专利号:US-8816050-B2 优先权日:2006-03-22 标题:Method of preparing glycopeptides 发明人:WONG CHI-HUEY; BRIK ASHRAF; YANG YU-YING; FICHT SIMON; PAYNE RICHARD 权利人:WONG CHI-HUEY; BRIK ASHRAF; YANG YU-YING; FICHT SIMON; PAYNE RICHARD; SCRIPPS RESEARCH INST 摘要:A method is provided for the synthesis of glycopeptides using a sugar assisted ligation strategy, wherein an N-terminal peptide portion in the form of a thioester is coopled with a C-terminal peptide portion bearing a carbohydrate moiety comprising a thiol group.
专利号:WO-2023179723-A1 优先权日:2022-03-25 标题:Cleavable fragment directed by affinity fragment, design and synthesis thereof, and use thereof in preparation of site-directed drug conjugate 发明人:HUANG WEI; TANG FENG; ZENG YUE 权利人:SHANGHAI INST MATERIA MEDICA CAS 摘要:Provided in the present invention are a cleavable fragment directed by an affinity fragment, the design and the synthesis thereof, and the use thereof in the preparation of a site-directed drug conjugate. Specifically, provided in the present invention is a conjugate with a ligand affinity directing group. The conjugate is as represented by formula I: AT-CL-R (I), wherein AT is an affinity moiety for a target protein (TP); CL is a cleavable fragment which has a self-cleaving reactivity; and R is a group to be modified to the target protein.
专利号:EP-1206494-B1 优先权日:1999-08-02 标 题:Computational design methods for making molecular mimetics 发明人:CASSET FLORENCE; GRANIER CLAUDE; KACZOREK MICHEL; LAHANA ROGER; REES ANTHONY; ROUX FLORENCE 权利人:SYNT EM SA 摘要:Methods are proposed for the design and synthesis of a molecule which mimics the activity of a parent molecule. In particular the methods relate to computationally identifying chemical groups of a parent molecule for inclusion in a mimetic, designing a mimetic taking into account the folding structure of the parent, designing a mimetic using a relative geometrical relationship of chemical groups in the parent molecule, designing a mimetic using a molecular dynamics simulation of the mimetic, and screening potential mimetics using molecular dynamics simulation.
专利号:US-8349899-B1 优先权日:2008-12-03 标题:Selective inhibitors of EG5 motors and methods of use 发明人:ARTERBURN JEFFREY; SHUSTER CHARLES 权利人:ARROWHEAD CT INC; ARTERBURN JEFFREY; SHUSTER CHARLES 摘要:Embodiments of the present invention comprises a compound of formula I or its enantiomer, diastereomer, stereoisomer or its pharmaceutically acceptable salt, methods of use and methods of synthesis.
专利号:US-9073978-B2 优先权日:2011-03-10 标 题:Method for producing glycopeptide having sialyl sugar chain, sialyl sugar chain-added amino acid derivative to be used in same, and glycopeptide 发明人:KAJIHARA YASUHIRO; MURAKAMI MASUMI; ISHII KAZUYUKI 权利人:KAJIHARA YASUHIRO; MURAKAMI MASUMI; ISHII KAZUYUKI; GLYTECH INC 摘要:[Technical Problem] n To provide a method for manufacturing that enables to obtain a targeted glycopeptide harboring a sialyl sugar chain in high yield without decomposing sialic acid at a non-reducing terminal of sugar chain when the glycopeptide is synthesized by a Boc solid phase synthesis method. n [Solution to Problem] n The present invention is characterized in that the Boc-sialylglycosylated amino acid derivative used in Boc solid phase synthesis method is one where the carboxyl group of the sialic acid at the sugar chain non-reducing terminal is protected with a phenacyl group.
专利号:CN-107903389-B 优先权日:2017-12-19 标题:Synthesis and application of E-selectin-targeted polyethylene glycol two-end double-modified antitumor drug
[参考文献]: Scott H Medina, Et Al. Cancer Cell Surface Induced Peptide Folding Allows Intracellular Translocation Of Drug. J Control Release. 2015 Jul 10:209:317-26.
合成参考文献
参考文献:10.1007/978-1-0716-0720-6_7 摘要:Pulido D, Royo M. Synthesis of Peptide-Oligoethylene Glycol (OEG) Conjugates for Multivalent Modification of Nanomaterials. 2020. In: Springer Protocols Handbooks.