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Delivery of Amonafide from Fructose-coated Nanodiamonds by Oxime Ligation for Treatment of Human Breast Cancer.

Introducing a strategy towards polymer/nanodiamond hybrids with high polymer grafting density and accessible polymer structural characterisation is of critical importance for nanodiamonds surface modification and bioagent attachment for their biomedical application. Here, we report a glycopolymer/nanodiamond hybrid drug delivery system, which was prepared by grafting amonafide-conjugated glycopolymers onto the surface of nanodiamonds via oxime ligation. Poly(1-O-methacryloyl-2,3:4,5-di-O-isopropylidene-β-D-fructopyranose)-b-poly(3-vinylbenzaldehyde-co-methyl methacrylate), featuring pendant aldehyde groups, is prepared via RAFT polymerization. The anticancer drug amonafide is conjugated to the polymer chains by via imine chemistry, resulting in acid degradable imine linkages. The obtained amonafide-conjugated glycopolymers are subsequently grafted onto the surface of aminooxy-functionalised nanodiamonds via oxime ligation. The molecular weight of the conjugated polymers is characterised by Size Exclusion Chromatography (SEC), while the successful conjugation and corresponding grafting density is characterised by Nuclear Magnetic Resonance (NMR), Fourier transform infrared spectroscopy (FTIR), and Thermogravimetric Aanalysis (TGA). Our results indicate that the mass percentage of amonafide in the polymer chains is around 17% and the surface density of polymer chains is 0.24 molecules/nm2. The prepared drug delivery system has a hydrodynamic size around 380 nm with low PDI (0.3) and can effectively deliver amonafide into breast cancer cell and significantly inhibit the cancer cell viability. In 2D cell culture models, the IC50 values of ND-Polymer-AMF delivery system (7.19 μM for MCF-7; 4.92 μM for MDA-MB-231) are lower than those of free amonafide (11.23 μM for MCF-7; 13.98 μM for MDA-MB-231). An inhibited cell viability of nanodiamonds/polymer delivery system is also observed in 3D spheroids models, suggesting that polymer-diamonds hybrid materials can be promising platforms for breast cancer therapy.

2173 related Products with: Delivery of Amonafide from Fructose-coated Nanodiamonds by Oxime Ligation for Treatment of Human Breast Cancer.

Breast cancer membrane pr Human breast invasive duc Human Breast Cancer Antig Bone Morphogenetic Protei Growth Differentiation Fa Mouse Anti-Human CA19-9 ( succinate-CoA ligase, GDP formin-like 1 antibody So succinate-CoA ligase, ADP serologically defined col Isopeptidase T (short for Isopeptidase T (long form

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Quantitative profiling of carbonyl metabolites directly in crude biological extracts using chemoselective tagging and nanoESI-FTMS.

The extensive range of chemical structures, wide range of abundances, and chemical instability of metabolites present in the metabolome pose major analytical challenges that are difficult to address with existing technologies. To address these issues, one approach is to target a subset of metabolites that share a functional group, such as ketones and aldehydes, using chemoselective tagging. Here we report a greatly improved chemoselective method for the quantitative analysis of hydrophilic and hydrophobic carbonyl-containing metabolites directly in biological samples. This method is based on direct tissue or cells extraction with simultaneous derivatization of stable and labile carbonylated metabolites using N-[2-(aminooxy)ethyl]-N,N-dimethyl-1-dodecylammonium (QDA) and 13CD3 labeled QDA. We combined innovations of direct quenching of biological sample with frozen derivatization conditions under the catalyst N,N-dimethyl-p-phenylenediamine, which facilitated the formation of oxime stable-isotope ion pairs differing by m/z 4.02188 while minimizing metabolite degradation. The resulting oximes were extracted by HyperSep C8 tips to remove interfering compounds, and the products were detected using nano-electrospray ionization interfaced with a Thermo Fusion mass spectrometer. The quaternary ammonium tagging greatly increased electrospray MS detection sensitivity and the signature ions pairs enabled simple identification of carbonyl compounds. The improved method showed the lower limits of quantification for carbonyl standards to be in the range of 0.20-2 nM, with linearity of R2 > 0.99 over 4 orders of magnitude. We have applied the method to assign 66 carbonyls in mouse tumor tissues, many of which could not be assigned solely by accurate mass and tandem MS. Fourteen of the metabolites were quantified using authentic standards. We also demonstrated the suitability of this method for determining 13C labeled isotopologues of carbonyl metabolites in 13C6-glucose-based stable isotope-resolved metabolomic (SIRM) studies.

1943 related Products with: Quantitative profiling of carbonyl metabolites directly in crude biological extracts using chemoselective tagging and nanoESI-FTMS.

