891491-99-9Relevant academic research and scientific papers
Histone deacetylase fluorescence probe, and preparation method and applications thereof
-
, (2018/07/30)
The invention provides a histone deacetylase fluorescence probe, and a preparation method and applications thereof. The structure formula of the histone deacetylase fluorescence probe is disclosed inthe invention. In synthesis, 6-(dimethylamino)-2-naphthaldehyde with two-photon effect is selected as a dye, so that further nucleophilic reaction is realized after deacetylation reaction, and fluorescence signals are generated; aldehyde group carbon is modified into cyanogroup alcohol structures, hydroxyl is connected with HDACs responsive groups, and the histone deacetylase fluorescence probe isused for detecting and imaging of the activity of histone deacetylase in tissue. According to the histone deacetylase fluorescence probe, cyanogroup with excellent electron-withdrawing capability isintroduced, so that after response of HDACs with the histone deacetylase fluorescence probe, intramolecular cyclization reaction is carried out rapidly, activation of fluorescence signals is realized,detecting and imaging on histone deacetylase in living cells and tissue are realized, and excellent clinical application value is achieved.
Discovery of a sensitive, selective, and tightly binding fluorogenic substrate of bovine plasma amine oxidase
Ling, Ke-Qing,Sayre, Lawrence M.
supporting information; experimental part, p. 339 - 350 (2009/04/11)
(Chemical Equation Presented) We report a novel fluorogenic substrate of bovine plasma amine oxidase (BPAO), namely, (2-(6-(aminomethyl)naphthalen-2- yloxy)ethyl)trimethylammonium (ANETA), which displays extremely tight binding to BPAO (Km 183 ± 14 nM) and yet is metabolized fairly quickly (kcat 0.690 ± 0.010 s-1), with the aldehyde turnover product (2-(6-formylnaphthalen-2-yloxy)ethyl)trimefhylammonium serving as a real time reporting fluorophore of the enzyme activity. This allowed for the development of a fluorometric noncoupled assay that is 2 orders of magnitude more sensitive than the spectrophotometric benzylamine assay. The discovery of ANETA involved elaboration of the lead compound 6-methoxy-2-naphthalene- methaneamine by structure-based design, which recognized the ancillary cation binding site of BPAO as the most significant structural features controlling binding affinity. Structure-based design further ensured a high level of selectivity: ANETA is a good substrate of BPAO but is not a substrate of either porcine kidney diamine oxidase (pkDAO) or rat liver monoamine oxidase (MAO-B). ANETA represents the first highly sensitive, selective, and tight binding fluorogenic substrate of a copper amine oxidase that is able to respond directly to the enzyme activity in real time.
Prodan-containing nucleotide and use thereof
-
Page/Page column 18; sheet 2, (2008/06/13)
A compound represented by formula (1): wherein R1 is a substituent represented by formula (2): wherein R2 is ═O or —NH2, with the proviso that when R2 is ═O, H is attached to the 1-position N of the pyrimidine ring, and the bond between the 1-position N and the 6-position C is a single bond; or a substituent represented by formula (3): wherein R3 is —OH, ═O, or —NH2, with the proviso that when R3 is —OH or —NH2, R4 is H; when R3 is ═O, R4 is —NH2; and when R3 is ═O, H is attached to the 1-position N of the purine ring, and the bond between the 1-position N and the 6-position C is a single bond.
