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181.
G4-FID (G-quadruplex fluorescent intercalator displacement) is a simple and fast method that allows to evaluate the affinity
of a compound for G-quadruplex DNA and its selectivity towards duplex DNA. This assay is based on the loss of fluorescence
of thiazole orange (TO) upon competitive displacement from DNA by a putative ligand. We describe here the development of a
high-throughput version of this assay performed in 96-well microplates, and fully transposable to 384-well microplates. The
test was calibrated with a set of G-quadruplex ligands characterized for their ability to bind quadruplex within a large range
of affinity. The comparison of the results obtained in microplates and in cuvettes was conducted indicating a full agreement.
Additionally, the spectral range of the test was enlarged using two other fluorescent on/off probes whose absorption are red-shifted
(TO-PRO-3) and blue-shifted (Hoechst 33258) as compared to that of TO. These labels enable to screen a large diversity of
compounds with various optical properties, which was exemplified by evaluation of affinity and selectivity of the porphyrin
TMPyP4 that could not be evaluated previously. Altogether, our study demonstrates that the HT-G4-FID assay offers the possibility
to label a large variety of G-quadruplexes of biological interest and should enable screening of collections of putative G4-ligands
of high structural diversity. It thus represents a powerful tool to bring into light new ligands able to discriminate between
quadruplexes of different structures. 相似文献
182.
Abstract Humic substances are the major organic constituents of soils and sediments. They also occur in small concentrations in natural surface waters and groundwaters. They form through the breakdown of plant and animal tissues by chemical and biological processes that tend to produce complex chemical structures that are more stable than the original material from which they were derived. One of the more important characteristics of humic substances is their ability to form water-soluble and water-insoluble complexes with metal ions and hydrous oxides and to interact with clay minerals and various organic compounds such as alkanes, fatty acids, and toxic organic substances such as pesticides. 相似文献
183.
Dr. Florian Hamon Dr. Marie‐Paule Teulade‐Fichou Prof. Dr. Anh Tuân Phan 《Angewandte Chemie (International ed. in English)》2014,53(4):999-1002
Phen‐DC3 is a highly promising compound that specifically targets G‐quadruplexes, with potent biological effects observed in vivo. We used NMR spectroscopy to solve the structure of the complex formed between Phen‐DC3 and an intramolecular G‐quadruplex derived from the c‐myc promoter. Structural information revealed that Phen‐DC3 interacts with the quadruplex through extensive π‐stacking with guanine bases of the top G‐tetrad. On the basis of our structure, modifications are proposed for the development of this compound for selective targeting of a specific G‐quadruplex conformation. 相似文献
184.
Llewellyn PL Bourrelly S Serre C Vimont A Daturi M Hamon L De Weireld G Chang JS Hong DY Kyu Hwang Y Hwa Jhung S Férey G 《Langmuir : the ACS journal of surfaces and colloids》2008,24(14):7245-7250
Mesoporous MOFs MIL-100 and MIL-101 adsorb huge amounts of CO2 and CH4. Characterization was performed using both manometry and gravimetry in different laboratories for isotherms coupled with microcalorimetry and FTIR to specify the gas-solid interactions. In particular, the uptake of carbon dioxide in MIL-101 has been shown to occur with a record capacity of 40 mmol g(-1) or 390 cm3STP cm(-3) at 5 MPa and 303 K. 相似文献
185.
Michele Petenzi Dr. Daniela Verga Dr. Eric Largy Dr. Florian Hamon Dr. Filippo Doria Dr. Marie‐Paule Teulade‐Fichou Aurore Guédin Dr. Jean‐Louis Mergny Prof. Mariella Mella Prof. Mauro Freccero 《Chemistry (Weinheim an der Bergstrasse, Germany)》2012,18(45):14487-14496
We report herein a solvent‐free and microwaved‐assisted synthesis of several water soluble acyclic pentaheteroaryls containing 1,2,4‐oxadiazole moieties ( 1 – 7 ). Their binding interactions with DNA quadruplex structures were thoroughly investigated by FRET melting, fluorescent intercalator displacement assay (G4‐FID) and CD spectroscopy. Among the G‐quadruplexes considered, attention was focused on telomeric repeats together with the proto‐oncogenic c‐kit sequences and the c‐myc oncogene promoter. Compound 1 , and to a lesser extent 2 and 5 , preferentially stabilise an antiparallel structure of the telomeric DNA motif, and exhibit an opposite binding behaviour to structurally related polyoxazole ( TOxaPy ), and do not bind duplex DNA. The efficiency and selectivity of the binding process was remarkably controlled by the structure of the solubilising moieties. 相似文献
186.
The understanding of the origin of the thickness (h) dependent glass transition temperature, Tg(h), reported over the last decade for supported and freely standing thin polymer films, is still unclear. Indeed, the spin-coating process, the interfacial adsorption as well as the freezing-in of non-equilibrated chain conformations and orientations caused by fast solvent evaporation could result in partially disentangled chains which can be depicted as a gel-like structure. The effect of PMMA stereoregularity on the chain conformation and orientation and its persistence length in thin films is discussed. Moreover, striking evolutions of Tg(h) by changing the nature of the solvent support the assumption of a specific organisation of the chains in thin films which can hold over thickness far above Rg. 相似文献