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WHITENING AGENT

Agents which contain at least one D-amino acid selected from the group consisting of D-asparagine, D-valine, D-allo-threonine, D-lysine, D-glutamine, D-histidine, D-leucine, D-phenylalanine, D-serine, D-tryptophan, and D-tyrosine are useful as whitening agents and are effective in preventing and inhibiting melanin pigmentation such as pigmented spot, freckles, and somberness.

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

Top Picks: new discover of H-D-Trp-OH

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Molecularly imprinted polymers for biomedical and biotechnological applications

This survey covers main advances in the preparation and application of molecularly imprinted polymers which are capable of specific recognition of biologically active compounds. The principles underlying the production of highly efficient and template-specific molecularly imprinted polymers are discussed. The focus is on the imprinting of highly structured macromolecular and supramolecular templates. The existing and potential applications of molecularly imprinted polymers in various fields of chemistry and molecular biology are considered.

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

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Enantioseparation and selective detection of D-amino acids by ultra-high-performance liquid chromatography/mass spectrometry in analysis of complex biological samples

The growing scientific attention in the biological function of D-amino acids leads to an increasing analytical interest for enantiomeric amino acid separation, which is still very challenging due to the lack of sufficiently sensitive, high-throughput analytical methods that can cope with often occurring matrix interferences and very low D-amino acid concentrations. Here, enantioseparation can benefit from improved resolution and chromatographic speed offered by modern UHPLC techniques and the precision of MS detection. We developed a RP-UHPLC-QqToF-MS method using pre-column OPA/IBLC derivatization for very precise discrimination of amino acids enantiomers. The method shows a superb sensitivity with limits of detection in the range of several pmol/l. It has neither shown matrix inferences in the tested very complex biological matrices (serum, plasma, urine and gut) nor stability or racemization problems.

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

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Enantiopure chiral coordination polymers of tetrahedral and octahedral cobalt(ii) alternate chains exhibiting slow magnetic relaxation behavior

The first two chiral homometallic coordination frameworks with homochiral helical [CoOctOTrpCoTdOTrp] n ferrimagnetic chains, exhibiting a unique coexistence of chirality and slow magnetic relaxation in one material, are reported. The Royal Society of Chemistry 2011.

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

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Substrate Fragmentation for the Design of M. tuberculosis CYP121 Inhibitors

The cyclo-dipeptide substrates of the essential M. tuberculosis (Mtb) enzyme CYP121 were deconstructed into their component fragments and screened against the enzyme. A number of hits were identified, one of which exhibited an unexpected inhibitor-like binding mode. The inhibitory pharmacophore was elucidated, and fragment binding affinity was rapidly improved by synthetic elaboration guided by the structures of CYP121 substrates. The resulting inhibitors have low micromolar affinity, good predicted physicochemical properties and selectivity for CYP121 over other Mtb P450s. Spectroscopic characterisation of the inhibitors? binding mode provides insight into the effect of weak nitrogen-donor ligands on the P450 heme, an improved understanding of factors governing CYP121?ligand recognition and speculation into the biological role of the enzyme for Mtb.

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

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Potentiation of metabotropic GABAB receptors by L-amino acids and dipeptides in rat neocortex

Selected neutral L-alpha-amino acids, and their dipeptides, were reversible, stereospecific, potentiators of GABAB receptor-mediated hyperpolarizing responses to baclofen (3-100 muM) in rat neocortical slices. These responses were sensitive to the GABAB receptor antagonist (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid (Sch50911) (30 muM). Most potent were L-Leu, L-Ile and L-Phe, as were the dipeptides L-Phe-Phe and L-Phe-Leu, and less potent were L-Met, L-Val, L-Cys, L-Cystine, L-Tyr, L-Thr, L-Arg and L-Ser. Inactive were L-Trp, L-His, L-Lys and L-Pro. These potentiators gave leftward shifts of the baclofen concentration-response curves with a Hill slope of 2, and a marked increase in the maximal hyperpolarizing responses. Selected L-amino acids and dipeptides are a class of naturally occurring GABAB potentiators, which may be allosteric modulators.

