专利号:US-2023212216-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins 发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH 权利人:GENIE BIOTECH UK LTD 摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.
专利号:AU-2020409711-A1 优先权日:2019-12-20 标题 :Synthesis of lactone derivatives and their use in the modification of proteins
专利号:US-10738028-B2 优先权日:2016-05-11 标题:Spiro three-membered ring, spiro five-membered ring peptide deformylase inhibitor and use thereof in antibacteria and anti-tumor 发明人:HU WENHAO; LV FENGPING; TANG YANG; LI ZIYAN; CHEN CHEN; WEI JIANHAI; DONG SUZHEN; QIAN YU 权利人:RUDONG RUIEN PHARMACEUTICAL TECH CO LTD 摘要:Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, can affect the energy balance of the cancer cells through inhibiting the peptide deformylase of the mitochondria in the cells, so that the mitochondrial membrane is depolarized, ATP is exhausted and cell apoptosis is promoted, and has good inhibitory activities on many cancer cell strains such as colorectal cancer, leukemia, lung cancer, gastric cancer, cervical cancer, breast cancer, prostatic cancer, liver cancer and osteosarcoma at relatively lower concentrations. The structure of exemplary invention spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitors are represented by one or more of:
专利号:EP-4076533-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins
专利号:CA-3164962-A1 优先权日:2019-12-20 标题 :Synthesis of lactone derivatives and their use in the modification of proteins
专利号:US-7585875-B2 优先权日:2006-06-06 标 题 :Substituted pyrazolo[1,5-a]pyridine compounds and their methods of use 发明人:GAETA FEDERICO C A; GROSS MATTHEW; JOHNSON KIRK W 权利人:AVIGEN INC 摘要:The present invention is directed to substituted pyrazolo[1,5-a]pyridines and related methods for their synthesis and use.
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合成参考文献
参考文献:10.1007/s00216-013-6917-y 摘要:Yang F, Mao J, He XW, Chen LX, Zhang YK. Preparation of a boronate-functionalized affinity hybrid monolith for specific capture of glycoproteins. Analytical and Bioanalytical Chemistry. 2013 Apr 04;405(15):5321–31. doi: 10.1007/s00216-013-6917-y. 参考文献:10.1007/s10337-023-04252-5 摘要:Li Q, Wang T, Hou Y, Wang D, Xiong S, Wei C, Cao Q, Wang F. Solid-Phase Extraction and Simultaneous Fluorescence Detection of Cis-Diol-Containing Biomolecules Based on a Novel Boronate Affinity Material. Chromatographia. 2023 Apr 12;86(5):387–99. doi: 10.1007/s10337-023-04252-5.