📜(3-羟基苯基)氨基甲酸酯置于硫酸,Potassium Hydroxide体系中,用 乙酸乙酯 用作溶剂,化学反应 2.5H,反应生成7-氨基-4-甲基香豆素 参考文献:Monoterpene-Containing Substituted Coumarins As Inhibitors Of Respiratory Syncytial Virus (Rsv) Replication 标题:Monoterpene-Containing Substituted Coumarins As Inhibitors Of Respiratory Syncytial Virus (Rsv) Replication 摘要:呼吸道合胞病毒(rsv)是婴儿死亡的一个重要原因.然而,目前尚无疫苗和足够的药物用于治疗.我们首次展示,O-连接的香豆素-单萜共轭物是有效的rsv抑制剂.最有效的化合物对rsv的a型和b型两种血清型都具有活性.根据添加时间实验的结果,这些共轭物在病毒周期的早期阶段起作用.根据分子模拟数据,Rsv F蛋白可能被视为一个可能的靶点. Doi:10.3390/molecules26247493
专利信息
专利号:US-2013267680-A1 优先权日:2010-09-15 标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof 发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL 权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST 摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.
专利号:US-6451543-B1 优先权日:1998-08-31 标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides 发明人:KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO 权利人:GRYPHON SCIENCES 摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.
专利号:US-5965746-A 优先权日:1997-06-02 标题:Efficient method for the synthesis of N-cyclic maleamic acids and N-cyclic maleimides 发明人:FUJITA SATOSHI; REDDY PAIDI YELLA; TORU TAKESHI 权利人:AISIN SEIKI 摘要:Provided are methods for the synthesis of N-cyclic maleamic acids and N-cyclic maleimide derivatives, as well as N-cyclic maleamic acids and N-cyclic maleimides synthesized thereby. The method for synthesis of an N-cyclic maleamic acid involves reacting an amino group-containing N-cyclic compound with maleic anhydride in acetic acid to obtain an N-cyclic maleamic acid. An N-cyclic maleimide can be formed by adding hexamethyldisilazane to an N-cyclic maleamic acid prepared according to the above-described method, thereby cyclizing a maleamic acid site of the N-cyclic maleamic acid. The described methods allow for the products to be obtained at high yields.
专利号:US-8759508-B2 优先权日:2007-05-18 标 题 :Chromophoric silyl protecting groups and their use in the chemical synthesis of oligonucleotides 发明人:DELANEY MICHAEL OREN 权利人:DELANEY MICHAEL OREN; GE HEALTHCARE DHARMACON INC 摘要:The compounds are of class of chromophoric 1,2,3-triazolyl equipped silyl linking groups that are useful in the chemical synthesis of RNA. An example of a nucleoside comprising this group is
专利号:US-7541165-B2 优先权日:2001-10-30 标 题 :Molecular detection systems utilizing reiterative oligonucleotide synthesis 发明人:HANNA MICHELLE M 权利人:RIBOMED BIOTECHNOLOGIES INC 摘要:The present invention provides methods for detecting the presence of a target molecule by generating multiple detectable oligonucleotides through reiterative enzymatic oligonucleotide synthesis events on a defined polynucleotide sequence. The methods generally comprise using a nucleoside, a mononucleotide, an oligonucleotide, or a polynucleotide, or analog thereof, to initiate synthesis of an oligonucleotide product that is substantially complementary to a target site on the defined polynucleotide sequence; optionally using nucleotides or nucleotide analogs as oligonucleotide chain elongators; using a chain terminator to terminate the polymerization reaction; and detecting multiple oligonucleotide products that have been synthesized by the polymerase. In one aspect, the invention provides a method for detecting a target protein, DNA or RNA by generating multiple detectable RNA oligoribonucleotides by abortive transcription.
专利号:US-11851651-B2 优先权日:2017-06-19 标 题 :Automated methods for scalable, parallelized enzymatic biopolymer synthesis and modification using microfluidic devices 发明人:BANAL JAMES; BERLEANT JOSEPH DON; SHEPHERD TYSON; BATHE MARK 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Methods for the automated template-free synthesis of user-defined sequence controlled biopolymers using microfluidic devices are described. The methods facilitate simultaneous synthesis of up to thousands of uniquely addressed biopolymers from the controlled movement and combination of regents as fluid droplets using microfluidic and EWOD-based systems. In some forms, biopolymers including nucleic acids, peptides, carbohydrates, and lipids are synthesized from step-wise assembly of building blocks based on a user-defined sequence of droplet movements. In some forms, the methods synthesize uniquely addressed nucleic acids of up to 1,000 nucleotides in length. Methods for adding, removing and changing barcodes on biopolymers are also provided. Biopolymers synthesized according to the methods, and libraries and databases thereof are also described. Modified biopolymers, including chemically modified nucleotides and biopolymers conjugated to other molecules are described.
1. Wildeboer, D., Jeganathan, F., Price, R.G., et al. Characterization of bacterial proteases with a panel of fluorescent peptide substrates. Anal. Biochem. 384(2), 321-328 (2009). 2. Kisselev, A.F., and Goldberg, A.L. Monitoring activity and inhibition of 26S proteasomes with fluorogenic peptide substrates. Methods Enzymol. 398, 364-378 (2005). 3. Prudnikov, I.M., and Smirnov, A.N. Short peptide tools for monitoring caspase and proteasome activities in embryonal and adult rat brain lysates: An approach for the differential identification of proteases. J. Biochem. 151(3), 299-316 (2012). 4. Zimmerman, M., Yurewicz, E., and Patel, G. A new fluorogenic substrate for chymotrypsin. Anal. Biochem. 70(1), 258-262 (1976).
合成参考文献
参考文献:10.5483/bmbrep.2011.44.7.458 摘要:Choi MG, Lee E, Chung HS, Jang SH, Lee C. A fluorogenic method for measuring enteropeptidase activity: spectral shift in the emission of GD4K-conjugated 7-amino-4-methylcoumarin. BMB Rep. 2011 Jul;44(7):458–61. doi: 10.5483/bmbrep.2011.44.7.458. 参考文献:10.1007/s00401-011-0856-5 摘要:Doeppner TR, Bretschneider E, Doehring M, Segura I, Sentürk A, Acker-Palmer A, Hasan MR, ElAli A, Hermann DM, Bähr M. Enhancement of endogenous neurogenesis in ephrin-B3 deficient mice after transient focal cerebral ischemia. Acta Neuropathologica. 2011 Jul 21;122(4):429. doi: 10.1007/s00401-011-0856-5.