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.
Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof
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Page/Page column 161; 162; 164, (2019/11/11)
Disclosed are an antibody drug conjugate IB, which uses ether linkages for connection, and improves the water solubility, stability and cytotoxicity in vivo and in intro, and an intermediate, a pharmaceutical composition, and uses of the antibody drug conjugate. The antibody drug conjugate has simple synthetic steps and a high yield.
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.
Nucleolipid nanovectors as molecular carriers for potential applications in drug delivery
Simeone, Luca,Mangiapia, Gaetano,Irace, Carlo,Di Pascale, Antonio,Colonna, Alfredo,Ortona, Ornella,De Napoli, Lorenzo,Montesarchio, Daniela,Paduano, Luigi
experimental part, p. 3075 - 3086 (2012/08/08)
Novel thymidine- or uridine-based nucleolipids, containing one hydrophilic oligo(ethylene glycol) chain and one or two oleic acid residues (called ToThy, HoThy and DoHu), have been synthesized with the aim to develop bio-compatible nanocarriers for drug d
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
Synthesis of bifunctional integrin-binding peptides containing PEG spacers of defined length for non-viral gene delivery
Pilkington-Miksa, Michael A.,Sarkar, Supti,Writer, Michele J.,Barker, Susie E.,Shamlou, Parviz Ayazi,Hart, Stephen L.,Hailes, Helen C.,Tabor, Alethea B.
experimental part, p. 2900 - 2914 (2009/04/11)
Improving the buffer and serum stability of non-viral gene delivery vectors, and increasing their circulation time in vivo, is an important focus of current research in gene therapy. The most successful strategies to date have involved shielding the complexes with large polydisperse PEG adducts. However, this approach is accompanied by a fall in transfection efficiency. In this paper we describe the solid-phase synthesis of a series of bifunctional peptides bearing short PEG spacers of defined structure as components of lipopolyplex gene delivery vectors. Short, high-yielding routes to a series of PEG-amino acids are described: these PEG-amino acids can be used in varying combinations to afford bifunctional peptides with varying lengths of PEG spacers by using standard solid-phase synthesis techniques. A series of lipopolyplexes were formulated using these bifunctional peptides, and their transfection properties assessed. Dynamic light scattering measurements on the complex with the best transfection properties showed that in phosphate-buffered saline this complex was considerably more stable, and aggregated more slowly, than a complex formulated using a similar peptide lacking the short PEG spacer. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
Pharmaceutical compositions of insulin drug-oligomer conjugates and methods of treating diseases therewith
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, (2008/06/13)
Pharmaceutical compositions that include an insulin drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The insulin drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating an insulin deficiency in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.
Carbohydrate rod conjugates: Ternary rod-coil molecules forming complex liquid crystal structures
Chen, Bin,Baumeister, Ute,Pelzl, Gerhard,Das, Malay Kumar,Zeng, Xiangbing,Ungar, Goran,Tschierske, Garsten
, p. 16578 - 16591 (2007/10/03)
T-shaped polyphilic triblock molecules, consisting of a rodlike p-terphenyl unit, a hydrophilic and flexible laterally attached oligo(oxyethylene) chain terminated by an 1-acylamino-1-deoxy-D-sorbitol unit, and two end-attached lipophilic alkyl chains, have been synthesized by palladium-catalyzed cross-coupling reactions as the key steps. The thermotropic liquid crystalline behavior of these compounds was investigated by polarized light microscopy, differential scanning calorimetry (DSC), and X-ray scattering. We investigated the mode of self-organization as a function of the length and position of the lateral polar chain and the length of the terminal alkyl chains. Depending on the size of the polar and lipophilic segments, a series of unusual liquid crystalline phases was detected. In three of these phases, the space is divided into three distinct periodic subspaces. In addition to a hexagonal channeled layer phase (ChLhex) consisting of layers that are penetrated by polar columns, there are also two honeycomb-like network structures formed by square (Colsqu/p4mm) or pentagonal cylinders (Colsqu/p4gm) . The cylinder walls consist of the terphenyl units fused by columns of alkyl chains, and the interior contains the polar side chains. In addition, a hexagonal columnar phase was observed in which the polar columns are organized in a continuum of terphenyls and alkyl chains with an organization of the terphenyl cores tangentially around the columns with the long axis perpendicular to the columns. For one compound, a reversal of birefringence was observed, which is explained by a reorientation of the terphenyl cores. The addition of protic solvents induces lamellar phases.
Multigram Synthesis of Well-Defined Extended Bifunctional Polyethylene Glycol (PEG) Chains
Loiseau, Francois A.,Hii, King Kuok,Hill, Alison M.
, p. 639 - 647 (2007/10/03)
A series of novel, well-defined, unsymmetrical poly(ethylene glycol) chains of the type X(OCH2-CH2)nY (where X = protecting group; Y = nucleofuge or a different protecting group; n = 3, 6, 9, 12, 15, 18, and 24) were prepared in high yields by applying orthogonal protecting groups. The purity of the compounds was fully verified by elemental and high-resolution mass spectrometry analyses.
Novel alkanoic acid derivaties
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, (2008/06/13)
There are provided according to the invention compounds of the formula (I) or a salt or solvate thereof, wherein: n represents an integer 1 to 6; N represents an integer 1 to 15; R1 represents (CO)xC1-9alkyl or (CO)xC1-9fluoroalkyl, which fluoroalkyl moiety contains at least 1 fluorine atom and not more than 3 consecutive perfluorocarbon atoms wherein x represents 0 or 1; and R2 and R3 independently represent C1-3alkyl or hydrogen. There are also provided pharmaceutical aerosol formulations employing said compounds as suspension stabilising agents.
