- Convenient Retinoid X Receptor Binding Assay Based on Fluorescence Change of the Antagonist NEt-C343
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Retinoid X receptor (RXR) modulators (rexinoids) are considered to have therapeutic potential for multiple diseases, such as Alzheimer's disease and Parkinson's disease. To overcome various disadvantages of prior screening methods, we previously developed an RXR binding assay using a fluorescent RXR ligand, CU-6PMN (4). However, this ligand binds not only at the ligand-binding domain (LBD) but also at the dimer-dimer interface of hRXRα. Here, we present a new fluorescent RXR antagonist 6-[N-ethyl-N-(5-isobutoxy-4-isopropyl-2-(11-oxo-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinoline-10-carboxamido)phenyl)amino]nicotinic acid (NEt-C343, 7), which emits strong fluorescence only when bound to the RXR-LBD. It allows us to perform a rapid, simple, and nonhazardous binding assay that does not require bound/free separation and uses a standard plate reader. The obtained Ki values of known compounds were correlated with the Ki values obtained using the standard [3H]9cis-retinoic acid assay. This assay should be useful for drug discovery as well as for research on endocrine disruptors, functional foods, and natural products.
- Yukawa-Takamatsu, Kayo,Wang, Yifei,Watanabe, Masaki,Takamura, Yuta,Fujihara, Michiko,Nakamura-Nakayama, Mariko,Yamada, Shoya,Kikuzawa, Shota,Makishima, Makoto,Kawasaki, Mayu,Ito, Sohei,Nakano, Shogo,Kakuta, Hiroki
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p. 861 - 870
(2021/02/03)
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- A julolidine-fused coumarin-NBD dyad for highly selective and sensitive detection of H2S in biological samples
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A new julolidine-fused coumarin-NBD probe 2 for H2S detection is rationally designed based on the DFT caculations. This improved probe exhibits faster and larger off-on response as well as higher sensitivity compared with the previous coumarin-NBD probe 1. Moreover, 2 possesses excellent selectivity and good biocompatibility, which can be employed to image H2S in living cells and in zebrafish.
- Ismail, Ismail,Wang, Dawei,Wang, Zhenghua,Wang, Dan,Zhang, Changyu,Yi, Long,Xi, Zhen
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p. 700 - 706
(2019/01/05)
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- Preparation method of large emission wavelength fluorescent dye
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The invention discloses a preparation method of a large emission wavelength fluorescent dye, comprising the following steps: first, modifying a naphthalimide by three-step reaction to obtain naphthalimide with activated methyl; second, carrying out four-step reaction to obtain aldehyde modified coumarin; third, reacting the naphthalimide with the activated methyl with the aldehyde modified coumarin to obtain a target product, the large emission wavelength fluorescent dye. Compared with the existing fluorescent dyes, the fluorescent dye synthesized in the invention has a near-infrared emission spectrum and Stokes shift up to 150 nm and is applicable to the fields such as laser, electroluminescence and fluorescent probes.
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- Host-guest interaction of coumarin-derivative dyes and cucurbit[7]uril: Leading to the formation of supramolecular ternary complexes with mercuric ions
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We investigated the photophysical behavior of the complexes formed between cucurbit[7]uril (CB7) and coumarin-derivative dyes: 7-(diethylamino)-N-(1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)-2-oxo-2H-chromene-3-carboxamide (1) and N-(1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)-11-oxo-2,3,5,6,7,11-hexahydro-1H-pyrano[2,3-f]pyrido[3,2,1-ij]quinoline-10-carboxamide (2), in the absence or presence of mercuric ions (Hg2+). The maximum absorption of 1 shows a bathochromic shift with the addition of CB7 and the fluorescence intensity is highly increased. In contrast, addition of CB7 has no noticeable effect on the spectroscopic properties of 2. However, fluorescence quenching was observed in both cases after the addition of Hg2+. Interestingly, in the absence of it fluorescence lifetime measurements for the 1-CB7 complex suggest that the macrocycle is able to prevent the aggregation of 1. The stoichiometry for these complexes, determined from the fluorescence titration measurements and mass spectrometry, indicates that 1:1 complexes are formed and the binding constants (Kb) are estimated to be around 105 M-1. The NMR studies indicate that both dyes are included in the CB7 cavity but different moieties interact with it. Considering the hydrophobic effect of the cavity, and metal-ligand and ion-dipole interactions, it can be concluded that both compounds are able to form a novel supramolecular assembly that comprises CB7, 1 or 2 and Hg2+. The binding observed between them displays a positive cooperative effect relative to the dyes alone, 1-CB7 being the most efficient complex (Kb ≈ 107 M-1) in acidic conditions. Thus, the potential for these types of complexes to be used as multifaceted functional systems appears warranted.
- Aliaga, Margarita E.,García-Río, Luis,Pessêgo, Márcia,Montecinos, Rodrigo,Fuentealba, Denis,Uribe, Iván,Martín-Pastor, Manuel,García-Beltrán, Olimpo
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supporting information
p. 3084 - 3092
(2015/04/22)
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- A highly selective water-soluble optical probe for endogenous peroxynitrite
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A colorimetric and fluorescent probe C-Py-1 for ONOO- was prepared and it could exhibit high sensitivity and excellent selectivity toward ONOO- among reactive oxygen species (ROS) and reactive nitrogen species (RNS) with a rapid response time in 100% water solution. Meanwhile, C-Py-1 was successfully applied in the imaging of endogenous ONOO- in RAW264.7 cells.
- Hou, Ji-Ting,Yang, Jin,Li, Kun,Liao, Ye-Xin,Yu, Kang-Kang,Xie, Yong-Mei,Yu, Xiao-Qi
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p. 9947 - 9950
(2014/08/18)
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- Development of an ICT-based ratiometric fluorescent hypochlorite probe suitable for living cell imaging
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We have judiciously constructed a novel ICT-based ratiometric OCl - probe capable of ratiometric imaging in the live cells based on the new OCl--promoted de-diaminomaleonitrile reaction. The Royal Society of Chemistry 2011.
- Yuan, Lin,Lin, Weiying,Song, Jizeng,Yang, Yueting
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supporting information; experimental part
p. 12691 - 12693
(2012/01/12)
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