Synthesis and Hierarchical Self-Assembly of Rod−Rod Block Copolymers via Click Chemistry between Mesogen-Jacketed Liquid Crystalline Polymers and Helical Polypeptides
摘要:
A series of novel rod-rod diblock copolymers containing poly{2,5-bis[(4-methoxyphenyl)oxycarbonyl]styrene} (PMPCS) and poly(gamma-benzyl-L-glutamate) (PBLG) were synthesized by click chemistry from alkyne- and azide-functionalized homopolymers The alpha-alkyne PM PCS homopolymers were synthesized by coppei -mediated atom ti ansfer radical polymerization with a In online-containing a-alkyne bifun( tional initiator, and a-azido PBLG homopolymers were synthesized by ring-opening polymerization of gamma-benzyl-L-glutamate N-car boxyanhydnde with an amino-containing a-azide mina tor The no struceares of the rod-rod block copcdymeis were confirmed by H-1 NM R spectroscopy, Fourier transform int) an.rd spectroscopy, and gel permeation chromatography analysis The self-assembling behavior of the rod t od block copolymers in bulk was investigated using differential scanning calonmetry, polar Ind light micro;copy, wide-angle X-ray diffraction, and transmission electron microscopy techniques A lamellar structure was observed with of f(PBLG) similar to 0 50, in which PMPCS was in a columnar nematie phase and PBLG assigned to a hexagonally packed-cylinder structure (Phi(II)) According to the TEM micrographs and simulated lengths of the copolymers. a stacked bdayei structure in a hexagon in lamella morphology for the selfassembly of the rod rod block copolymers was proposed Finally, by increasing f(PBLG) to similar to 0 69, a micro?hase-sepat riled hexagon in cylinder morphology was found, in which PM PCS formed the core of the cylinders sur rounded by PBLG in Phi(II) phase and both rods were in an inter digitated packing
The present invention provides compounds, compositions thereof, and methods of using the same.
本发明提供了化合物、其组合物以及使用这些化合物的方法。
[EN] COMPOSITIONS AND METHODS RELATED TO ANTI-CD19 ANTIBODY DRUG CONJUGATES<br/>[FR] COMPOSITIONS ET MÉTHODES ASSOCIÉES À DES CONJUGUÉS ANTICORPS ANTI-CD19-MÉDICAMENTS
申请人:LEGOCHEM BIOSCIENCES INC
公开号:WO2017051249A1
公开(公告)日:2017-03-30
In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-CD 19 antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
[EN] COMPOSITIONS AND METHODS RELATED TO ANTI-EGFR ANTIBODY DRUG CONJUGATES<br/>[FR] COMPOSITIONS ET MÉTHODES ASSOCIÉES À DES CONJUGUÉS ANTICORPS ANTI-EGFR-MÉDICAMENTS
申请人:LEGOCHEM BIOSCIENCES INC
公开号:WO2017051254A1
公开(公告)日:2017-03-30
In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-epidermal growth factor receptor ("EGFR") antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the drug; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
Benzoazine mono-N-oxides and benzoazine 1,4 dioxides and compositions therefrom for the therapeutic use in cancer treatments
申请人:Auckland Uniservices Limited
公开号:EP1468688A2
公开(公告)日:2004-10-20
The present invention relates to a synergetistic composition comprising one or more benzoazine-mono-N-oxides, and one or more benzoazine 1,4 dioxides for use in cancer therapy.
The invention also provides a range of novel 1,2,4 benzoazine-mono-N-oxides and related analogues. These can be used as potentiators of the cytotoxicity of existing anticancer drugs and therapies for cancer treatment.
Selective and Potent Proteomimetic Inhibitors of Intracellular Protein-Protein Interactions
作者:Anna Barnard、Kérya Long、Heather L. Martin、Jennifer A. Miles、Thomas A. Edwards、Darren C. Tomlinson、Andrew Macdonald、Andrew J. Wilson
DOI:10.1002/anie.201410810
日期:2015.3.2
discovery. α‐Helix mediated PPIs may be amenable to modulation using generic chemotypes, termed “proteomimetics”, which can be assembled in a modular manner to reproduce the vectoral presentation of key side chains found on a helical motif from one partner within the PPI. In this work, it is demonstrated that by using a library of N‐alkylated aromatic oligoamide helixmimetics, potent helixmimetics which
抑制蛋白质-蛋白质相互作用 (PPI) 是化学生物学和药物发现的主要挑战。α-螺旋介导的 PPI 可能适合使用称为“蛋白质模拟物”的通用化学型进行调节,该化学型可以以模块化方式组装,以重现 PPI 内一个伙伴在螺旋基序上发现的关键侧链的矢量呈现。在这项工作中,证明通过使用 N-烷基化芳族寡酰胺螺旋模拟物库,可以识别在细胞环境中重现其生物物理结合选择性的有效螺旋模拟物。