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

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Chemistry is traditionally divided into organic and inorganic chemistry. COA of Formula: C11H12N2O2. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 153-94-6

Potentiation of metabotropic GABAB receptors by L-amino acids and dipeptides in rat neocortex

Selected neutral L-alpha-amino acids, and their dipeptides, were reversible, stereospecific, potentiators of GABAB receptor-mediated hyperpolarizing responses to baclofen (3-100 muM) in rat neocortical slices. These responses were sensitive to the GABAB receptor antagonist (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid (Sch50911) (30 muM). Most potent were L-Leu, L-Ile and L-Phe, as were the dipeptides L-Phe-Phe and L-Phe-Leu, and less potent were L-Met, L-Val, L-Cys, L-Cystine, L-Tyr, L-Thr, L-Arg and L-Ser. Inactive were L-Trp, L-His, L-Lys and L-Pro. These potentiators gave leftward shifts of the baclofen concentration-response curves with a Hill slope of 2, and a marked increase in the maximal hyperpolarizing responses. Selected L-amino acids and dipeptides are a class of naturally occurring GABAB potentiators, which may be allosteric modulators.

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

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Amide Bond Replacements Incorporated into CCK-B Selective “Dipeptoids”

This paper describes the chemical synthesis and CCK-B and CCK-A receptor binding affinities of a series of compounds in which the central amide bond of the CCK-B “dipeptoid” ligand tricyclo<3.3.1.13,7>dec-2-yl–<2<<1-(hydroxymethyl)-2-phenylethyl>amino>-1-(1H-indol-3-ylmethyl)-2-oxoethyl>carbamate (4) (CCK-B IC50 = 852 nM), and tricyclo<3.3.1.13,7>dec-2-yl(R)-<1-(1H-indol-3-ylmethyl)-1-methyl-2-oxo-2-<(2-phenylethyl)amino>ethyl>carbamate (23) (CCK-B IC50 = 32 nM) is replaced by 11 different amide replacements.These replacements are the methyleneamino (CH2NH ), the reverse amide (NHCO), the ester (COO), the N-methylamide (CONMe), the thioamide (CSNH), the N-acetylmethyleneamino (CH2NAc), the cis double bond (CHCH), the ethylene (CH2CH2), the thiolester (COS), the hydroxyethylene (CHOHCH2), and a 4,5-dihydro-1,3-thiazole.Most of the replacements have weaker affinity and reduced selectivity for the CCK-B receptor than the parent amide.However, this affinity can be improved by appending a fumarate side chain to the phenethyl group e.g. tricyclo<3.3.1.13,7>dec-2-yl-3-(1H-indol-3-yl-methyl)-3-methyl-4,9-dioxo-7-phenyl-5,13-dioxa-2,8-diazatetradec-10-enoate (36) (CCK-B IC50 = 38.8 nM).Replacement of the amide of compound 4 with a 4,5-dihydro-1,3-thiazole gives tricyclo<3.3.1.13,7>dec-2-yl-<1-<4,5-dihydro-4-(phenylmethyl)-2-thiazolyl>-2-(1H-indol-3-yl)ethyl>carbamate (5), which is selective for the CCK-A receptor (CCK-A IC50 = 125 nM, CCK-B IC50 = 2580 nM, ratio = 21).The methyleneamino and hydroxyetylene replacements, which have been used elsewhere as transition-state inhibitors of enzymes, are poor mimics of the amide in these CCK-B receptor ligands.Some of the steric, lipophilic, and and hydrogen bonding properties of amide replacements incorporated into the simple amide, N-methylacetamide, have been quantified with the aid of molecular modeling.These data will contribute to the rational selection of amide bond replacements in other substrates.

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

Simple exploration of H-D-Trp-OH

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Histone demethylating agents as potential S-adenosyl-l-methionine-competitors

Histone H3 methylation on K9 and/or K27 depends on histone lysine methyltransferases (KMTs). EZH2, one of the components of the PRC2 complex, catalyzes the trimethylation of histone H3K27, which is associated with transcriptional repression and tumor development. H3K9me3 mediated gene silencing may result from other KDMs such as G9a/GLP, SUV39H1-2, SETDB1, CCLD8 and RIZ1. Their disturbance leads to defective cell mitosis. It is therefore desirable to find small molecules that are able to decrease H3K9 and K27 tagging to reinitiate gene transcription. Most KDM inhibitors are still based on SAM co-factor competition/modulation. Herein, functional screening of a diversity library proved to be a useful tool for finding new specific KDM inhibitors; the use of SAM-based pharmacophoric models facilitated the understanding of their possible mechanism of action.

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

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Dipeptide analogs for treating conditions associated with amyloid fibril formation

Dipeptide analogs comprising a tryptophan (Trp) moiety coupled to a beta-sheet breaker moiety derived from alpha-aminoisobutyric acid (Aib) are disclosed. The dipeptide analogs exhibit an improved performance in inhibiting amyloid fibril formation, as compared to previously described dipeptides. Compositions containing the dipeptide analogs and uses thereof in treating amyloid-associated diseases and disorders are also disclosed.

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