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马来酰亚胺,氯甲酸甲酯 反应 1.0H,反应生成 N-甲氧基羰基顺丁烯二酰亚胺
参考文献:在定制控制释放的碳酸盐/氨基甲酸酯键与还原键敏感的二硫键连接基团之间寻求平衡:原位共价结合白蛋白的吉西他滨前药可促进生物利用度和肿瘤蓄积.
标题:在定制控制释放的碳酸盐/氨基甲酸酯键与还原键敏感的二硫键连接基团之间寻求平衡:原位共价结合白蛋白的吉西他滨前药可促进生物利用度和肿瘤蓄积.
摘要:为了解决快速酶灭活,不良肿瘤靶向以及吉西他滨(gem)应用中获得的耐药性的挑战,我们报道了两组由马来酰亚胺官能化的gem前药与血液循环白蛋白的cys-34共价共价结合,然后产生静脉给药后在大分子前药中的作用.通过链接键的不同组合(相对稳定和不稳定(分别为氨基甲酸酯和碳酸酯)以及带有或不带有二硫键的连接子)可以实现量身定制的精确控制释放.有趣的是,我们发现二硫键带来的总体优缺点随着连接键的稳定性而变化.最后,带有碳酸酯键的基团,尤其是带有缺乏二硫键的连接基的基团,体内抗肿瘤功效.
DOI:10.1021/acs.Jmedchem.8B00293

专利信息

专利号:US-11945838-B2
优先权日:2018-12-20
标 题:Method for synthesis of protein amphiphiles
发明人：BRITTO Sandanaraj Selvaraj; REDDY Mullapudi Mohan
权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES
摘要:The present invention discloses a novel cost effective method for synthesis of protein/peptide amphiphiles irrespective of functional and structural classification of proteins useful in designing a vaccine candidate from antigenic protein. The protein modification of the present invention is universal and hence any protein/peptide can be converted into amphiphilic proteins/peptides.

专利号:US-6262251-B1
优先权日:1995-10-19
标题 :Method for solution phase synthesis of oligonucleotides
发明人：PIEKEN WOLFGANG; MCGEE DANNY; SETTLE ALECIA; ZHAI YANSHENG; HUANG JIANPING
权利人:PROLIGO LLC
摘要:This invention discloses an improved method for the sequential solution phase synthesis of oligonucleotides. The method lends itself to automation and is ideally suited for large scale manufacture of oligonucleotides with high efficiency.

专利号:US-2025250302-A1
优先权日:2024-02-05
标题:Synthesis of self-assembling artificial proteins utilizing a host-guest system and uses thereof
发明人：SANDANARAJ BRITTO S; KHYADE ASHWINI RAJENDRA; HATI KSHITISH CHANDRA
权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE
摘要:The invention relates to an efficient method for synthesizing self-assembling artificial proteins (SAPs) utilizing a catalytic host-guest system. The process involves encapsulating hydrophobic probes with cyclodextrin, performing site-specific protein bioconjugation, and employing a second catalysis cycle for enhanced labeling. SAPs produced through this method are versatile and find applications in therapeutic delivery and diagnostics. The process is simplified, scalable, cost-effective, and environmentally sustainable, addressing the challenges of traditional SAP synthesis. By offering improved yield, functionality, and structural integrity, this invention advances the potential of SAPs in medical and industrial fields.

专利号:US-11359004-B2
优先权日:2012-04-03
标 题:Succinimide-activated nitroxyl compounds and methods for the use thereof for nitroxylation of proteins
发明人：VANDEGRIFF KIM D; MALAVALLI ASHOK; MKRTCHYAN GNEL
权利人:SCHINDLER WILLIAM
摘要:The present invention relates to succinimide-activated nitroxyl compounds and methods for the synthesis of such compounds. The present invention also relates to the use of succinimide-activated nitroxyl compounds to prepare nitroxylated proteins, for example nitroxylated heme proteins (e.g., nitroxylated hemoglobin and nitroxylated myoglobin). The nitroxylated proteins are optionally also conjugated to a polyalkylene oxide (PAO), for example to a polyethylene glycol (PEG). Polynitroxylated heme proteins are useful as oxygen therapeutic agents (OTAs). The invention further relates to pharmaceutical compositions of the nitroxylated proteins and methods for the use of nitroxylated proteins in the treatment of various conditions.

专利号:US-5262524-A
优先权日:1990-03-09
标题 :Method for the synthesis of trifunctional maleimide-antibody complex
发明人：ANDERSON LESLIE D; AHLEM CLARENCE N; HUANG ANN E
权利人:HYBRITECH INC
摘要:The present invention is directed to a method for extending the length of one of the three linker arms of the compound of Formula I in the production of novel trifunctional antibody-like compounds. Formula I is defined as follows: wherein X is wherein k=1 or 0; wherein Z is wherein s=1 or 0; wherein n=1 or 0; wherein q=1 or 0; wherein Y is wherein Y' is wherein p or m may be the same or different and are integers ranging from 0 to 20 with the provisos that when n=0, the sum of m and p is an integer ranging from 1 to 20, whereas when n=1, p and m are each an integer that is at least 1 and the sum of p and m is an integer ranging from 2 to 20; wherein R1 is straight or branched chain lower alkyl having from 1 to 6 carbon atoms or lower alkoxy having from 1-6 carbon atoms; and wherein R2 is hydrogen, phenyl, -COOH, or straight or branched chain lower alkyl having from 1-6 carbon atoms, with the proviso that the lower alkyl moiety may be mono substituted by -NH2, -OH, or -COOH. The compound of the present invention is useful as a trivalent coupling agent for linking Fab'-like fragments to form both bifunctional and trifunctional antibody-like compounds.

专利号:US-2020199175-A1
优先权日:2018-12-20
标题 :Method for synthesis of protein amphiphiles