24342-68-5Relevant articles and documents
TARGET PROTEIN EED DEGRADATION-INDUCING DEGRADUCER, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DISEASES RELATED TO EED, EZH2, OR PRC2, COMPRISING SAME AS ACTIVE INGREDIENT
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, (2021/12/23)
The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound represented by formula 1, according to the present invention is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient.
AS1411-decorated niosomes as effective nanocarriers for Ru(III)-based drugs in anticancer strategies
Riccardi, Claudia,Fàbrega, Carme,Grijalvo, Santiago,Vitiello, Giuseppe,D'Errico, Gerardino,Eritja, Ramon,Montesarchio, Daniela
supporting information, p. 5368 - 5384 (2018/09/09)
Niosomes are self-assembled vesicles made up of single chain non-ionic surfactants combined with appropriate amounts of cholesterol or other lipids, exploited as carriers for hydrophilic or lipophilic drugs. Compared to liposomes, niosomes are typically more stable, less expensive and, being generally obtained from synthetic surfactants, more easily derivatizable, providing vesicular structures with a higher versatility and chemical diversity. Herein, we investigated the physico-chemical and biological properties of niosomes loaded with two active ingredients, i.e. the nucleolipidic Ru(iii)-complex HoThyRu, selected as an anticancer agent, and the nucleolin-targeting AS1411 aptamer, allowing selective recognition of cancer cells. The morphology, average size, zeta potential, electrophoretic mobility, and stability over time of the functionalized niosomes were analyzed using different biophysical techniques. These formulations, tested on both cancer and normal cells, showed promising antiproliferative activity on HeLa cells, with a higher efficacy associated with the nanosystems containing both AS1411 and HoThyRu with respect to the controls. In all the tested cell lines, AS1411 proved to markedly enhance the bioactivity of the Ru(iii)-containing niosomes.
Synthesis of novel fluorous surfactants for microdroplet stabilisation in fluorous oil streams
Holt, Daniel J.,Payne, Richard J.,Abell, Chris
experimental part, p. 398 - 407 (2010/04/24)
The synthesis of a number of potential fluorous surfactants, prepared with a view to stabilising microdroplets in microfluidic systems is described. The surfactants comprised compounds with both perfluoropolyether (PFPE) and perfluoroalkyl (PFA) tails with three classes of hydrophilic head group, including crown ethers and hexaethylene glycol. Hydrophilic head groups and alkyl fluorous-based tails were coupled together via amide, ester and ether linkages to afford the fluorous surfactant candidates in good yields. The resulting molecules show promise in forming and stabilising both aqueous and non-aqueous microdroplets in fluorous oil streams within poly(dimethylsiloxane) (PDMS) devices to a greater degree than the pseudosurfactants commonly employed in microdroplet research. Crown Copyright
