790230-04-5Relevant academic research and scientific papers
Self-flickering super-resolution fluorescent dye based on SNAP-tag technology as well as synthesis and application thereof
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Paragraph 0096; 0100-0102; 0140; 0144-0146; 0175; 0179-0181, (2020/07/15)
The invention provides self-flickering super-resolution fluorescent dye based on an SNAP-tag technology and synthesis and application thereof. The structure (1) of the fluorescent dye is shown in thespecification, intramolecular rotation of silicon rhodamine is inhibited by introducing azetidine, and therefore the fluorescent dye has the characteristics of high light stability, high quantum yieldand the like. Because of thermodynamic equilibrium of intramolecular spiralization of the dye, the fluorescent dye can flicker continuously and is further applied to super-resolution fluorescence imaging. In addition, the probe can be used for specifically labeling multiple target proteins fused with SNAP-tag labels in living cells, so that the tracing of the target proteins in the living cells is realized. The SNAP-tag self-flickering super-resolution fluorescent dye provided by the invention has wide application in the fields of protein labeling, protein-protein interaction, super-resolution fluorescence imaging and the like.
Self-flickering fluorescent dye for super-resolution fluorescence imaging and synthesis and application thereof
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Paragraph 0087; 0091-0093; 0130; 0134-0136; 0162; 0166-0168, (2020/07/13)
The invention provides a self-flickering fluorescent dye for super-resolution fluorescence imaging as well as synthesis and application thereof. According to the dye, azetidine is introduced into the4,5-sites of silicon rhodamine to inhibit intramolecular rotation, so that the characteristics of high quantum yield and high stability are achieved; meanwhile, under normal physiological conditions,fluorescence and non-fluorescence forms of the probe can be mutually converted through intramolecular interaction, so that the probe can be applied to living cell super-resolution imaging, the structural formula of the probe is shown as (1), and the dye can be combined with an antibody to perform specific labeling imaging on tubulin in cells. The dye can be widely applied to the fields of proteinlabeling, super-resolution fluorescence imaging and the like.
Descriptor ΔGC-O Enables the Quantitative Design of Spontaneously Blinking Rhodamines for Live-Cell Super-Resolution Imaging
Chi, Weijie,Jiang, Xiao,Liu, Xiaogang,Qiao, Qinglong,Tan, Davin,Wang, Chao,Wu, Xia,Xu, Ning,Xu, Zhaochao,Zheng, Jiazhu,Zhou, Wei
supporting information, p. 20215 - 20223 (2020/09/21)
Herein, we reported a simple, fast, and quantitative theoretical descriptor ΔGC-O that allows accurate predictions of a wide range of spontaneously blinking rhodamines. ΔGC-O denotes the Gibbs free energy differences between the closed and open forms of rhodamines and has a good linear relationship with experimental pKcycl values. This correlation affords an effective guide for the quantitative designs of spontaneously blinking rhodamines and eliminates trial-and-error. We have validated the predictive power of ΔGC-O via the development of two spontaneously blinking rhodamines of different colors and enhanced brightness. We also demonstrated their super-resolution imaging utilities in dynamic live-cell imaging. We expect that ΔGC-O will greatly facilitate the efficient creations of spontaneously blinking fluorophores and aid the advancements of super-resolution bioimaging techniques.
BTK INHIBITORS
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Page/Page column 136, (2016/07/27)
Provided are Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
BIS-(SULFONYLAMINO) DERIVATIVES FOR TREATMENT OF PAIN AND INFLAMMATION
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Page/Page column 74, (2010/12/17)
The invention provides compounds of formula (I) wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together
Design, synthesis and identification of novel colchicine-derived immunosuppressant
Chang, Dong-Jo,Yoon, Eun-Young,Lee, Geon-Bong,Kim, Soon-Ok,Kim, Wan-Joo,Kim, Young-Myeong,Jung, Jong-Wha,An, Hongchan,Suh, Young-Ger
scheme or table, p. 4416 - 4420 (2010/04/05)
Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A.
BIS-(SULFONYLAMINO) DERIVATIVES IN THERAPY 065
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Page/Page column 51, (2009/05/28)
The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1
BIS-(SULFONYLAMINO) DERIVATIVES IN THERAPY 066
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Page/Page column 103-104, (2009/06/27)
The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
Potent and selective TF/FVIIa inhibitors containing a neutral P1 ligand
Miura, Masanori,Seki, Norio,Koike, Takanori,Ishihara, Tsukasa,Niimi, Tatsuya,Hirayama, Fukushi,Shigenaga, Takeshi,Sakai-Moritani, Yumiko,Kawasaki, Tomihisa,Sakamoto, Shuichi,Okada, Minoru,Ohta, Mitsuaki,Tsukamoto, Shin-ichi
, p. 7688 - 7705 (2007/10/03)
Inhibition of tissue factor/factor VIIa complex (TF/FVIIa) is an attractive strategy for antithrombotic therapies. We began with an investigation of a non-amidine TF/FVIIa inhibitor based on a modification of amidine compound 1. Optimization of the substituents on the P1 phenyl portion of the compound 1 led to a neutral or less basic alternative for the 4-amidinophenyl moiety. By further optimization of the substituents on the central phenyl ring, a highly potent and selective TF/FVIIa inhibitor 17d was discovered.
