专利号:WO-2023030277-A1 优先权日:2021-08-30 标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog 发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN 权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD 摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.
专利号:WO-2024181781-A1 优先权日:2023-02-27 标 题:Substrate for synthesis of biological polymers having anti-aggregation function and biological polymer synthesis method using same 发明人:JANG MYOUNG HOON; CHOI JAE SUN 权利人:SP2 TX INC 摘要:The present invention relates to a substrate for the synthesis of biological polymers having an anti-aggregation function, and a biological polymer synthesis method using the substrate. The substrate according to an aspect may have anti-aggregation functionality to enable high-yield and high-purity processes in the synthesis of biological polymers.
专利号:WO-9312076-A1 优先权日:1991-12-13 标题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS ROY 权利人:CORVAS INT INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:US-2024035023-A1 优先权日:2022-06-24 标题 :Computer implemented method for engineering fluorinase enzymes for synthesis of fluorophenyl compounds 发明人:R PRAVIN KUMAR; G GLADSTONE SIGAMANI; L ROOPA; B K NAVEEN; SHETTY ANUJ J; M LIKITH 权利人:KCAT ENZYMATIC PRIVATE LTD 摘要:The present invention discloses a computer-implemented method for engineering fluorinase enzymes towards the synthesis of fluorophenyl compounds. Limited or no mechanistic details of fluorinase enzymes have hindered progress in understanding their catalytic mechanisms for synthesizing synthetic organofluorine compounds. Through a comprehensive computational screening process, specific methionine-sulfonium phenyl substrates, including [(3S)-3-amino-3-carboxypropyl][2,5-difluoro-4-(4-methoxy-2,4-dioxobutyl)phenyl]methylsulfonium, were designed and optimized using quantum chemical optimization techniques. This methodology uncovers crucial information on F— ion attack conformation and the catalytic mechanism of the substrate, leading to the formation of Methyl 3-oxo-4-(2,4,5-trifluorophenyl)butanoate. Furthermore, a protein sequence and 3D modeling-based enzyme screening process was employed to identify the most suitable enzyme for this substrate. The identified enzyme was then engineered using the mechanistic insights gained from the studies, resulting in improved substrate scope, stability and catalytic efficiency. This computer-based approach offers an efficient and precise alternative to traditional trial-and-error methods, advancing the field towards the successful synthesis fluorophenyl compounds.
专利号:US-5283293-A 优先权日:1990-12-14 标 题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS R 权利人:CORVAS INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:WO-2008096846-A1 优先权日:2007-02-09 标 题 :Composition for synthesis of protein labeled with stable isotope and method for production of protein labeled with stable isotope 发明人:YOKOYAMA SHIGEYUKI; KIGAWA TAKANORI; YOKOYAMA JUN 权利人:RIKEN; TAIYO NIPPON SANSO CORP; YOKOYAMA SHIGEYUKI; KIGAWA TAKANORI; YOKOYAMA JUN 摘要:Disclosed is a means for synthesizing a protein labeled with a stable isotope (which is useful in the fields of nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry) at low cost. Specifically disclosed is a composition for use in the synthesis of a protein labeled with a stable isotope, which comprises (A) an amino acid mixture comprising 16 kinds of amino acids consisting of L-alanine, L-arginine, L-aspartic acid, L-glutamic acid, glycine, L-histidine, L-isoleucine, L-leucine, L-lysine, L-methionine, L-phenylalanine, L-proline, L-serine, L-threonine, L-tyrosine and L-valine, (B) an indole, (C) hydrogen sulfide or sodium sulfide and (D) an ammonium salt, wherein at least one of the amino acids in the amino acid mixture and/or any one or all of the indole, hydrogen sulfide or the sulfide salt and the ammonium salt is labeled with a stable isotope. Also specifically disclosed is a method for the synthesis of a protein labeled with a stable isotope using the composition.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144. [参考文献]: Adi Dror, Et Al. Structural Insights Into Methanol-Stable Variants Of Lipase T6 From Geobacillus Stearothermophilus. Appl Microbiol Biotechnol. 2015 Nov;99(22):9449-61. [参考文献]: Anna-Lena Henche, Et Al. Dissection Of Key Determinants Of Cleavage Activity In Signal Peptidase Iii (Spaseiii) Pibd. Extremophiles. 2014 Sep;18(5):905-13. [参考文献]: Carole Laffont, Et Al. The Cre1 Cytokinin Pathway Is Differentially Recruited Depending On Medicago Truncatula Root Environments And Negatively Regulates Resistance To A Pathogen. Plos One. 2015 Jan 6;10(1):E0116819. [参考文献]: Chunlei Wang, Et Al. Investigation Of A Degradant In A Biologics Formulation Buffer Containing L-Histidine. Pharm Res. 2015 Aug;32(8):2625-35.
合成参考文献
参考文献:10.1007/s10895-011-0923-2 摘要:Kaczmarek M. Chemiluminescence of the Reaction System Ce(IV) - Non-Steroidal Anti-Inflammatory Drugs Containing Europium(III) Ions and its Application to the Determination of Naproxen in Pharmaceutical Preparations and Urine. Journal of Fluorescence. 2011 Jul 13;21(6):2201. doi: 10.1007/s10895-011-0923-2.