little activity in the absence of a reducing agent; ascorbate, at 50 mM, was the preferred reductant providing almost a 50-fold increase in enzyme activity. The regulation of tryptophan dioxygenase synthesis and activity is described. The expression of the enzyme is correlated with the biosynthesis of actinomycin D in S. parvulus. These results support the hypothesis that tryptophan dioxygenase functions as the first enzyme in the sequence converting L-tryptophan to the chromophore of this antibiotic.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI