Search results for "LAB"
showing 10 items of 7932 documents
Phasor-FLIM analysis of Thioflavin T self-quenching in Concanavalin amyloid fibrils
2020
The formation of amyloid structures has traditionally been related to human neurodegenerative pathologies and, in recent years, the interest in these highly stable nanostructures was extended to biomaterial sciences. A common method to monitor amyloid growth is the analysis of Thioflavin T fluorescence. The use of this highly selective dye, diffused worldwide, allows mechanistic studies of supramolecular assemblies also giving back important insight on the structure of these aggregates. Here we present experimental evidence of self-quenching effect of Thioflavin T in presence of amyloid fibrils. A significant reduction of fluorescence lifetime of this dye which is not related to the propert…
Site-specific near-infrared fluorescent labelling of proteins on cysteine residues with meso -chloro-substituted heptamethine cyanine dyes
2018
International audience; Near-infrared (NIR) fluorescence imaging is a promising new medical imaging modality. Associated with a targeting molecule, NIR fluorophores can accumulate selectively in tissues of interest and become valuable tools for the diagnosis and therapy of various pathologies. To facilitate the design of targeted NIR imaging agents, it is important to identify simple and affordable fluorescent probes, allowing rapid labelling of biovectors such as proteins, ideally in a site-specific manner. Here, we demonstrate that heptamethine cyanine based fluorophores, such as IR-783, that contain a chloro-cyclohexyl moiety within their polymethine chain can react selectively, at neutr…
Monitoring Human Neutrophil Differentiation by Digital Holographic Microscopy
2021
We report on the usefulness of digital holographic microscopy (DHM) for the assessment of human neutrophil differentiation from myeloid cells. The cell and nuclear regions have been designated by image segmentation of the optical phase function, and the changes of the cell nucleus morphology in relation to the whole cell morphology have been examined during the process of granulocytic differentiation into mature neutrophils in PLB-985 cell line. Nucleus phase volume and circularity and the ratios between the nucleus and the cell projected area and volume provide a reliable set of parameters to characterize the maturation process. As control, cell differentiation has been monitored in parall…
Site-Specific Dual Labeling of Proteins on Cysteine Residues with Chlorotetrazines
2018
International audience; Dual-labeled biomolecules constitute a new generation of bioconjugates with promising applications in therapy and diagnosis. Unfortunately, the development of these new families of biologics is hampered by the technical difficulties associated with their construction. In particular, the site specificity of the conjugation is critical as the number and position of payloads can have a dramatic impact on the pharmacokinetics of the bioconjugate. Herein, we introduce dichlorotetrazine as a trivalent platform for the selective double modification of proteins on cysteine residues. This strategy is applied to the dual labeling of albumin with a macrocyclic chelator for nucl…
18F-labeling of peptides by means of an organosilicon-based fluoride acceptor.
2006
Fluorine-18 is among the most commonly used radionuclides for positron emission tomography (PET). This non-invasive imaging technique is capable of providing in vivo information about the distribution of radiolabeled biomolecules by 1808 coincidence detection of two simultaneously emitted photons from positron–electron annihilation. Although a number of different radiotracers have been successfully employed in PET, only a few, such as 2-[F]fluoro-2-deoxy-d-glucose (FDG) and [F]fluorodopa, have gained widespread application in nuclear medicine. The reason for this is that the regioselective introduction of F into tracer molecules is often non-specific and radiochemical yields (RCY) of the Fl…
Synthesis and evaluation of (S)-2-(2-[18F]fluoroethoxy)-4-([3-methyl-1-(2-piperidin-1-yl-phenyl)-butyl-carbamoyl]-methyl)-benzoic acid ([18F]repaglin…
2004
18F-labeled non-sulfonylurea hypoglycemic agent (S)-2-(2-[(18)F]fluoroethoxy)-4-((3-methyl-1-(2-piperidin-1-yl-phenyl)-butylcarbamoyl)-methyl)-benzoic acid ([(18)F]repaglinide), a derivative of the sulfonylurea-receptor (SUR) ligand repaglinide, was synthesized as a potential tracer for the non-invasive investigation of the sulfonylurea 1 receptor status of pancreatic beta-cells by positron emission tomography (PET) in the context of type 1 and type 2 diabetes. [(18)F]Repaglinide could be obtained in an overall radiochemical yield (RCY) of 20% after 135 min with a radiochemical purity higher than 98% applying the secondary labeling precursor 2-[(18)F]fluoroethyltosylate. Specific activity w…
18F-Labeling Using Click Cycloadditions
2014
Due to expanding applications of positron emission tomography (PET) there is a demand for developing new techniques to introduce fluorine-18 (t1/2=109.8 min). Considering that most novel PET tracers are sensitive biomolecules and that direct introduction of fluorine-18 often needs harsh conditions, the insertion of18F in those molecules poses an exceeding challenge. Two major challenges during18F-labeling are a regioselective introduction and a fast and high yielding way under mild conditions. Furthermore, attention has to be paid to functionalities, which are usually present in complex structures of the target molecule. The Cu-catalyzed azide-alkyne cycloaddition (CuAAC) and several copper…
(18) F-labeled folic acid derivatives for imaging of the folate receptor via positron emission tomography.
2013
The folate receptor (FR) is already known as a proven target in diagnostics and therapy of cancer. Furthermore, the FR is involved in inflammatory and autoimmune diseases. The major advantage as a valuable target is its strongly limited expression in healthy tissues. Over the past two decades, several folic acid-based radiopharmaceuticals addressing the FR have been developed, and some of them show great potential for applications in clinical routine. However, most of these radiofolates were developed for single photon emission computed tomography imaging, and only a few can be used for positron emission tomography (PET) imaging. The development of suitable (18) F-labeled derivatives for PE…
Selective binding to monoamine oxidase A: in vitro and in vivo evaluation of (18)F-labeled β-carboline derivatives.
2015
In this study we synthesized four different (18)F-labeling precursors for the visualization of the monoamino oxidase A using harmol derivatives. Whereas two are for prosthetic group labeling using [(18)F]fluoro-d2-methyl tosylate and 2-[(18)F]fluoroethyl-tosylate, the other three precursors are for direct nucleophilic (18)F-labeling. Additionally the corresponding reference compounds were synthesized. The syntheses of [(18)F]fluoro-d2-methyl-harmol and 2-[(18)F]fluoroethyl-harmol were carried out using harmol as starting material. For direct nucleophilic (18)F-labeling of the tracers carrying oligoethyled spacers (PEG), a toluenesulfonyl leaving group was employed. The radiolabeling, purifi…
Total synthesis and evaluation of [18F]MHMZ.
2007
Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[(18)F]fluoroethyltosylate ([(18)F]FETos) was carried out in yields of approximately 90% synthesizing [(18)F]MHMZ in a specific activity of approximately 50MBq/nmol with a starting activity of approximately 3GBq. Overall radiochemical yield including [(18)F]FETos synthon synthesis, [(18)F]fluoroalkylation and preparing the injectable [(18)F]MHMZ solution was 42% within a synthesis time of approximately 100 min. The novel compound showed excellent specific binding to the 5-HT(2A) receptor (K(i)=9.0 nM) in vitro and promising in vivo characteristics.