Inflammation (Human) Quan Inflammation (Human) Quan Inflammation (Human) Quan Inflammation (Mouse) Quan Inflammation (Rat) Quanti Rat Inflammation ELISA St Cortisol Enzyme Immunoass Alamar Blue™, REDOX ind Alamar Blue™, REDOX ind Interleukin-34 IL34 (N-t Interleukin-34 IL34 anti Sterile filtered goat se

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Reductive oxyamination: a method for the qualitative and quantitative analysis of monosaccharides with a new aminooxy reagent using high-performance liquid chromatography with fluorescence detection.

Derivatization of carbohydrates with aminooxy agents to form oximes can be used for qualitative and quantitative analysis of carbohydrates; however, the formation of isomeric products limits its application. A new reductive oxyamination procedure developed for the analysis of monosaccharides with a novel fluorescent O-substituted aminooxy reagent, 4-((aminooxy)methyl)-6-chloro-7-hydroxycoumarin (AOCC), is reported. In this procedure, monosaccharides undergo an oxime formation reaction with AOCC and are then readily reduced with 2-picoline-borane, followed by analysis with high-performance liquid chromatography with fluorescence detection. Good separation of five monosaccharide derivatives was achieved within 40 min with acetonitrile-water-tetrahydrofuran as the mobile phase. The detection limits were on the order of femtomoles. The linear range was 0.2-4000 nM, with a good correlation coefficient (R ≥ 0.9985). Furthermore, the method was applied for analysis of real samples, such as bovine milk powder, without complicated and tedious sample treatment. This reductive oxyamination method circumvents the problem caused by oxime isomers and can be used for the highly sensitive and selective analysis of monosaccharides with high accuracy, providing an effective and promising method for the analysis of carbonyls with aminooxy agents.

2350 related Products with: Reductive oxyamination: a method for the qualitative and quantitative analysis of monosaccharides with a new aminooxy reagent using high-performance liquid chromatography with fluorescence detection.

QuantiChrom™ Acetylchol QuantiChrom™ Formaldehy QuantiChrom™ BCP Albumi EnzyChrom™ Acetylcholin EnzyChrom™ Ascorbic Aci EnzyChrom™ Catalase Ass EnzyChrom™ D-Lactate As EnzyChrom™ Free Fatty A EnzyChrom™ Fructose Ass EnzyChrom™ Lactose Assa EnzyChrom™ Pyruvate Ass Amplite™ Fluorimetric F

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Oriented, molecularly imprinted cavities with dual binding sites for highly sensitive and selective recognition of cortisol.

Novel, molecularly imprinted polymers (MIPs) were developed for the highly sensitive and selective recognition of the stress marker cortisol. Oriented, homogeneous cavities with two binding sites for cortisol were fabricated by surface-initiated atom transfer radical polymerization, using a cortisol motif template molecule (TM1) which consists of a polymerizable moiety attached at the 3-carbonyl group of cortisol via an oxime linkage and an adamantane carboxylate moiety coupled with the 21-hydroxyl group. TM1 was orientationally immobilized on a β-cyclodextrin (β-CD)-grafted gold-coated sensor chip by inclusion of the adamantane moiety of TM1, followed by copolymerization of a hydrophilic comonomer, 2-methacryloyloxyethyl phosphorylcholine, with or without a cross-linker, N,N'-methylenebisacrylamide. Subsequent cleavage of the oxime linkage leaves the imprinted cavities that contain dual binding sites-namely, the aminooxy group and β-CD-capable of oxime formation and hydrophobic interaction, respectively. As an application, MIP-based picomolar level detection of cortisol was demonstrated by a competitive binding assay using a fluorescent competitor. Cross-linking of the MIP imparts rigidity to the binding cavities, and improves the selectivity and sensitivity significantly, reducing the limit of detection to 4.8 pM. In addition, detection of cortisol in saliva samples was demonstrated as a feasibility study.

1646 related Products with: Oriented, molecularly imprinted cavities with dual binding sites for highly sensitive and selective recognition of cortisol.

Cortisol Binding Globulin Beta Amyloid (1 42) High Sheep Anti-Human Cortisol Rabbit Anti-Rat Androgen Highly Sensitive 8 OHdG C 8 Octadecyloxypyrene 1,3, 4 Methylumbelliferyl sulf Cellufine Formyl , 50 ml Cellufine Formyl Media Cellufine Formyl , 500 ml Cellufine Formyl Media Cellufine Formyl Media

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Cross-Linked Collagen Triple Helices by Oxime Ligation.

