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:US-5596123-A 优先权日:1992-11-25 标 题 :Boric ester synthesis 发明人:ELGENDY SAID M A; DEADMAN JOHN J; PATEL GEETA; GREEN DONOVAN S; BABAN JEHAN A; KAKKAR VIJAY V; CLAESON GORAN K 权利人:THROMBOSIS RES INST 摘要:Stable alpha -substituted boronic esters, e.g. for use in peptide synthesis, are prepared by reacting a substituted alkene of the formula: with a disubstituted borane of the formula: wherein: (i) R1 and R2 are each selected from various groups which are preferably not leaving groups; (ii) X is halogen or other leaving group; (iii) Y is H or lower alkyl; (iv) Q1 and Q2 are each selected from various groups which are preferably such that the borane is non-hydrolyzable, and particularly Q1 and Q2 together may represent a residue of a diol such as catechol or pinanediol.
专利号:EP-1888227-A4 优先权日:2005-05-12 标题 :HYDROPHOBIC ABSORBENT COMPLEXES OF GALACTOMANNAN AND BORONATES AND PROCESS FOR THE SYNTHESIS OF SAID COMPLEXES
专利号:WO-9800398-A1 优先权日:1996-06-28 标题 :Method for the synthesis of amines and amino acids with organoboron derivatives
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:EP-4076533-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins
[参考文献]: A Tulinsky, Et Al. Structure Of A Tetrahedral Transition State Complex Of Alpha-Chymotrypsin Dimer At 1.8-A Resolution. J Biol Chem. 1987 Jun 5;262(16):7737-43. [参考文献]: B Goz, Et Al. Compounds That Inhibit Chymotrypsin And Cell Replication. Biochem Pharmacol. 1986 Oct 15;35(20):3587-91.
合成参考文献
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