Cycloaddition-Promoted Self-Assembly of a Polymer into Well-Defined β Sheets and Hierarchical Nanofibrils
作者:Ting-Bin Yu、Jane Z. Bai、Zhibin Guan
DOI:10.1002/anie.200805009
日期:2009.1.26
CuI‐catalyzed azide–alkyne cycloaddition polymerization of a peptide monomer induced folding of the resultant polymer into well‐defined βsheets, which further self‐assemble into hierarchicalnanofibrils. The antiparallel β‐sheet structure was confirmed by several techniques. Scanning probe micrographs confirm the formation of hierarchical amyloid‐like nanofibrils.
[EN] CAMPTOTHECIN DERIVATIVES AND CONJUGATES THEREOF<br/>[FR] DÉRIVÉS DE CAMPTOTHÉCINE ET LEURS UTILISATIONS
申请人:MEDIBOSTON INC
公开号:WO2021173773A1
公开(公告)日:2021-09-02
The invention provides, camptothecins, camptothecin payloads, and camptothecin conjugates, methods of preparing and using, and intermediates useful in the preparation thereof. Also provided herein are methods of treating cancer and autoimmune diseases with the camptothecin conjugates described herein.
Synthetic and mechanistic insight into nosylation of glycine residues
作者:Nicolai Stuhr-Hansen、Theis Ivan Sølling、Kristian Strømgaard
DOI:10.1039/c3ob00014a
日期:——
The Fukuyama–Mitsunobu alkylation procedure is widely used to introduce alkyl substituents to amino groups in general and N-alkylation of peptides in particular. Here we have investigated the procedure in detail for N-alkylation of peptides with N-terminal glycine residues, based on the observation that standard conditions lead to substantial bis-nosylation of the glycine amino group. A systematic evaluation of this observation was carried out and it was demonstrated that for peptides with alanine, β-alanine or γ-aminobutyric acid (GABA) as N-terminal residues mono-nosylation was observed under the same conditions. Moreover, bis-nosylation was independent of the type of resin, neighboring amino acid and nature of the peptide. Calculations suggest that the reason for the bis-nosylation is the fact that the deprotonated mono-nosyl species is particularly stable in the case of the terminal Gly residue because the N− residue can become closer to the SO2 unit. Finally, the mono-nosylated N-terminal glycine could be obtained by careful optimization of the procedure, adding only one equivalent of 2-nitrobenzenesulfonyl chloride.
Fukuyama-Mitsunobu 烷基化程序被广泛用于在氨基上引入烷基取代基,特别是肽的 N-烷基化。在此,我们根据标准条件会导致甘氨酸氨基发生大量双烷基化的观察结果,详细研究了该程序对具有 N 端甘氨酸残基的肽进行 N- 烷基化的过程。我们对这一观察结果进行了系统评估,结果表明,在相同条件下,以丙氨酸、β-丙氨酸或γ-氨基丁酸(GABA)为 N 端残基的肽也会发生单烷基化。此外,双糖基化与树脂类型、邻近氨基酸和肽的性质无关。计算结果表明,双糖基化的原因是,在末端 Gly 残基的情况下,去质子化的单糖基物种特别稳定,因为 N-残基可以变得更接近 SO2 单元。最后,通过仔细优化程序,只加入一个当量的 2-硝基苯磺酰氯,就可以得到单 Nosyl 化的 N 端甘氨酸。
Temperature and ion dual responsive biphenyl-dipeptide supramolecular hydrogels as extracellular matrix mimic-scaffolds for cell culture applications
Survival of the fittest: Self‐assemblies made of dynamic block copolymers (dynablocks) can self‐replicate by catalyzing the formation of their own building blocks. Moreover, in competition experiments, the differential thermodynamic stabilities and autocatalytic efficiencies of these self‐assemblies lead to sigmoid growth of the most efficient self‐replicator and to depletion of its competitors.