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综述了典型的固相合成法,及其在多肽、低聚核苷酸和寡糖合成中的应用。比较了固相合成法与传统的液相合成法之优缺点。介绍了固相合成法中常用的高分子载体;氨基、羧基、羟基、磷酸基等功能基的化学保护方法。介绍了1984年诺贝尔奖金获得者,固相合成创始人R.B.Merrifield在此领域中的成就。引用了1963~1986年的60篇文献。 相似文献
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在固相多肽合成中,Dmab作为羧基保护基具有脱保护条件温和、步骤简便、选择性高的特点,但有时脱保护效率并不稳定.为此,基于Fmoc/t Bu/Dmab三维正交保护策略,利用固相多肽合成技术设计并合成了4个肽树脂,对固相多肽合成中Glu和Asp主链和侧链羧基的Dmab保护基脱除规律进行了研究.结果显示,树脂上α-ODmab的脱保护快速、完全,β-ODmab和γ-ODmab脱保护反应较慢,可以检测到相应的中间产物(4-氨基苄酯肽),推测脱保护效率由快到慢依次为α-ODmabβ-ODmabγ-ODmab.该结果表明Dmab作为α-COOH保护基具有较高的应用价值,但用于β-COOH和γ-COOH保护时,其脱保护条件尚不成熟. 相似文献
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血红蛋白片段的合成及生物活性 总被引:1,自引:0,他引:1
采用多肽固相合成方法, 以Wang 树脂为载体, Fmoc为N-端氨基酸保护基, HOBt-HBTU为缩合试剂, 合成了一系列血红蛋白α链的片段, 产物经RP-HPLC和质谱进行了确定. 生物活性研究结果表明, 该系列多肽具有较高的血管紧张素Ⅰ转换酶抑制活性, 但不具有α-葡萄糖苷酶抑制活性. 相似文献
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一些多羟基酚酸芳基酯具有显著的生理活性,可用于医药、饮料和食品等方面。但目前关于多羟基酚酸芳基酯的合成还研究得不多。传统的方法是(1)保护多羟基酚酸中的酚羟基,(2)活化羧基成酰氯,(3)酯化,(4)去保护基的四步方法。本文将报道多羟基酚酸——2.4——二羟基苯甲酸(1)直接与酚类成酯的反应。即将二氯磷酸芳基酯(ROPOCI_2)(3)作为缩合剂,应用于一步法合成(1)芳基酯,以较好产率得到了(1)的七个新芳基酯(2_a—2_g),并经元素分析及波谱鉴定。同时还首次研究了缩合剂 相似文献
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High-throughput quantification with label-free methods has received considerable attention in electrospray ionization(ESI)-mass spectrometry(MS),but the manner by which MS signals respond to peptide concentration remains unclear in proteomics.We developed a new mathematical formula to describe the intrinsic log-log relationship between the MS intensity response and peptide concentration in an analytical ESI process.Experimental results showed that the calibration curve is fairly fit to the log-log formula with a linear dynamic range of approximate four to five orders of magnitude.However,we found that the ionization of analytical peptides can be severely suppressed by coexisting matrix peptides,such that the calibration curve can be poorly leveled off on both ends.Our study suggests that the interferences from coexisting matrix peptides should be reduced in the ESI process to use the log-log calibration curve successfully for the high-throughput quantification. 相似文献
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Dr. Richard Raz Dr. Fabienne Burlina Dr. Mohamed Ismail Dr. Julian Downward Dr. Jiejin Li Dr. Stephen J. Smerdon Martin Quibell Dr. Peter D. White Dr. John Offer 《Angewandte Chemie (International ed. in English)》2016,55(42):13174-13179
We have developed a convenient method for the direct synthesis of peptide thioesters, versatile intermediates for peptide ligation and cyclic peptide synthesis. The technology uses a modified Boc SPPS strategy that avoids the use of anhydrous HF. Boc in situ neutralization protocols are used in combination with Merrifield hydroxymethyl resin and TFA/TMSBr cleavage. Avoiding HF extends the scope of Boc SPPS to post‐translational modifications that are compatible with the milder cleavage conditions, demonstrated here with the synthesis of the phosphorylated protein CHK2. Peptide thioesters give easy, direct, access to cyclic peptides, illustrated by the synthesis of cyclorasin, a KRAS inhibitor. 相似文献
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We present a nonredundant benchmark, coined PepPro, for testing peptide–protein docking algorithms. Currently, PepPro contains 89 nonredundant experimentally determined peptide–protein complex structures, with peptide sequence lengths ranging from 5 to 30 amino acids. The benchmark covers peptides with distinct secondary structures, including helix, partial helix, a mixture of helix and β-sheet, β-sheet formed through binding, β-sheet formed through self-folding, and coil. In addition, unbound proteins' structures are provided for 58 complexes and can be used for testing the ability of a docking algorithm handling the conformational changes of proteins during the binding process. PepPro should benefit the docking community for the development and improvement of peptide docking algorithms. The benchmark is available at http://zoulab.dalton.missouri.edu/PepPro_benchmark . © 2019 Wiley Periodicals, Inc. 相似文献