Covalent cross-links are crucial for the folding and stability of triple-helical collagen, the most abundant protein in nature. Cross-linking is also an attractive strategy for the development of synthetic collagen-based biocompatible materials. Nature uses interchain disulfide bridges to stabilize collagen trimers. However, their implementation into synthetic collagen is difficult and requires the replacement of the canonical amino acids (4R)-hydroxyproline and proline by cysteine or homocysteine, which reduces the preorganization and thereby stability of collagen triple helices. We therefore explored alternative covalent cross-links that allow for connecting triple-helical collagen via proline residues. Here, we present collagen model peptides that are cross-linked by oxime bonds between 4-aminooxyproline (Aop) and 4-oxoacetamidoproline placed in coplanar Xaa and Yaa positions of neighboring strands. The covalently connected strands folded into hyperstable collagen triple helices (Tm ≈ 80 °C). The design of the cross-links was guided by an analysis of the conformational properties of Aop, studies on the stability and functionalization of Aop-containing collagen triple helices, and molecular dynamics simulations. The studies also show that the aminooxy group exerts a stereoelectronic effect comparable to fluorine and introduce oxime ligation as a tool for the functionalization of synthetic collagen.

1041 related Products with: Cross-Linked Collagen Triple Helices by Oxime Ligation.

CL APC (Cross linked Phyc Polystyrene Particle Size Picro-Sirius Red Stain K ELCI ELISA grade chick ty ELCI ELISA grade chick ty ELISA grade chick type I ELBI ELISA grade bovine t ELBI ELISA grade bovine t ELISA grade bovine type I ELISA grade porcine type ELPI ELISA grade porcine ELPI ELISA grade porcine

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New method for estimating clustering of DNA lesions induced by physical/chemical mutagens using fluorescence anisotropy.

We have developed a new method for estimating the localization of DNA damage such as apurinic/apyrimidinic sites (APs) on DNA using fluorescence anisotropy. This method is aimed at characterizing clustered DNA damage produced by DNA-damaging agents such as ionizing radiation and genotoxic chemicals. A fluorescent probe with an aminooxy group (AlexaFluor488) was used to label APs. We prepared a pUC19 plasmid with APs by heating under acidic conditions as a model for damaged DNA, and subsequently labeled the APs. We found that the observed fluorescence anisotropy (robs) decreases as averaged AP density (λAP: number of APs per base pair) increases due to homo-FRET, and that the APs were randomly distributed. We applied this method to three DNA-damaging agents, 60Co γ-rays, methyl methanesulfonate (MMS), and neocarzinostatin (NCS). We found that robs-λAP relationships differed significantly between MMS and NCS. At low AP density (λAP < 0.001), the APs induced by MMS seemed to not be closely distributed, whereas those induced by NCS were remarkably clustered. In contrast, the AP clustering induced by 60Co γ-rays was similar to, but potentially more likely to occur than, random distribution. This simple method can be used to estimate mutagenicity of ionizing radiation and genotoxic chemicals.

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Amplite™ Fluorimetric F QuantiChrom™ Formaldehy QuantiChrom™ Urea Assay 5 Carboxy X Rhodamine, NH OxiSelect™ Cellular UV- MOUSE ANTI APAAP COMPLEX, Cellufine Formyl , 50 ml Cellufine Formyl Media Cellufine Formyl , 500 ml Cellufine Formyl Media Cellufine Formyl Media Protease, DNASE free hea

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Metabolic control of TH17 and induced Treg cell balance by an epigenetic mechanism.

Metabolism has been shown to integrate with epigenetics and transcription to modulate cell fate and function. Beyond meeting the bioenergetic and biosynthetic demands of T-cell differentiation, whether metabolism might control T-cell fate by an epigenetic mechanism is unclear. Here, through the discovery and mechanistic characterization of a small molecule, (aminooxy)acetic acid, that reprograms the differentiation of T helper 17 (TH17) cells towards induced regulatory T (iTreg) cells, we show that increased transamination, mainly catalysed by GOT1, leads to increased levels of 2-hydroxyglutarate in differentiating TH17 cells. The accumulation of 2-hydroxyglutarate resulted in hypermethylation of the Foxp3 gene locus and inhibited Foxp3 transcription, which is essential for fate determination towards TH17 cells. Inhibition of the conversion of glutamate to α-ketoglutaric acid prevented the production of 2-hydroxyglutarate, reduced methylation of the Foxp3 gene locus, and increased Foxp3 expression. This consequently blocked the differentiation of TH17 cells by antagonizing the function of transcription factor RORγt and promoted polarization into iTreg cells. Selective inhibition of GOT1 with (aminooxy)acetic acid ameliorated experimental autoimmune encephalomyelitis in a therapeutic mouse model by regulating the balance between TH17 and iTreg cells. Targeting a glutamate-dependent metabolic pathway thus represents a new strategy for developing therapeutic agents against TH17-mediated autoimmune diseases.