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V. V. Pak M. Ku N. Li M. S. Kim T. D. Kasymova D. Y. Kwon 《Chemistry of Natural Compounds》2005,41(1):69-74
The capability of peptides Leu-Pro-Tyr-Pro (LPYP), Leu-Pro-Tyr-Pro-Arg (LPYPR), and Ser-Pro-Tyr-Pro-Arg (SPYPR) to occupy the part of the binding site ascribed to NADPH in the active center of 3-hydroxy-3-methylglutaryl-coenzyme-A-reductase was analyzed using results from a semi-empirical PM3 method. The similarity of the peptide structures to NADPH was determined by comparing the relative contribution from projections of selected bond lengths in the peptides in two mutually perpendicular planes to the corresponding bond lengths in the nicotinamide part of the substrate. The correlation coefficient between the calculated average values of the relative contributions of the bonds and the inhibitory activity of these peptides is rather high (R = 0.926). This indicates that these peptides can occupy the part of the binding site for NADPH in the active center of the enzyme.__________Translated from Khimiya Prirodnykh Soedinenii, No. 1, pp. 56–59, January–February, 2005. 相似文献
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本文综述了多肽和蛋白质合成中的片段连接方法,这是近年来多肽和蛋白质合成领域中方法学上的重要进展.该方法使用非保护的多肽片段,无需酶或化学活化试剂,在缓冲溶液中能够高产率地获得多肽和蛋白质.还介绍了与多肽片段连接有关的肽硫酯和肽醛的合成方法. 相似文献
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Gui Yang XIE Jia Hua CHEN* Shrong Shi LIN Sheng JIN Ministry of Education Key Lab of Bioorganic Chemistry &Molecular Engineering College of Chemistry Molecular Engineering Peking University Beijing 《中国化学快报》2001,(6)
The hydrolysis of peptide is one of the most important chemical processes in life chemistry. It is of great significance to study catalytic antibody, which is capable of catalyzing the hydrolysis on a specific peptide bond. In recent years, we have successfully synthesized some tetrahedral geometry analogues mimicking that of the hippuryl phenylalanine 1 hydrolyzing transition state catalyzed by carboxypeptidase A(CPA)1,2, which is specific for cleavage of the C-terminal amino acid from an o… 相似文献
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Peptidyl mono-fluoromethyl ketones (FMKs) are a class of biologically active molecules that show potential as both protease inhibitors for the treatment of a range of diseases and as chemical probes for the interrogation of cellular processes. This review describes the current solid- and solution-phase routes employed for the synthesis of peptidyl mono-FMKs. In addition, it provides a brief overview of some of the key applications of FMKs in the fields of chemical biology and medicinal chemistry. 相似文献
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Diaminodiacid Bridges to Improve Folding and Tune the Bioactivity of Disulfide‐Rich Peptides 下载免费PDF全文
Ye Guo De‐Meng Sun Feng‐Liang Wang Yao He Prof. Lei Liu Prof. Chang‐Lin Tian 《Angewandte Chemie (International ed. in English)》2015,54(48):14276-14281
Disulfide‐rich peptides containing three or more disulfide bonds are promising therapeutic and diagnostic agents, but their preparation is often limited by the tedious and low‐yielding folding process. We found that a single cystine‐to‐diaminodiacid replacement could significantly increase the folding efficiency of disulfide‐rich peptides and thus improve their production yields. The practicality of this strategy was demonstrated by the synthesis and folding of derivatives of the μ‐conotoxin SIIIA, the preclinical hormone hepcidin, and the trypsin inhibitor EETI‐II. NMR and X‐ray crystallography studies confirmed that these derivatives of disulfide‐rich peptide retained the correct three‐dimensional conformations. Moreover, the cystine‐to‐diaminodiacid replacement enabled structural tuning, thereby leading to an EETI‐II derivative with higher bioactivity than the native peptide. 相似文献