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Cell Cycle Control Phosph Mouse Anti-Human CD34 Tar EZH2 KMT6 Control Peptid GFP control peptide anti Anti C Reactive Protein A Anti AGO2 Human, Monoclon Anti AGO2 Mouse, Monoclon Anti AGO2 Human, Monoclon Anti AGO2 Mouse, Monoclon anti HSV (II) gB IgG1 (mo anti HCMV IE pp65 IgG1 (m anti HCMV gB IgG1 (monocl

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Detecting Protein ADP-Ribosylation Using a Clickable Aminooxy Probe.

ADP-ribosylation, a posttranslational modification catalyzed by a family of enzymes known as poly(ADP-ribose) polymerases (PARPs, 17 in humans), regulates diverse cellular processes. To aid in understanding the functions of ADP-ribosylation in cells, we developed a clickable aminooxy probe, AO-alkyne, which detects ADP-ribosylation of acidic amino acids. AO-alkyne can be used to detect auto-ADP-ribosylation of PARP10 in cells following Cu-catalyzed click conjugation to an azide reporter. This method can be extended to other PARP family members that catalyze ADP-ribosylation on acidic amino acids, providing a convenient and direct readout of PARP activity in cells.

2059 related Products with: Detecting Protein ADP-Ribosylation Using a Clickable Aminooxy Probe.

Anti-ARL1(ADP-ribosylatio Anti ARL1(ADP ribosylatio Anti-ARL5B(ADP-ribosylati Anti ARL5B(ADP ribosylati Anti-ARL6(ADP-ribosylatio Anti ARL6(ADP ribosylatio ADP-ribosylation factor 3 Polyclonal Antibody ADP-R 7-(Diethylamino)coumarin- Anti-ADP Ribosylation Fac Anti ADP Ribosylation Fac Glial Fibrillary Acidic

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Aminooxylated Carbohydrates: Synthesis and Applications.

Among other classes of biomolecules, carbohydrates and glycoconjugates are widely involved in numerous biological functions. In addition to addressing the related synthetic challenges, glycochemists have invested intense efforts in providing access to structures that can be used to study, activate, or inhibit these biological processes. Over the past few decades, aminooxylated carbohydrates have been found to be key building blocks for achieving these goals. This review provides the first in-depth overview covering several aspects related to the syntheses and applications of aminooxylated carbohydrates. After a brief introduction to oxime bonds and their relative stabilities compared to related C═N functions, synthetic aspects of oxime ligation and methodologies for introducing the aminooxy functionality onto both glycofuranosyls and glycopyranosyls are described. The subsequent section focuses on biological applications involving aminooxylated carbohydrates as components for the construcion of diverse architectures. Mimetics of natural structures represent useful tools for better understanding the features that drive carbohydrate-receptor interaction, their biological output and they also represent interesting structures with improved stability and tunable properties. In the next section, multivalent structures such as glycoclusters and glycodendrimers obtained through oxime ligation are described in terms of synthetic design and their biological applications such as immunomodulators. The second-to-last section discusses miscellaneous applications of oxime-based glycoconjugates, such as enantioselective catalysis and glycosylated oligonucleotides, and conclusions and perspectives are provided in the last section.

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MOUSE ANTI BOVINE ROTAVIR Androgen Receptor (Phosph Androgen Receptor (Phosph Rabbit Anti-Human Androge Rabbit Anti-Human Androge Androgen Receptor (Ab 650 NATIVE HUMAN PROLACTIN, P BriteRuler™ 1 kb DNA La BriteRuler Prestained Pro AZD-3514 Mechanisms: Andr 17β-Acetoxy-2α-bromo-5 (5α,16β)-N-Acetyl-16-[2

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Targeting Prostate-Specific Membrane Antigen (PSMA) with F-18-Labeled Compounds: the Influence of Prosthetic Groups on Tumor Uptake and Clearance Profile.

Prostate-specific membrane antigen (PSMA) is an important biomarker expressed in the majority of prostate cancers. The favorable positron emission tomography (PET) imaging profile of the PSMA imaging agent 2-(3-(1-carboxy-5-[(6-[18F]fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-pentane-dioic acid [18F]DCFPyL in preclinical prostate cancer models and in prostate cancer patients stimulated the development and validation of other fluorine-containing PSMA inhibitors to further enhance pharmacokinetics and simplify production methods. Here, we describe the synthesis and radiopharmacological evaluation of various F-18-labeled PSMA inhibitors which were prepared through different prosthetic group chemistry strategies.

1039 related Products with: Targeting Prostate-Specific Membrane Antigen (PSMA) with F-18-Labeled Compounds: the Influence of Prosthetic Groups on Tumor Uptake and Clearance Profile.

Mouse Anti-Prostate Speci PSA (Prostate Specific A PSA (Prostate Specific A PSA (Prostate Specific A PSA (Prostate Specific A PSA (Prostate Specific A PSA (Prostate Specific A Human Prostate Specific A Multiple organ cancer tis Multiple organ tumor tiss Prostate cancer, hyperpla Prostate-Specific Antigen

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